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PADELIPORFIN
PADELIPORFIN
759457-82-4; 457P824,
RN: 759457-82-4
UNII: EEO29FZT86
3-[(2S,3S,12R,13R)-8-acetyl-13-ethyl-20-(2-methoxy-2-oxoethyl)-3,7,12,17-tetramethyl-18-(2-sulfoethylcarbamoyl)-2,3,12,13-tetrahydroporphyrin-22,24-diid-2-yl]propanoic acid;palladium(2+)
(SP-4-2)-[(7S,8S,17R,18R)-13-acetyl-18-ethyl-5-(2-methoxy-2-oxoethyl)-2,8,12,17-tetramethyl-3-[[(2-sulfoethyl)amino]carbonyl]-21H,23H-porphine-7-propanoato (4-)-kN21,kN22,kN23,kN24] palladate(2-)
Other Names
- (SP-4-2)-[(7S,8S,17R,18R)-13-Acetyl-18-ethyl-7,8-dihydro-5-(2-methoxy-2-oxoethyl)-2,8,12,17-tetramethyl-3-[[(2-sulfoethyl)amino]carbonyl]-21H,23H-porphine-7-propanoato(4-)-κN21,κN22,κN23,κN24]palladate(2-)
Molecular Formula: | C37H43N5O9PdS |
---|---|
Molecular Weight: | 840.257 g/mol |
Chemical Formula: C37H41K2N5O9PdS
Molecular Weight: 916.43
cas 698393-30-5
WST11; WST-11; WST 11; Stakel; padeliporfin; palladiumbacteriopheophorbide monolysine taurine.
Palladate(2-), [(7S,8S,17R,18R)-13-acetyl-18-ethyl-7,8-dihydro-5-(2-methoxy-2-oxoethyl)-2,8,12,17-tetramethyl-3-[[(2-sulfoethyl)amino]carbonyl]-21H,23H-porphine-7-propanoato(4-)-κN21,κN22,κN23,κN24]-, potassium (1:2), (SP-4-2)-
Tookad : EPAR -Product Information
Tookad : EPAR – Summary for the public | (English only) | 29/11/2017 |
Product details
Pharmacotherapeutic group
Antineoplastic agents
Therapeutic indication
Tookad is indicated as monotherapy for adult patients with previously untreated, unilateral, low risk, adenocarcinoma of the prostate with a life expectancy ≥ 10 years and:
- Clinical stage T1c or T2a;
- Gleason Score ≤ 6, based on high-resolution biopsy strategies;
- PSA ≤ 10 ng/mL;
- 3 positive cancer cores with a maximum cancer core length of 5 mm in any one core or 1-2 positive cancer cores with ≥ 50 % cancer involvement in any one core or a PSA density ≥ 0.15 ng/mL/cm³.
Name | Tookad |
---|---|
Agency product number | EMEA/H/C/004182 |
Active substance | padeliporfin di-potassium |
International non-proprietary name(INN) or common name | padeliporfin |
Therapeutic area | Prostatic Neoplasms |
Anatomical therapeutic chemical (ATC) code | L01XD07 |
Additional monitoring | This medicine is under additional monitoring. This means that it is being monitored even more intensively than other medicines. For more information, see medicines under additional monitoring. |
Marketing-authorisation holder | STEBA Biotech S.A |
---|---|
Revision | 0 |
Date of issue of marketing authorisation valid throughout the European Union | 10/11/2017 |
Contact address:
STEBA Biotech S.A
7 place du theatre
L-2613 Luxembourg
Luxembourg
Padeliporfin is a vascular-acting photosensitizer consisting of a water-soluble, palladium-substituted bacteriochlorophyll derivative with potential antineoplastic activity. Upon administration, paldeliporfin is activated locally when the tumor bed is exposed to low-power laser light; reactive oxygen species (ROS) are formed upon activation and ROS-mediated necrosis may occur at the site of interaction between the photosensitizer, light and oxygen. Vascular-targeted photodynamic therapy (VTP) with padeliporfin may allow tumor-site specific cytotoxicity while sparing adjacent normal tissues.
WST-11 (Stakel) is a water-soluble bacteriochlorophyll (chemical structure shown below) derivative coordinated with palldium, which has maximum absorption wavelength in the near infrared (753 nm) and rapid clearance from the body ( t 1/2 = 0.37 hour for a 10-mg/kg drug dose in the rat and t 1/2 = 0.51 hour, 1 hour, and 2.65 hours for 1.25-, 2.5-, and 5-mg/kg drug doses, respectively. It binds to serum albumin and has potent antivascular activity through the generation of hydroxyl radicals when stimulated by the proper light wavelength.
Photodynamic therapy (PDT) is a non-surgical treatment of tumors in which non-toxic drugs and non-hazardous photosensitizing irradiation are combined to generate cytotoxic reactive oxygen species in situ. This technique is more selective than the commonly used tumor chemotherapy and radiotherapy. To date, porphyrins have been employed as the primary photosensitizing agents in clinics. However, current sensitizers suffer from several deficiencies that limit their application, including mainly: (1) relatively weak absorption in the visible spectral range which limits the treatment to shallow tumors; (2) accumulation and long retention of the sensitizer in the patient skin, leading to prolonged (days to months) skin phototoxicity; and (3) small or even no differentiation between the PDT effect on illuminated tumor and non-tumor tissues. The drawbacks of current drugs inspired an extensive search for long wavelength absorbing second-generation sensitizers that exhibit better differentiation between their retention in tumor cells and skin or other normal tissues.
In order to optimize the performance of the porphyrin drugs in therapeutics and diagnostics, several porphyrin derivatives have been proposed in which, for example, there is a central metal atom (other than Mg) complexed to the four pyrrole rings, and/or the peripheral substituents of the pyrrole rings are modified and/or the macrocycle is dihydrogenated to chlorophyll derivatives (chlorins) or tetrahydrogenated to bacteriochlorophyll derivatives (bacteriochlorins).
Due to their intense absorption in favorable spectral regions (650-850 nm) and their ready degradation after treatment, chlorophyll and bacteriochlorophyll derivatives have been identified as excellent sensitizers for PDT of tumors and to have superior properties in comparison to porphyrins, but they are less readily available and more difficult to handle.
Bacteriochlorophylls are of potential advantage compared to the chlorophylls because they show intense near-infrared bands, i.e. at considerably longer wavelengths than chlorophyll derivatives.
The spectra, photophysics, and photochemistry of native bacteriochlorophylls (Bchls) have made them optimal light-harvesting molecules with clear advantages over other sensitizers presently used in PDT. In particular, these molecules have a very high extinction coefficient at long wavelengths (λmax=760-780 nm, ε=(4-10)xl04 M-1cm-1), where light penetrates deeply into tissues. They also generate reactive oxygen species (ROS) at a high quantum yield (depending on the central metal).
Under normal delivery conditions, i.e. in the presence of oxygen at room temperature and under normal light conditions, the BChl moieties are labile and have somewhat lower quantum yields for triplet state formation, when compared with, e.g., hematoporphyrin derivative (HPD). However, their possible initiation of biological redox reactions, favorable spectral characteristics and their ready degradation in vivo result in the potential superiority of bacteriochlorophylls over other compounds, e.g. porphyrins and chlorophylls, for PDT therapy and diagnostics and for killing of cells, viruses and bacteria in samples and in living tissue. Chemical modification of bacteriochlorophylls is expected to further improve their properties, but this has been very limited due to lack of suitable methods for the preparation of such modified bacteriochlorophylls .
The biological uptake and PDT efficacy of metal-free derivatives of Bchl have been studied with the objective to manipulate the affinity of the sensitizers to the tumor cellular compartment. Cardinal to this approach is the use of highly lipophilic drugs that may increase the accumulation of the drug in the tumor cells, but also renders its delivery difficult. In addition, the reported biodistribution shows significant phototoxic drug levels in non-tumor tissues over prolonged periods (at least days) after administering the drug.
In applicant’s previous Israel Patent No. 102645 and corresponding EP 0584552, US 5,726,169, US 5,726,169, US 5,955,585 and US 6,147,195, a different approach was taken by the inventors. Highly efficient anti- vascular sensitizers that do not extravasate from the circulation after administration and have short lifetime in the blood were studied. It was expected that the inherent difference between vessels of normal and abnormal tissues such as tumors or other tissues that rely on neovessels, would enable relatively selective destruction of the abnormal tissue. Hence, it was aimed to synthesize Bchl derivatives that are more polar and, hence, have better chance to stay in the vascular compartment, where they convey the primary photodynamic effect. To this end, the geranylgeranyl residue at the C-17 position of Bchl a (Compound 1, depicted in Scheme 1 herein) has been replaced by various residues such as amino acids, peptides, or proteins, which enhance the sensitizer hydrophilicity. One particular derivative, Bchl-Ser (Scheme 1, Compound 1, wherein R is seryl), was found to be water-soluble and highly phototoxic in cell cultures. Following infraperitoneal injection, the Bchl-Ser cleared from the mouse blood and tissues bi-exponentially in a relatively short time (t1/2~2 and 16 h, respectively). Clearance from the circulation was even faster following intravenous injection. Under the selected treatment protocol (light application within minutes after drug injection), phototoxicity was predominantly conferred to the tumor vasculature (Rosenbach-
Belkin et al., 1996; Zilberstein et al., 2001 and 1997). However, unfortunately, like native Bchl, the Bchl-Ser derivative undergoes rapid photo-oxidation, forming the corresponding 2-desvinyl-2-acetyl-chlorophyllide ester and other products.
To increase the stability of the Bchl derivatives, the central Mg atom was replaced by Pd in the later applicant’s PCT Publication WO 00/33833 and US 6,569,846. This heavy atom was previously shown to markedly increase the oxidation potential of the Bchl macrocycle and, at the same time, to greatly enhance the intersystem-crossing (ISC) rate of the molecule to its triplet state. The metal replacement was performed by direct incorporation of Pd2+ ion into a Bpheid molecule, as described in WO 00/33833. Based on the pigment biodistribution and pharmacokinetics, it was assumed that the derivative Pd-Bpheid remained in the circulation for a very short time with practically no extravasation to other tissues, and is therefore a good candidate for vascular-targeting PDT that avoids skin phototoxicity. The treatment effect on the blood vessels was demonstrated by intravital microscopy of treated blood vessels and staining with Evans-Blue. Using a treatment protocol with a minimal drug-to-light interval, Pd-Bpheid (also designated Tookad) was found to be effective in the eradication of different tumors in mice, rats and other animal models and is presently entering Phase I/II clinical trials in patients with prostate cancer that failed radiation therapy (Chen et al, 2002; Schreiber et al., 2002; Koudinova et al., 2003).
Because of its low solubility in aqueous solutions, the clinical use of Pd-Bpheid requires the use of solubilizing agents such as Cremophor that may cause side effects at high doses. It would be highly desirable to render the Pd-Bpheid water-soluble while retaining its physico-chemical properties. Alternatively, it would be desirable to prepare Bchl derivatives that are cytophototoxic and, at the same time, more water-soluble than Pd-Bpheid itself. Such water solubility is expected to further enhance the drug retention in the circulation and, thereby, the aforementioned selectivity. In addition, having no need to use carriers such as detergents or lyposomes, may prevent side effects.
SYNTHESIS
START FROM CAS 17499-98-8, Phorbine, magnesium deriv., Bacteriochlorophyll aP
PADELIPORFIN
Paper
Novel water-soluble bacteriochlorophyll derivatives for vascular-targeted photodynamic therapy: Synthesis, solubility, phototoxicity and the effect of serum proteins
Photochemistry and Photobiology (2005), 81, (July/Aug.), 983-993
PAPER
Journal of Medicinal Chemistry (2014), 57(1), 223-237

With the knowledge that the dominant photodynamic therapy (PDT) mechanism of 1a (WST09) switched from type 2 to type 1 for 1b (WST11) upon taurine-driven E-ring opening, we hypothesized that taurine-driven E-ring opening of bacteriochlorophyll derivatives and net-charge variations would modulate reactive oxygen species (ROS) photogeneration. Eight bacteriochlorophyll a derivatives were synthesized with varying charges that either contained the E ring (2a–5a) or were synthesized by taurine-driven E-ring opening (2b–5b). Time-dependent density functional theory (TDDFT) modeling showed that all derivatives would be type 2 PDT-active, and ROS-activated fluorescent probes were used to investigate the photogeneration of a combination of type 1 and type 2 PDT ROS in organic- and aqueous-based solutions. These investigations validated our predictive modeling calculations and showed that taurine-driven E-ring opening and increasing negative charge generally enhanced ROS photogeneration in aqueous solutions. We propose that these structure–activity relationships may provide simple strategies for designing bacteriochlorins that efficiently generate ROS upon photoirradiation.
Modulation of Reactive Oxygen Species Photogeneration of Bacteriopheophorbide a Derivatives by Exocyclic E-Ring Opening and Charge Modifications
CHEMICAL EXAMPLES
Example 1. Palladium 31-oxo-15-methoxycarbonylmethyl-Rhodobacteriochlorin 131-(2-sulfoethyl)amide dipotassium salt ( Compound 4)
Nine hundred and thirty five (935) mg of Pd-Bpheid (3) were dissolved in a 1 L round bottom flask with 120 ml of DMSO while stirring under Argon (bubbled in the solution). Taurine (1288 mg) was dissolved in 40 ml of 1M K2HPO4 buffer, and the pH of the solution was adjusted to 8.2 (with HCl ). This aqueous solution was added into the DMSO solution while stirring, and the Argon was bubbled in the solution for another 20 minutes. Then the reaction mixture was evaporated at 30°C for 3.5 hours under ~2 mbar and then for another 2 hours at 37°C to a complete dryness. The dry solids were dissolved in 300 ml of MeOH and the colored solution was filtered through cotton wool to get rid of buffer salts and taurine excess.
The progress of the reaction was determined by TLC (Rf of unreacted Pd- Bpheid is 0.8-0.85 and of the reaction (aminolysis) product is 0.08-0.1) and by following the optical absorption spectrum of the reaction mixture after liophylization and resolubihzation in MeOH. The absorption spectrum was characterized by a Qytransition shift from 756 nm (for Pd-Bpheid) to 747 nm (for the product 4) and by Qx shift from 534 nm of Pd-Bpheid to 519 nm (of the product 4). The MeOH was evaporated and the product 4 was purified by HPLC with ODS-A 250X20 S10P μm column (YMC, Japan). Solvent A: 95% 0.005 M phosphate buffer, pH 8.0 and 5% MeOH. Solvent B: 100% MeOH. The dry solid was dissolved in 42 ml of distilled water and injected in portions of 1.5 ml each .
The elution profile is described in Table 1. The product 4_(Scheme 1, see below) was eluted and collected at ~ 9-11 minutes. The main impurities, collected after at 4-7 min (ca 5-10%), corresponded to byproduct(s) with the proposed structure 7. Peaks at 22-25 min (ca 2-5%) possibly corresponded to the iso-form of the main product 4 and untreated Pd-Bpheid residues.
The solvent (aqueous methanol) was evaporated under reduced pressure. Then, the purified product 4 ]was re-dissolved in ~150 ml MeOH and filtered through cotton wool. The solvent was evaporated again and the solid pigment 4 was stored under Ar in the dark at -20°C. The reaction yield: ~90% (by weight, relative to 3).
The structure of product 4 was confirmed by electrospray mass spectroscopy. (ESI-MS, negative mode, Fig.2), (peaks at 875 (M–K-H), 859 (M–2K-H+Na), 837 (M–2K), 805 (M2K-H-OMe), 719) and 1H-NMR spectrum (Fig. 4 in MeOH-d4). Table 4 provides the shifts (in ppm units) of the major NMR peaks.
Optical absorption (UN-VIS) spectrum (MeOH): λ, 747 (1.00), 516 (0.13), 384 (0.41), 330 (0.50); ε747 (MeOH) is 1.2 x 105 mol-1 cm _1.
ΝMR (MeOH-d4): 9.38 (5-H, s), 8.78 (10-H, s), 8.59 (20-H, s), 5.31 and 4.95 (151-CH2, dd), 4.2-4.4 (7,8,17,18-H, m), 3.88 (153-Me, s), 3.52 (21-Me, s), 3.19 (121 -Me, s), 3.09 (32-Me, s), 1.92-2.41, 1.60-1.75 (171, 172-CH2, m), 2.19 (81-CH2, m), 1.93 (71-Me, d), 1.61 (181-Me, d), 1.09 (82-Me, t), 3.62, 3.05 (CH2‘s of taurine).
Octanol/water partition ratio is 40:60.
Example 2. Preparation of 31-oxo-15-methoxycarbonylmethyl- Rhodobacteriochlorin 131-(2-sulfoethyl)amide dipotassium salt (Compound 5) One hundred and sixty (160) mg of taurine were dissolved in 5 ml of 1M
K2HPO4 buffer, and the pH of the solution was adjusted to 8.2. This solution was added to 120 mg of compound 2 dissolved in 15 ml of DMSO, and the reaction and following purification were analogous to those described in previous Example.
Absorption spectrum (MeOH): λ, 750 (1.00), 519 (0.30), 354 (1.18) nm.
ESI-MS (-): 734 (M–2K).
ΝMR (MeOH-d4): 9.31 (5-H, s), 8.88 (10-H, s), 8.69 (20-H, s), 5.45 and 5.25 (151-CH2, dd), 4.35 (7,18-H, m), 4.06 (8,17-H, m), 4.20 and 3.61 (2-CH2, m of taurine), 3.83 (153-Me, s), 3.63 (21-Me, s), 3.52 (3-CH2, m oftaurine), 3.33 (121-Me, s), 3.23 (32-Me, s), 2.47 and 2.16 (171-CH2, m), 2.32 and 2.16 (81-CH2, m), 2.12 and 1.65 (172-CH2, m), 1.91 (71-Me, d), 1.66 (181– Me, d), 1.07 (82-Me, t).
Octanol/water partition ratio is 60:40.
Example 3. Preparation of copper(II) 31-oxo-15-methoxycarbonylmethyl- Rhodobacteriochlorin 131-(2-sulfoethyl)amide dipotassium salt (Compound 10)
Fifty (50) mg of compound 5 of Example 2 and 35 mg of copper (II) acetate were dissolved in 40 ml of methanol, and argon was bubbled into solution for 10 minutes. Then 500 mg of palmitoyl ascorbate was added, and the solution was stirred for 30 min. The absorption spectrum was characterized by a Qy transition shift from 750 nm (for 5) to 768 nm (for the product 10) and by Qx shift from 519 nm of 5 to 537 nm (of the product 10). Then the reaction mixture was evaporated, re-dissolved in acetone and filtered through cotton wool to get rid of acetate salt excess. The acetone was evaporated and the product was additionally purified by HPLC at the conditions mentioned above with the elution profile, described in Table 2.
The solvent (aqueous methanol) was evaporated under reduced pressure. Then, the purified pigment 10 was re-dissolved in methanol and filtered through cotton wool. The solvent was evaporated again and the solid pigment 10 was stored under Ar in the dark at -20°C. Reaction yield: -90%.
Absorption spectrum (MeOH): λ, 768 (1.00), 537 (0.22), 387 (0.71) and 342 (0.79) nm.
ESI-MS (-): 795 (M–2K).
Octanol/water partition ratio is 40:60.
Example 4. Preparation of zinc 31-oxo-15-methoxycarbonylmethyl-Rhodobacteriochlorin 131-(2-sulfoethyl)amide dipotassium salt (Compound 11)
Zn insertion into compound 5 was carried out with Zn acetate in acetic acid as previously described (US Patent No. 5,726,169). Final purification was carried out by HPLC in the same conditions as for compound 5 in Example 2 above.
Absorption spectrum (MeOH): λ, 762 (1.00), 558 (0.26), 390 (0.62) and 355 (0.84) nm.
Octanol/water partition ratio is 50:50.
Example 5. Preparation of manganese(III) 31-oxo-15-methoxycarbonylmethyl-Rhodobacteriochlorin 131-(2-sulfoethyl)amide dipotassium salt (Compound 12)
Mn insertion into compound 5 was carried out with Zn acetate in acetic acid as previously described (WO 97/19081; US 6,333,319) with some modifications. Thus, fifty (50) mg of compound 5 in 10 ml of DMF were stirred with 220 mg of cadmium acetate and heated under argon atmosphere at 110°C about 15 min (Cd-complex formation is monitored by shifting Qx transition absorption band from 519 to 585 nm in acetone). Then the reaction mixture was cooled and evaporated. The dry residue was re-dissolved in 15 ml of acetone and stirred with manganese (II) chloride to form the Mn(III)-product 12. The product formation is monitored by shifting Qx transition band from 585 to 600 nm and Qy transition band from 768 to 828 nm in acetone. The acetone was evaporated and the product 12 was additionally purified by HPLC in the conditions mentioned in Example 2 above with the elution profile described in Table 3 below where the] solvent system consists of: A – 5% aqueous methanol, B -methanol.
The solvent (aqueous methanol) was evaporated under reduced pressure and the solid pigment 12 was stored under Ar in the dark at -20°C.
Absorption spectrum (MeOH): λ, 828 (1.00), 588 (0.32) and 372 (0.80) nm. Octanol/water partition ratio is 5:95.
Example 6. Preparation of palladium bacteriopheophorbide a 17 -(3-sulfo-1-oxy- succinimide)ester sodium salt (Compound 6)
Fifty (50) mg of Pd-Bpheid (compound 2), 80 mg of N-hydroxy- sulfosuccinimide (sulfoNHS) and 65 mg of 1-(3-dimethylaminopropyl)-3- ethylcarbodiimide (EDC) were mixed in 7 ml of dry DMSO for overnight at room temperature. Then the solvent was evacuated under reduced pressure. The dry residue was re-dissolved in chloroform (ca. 50 ml), filtered from insoluble material, and evaporated. The conversion was ab. 95%) (TLC). The product 6 was used later on without further chromatographic purification. ESI-MS (-): 890 (M–Na).
NMR (CDCl3): 9.19 (5-H, s), 8.49 (10-H, s), 8.46 (20-H, s), 5.82 (132-H, s), 4.04- 4.38 (7,8,17,18-H, m), 3.85 (134-Me, s), 3.47 (21-Me, s), 3.37 (^-Me, s), 3.09 (32– Me, s), 1.77 (71-Me, d), 1.70 (lδ’-Me, d), 1.10 (82-Me, t), 4.05 (CH2 of sNHS), 3.45 (CH ofs NHS).
Example 7. Preparation of palladium bacteriopheophorbide a 173-(3-sulfopropyl) amide potassium salt (Compound 7)
Ten (10) mg of compound 6 in 1 ml of DMSO was mixed with 20 mg of homotaurine (3-amino-1-propane-sulfonic acid) in 1 ml of 0.1 M K-phosphate buffer, pH 8.0 for overnight. Then the reaction mixture was partitioned in chloroform/water. The organic layer was dried over anhydrous sodium sulfate and evaporated. The dry residue was re-dissolved in chloroform-methanol (19:1) and applied to a chromatographic column with silica. The product 7 was obtained with chloroform-methanol (4:1) elution. The yield was about 80-90%.
ESI-MS (-): 834 (M-K) m/z.
NMR (MeOH-d4): 9.16 (5-H, s), 8.71 (10-H, s), 8.60 (20-H, s), 6.05 (132-H, s), 4.51, 4.39, 4.11, 3.98 (7,8,17,18-H, all m), 3.92 (134-Me, s), 3.48 (21-Me, s), 3.36 (121-Me, s), 3.09 (32-Me, s), 2.02-2.42 (171 arid 172-CH2, m), 2.15 ( 81-CH2, q), 1.81 (71-Me, d), 1.72 (181-Me, d), 1.05 (82-Me, t), 3.04, 2.68, and 2.32 (CH2‘s of homotaurine, m).
Example 8. Preparation of palladium 31-oxo-15-methoxycarbonylmethyl-Rhodo-bacteriochlorin 13 ,17 -di(3-sulfopropyl)amide dipotassium salt (Compound 8)
Ten (10) mg of compound 6 or 7 were dissolved in 3 ml of DMSO, mixed with 100 mg of homotaurine in 1 ml of 0.5 M K-phosphate buffer, pH 8.2, and incubated overnight at room temperature. The solvent was then evacuated under reduced pressure as described above, and the product 8 was purified on HPLC. Yield: 83%.
Absorption spectrum (MeOH): 747 (1.00), 516 (0.13), 384 (0.41), 330 (0.50), ε747 =1.3×105 modern-1.
ESI-MS(-):1011 (M–K), 994 (M–2K+Na),972 (M–2K), 775 (M–2K-CO2Me-homotaurineNHCH2CH2CH2SO3), 486 ([M-2K]/2)
NMR (MeOH-d4): 9.35 (5-H, s), 8.75 (10-H, s), 8.60 (20-H, s), 5.28 and 4.98 (15-1-CH2, dd), 4.38, 4.32, 4.22, 4.15 (7,8,17,18-H, all m), 3.85 (15~3-Me, s), 3.51 (21-Me, s), 3.18 (121-Me, s), 3.10 (32-Me, s 2.12-2.41 (171-CH2, m), 2.15-2.34 (81-CR2, m), 1.76-2.02 (172-CH2, m), 1.89 (71-Me, d), 1.61 (lδ^Me, d), 1.07 (82-Me, t). 3.82, 3.70,
3.20, 3.10, 2.78, 2.32, 1.90 (CH2‘s of homotaurine at C-131 and C-173)
Example 9. Palladium 31-(3-sulfopropylimino)-15-methoxycarbonylmethyl-Rhodo-bacteriochlorin 131,173-di(3-sulfopropyl)amide tripotassium salt (Compound 9)
Compound 9 was obtained from HPLC as a minor product during synthesis of 8.
Absorption spectrum (MeOH): 729 (1.00), 502 (0.10), 380 (0.69), 328 (0.57).
ESI-MS (30.4.2000): 1171 (M-K+H), 1153 (M–2K-H+Na), 1131 (M-2K), 566 ([M-K]/2), 364 ([M-3K]/3).
NMR (MeOH-d4): 8.71 (1H), 8.63 (1.5H), 8.23 (0.5H) (5-, 10- and 20-H, all-m), 5.30 and 4.88 (151-CH2, dd), 4.43 and 4.25 (7,8,17,18-H, m), 3.85 (15~3-Me, s), 3.31 (21-Me, s), 3.22 (121-Me, s), 3.17 (32-Me, m), 1.89-2.44 (171 and 172-CH2, m), 2.25 (81-CH2, m), 1.91 (71-Me, s), 1.64 (181– Me, s), 1.08 (82-Me, t), 4.12, 3.56, 3.22, 3.16, 2.80 and 2.68 (CH2‘s of homotaurine).
Example 10. Palladium 31-oxo-15-methoxycarbonylmethyl-Rhodobacteriochlorin 131-(2-sulfoethyl)amide, 173-(N-immunoglobulin G)amide potassium salt (Compound 13)
Ten (10) mg of compound 4 were reacted with 20 mg of sulfo-NHS and 15 mg of EDC in 1 ml of dry DMSO for 1 hour at room temperature, then rabbit IgG (0.6 mg) in PBS (2.5 ml) was added, and the mixture was further incubated overnight at room temperature. The mixture was evaporated to dryness, then re-dissolved in 1 ml of PBS and loaded on Sephadex G-25 column equilibrated with PBS. A colored band was eluted with 4-5 ml of PBS. The pigment/protein ratio in the obtained conjugate 13 was determined by optical density at 753 and 280 mn, respectively, and varied between 0.5/1 to 1/1 of pigment 13/protein.
Example 11. Preparation of palladium 31-oxo-15-methoxycarbonylmethyl-Rhodobacteriochlorin 131-(2-carboxyethyl)amide dipotassium salt (Compound
M)
The preparation and purification of the title compound 14 were carried out as described in Example 2, by reaction of compound 2 with 3-aminopropionic acid (β-alanine) (150 mg) instead of taurine. Yield: 85%.
Example 12. Preparation of palladium 31-oxo-15-methoxycarbonylmethyl-Rhodobacteriochlorin 131-(3-phosphopropyl)amide tripotassium salt (Compound
15)
The preparation and purification of the title compound 15 were carried out as described in Example 2, by reaction of compound 2 with 3 -amino- 1-propanephosphonic acid (180 mg) instead of taurine. Yield: 68%.
Example 13. Palladium 31-(3-sulfopropylamino)-15-methoxycarbonylmethyl-Rhodobacteriochlorin 131,173-di(3-sulfopropyl)amide tripotassium salt (Compound 16)
For reduction of the imine group in 31-(3-sulfopropylimino) to the correspondent 31-(3-sulfopropylamino) group, compound 9 (8 mg) was reacted by stirring with sodium cyanoborohydride (15 mg) in 5 ml of methanol overnight at room temperature. Then the reaction mixture was treated with 0.05 M HCl (5 ml), neutralized with 0.01 M KOH, and evaporated. The title product 16 was purified using HPLC conditions as described in Example 2. Yield: 80-90%).
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3: Chevalier S, Anidjar M, Scarlata E, Hamel L, Scherz A, Ficheux H, Borenstein N, Fiette L, Elhilali M. Preclinical study of the novel vascular occluding agent, WST11, for photodynamic therapy of the canine prostate. J Urol. 2011 Jul;186(1):302-9. Epub 2011 May 20. PubMed PMID: 21600602.
4: Dandler J, Wilhelm B, Scheer H. Photochemistry of bacteriochlorophylls in human blood plasma: 1. Pigment stability and light-induced modifications of lipoproteins. Photochem Photobiol. 2010 Mar-Apr;86(2):331-41. Epub 2009 Nov 23. PubMed PMID: 19947966.
5: Dandler J, Scheer H. Inhibition of aggregation of [Pd]-bacteriochlorophyllides in mesoporous silica. Langmuir. 2009 Oct 20;25(20):11988-92. PubMed PMID: 19772311.
6: Ashur I, Goldschmidt R, Pinkas I, Salomon Y, Szewczyk G, Sarna T, Scherz A. Photocatalytic generation of oxygen radicals by the water-soluble bacteriochlorophyll derivative WST11, noncovalently bound to serum albumin. J Phys Chem A. 2009 Jul 16;113(28):8027-37. PubMed PMID: 19545111.
7: Moore CM, Pendse D, Emberton M. Photodynamic therapy for prostate cancer–a review of current status and future promise. Nat Clin Pract Urol. 2009 Jan;6(1):18-30. Review. PubMed PMID: 19132003.
8: Preise D, Oren R, Glinert I, Kalchenko V, Jung S, Scherz A, Salomon Y. Systemic antitumor protection by vascular-targeted photodynamic therapy involves cellular and humoral immunity. Cancer Immunol Immunother. 2009 Jan;58(1):71-84. Epub 2008 May 17. PubMed PMID: 18488222.
9: Fleshker S, Preise D, Kalchenko V, Scherz A, Salomon Y. Prompt assessment of WST11-VTP outcome using luciferase transfected tumors enables second treatment and increase in overall therapeutic rate. Photochem Photobiol. 2008 Sep-Oct;84(5):1231-7. Epub 2008 Apr 8. PubMed PMID: 18399928.
10: Berdugo M, Bejjani RA, Valamanesh F, Savoldelli M, Jeanny JC, Blanc D, Ficheux H, Scherz A, Salomon Y, BenEzra D, Behar-Cohen F. Evaluation of the new photosensitizer Stakel (WST-11) for photodynamic choroidal vessel occlusion in rabbit and rat eyes. Invest Ophthalmol Vis Sci. 2008 Apr;49(4):1633-44. PubMed PMID: 18385085.
11: Fabre MA, Fuseau E, Ficheux H. Selection of dosing regimen with WST11 by Monte Carlo simulations, using PK data collected after single IV administration in healthy subjects and population PK modeling. J Pharm Sci. 2007 Dec;96(12):3444-56. PubMed PMID: 17854075.
12: Brandis A, Mazor O, Neumark E, Rosenbach-Belkin V, Salomon Y, Scherz A. Novel water-soluble bacteriochlorophyll derivatives for vascular-targeted photodynamic therapy: synthesis, solubility, phototoxicity and the effect of serum proteins. Photochem Photobiol. 2005 Jul-Aug;81(4):983-93. PubMed PMID: 15839743.
13: Mazor O, Brandis A, Plaks V, Neumark E, Rosenbach-Belkin V, Salomon Y, Scherz A. WST11, a novel water-soluble bacteriochlorophyll derivative; cellular uptake, pharmacokinetics, biodistribution and vascular-targeted photodynamic activity using melanoma tumors as a model. Photochem Photobiol. 2005 Mar-Apr;81(2):342-51. PubMed PMID: 15623318.
14: Plaks V, Posen Y, Mazor O, Brandis A, Scherz A, Salomon Y. Homologous adaptation to oxidative stress induced by the photosensitized Pd-bacteriochlorophyll derivative (WST11) in cultured endothelial cells. J Biol Chem. 2004 Oct 29;279(44):45713-20. Epub 2004 Aug 31. PubMed PMID: 15339936.
////////PADELIPORFIN, WST11, WST-11, WST 11, Stakel, padeliporfin, palladiumbacteriopheophorbide monolysine taurine, EU 2017, EMA 2017
CCC1C(C2=NC1=CC3=C(C(=C([N-]3)C(=C4C(C(C(=N4)C=C5C(=C(C(=C2)[N-]5)C(=O)C)C)C)CCC(=O)O)CC(=O)OC)C(=O)NCCS(=O)(=O)O)C)C.[Pd+2]
Novel Drug Approvals for 2017, A Review/Compilation
CDSCO
DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO, Novel Drug Approvals for 2017, A Review Compilation (USFDA, EMA, PMDA, CDSCO).
Any errors in this compilation, email amcrasto@gmail.com, Call +919323115463
Some gaps will be filled up soon keep watching……………..
INDEX, NAME (click on the title, it contains link)
SECTION A; USFDA Approvals
6 BENRALIZUMAB
17 DURVALUMAB
24 GUSELKUMAB
36 OZENOXACIN
40 SARILUMAB
41 SECNIDAZOLE
INDEX, FORMULATION NAME
USFDA
•Aliqopa (COPANLISIB) to treat adults with relapsed follicular lymphoma — a slow-growing type of nonHodgkin lymphoma (a cancer of the lymph system) — who have received at least two prior systemic therapies;
• ALUNBRIG, BRIGATINIB, To treat patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib
• Austedo, Deutetrabenazine For the treatment of chorea associated with Huntington’s disease
• Bavencio (avelumab) for the treatment of patients 12 years and older with a rare and aggressive form of cancer called metastatic Merkel cell carcinoma, including those who have not received prior chemotherapy;
•BAXDELLA, Delafloxacin, BACTERIAL INFECTIONS
• Benznidazole to treat children ages 2 to 12 years with Chagas disease, a parasitic infection that can cause serious heart illness after years of infection, and can also affect swallowing and digestion. This is the first treatment approved in the United States for this rare disease;
• Besponsa (inotuzumab ozogamicin) for the treatment of adults with a type of cancer of the blood called relapsed or refractory B-cell precursor acute lymphoblastic leukemia;
•BEVYXXA, BETRIXABAN, For the prophylaxis of venous thromboembolism (VTE) in adult patients hospitalized for an acute medical illness
• BRINEURA, CERLIPONASE ALFA, To treat a specific form of Batten disease
• Calquence (ACALABRUTINIB) to treat adults with mantle cell lymphoma who have received at least one prior therapy. Mantle cell lymphoma is a particularly aggressive cancer;
• DUPIXENT, (DUPILUMAB) To treat adults with moderate-to-severe eczema (atopic dermatitis)
• Emflaza (deflazacort) to treat patients age 5 years and older with Duchenne muscular dystrophy, a rare genetic disorder that causes progressive muscle deterioration and weakness;
• FASENRA, BENRALIZUMAB, For add-on maintenance treatment of patients with severe asthma aged 12 years and older, and with an eosinophilic phenotype
• Giapreza (angiotensin II), for the treatment of hypotension in adults with distributive or vasodilatory shock (dangerously low blood pressure despite adequate heart function) whose blood pressure remains low despite receiving fluids and treatment with drugs called vasopressors;
• HEMLIBRA EMICIZUMAB To prevent or reduce the frequency of bleeding episodes in adult and pediatric patients with hemophilia A who have developed antibodies called Factor VIII (FVIII) inhibitors.
• Idhifa (enasidenib) for the treatment of adults with relapsed or refractory acute myeloid leukemia, a form of blood cancer, who have a specific genetic mutation;
• IMFINZI, DURVALUMAB To treat patients with locally advanced or metastatic urothelial carcinoma
• Ingrezza (valbenazine) to treat adults with tardive dyskinesia, a side effect of some antipsychotic medications whereby patients can experience uncontrollable stiff, jerky movements of their face and body, and other uncontrolled movements such as eye-blinking, sticking out the tongue, and arm-waving;
• KEVZARA SARILUMAB, RHEUMATOID ARTHRITIS
• KISQALI, RIBOCICLIB, To treat postmenopausal women with a type of advanced breast cancer
• Macrilen macimorelin acetate, For the diagnosis of adult growth hormone deficiency
• Mavyret (glecaprevir and pibrentasvir) to treat adults with chronic hepatitis C virus genotypes 1-6 without cirrhosis (liver disease) or with mild cirrhosis, including patients with moderate to severe kidney disease, as well as those who are on hemodialysis;
• Mepsevii (vestronidase alfa-vjbk) to treat patients with Sly syndrome or mucopolysaccharidosis type 7 – a rare genetic disorder where an enzyme deficiency results in skeletal abnormalities, developmental delay, enlarged liver and spleen, and narrowed airways, which can lead to respiratory infections;
• Nerlynx (neratinib) for the extended adjuvant treatment — a form of therapy administered after an initial treatment to further lower the risk of the cancer coming back — of early-stage, human epidermal growth factor receptor 2 (HER2)-positive breast cancer;
• OCREVUS, OCRELIZUMAB, To treat patients with relapsing and primary progressive forms of multiple sclerosis
• OZEMPIC SEMAGLUTIDE To improve glycemic control in adults with type 2 diabetes mellitus
•PARSABIV, ETELCALCETIDE, To treat secondary hyperparathyroidism in adult patients with chronic kidney disease undergoing dialysis
• Prevymis (letermovir) for prevention of an infection called cytomegalovirus (CMV) in patients who are receiving a bone marrow transplant. CMV disease can cause serious health issues in these patients;
• Radicava (edaravone) to treat patients with amyotrophic lateral sclerosis, commonly referred to as Lou Gehrig’s disease, a rare disease that attacks and kills the nerve cells that control voluntary muscles;
• RHOPRESSA, NETARSUDIL, To treat glaucoma or ocular hypertension
• Rydapt (midostaurin) to treat adults newly diagnosed with a form of blood cancer known as acute myeloid leukemia who have a specific genetic mutation called FLT3, in combination with chemotherapy;
• Siliq (brodalumab) to treat adults with moderate-to-severe plaque psoriasis, a chronic disorder in which the body’s immune system sends out faulty signals that speed growth of skin cells that then accumulate, causing red, flaky patches that can appear anywhere on the body;
•SOLOSEC, SECNIDAZOLE To treat bacterial vaginosis
• STEGLATRO ERTUGLIFLOZIN To improve glycemic control in adults with type 2 diabetes mellitus
• Symproic (Naldemedine) for the treatment of opioid-induced constipation in adults with chronic noncancer pain; • Tremfya (guselkumab) for the treatment of adults with moderate-to-severe plaque psoriasis;
• Trulance (plecanatide) to treat adults with chronic idiopathic constipation, which is a persistent condition of constipation due to unknown origin;
• TYMLOS, Abaloparatide, To treat osteoporosis in postmenopausal women at high risk of fracture or those who have failed other therapies
• Vabomere (vaborbactam and meropenem) for treatment of adults with complicated urinary tract infections, including pyelonephritis (kidney infection) caused by bacteria;
• Verzenio (abemaciclib) to treat adults who have hormone receptor (HR)-positive, HER2-negative advanced or metastatic breast cancer that has progressed after taking therapy that alters a patient’s hormones (endocrine therapy);
• Vosevi (sofosbuvir/velpatasvir/voxilaprevir) to treat adults with chronic hepatitis C virus genotypes 1-6 without cirrhosis (liver disease) or with mild cirrhosis;
• Xadago (safinamide) as an add-on treatment for patients with Parkinson’s disease who are currently taking levodopa/carbidopa and experiencing “off” episodes;
• XERMELO, TELOTRISTAT ETHYL combined with somatostatin analog (SSA) therapy to treat adults with carcinoid syndrome diarrhea that SSA therapy alone has inadequately controlled, and;
• XEPI OZENOXACIN TO TREAT IMPETIGO
•XERMELO, TELOTRISTAT ETHYL, To treat carcinoid syndrome diarrhea
• Zejula (niraparib) for the maintenance treatment (intended to delay cancer growth) of adults with recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer, whose tumors have completely or partially shrunk (complete or partial response, respectively) in response to platinum-based chemotherapy
USFDA
No. | Drug Name |
Active Ingredient | Approval Date | FDA-approved use on approval date |
---|---|---|---|---|
46. | Giapreza | angiotensin II | 12/21/2017 | To increase blood pressure in adults with septic or other distributive shock |
45. | Macrilen | macimorelin acetate | 12/20/2017 | For the diagnosis of adult growth hormone deficiency |
44. | Steglatro | ertugliflozin | 12/19/2017 | To improve glycemic control in adults with type 2 diabetes mellitus |
43. | Rhopressa | netarsudil | 12/18/2017 | To treat glaucoma or ocular hypertension |
42. | Xepi | ozenoxacin | 12/11/2017 | To treat impetigo Drug Trials Snapshot |
41. | Ozempic | semaglutide | 12/5/2017 | To improve glycemic control in adults with type 2 diabetes mellitus |
40. | Hemlibra | emicizumab | 11/16/2017 | To prevent or reduce the frequency of bleeding episodes in adult and pediatric patients with hemophilia A who have developed antibodies called Factor VIII (FVIII) inhibitors. |
39. | Mepsevii | vestronidase alfa-vjbk | 11/15/2017 | To treat pediatric and adult patients with an inherited metabolic condition called mucopolysaccharidosis type VII (MPS VII), also known as Sly syndrome. |
38. | Fasenra | benralizumab | 11/14/2017 | For add-on maintenance treatment of patients with severe asthma aged 12 years and older, and with an eosinophilic phenotype Drug Trials Snapshot |
37. | Prevymis | letermovir | 11/8/2017 | To prevent infection after bone marrow transplant Drug Trials Snapshot |
36. | Vyzulta | latanoprostene bunod ophthalmic solution | 11/2/2017 | To treat intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Drug Trials Snapshot |
35. | Calquence | acalabrutinib | 10/31/2017 | To treat adults with mantle cell lymphoma Press Release Drug Trials Snapshot |
34. | Verzenio | abemaciclib | 9/28/2017 | To treat certain advanced or metastatic breast cancers Press Release Drug Trials Snapshot |
33. | Solosec | secnidazole | 9/15/2017 | To treat bacterial vaginosis Drug Trials Snapshot |
32. | Aliqopa | copanlisib | 9/14/2017 | To treat adults with relapsed follicular lymphoma Press Release Drug Trials Snapshot |
31. | benznidazole | benznidazole | 8/29/2017 | To treat children ages 2 to 12 years old with Chagas disease Press Release Drug Trials Snapshot |
30. | Vabomere | meropenem and vaborbactam | 8/29/2017 | To treat adults with complicated urinary tract infections Press Release Drug Trials Snapshot |
29. | Besponsa | inotuzumab ozogamicin | 8/17/2017 | To treat adults with relapsed or refractory acute lymphoblastic leukemia Press Release Drug Trials Snapshot |
28. | Mavyret | glecaprevir and pibrentasvir | 8/3/2017 | To treat adults with chronic hepatitis C virus Press Release Drug Trials Snapshot |
27. | Idhifa | enasidenib | 8/1/2017 | To treat relapsed or refractory acute myeloid leukemia Press Release Drug Trials Snapshot |
26. | Vosevi | sofosbuvir, velpatasvir and voxilaprevir | 7/18/2017 | To treat adults with chronic hepatitis C virus Press Release Drug Trials Snapshot |
25. | Nerlynx | neratinib maleate | 7/17/2017 | To reduce the risk of breast cancer returning Press Release Drug Trials Snapshot |
24. | Tremfya | guselkumab | 7/13/2017 | For the treatment of adult patients with moderate-to-severe plaque psoriasis Drug Trials Snapshot |
23. | Bevyxxa | betrixaban | 6/23/2017 | For the prophylaxis of venous thromboembolism (VTE) in adult patients hospitalized for an acute medical illness Drug Trials Snapshot |
22. | Baxdela | delafloxacin | 6/19/2017 | To treat patients with acute bacterial skin infections Drug Trials Snapshot |
21. | Kevzara | sarilumab | 5/22/2017 | To treat adult rheumatoid arthritis Drug Trials Snapshot |
20. | Radicava | edaravone | 5/5/2017 | To treat patients with amyotrophic lateral sclerosis (ALS) Press Release Drug Trials Snapshot |
19. | Imfinzi | durvalumab | 5/1/2017 | To treat patients with locally advanced or metastatic urothelial carcinoma Web Post Drug Trials Snapshot |
18. | Tymlos | abaloparatide | 4/28/2017 | To treat osteoporosis in postmenopausal women at high risk of fracture or those who have failed other therapies Drug Trials Snapshot |
17. | Rydapt | midostaurin | 4/28/2017 | To treat acute myeloid leukemia Press Release Chemistry Review(s) (PDF) Drug Trials Snapshot |
16. | Alunbrig | brigatinib | 4/28/2017 | To treat patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib Drug Trials Snapshot |
15. | Brineura | cerliponase alfa | 4/27/2017 | To treat a specific form of Batten disease Press Release Drug Trials Snapshot |
14. | Ingrezza | valbenazine | 4/11/2017 | To treat adults with tardive dyskinesia Press Release Chemistry Review(s) (PDF)Drug Trials Snapshot |
13. | Austedo | deutetrabenazine | 4/3/2017 | For the treatment of chorea associated with Huntington’s disease Drug Trials Snapshot, Chemistry Review(s) (PDF) |
12. | Ocrevus | ocrelizumab | 3/28/2017 | To treat patients with relapsing and primary progressive forms of multiple sclerosis Press Release Drug Trials Snapshot |
11. | Dupixent | dupilumab | 3/28/2017 | To treat adults with moderate-to-severe eczema (atopic dermatitis) Press Release Drug Trials Snapshot |
10. | Zejula | niraparib | 3/27/2017 | For the maintenance treatment for recurrent epithelial ovarian, fallopian tube or primary peritoneal cancers Press Release Drug Trials Snapshot |
9. | Symproic | naldemedine | 3/23/2017 |
For the treatment of opioid-induced constipation |
8. | Bavencio | avelumab | 3/23/2017 | To treat metastatic Merkel cell carcinoma Press Release Drug Trials Snapshot |
7. | Xadago | safinamide | 3/21/2017 | To treat Parkinson’s disease Press Release Drug Trials SnapshotChemistry Review(s) (PDF) |
6. | Kisqali | ribociclib | 3/13/2017 | To treat postmenopausal women with a type of advanced breast cancer Drug Trials Snapshot |
5. | Xermelo | telotristat ethyl | 2/28/2017 | To treat carcinoid syndrome diarrhea Press Release Drug Trials Snapshot |
4. | Siliq | brodalumab | 2/15/2017 | To treat adults with moderate-to-severe plaque psoriasis Press Release Drug Trials Snapshot |
3. | Emflaza | deflazacort | 2/9/2017 | To treat patients age 5 years and older with Duchenne muscular dystrophy (DMD) Press Release Drug Trials Snapshot |
2. | Parsabiv | etelcalcetide | 2/7/2017 | To treat secondary hyperparathyroidism in adult patients with chronic kidney disease undergoing dialysis Drug Trials Snapshot |
1. | Trulance | plecanatide | 1/19/2017 | To treat Chronic Idiopathic Constipation (CIC) in adult patients. Press Release Drug Trials Snapshot |
* This information is currently accurate. In rare instances, it may be necessary for FDA to change a drug’s new molecular entity (NME) designation or the status of its application as a novel new biologics license application (BLA). For instance, new information may become available which could lead to a reconsideration of the original designation or status. If changes must be made to a drug’s designation or the status of an application as a novel BLA, the Agency intends to communicate the nature of, and the reason for, any revisions as appropriate.
USFDA 2017 | ||||||
2017/12/21 | Angiotensin II | Giapreza | La Jolla Pharmaceutical | |||
2017/12/20 | Ertugliflozin | Steglatro | Merck Sharp Dohme | |||
2017/12/20 | Macimorelin acetate | Macrilen | Aeterna Zentaris GmbH | |||
2017/12/18 | Netarsudil mesylate | Rhopressa | Aerie Pharmaceuticals | |||
2017/12/11 | Ozenoxacin | Xepi | Ferrer Internacional S.A. | |||
2017/12/5 | Semaglutide | Ozempic | Novo Nordisk Inc | |||
2017/11/16 | Emicizumab | Hemlibra | Genentech | BLA | ||
2017/11/15 | Vestronidase alfa | Mepsevii | Ultragenyx Pharmaceutical | BLA | ||
2017/11/14 | Benralizumab | Fasenra | AstraZeneca AB | BLA | ||
2017/11/8 | Letermovir | Prevymis | Merck Sharp Dohme | |||
2017/11/2 | Latanoprostene bunod | Vyzulta | Bausch & Lomb Incorporated | |||
2017/10/31 | Acalabrutinib | Calquence | AstraZeneca Pharmaceuticals LP | |||
2017/9/28 | Abemaciclib | Verzenio | Eli Lilly | |||
2017/9/15 | Secnidazole | Solosec | Symbiomix Therapeutics | |||
2017/9/14 | Copanlisib | Aliqopa | Bayer Healthcare Pharmaceuticals | |||
2017/8/29 | Benznidazole | Chemo Research | ||||
2017/8/29 | Meropenem – Vaborbactam | Vabomere | Rempex Pharmaceuticals | |||
2017/8/17 | Inotuzumab ozogamicin | Besponsa | Wyeth Pharmaceuticals | BLA | ||
2017/8/3 | Glecaprevir – Pibrentasvir | Mavyret | AbbVie | |||
2017/8/1 | Enasidenib | Idhifa | Celgene Corporation | |||
2017/7/18 | Sofosbuvir – Velpatasvir – Voxilaprevir | Vosevi | Gilead Sciences | |||
2017/7/17 | Neratinib maleate | Nerlynx | Puma Biotechnology | |||
2017/7/13 | Guselkumab | Tremfya | Janssen Biotech | BLA | ||
2017/6/23 | Betrixaban | Bevyxxa | Portola Pharmaceuticals | |||
2017/6/19 | Delafloxacin meglumine | Baxdela | Melinta Therapeutics | |||
2017/5/22 | Sarilumab | Kevzara | Sanofi Synthelabo | BLA | ||
2017/5/5 | Edaravone | Radicava | Mitsubishi Tanabe Pharma America | |||
2017/5/1 | Durvalumab | Imfinzi | AstraZeneca UK | BLA | ||
2017/4/28 | Abaloparatide | Tymlos | Radius Health | |||
2017/4/28 | Midostaurin | Rydapt | Novartis Pharmaceuticals | |||
2017/4/28 | Brigatinib | Alunbrig | Ariad Pharmaceuticals | |||
2017/4/27 | Cerliponase alfa | Brineura | BioMarin Pharmaceutical | BLA | ||
2017/4/11 | Valbenazine | Ingrezza | Neurocrine Biosciences | |||
2017/4/3 | Deutetrabenazine | Austedo | Teva Pharmaceuticals | |||
2017/3/28 | Ocrelizumab | Ocrevus | Genentech | BLA | ||
2017/3/28 | Dupilumab | Dupixent | Regeneron Pharmaceuticals | BLA | ||
2017/3/27 | Niraparib | Zejula | Tesaro | |||
2017/3/23 | Naldemedine tosylate | Symproic | Shionogi | |||
2017/3/23 | Avelumab | Bavencio | EMD Serono | BLA | ||
2017/3/23 | Safinamide mesylate | Xadago | Newron Pharmaceuticals | |||
2017/3/21 | Ribociclib | Kisqali | Novartis Pharmaceuticals | |||
2017/2/28 | Telotristat ethyl | Xermelo | Lexicon Pharmaceuticals | |||
2017/2/15 | Brodalumab | Siliq | Valeant Pharmaceuticals | BLA | ||
2017/2/9 | Deflazacort | Emflaza | Marathon Pharmaceuticals | |||
2017/2/8 | Etelcalcetide hydrochloride | Parsavib | KAI Pharmaceuticals | |||
2017/1/19 | Plecanatide | Trulance | Synergy Pharmaceuticals |
1 Abaloparatide
RADIUS
FDA 4/28/2017
To treat osteoporosis in postmenopausal women at high risk of fracture or those who have failed other therapies
Drug Trials Snapshot
2 Abemaciclib
ELI LILLY
Verzenio | abemaciclib | FDA 9/28/2017 | To treat certain advanced or metastatic breast cancers Press Release Drug Trials Snapshot |
LINK https://newdrugapprovals.org/2015/10/19/abemaciclib-bemaciclib/
3 Acalabrutinib
Calquence | FDA APPROVED
10/31/2017 |
To treat adults with mantle cell lymphoma Press Release Drug Trials Snapshot |
4 Angiotensin II
LA JOLLA
Giapreza | angiotensin II | 12/21/2017 | To increase blood pressure in adults with septic or other distributive shock Press Release Drug Trials Snapshot |
5 AVELUMAB
MERCK
Bavencio | FDA 3/23/2017 | To treat metastatic Merkel cell carcinoma Press Release Drug Trials Snapshot |
6 BENRALIZUMAB
ASTRA ZENECA
Fasenra benralizumab
FDA 11/14/2017
For add-on maintenance treatment of patients with severe asthma aged 12 years and older, and with an eosinophilic phenotype
Drug Trials Snapshot
7 Benznidazole
CHEMO RESEARCH
benznidazole | FDA
8/29/2017 |
To treat children ages 2 to 12 years old with Chagas disease Press Release Drug Trials Snapshot |
8 BETRIXABAN
PORTOLA PHARMA
Bevyxxa | FDA
6/23/2017 |
For the prophylaxis of venous thromboembolism (VTE) in adult patients hospitalized for an acute medical illness Drug Trials Snapshot
|
9 BRIGATINIB
TAKEDA
Alunbrig | FDA
4/28/2017 |
To treat patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib Drug Trials Snapshot |
10 BRODALUMAB
VALEANT PHARMA
Siliq | FDA
2/15/2017 |
To treat adults with moderate-to-severe plaque psoriasis Press Release Drug Trials Snapshot |
LINK ,,,,https://newdrugapprovals.org/2017/02/16/fda-approves-new-psoriasis-drug-siliq-brodalumab/
11 CERLIPONASE ALFA
Brineura | FDA 4/27/2017 | To treat a specific form of Batten disease Press Release Drug Trials Snapshot |
12 Copanlisib
Aliqopa | FDA APPROVED
9/14/2017 |
To treat adults with relapsed follicular lymphoma Press Release Drug Trials Snapshot |
LINK…..https://newdrugapprovals.org/2017/11/20/copanlisib/
13 DEFLAZACORT
MARATHON PHARMA
Emflaza | FDA 2/9/2017 | To treat patients age 5 years and older with Duchenne muscular dystrophy (DMD) Press Release Drug Trials Snapshot |
LINK……https://newdrugapprovals.org/2017/02/17/deflazacort/
14 DELAFLOXACIN
Baxdela | FDA APPROVED
6/19/2017 |
To treat patients with acute bacterial skin infections |
LINK……..https://newdrugapprovals.org/2018/01/25/delafloxacin/
15 Deutetrabenazine
TEVA
LINK……………https://newdrugapprovals.org/2015/08/15/sd-809-deutetrabenazine-nda-submitted-by-teva/
Austedo | FDA 4/3/2017 | For the treatment of chorea associated with Huntington’s disease Drug Trials Snapshot Chemistry Review(s) (PDF) |
16 DUPILUMAB
SANOFI/REGENERON
Dupixent | FDA | 3/28/2017 | To treat adults with moderate-to-severe eczema (atopic dermatitis) Press Release Drug Trials Snapshot |
LINK…….https://newdrugapprovals.org/2017/03/29/fda-approves-new-eczema-drug-dupixent-dupilumab/
17 DURVALUMAB
ASTRA ZENECA
durvalumab FDA 5/1/2017To treat patients with locally advanced or metastatic urothelial carcinoma
Web Post
Drug Trials Snapshot
18 EDAVARONE
MITSUBISHI TANABE
Radicava | FDA 5/5/2017 | To treat patients with amyotrophic lateral sclerosis (ALS) Press Release Drug Trials Snapshot |
19 EMICIZUMAB
ROCHE
Hemlibra | emicizumab | FDA 11/16/2017 | To prevent or reduce the frequency of bleeding episodes in adult and pediatric patients with hemophilia A who have developed antibodies called Factor VIII (FVIII) inhibitors. Press Release Drug Trials Snapshot |
20 Enasidenib
Idhifa | FDA
8/1/2017 |
To treat relapsed or refractory acute myeloid leukemia Press Release Drug Trials Snapshot |
21 Ertugliflozin
MERCK
Steglatro | ertugliflozin | FDA
12/19/2017 |
To improve glycemic control in adults with type 2 diabetes mellitus Drug Trials Snapshot |
LINK https://newdrugapprovals.org/2014/02/10/ertugliflozin/
22 ETELCALCETIDE
Amgen
Parsabiv | FDA APPROVED
2/7/2017 |
To treat secondary hyperparathyroidism in adult patients with chronic kidney disease undergoing dialysis Drug Trials SnapshotSYNTHESIS LINK……..https://cen.acs.org/articles/96/i4/the-year-in-new-drugs-2018.html |
SYNTHESIS LINK……..https://cen.acs.org/articles/96/i4/the-year-in-new-drugs-2018.html
23 GLECAPREVIR
ABBVIE
Mavyret | glecaprevir and pibrentasvir | FDA 8/3/2017 | To treat adults with chronic hepatitis C virus Press Release Drug Trials Snapshot |
LINK https://newdrugapprovals.org/2016/10/05/glecaprevir-abt-493/
24 GUSELKUMAB
JOHNSON AND JOHNSON
guselkumab
FDA 7/13/2017
For the treatment of adult patients with moderate-to-severe plaque psoriasis
Drug Trials Snapshot
25 Inotuzumab ozogamicin
PFIZER
Besponsa | FDA
8/17/2017 |
To treat adults with relapsed or refractory acute lymphoblastic leukemia Press Release Drug Trials Snapshot |
26 LATANOPROSTENE
VALEANT
latanoprostene bunod ophthalmic solution
FDA 11/2/2017
To treat intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
Drug Trials Snapshot
27 LETERMOVIR
MERCK
Prevymis | FDA 11/8/2017 | To prevent infection after bone marrow transplant Drug Trials Snapshot |
LINK https://newdrugapprovals.org/2016/05/16/letermovir-aic-246/
28 Macimorelin acetate
AETERNA ZENTARIS
Macrilen | macimorelin acetate | FDA
12/20/2017 |
For the diagnosis of adult growth hormone deficiency Drug Trials Snapshot |
29 MEROPENEM
30 MIDOSTAURIN
NOVARTIS
- Chemistry Review(s) (PDF)
Rydapt | FDA
4/28/2017 |
To treat acute myeloid leukemia Press Release Drug Trials Snapshot |
31 Naldemedine
FDA 3/23/2017, Symproic, For the treatment of opioid-induced constipation
32 NERATINIB MALEATE
PUMA BIOTECH
Nerlynx | FDA | 7/17/2017 | To reduce the risk of breast cancer returning Press Release Drug Trials Snapshot |
33 NETARSUDIL
Rhopressa | FDA APPROVED
12/18/2017 |
To treat glaucoma or ocular hypertension |
LINK……https://newdrugapprovals.org/2018/01/29/netarsudil/
34 NIRAPARIB
TESARO
Zejula | FDA | 3/27/2017 | For the maintenance treatment for recurrent epithelial ovarian, fallopian tube or primary peritoneal cancers Press Release Drug Trials Snapshot |
LINK…https://newdrugapprovals.org/2016/12/22/niraparib-mk-4827/
35 OCRELIZUMAB
ROCHE
Ocrevus | FDA | 3/28/2017 | To treat patients with relapsing and primary progressive forms of multiple sclerosis Press Release Drug Trials Snapshot |
36 OZENOXACIN
MEDIMETRIX
Xepi | ozenoxacin | FDA
12/11/2017 |
To treat impetigo Drug Trials Snapshot |
37 Pibrentasvir
ABBVIE
Mavyret | glecaprevir and pibrentasvir | FDA 8/3/2017 | To treat adults with chronic hepatitis C virus Press Release Drug Trials Snapshot |
LINK https://newdrugapprovals.org/2016/06/08/abt-530-pibrentasvir/
38 PLECANATIDE
Plecanatide 普卡那肽 ليكاناتيد плеканатид
SYNERGY PHARMA
Trulance | FDA APPROVED
1/19/2017 |
To treat Chronic Idiopathic Constipation (CIC) in adult patients. Press Release Drug Trials Snapshot |
39 RIBOCICLIB
NOVARTIS
Structure..link for correct structure
Kisqali | FDA 3/13/2017 | To treat postmenopausal women with a type of advanced breast cancer Drug Trials Snapshot |
LINK https://newdrugapprovals.org/2015/10/19/ribociclib/
40 SARILUMAB
SANOFI /REGENERON
Kevzara | sarilumab | FDA 5/22/2017 | To treat adult rheumatoid arthritis Drug Trials Snapshot |
LINK https://newdrugapprovals.org/2013/11/25/late-stage-success-for-sanofiregeneron-ra-drug-sarilumab/
41 SECNIDAZOLE
SYMBIOMIX
Solosec | FDA | 9/15/2017 | To treat bacterial vaginosis Drug Trials Snapshot |
42 SAFINAMIDE
NEWRON PHARMA
- Chemistry Review(s) (PDF) for correct structure
Xadago | FDA 3/21/2017 | To treat Parkinson’s disease Press Release Drug Trials Snapshot |
43 Semaglutide
NOVO NORDISK
Ozempic | semaglutide | FDA
12/5/2017 |
To improve glycemic control in adults with type 2 diabetes mellitus Drug Trials Snapshot |
LINK https://newdrugapprovals.org/2013/07/22/a-survey-of-promising-late-stage-diabetes-drugs/
44 SOFOSBUVIR
45 TELOTRISTAT ETHYL
LEXICON
Xermelo | FDA
2/28/2017 |
To treat carcinoid syndrome diarrhea Press Release Drug Trials Snapshot |
46 VABORBACTAM
THE MEDICINES CO
Vabomere | meropenem and vaborbactam | FDA
8/29/2017 |
To treat adults with complicated urinary tract infections Press Release Drug Trials Snapshot |
47 VALBENAZINE
NEUROCRINE
- Chemistry Review(s) (PDF)
Ingrezza | FDA
4/11/2017 |
To treat adults with tardive dyskinesia Press Release Drug Trials Snapshot |
48 Vestronidase alfa-vjbk
ULTRAGENYX
Mepsevii | vestronidase alfa-vjbk | FDA 11/15/2017 | To treat pediatric and adult patients with an inherited metabolic condition called mucopolysaccharidosis type VII (MPS VII), also known as Sly syndrome. Press Release Drug Trials Snapshot |
49 VELPATASVIR
50 VOXILAPREVIR
GILEAD
Vosevi | sofosbuvir, velpatasvir and voxilaprevir | FDA 7/18/2017 | To treat adults with chronic hepatitis C virus Press Release Drug Trials Snapshot |
SECTION B; EMA approvals
European Medicines Agency’s – Human medicines: Highlights of 2017
Advances in medicines authorizations are essential for public health as they have the potential to improve treatment of diseases. In 2017, EMA recommended 92 medicines for marketing authorization. Of these, 35 had a new active substance, which has never been authorized in the European Union (EU) before. Many of these medicines represent a significant improvement in their therapeutic areas; they include medicines for children, for rare diseases and advanced therapies42. Amongst the 35 new active substances (NAS) that EMA recommended, 11 were new drugs and biologics to treat cancer, 05 to treat neurological disorders, 04 for infectious diseases, 04 for immunology/rheumatology, 03 for endocrinology, 02 each for Uro-nephrology, haematology, and dermatology, 01 for Pneumonology, and 01 for hepatology/gastroenterology class of drugs.
EUROPE
2017/11/16 | Niraparib | Zejula | Tesaro UK Limited | O | NME | ||
2017/11/10 | Adalimumab | Cyltezo | Boehringer Ingelheim International GmbH | B | |||
2017/11/10 | Miglustat | Miglustat Gen.Orph | Gen.Orph | G | |||
2017/11/10 | Ritonavir | Ritonavir Mylan | MYLAN S.A.S | G | |||
2017/11/10 | Padeliporfin | Tookad | STEBA Biotech S.A | ||||
2017/11/10 | Guselkumab | Tremfya | Janssen-Cilag International N.V. | BLA | |||
2017/9/27 | Dupilumab | Dupixent | sanofi-aventis groupe | BLA | |||
2017/9/21 | Darunavir / Cobicistat / Emtricitabine / Tenofovir alafenamide | Symtuza | Janssen-Cilag International N.V. | ||||
2017/9/21 | Atezolizumab | Tecentriq | Roche Registration Limited | BLA | |||
2017/9/18 | Avelumab | Bavencio | Merck Serono Europe Limited | O | BLA | ||
2017/9/18 | Entecavir | Entecavir Mylan | Mylan S.A.S | G | |||
2017/9/18 | Lacosamide | Lacosamide Accord | Accord Healthcare Ltd | G | |||
2017/9/18 | Midostaurin | Rydapt | Novartis Europharm Ltd | O | NME | ||
2017/9/18 | Telotristat ethyl | Xermelo | Ipsen Pharma | O | NME | ||
2017/9/5 | Trientine | Cuprior | GMP-Orphan SA | ||||
2017/9/5 | Efavirenz / Emtricitabine / Tenofovir disoproxil | Efavirenz/Emtricitabine/Tenofovir disoproxil Mylan | Mylan S.A.S | G | |||
2017/8/24 | Tivozanib hydrochloride monohydrate | Fotivda | EUSA Pharma (UK) Limited | NME | |||
2017/8/24 | Adalimumab | Imraldi | Samsung Bioepis UK Limited (SBUK) | B | |||
2017/8/24 | Nitisinone | Nitisinone MDK (previously Nitisinone MendeliKABS) | MendeliKABS Europe Ltd | G | |||
2017/8/22 | Ribociclib | Kisqali | Novartis Europharm Ltd | NME | |||
2017/8/22 | Cladribine | Mavenclad | Merck Serono Europe Limited | ||||
2017/7/26 | Glecaprevir / Pibrentasvir | Maviret | AbbVie Limited | NME | |||
2017/7/26 | Sofosbuvir / Velpatasvir / Voxilaprevi | Vosevi | Gilead Sciences International Ltd | NME | |||
2017/7/19 | Insulin lispro | Insulin lispro Sanofi | sanofi-aventis groupe | B | |||
2017/7/19 | Patiromer sorbitex calcium | Veltassa | Vifor Fresenius Medical Care Renal Pharma France | NME | |||
2017/7/17 | Efavirenz / Emtricitabine / Tenofovir disoproxil | Efavirenz/Emtricitabine/Tenofovir disoproxil Zentiva | Zentiva k.s. | G | |||
2017/7/17 | Brodalumab | Kyntheum | LEO Pharma A/S | BLA | |||
2017/7/17 | beclometasone / formoterol / glycopyrronium bromide | Trimbow | Chiesi Farmaceutici S.p.A. | ||||
2017/7/13 | Rituximab | Blitzima | Celltrion Healthcare Hungary Kft. | B | |||
2017/7/13 | Cariprazine | Reagila | Gedeon Richter | ||||
2017/7/10 | Spheroids of human autologous matrix-associated chondrocytes | Spherox | CO.DON AG | ||||
2017/7/6 | Cenegermin | Oxervate | Dompe farmaceutici s.p.a. | O | BLA | ||
2017/6/29 | Inotuzumab ozogamicin | Besponsa | Pfizer Limited | O | BLA | ||
2017/6/23 | Etanercept | Erelzi | Sandoz GmbH | ||||
2017/6/23 | Sarilumab | Kevzara | Sanofi-Aventis Groupe | NME | |||
2017/6/23 | Dimethyl fumarate | Skilarence | Almirall S.A | ||||
2017/6/23 | Carglumic acid | Ucedane | Lucane Pharma | G | |||
2017/6/15 | Rituximab | Rixathon, Riximyo B | Sandoz GmbH | ||||
2017/6/2 | Pentosan polysulfate sodium | Elmiron | bene-Arzneimittel GmbH | ||||
2017/6/2 | Nonacog beta pegol | Refixia | Novo Nordisk A/S | BLA | |||
2017/5/30 | Cerliponase alfa | Brineura | BioMarin International Limited | O E | BLA | ||
2017/5/30 | Nusinersen | Spinraza | Biogen Idec Ltd | O | NME | ||
2017/5/24 | Meningococcal group b vaccine (recombinant, adsorbed) | Trumenba | Pfizer Limited | ||||
2017/5/22 | Ivabradine | Ivabradine Accord | Accord Healthcare Ltd | G | |||
2017/5/8 | Dinutuximab beta | Dinutuximab beta Apeiron | Apeiron Biologics AG | O E | |||
2017/4/28 | Emtricitabine – tenofovir disoproxil mixt | Emtricitabine/Tenofovir disoproxil Krka d.d. | KRKA, d.d., Novo mesto | G | |||
2017/4/24 | Parathyroid hormone | Natpar | Shire Pharmaceuticals Ireland Ltd | O C | BLA | ||
2017/4/20 | Edoxaban | Roteas | Daiichi Sankyo Europe GmbH | ||||
2017/3/22 | Tofacitinib citrate | Xeljanz | Pfizer Limited | NME | |||
2017/3/20 | Umeclidinium | Rolufta | GlaxoSmithKline Trading Services Limited | ||||
2017/3/3 | Chlormethine | Ledaga | Actelion Registration Ltd. | O | |||
2017/2/27 | Pregabalin | Pregabalin Zentiva | Zentiva k.s. | G | |||
2017/2/17 | Rituximab | Truxima | Celltrion Healthcare Hungary Kft. | B | |||
2017/2/13 | Etanercept | Lifmior | Pfizer Limited | ||||
2017/2/13 | Baricitinib | Olumiant | Eli Lilly Nederland B.V. | NME | |||
2017/1/19 | Mercaptamine | Cystadrops | Orphan Europe S.A.R.L. | O | |||
2017/1/18 | Bezlotoxumab | Zinplava | Merck Sharp & Dohme Limited | NME | |||
2017/1/11 | Teriparatide | Movymia | STADA Arzneimittel AG | B | |||
2017/1/11 | Insulin glargine / lixisenatide | Suliqua | Sanofi-Aventis Groupe | ||||
2017/1/9 | Insulin aspart | Fiasp | Novo Nordisk A/S | ||||
2017/1/9 | Tadalafil | Tadalafil | Mylan S.A.S | G | |||
2017/1/9 | Tenofovir alafenamide | Vemlidy | Gilead Sciences International Ltd | ||||
2017/1/4 | Lonoctocog alfa | Afstyla | CSL Behring GmbH | BLA | |||
2017/1/4 | Darunavir | Darunavir Mylan | Mylan S.A.S. | G | |||
2017/1/4 | Insulin glargine | Lusduna | Merck Sharp & Dohme Limited | B | |||
2017/1/4 | Teriparatide | Terrosa | Gedeon Richter Plc. | B |
SECTION B; EMA Approvals
Combined drugs USFDA+EMA +PMDA list are listed below. trying to simplify search
1 Abaloparatide USFDA
2 Abemaciclib USFDA
3 ACALABRUTINIB USFDA
3A ALOFISEL EMA
3B AMENAMEVIR JAPAN
4 ANGIOTENSIN II USFDA
4A Atezolizumab EMA
5 AVELUMAB USFDA+EMA
6 BENRALIZUMAB USFDA+EMA
6A BARICITINIB JAPAN
7 BENZNIDAZOLE USFDA
8 BETRIXABAN USFDA
9 BRIGATINIB USFDA
10 BRODALUMAB USFDA+EMA
10A BUROSUMAB EMA
10B CARIPRAZINE HYDROCHLORIDE EMA
11 CERLIPONASE ALPA USFDA+EMA
12 COPANLISIB USFDA
13 DEFLAZACORT USFDA
14 Delafloxacin USFDA
15 Deutetrabenazine USFDA
16DUPILUMAB USFDA+EMA
17 DURVALUMAB USFDA
18 EDAVARONE USFDA
19 EMICIZUMAB USFDA
20 Enasidenib USFDA
21 ERTUGLIFLOZIN USFDA
22 ETELCALCETIDE USFDA
22A FORODESINE JAPAN
22B FLUCICLOVINE EMA
23 GLECAPREVIR USFDA+EMA
24 GUSELKUMAB USFDA+EMA
25 INOTUZUMAB OZOGAMICIN USFDA+EMA
26 LATANOPROSTENE USFDA
27 LETERMOVIR USFDA+EMA
27A Utetium lu 177 dotatate EMA
28 MACIMORELIN ACETATE USFDA
29 MEROPENEM USFDA
30 MIDOSTAURIN USFDA+EMA
31 NALDEMEDINE USFDA
32 NERATINIB USFDA
33 NETARSUDIL USFDA
34A NONACOG EMA
34B NUCINERSEN EMA +Japan
35 Ocrelizumab USFDA+EMA
35A OXERVATE EMA
36 OZENOXACIN USFDA
36A PATIROMER EMA
36B PADELIPORFIN EMA
36C PEMAFIBRATE JAPAN
37 PIBRENTASVIR USFDA+EMA
38 PLECANATIDE USFDA
39A ROLAPITANT EMA
39BRURLOCTOCOG EMA
40 SARILUMAB USFDA+EMA
41 SECNIDAZOLE USFDA
42 SAFINAMIDE USFDA
43 SEMAGLUTIDE USFDA+EMA
43A SODIUM ZIRCONIUM CYCLOCYLICATE EMA
44 SOFOSBUVIR USFDA+EMA
44A SPHEROX EMA
45 TELOTRISTAT ETHYL USFDA+EMA
45A TIVOZANIB EMA
45B TOFACITINIB EMA
45C TRUMENBA EMA
46 VABORBACTAM USFDA
47 VALBENAZINE USFDA
48 VESTRONIDASE ALFA-VJBK USFDA
49 VELPATASVIR USFDA+EMA
50 VOXILAPREVIR USFDA+EMA
Drugs EMA list missed out in usfda list
3A ALOFISEL
link………https://newdrugapprovals.org/2018/03/02/alofisel-darvadstrocel-cx-601/
4A Atezolizumab
WILL BE UPDATED
10A BUROSUMAB
WILL BE UPDATED
10B CARIPRAZINE HYDROCHLORIDE
WILL BE UPDATED
22B FLUCICLOVINE
SEE EMA
Axumin : EPAR – Summary for the public | EN = English | 06/07/2017 |
27A Lutetium lu 177 dotatate
WILL BE UPDATED
34A NONACOG
WILL BE UPDATED
34B NUCINERSEN
EMA AND JAPAN 2017 APPROVED
35A OXERVATE
WILL BE UPDATED
36A PATIROMER
WILL BE UPDATED
36B PADELIPORFIN
NAME | Tookad |
---|---|
AGENCY PRODUCT NUMBER | EMEA/H/C/004182 |
ACTIVE SUBSTANCE | padeliporfin di-potassium |
INTERNATIONAL NON-PROPRIETARY NAME(INN) OR COMMON NAME | padeliporfin |
THERAPEUTIC AREA | Prostatic Neoplasms |
ANATOMICAL THERAPEUTIC CHEMICAL (ATC) CODE | L01XD07 |
ADDITIONAL MONITORING | This medicine is under additional monitoring. This means that it is being monitored even more intensively than other medicines. For more information, see medicines under additional monitoring. |
MARKETING-AUTHORISATION HOLDER | STEBA Biotech S.A |
---|---|
REVISION | 0 |
DATE OF ISSUE OF MARKETING AUTHORISATION VALID THROUGHOUT THE EUROPEAN UNION | 10/11/2017 |
Contact address:
STEBA Biotech S.A
7 place du theatre
L-2613 Luxembourg
Luxembourg
38A PRALATREXATE
Japan approved 2017
2017/7/3 | PMDA | JAPAN | Pralatrexate | Difolta | Mundipharma | NME |
39A ROLAPITANT
WILL BE UPDATED
39B RURLOCTOCOG
WILL BE UPDATED
43A SODIUM ZIRCONIUM
WILL BE UPDATED
44A SPHEROX
WILL BE UPDATED
45A TIVOZANIB
Pharmacotherapeutic group
Antineoplastic agents
Therapeutic indication
Fotivda is indicated for the first line treatment of adult patients with advanced renal cell carcinoma (RCC) and for adult patients who are VEGFR and mTOR pathway inhibitor-naïve following disease progression after one prior treatment with cytokine therapy for advanced RCC.
Treatment of advanced renal cell carcinoma
Fotivda : EPAR -Product Information
Tivozanib is synthesized in three main steps using well defined starting materials with acceptable
specifications.
Adequate in-process controls are applied during the synthesis. The specifications and control methods for
intermediate products, starting materials and reagents have been presented. The critical process
parameters are duly justified, methodology is presented and control is adequate.
The characterisation of the active substance and its impurities are in accordance with the EU guideline on
chemistry of new active substances. Potential and actual impurities were well discussed with regards to
their origin and characterised.
The active substance is packaged in a low-density polyethylene (LDPE) bag which complies with the EC
directive 2002/72/EC and EC 10/2011 as amended.
Product details
Name | Fotivda |
---|---|
Agency product number | EMEA/H/C/004131 |
Active substance | tivozanib |
International non-proprietary name(INN) or common name | tivozanib hydrochloride monohydrate |
Therapeutic area | Carcinoma, Renal Cell |
Anatomical therapeutic chemical (ATC) code | L01XE |
Publication details
Marketing-authorisation holder | EUSA Pharma (UK) Limited |
---|---|
Revision | 0 |
Date of issue of marketing authorisation valid throughout the European Union | 24/08/2017 |
Contact address:
EUSA Pharma (UK) Limited
Breakspear Park, Breakspear Way
Hemel Hempstead, HP2 4TZ
United Kingdom
45B TOFACITINIB
WILL BE UPDATED
45C TRUMENBA
WILL BE UPDATED
SECTION C JAPANFORODOS
SECTION C New Drugs JAPAN
https://www.pmda.go.jp/english/review-services/reviews/approved-information/drugs/0002.html
JAPAN 2017
2017/9/27 | Avelumab (genetical recombination) | Bavencio | Merck Serono | BLA |
2017/9/27 | Glecaprevir – pibrentasvir mixt | Maviret | Abbvie | NME |
2017/9/27 | Daratumumab (genetical recombination) | Darzalex | Janssen Pharmaceutical | BLA |
2017/9/27 | Belimumab (genetical recombination) | Benlysta | GlaxoSmithKline | BLA |
2017/9/27 | Bezlotoxumab (genetical recombination) | Zinplava | MDS | BLA |
2017/9/27 | Palbociclib | Ibrance | Pfizer | NME |
2017/9/27 | Lonoctocog alfa (genetical recombination) | Afstyla | CSL Behring | BLA |
2017/9/27 | Rupatadine fumarate | Rupafin | Teikoku seiyaku | NME |
2017/9/27 | Sarilumab (genetical receombination) | Kevzara | Sanofi | BLA |
2017/9/27 | Flutemetamol (18F) | Vizamyl | Nihon Medi-Physics | NME |
2017/7/3 | Nusinersen sodium | Spinraza | Biogen Japan | |
2017/7/3 | Romidepsin | Istodax | Celgene | NME |
2017/7/3 | Pralatrexate | Difolta | Mundipharma | NME |
2017/7/3 | Amenamevir | Amenalief | Maruho | NME |
2017/7/3 | Baricitinib | Olumiant | Lilly | NME |
2017/7/3 | Pemafibrate | Parmodia | Kowa | NME |
2017/3/30 | Human prothrombin complex, freeze-dried concentrated | Kcentra | CSL Behring | |
2017/3/30 | Ixazomib citrate | Ninlaro | Takeda | NME |
2017/3/30 | Forodesine hydrochloride | Mundesine | Mundipharma | |
2017/3/30 | Aflibercept beta (genetical recombination) | Zaltrap | Sanofi | |
2017/3/30 | Hydromorphone hydrochloride | Narusus, Narurapid | DaiichiSankyo-pp | |
2017/3/30 | Naldemedine tosylate | Symproic | Shionogi | NME |
2017/3/30 | Guanfacine hydrochloride | Intuniv | Shionogi |
3B AMENAMEVIR
Originally developed by Astellas, the drug was licensed to Maruho. Amenamevir treats herpes zoster by inhibiting the activity of the helicase-primer enzyme during viral DNA replication and blocking the virus’s proliferation.
Amenalief® is an oral film-coated tablet containing 200 mg of amenamevir per tablet. Recommended dose of 1 day, 400mg each time, after meals.
22A FORODESINE HYDROCHLORIDE
LINK https://newdrugapprovals.org/2018/03/06/forodesine-hydrochloride/
6A BARICITINIB JAPAN
Originally developed by Incyte, Baricitinib was later licensed to and for sale by Lilly under the trade name Olumiant®. Baricitinib is an irreversible inhibitor of Janus kinase 1 (JAK1) and Janus kinase 2 (JAK2). Olumiant® is approved for the treatment of mild to moderate rheumatoid arthritis in adult patients who are not responsive or intolerant to other anti-arthritic drugs. This product can be used alone or in combination with methotrexate.
Olumiant® is a film-coated tablet containing 2 mg or 4 mg per tablet. Recommended oral dose is 4mg daily, with meals or fasting food, you can take any time period.
2017/7/3PMDA Baricitinib Olumiant Lilly
36C PEMAFIBRATE
LINK https://newdrugapprovals.org/2016/04/24/pemafibrate/
SECTION D
CDSCO INDIA
http://www.cdsco.nic.in/forms/list.aspx?lid=2034&Id=11 http://www.cdsco.nic.in/forms/list.aspx?lid=2034&Id=11
KEEP WATCHING UNDER CONSTRUCTION AND WILL BE PASTED SOON………………………………………..
KEEP WATCHING UNDER CONSTRUCTION AND WILL BE PASTED SOON………………………………………..
KEEP WATCHING UNDER CONSTRUCTION AND WILL BE PASTED SOON………………………………………..
KEEP WATCHING UNDER CONSTRUCTION AND WILL BE PASTED SOON………………………………………..
REFERENCES
2 http://www.ema.europa.eu/docs/en_GB/document_library/Report/2018/01/WC500242079.pdf
“NEW DRUG APPROVALS” CATERS TO EDUCATION GLOBALLY, No commercial exploits are done or advertisements added by me. This is a compilation for educational purposes only. P.S. : The views expressed are my personal and in no-way suggest the views of the professional body or the company that I represent
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////////EMA APPROVALS, USFDA Approvals, ACALABRUTINIB, AVELUMAB, BETRIXABAN, BRODALUMAB, COPANLISIB, DEFLAZACORT, Delafloxacin, Deutetrabenazine, DUPILUMAB, ETELCALCETIDE, Naldemedine, NETARSUDIL, NIRAPARIB, Ocrelizumab, PLECANATIDE, RIBOCICLIB, SAFINAMIDE, TELOTRISTAT ETHYL, VALBENAZINE, CERLIPONASE, BRIGATINIB, MIDOSTAURIN, Abaloparatide, BENZNIDAZOLE, NERATINIB, inotuzumab ozogamicin, Enasidenib, LETERMOVIR, GLECAPREVIR, PIBRENTASVIR, VOXILAPREVIR, SOFOSBUVIR, EDAVARONE, abemaciclib, ANGIOTENSIN II, VESTRONIDASE, macimorelin acetate, ERTUGLIFLOZIN, SEMAGLUTIDE, EMICIZUMAB, eu 2017, fda 2017, BENRALIZUMAB, DURVALUMAB, GUSELKUMAB, LATANOPROSTENE, OZENOXACIN, SARILUMAB, SECNIDAZOLE, BENRALIZUMAB, TIVOZANIB, SARILUMAB, FLUCICLOVINE,