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Newly approved drugs: EMA presents figures

May 3, 2014 4:47 am / 1 Comment on Newly approved drugs: EMA presents figures

In the EU, the number of approved drugs is rising with a new active ingredient; however, stagnated, the number of newly approved generics.

read at

http://www.pharmazeutische-zeitung.de/index.php?id=52016

loxoprofen

May 3, 2014 4:16 am / Leave a comment

loxoprofen

cas 68767-14-6, 80382-23-6 Koloxo, Loxoprofene, Loxoprofeno, Loxoprofenum, Loxoprofen [INN], Loxoprofene [French], Loxoprofenum [Latin]

Molecular Formula: C₁₅H₁₈O₃

Molecular Weight: 246.30162

(RS)-2-{4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid

Cyclooxygenase inhibitor; Prostanoid receptor antagonist

Inflammatory disease; Pain

Loxoprofen (INN) is a non-steroidal anti-inflammatory drug in the propionic acid derivatives group, which also includes ibuprofen and naproxen among others. It is marketed in Brazil, Mexico and Japan by Sankyo as its sodium salt, loxoprofen sodium, under the trade name Loxonin, Argentina as Oxeno and in India as Loxomac. It is available in these countries for oral administration, and a transdermal preparation was approved for sale in Japan on January 2006.^[1]

Pharmacokinetics

Loxoprofen is a prodrug. It is quickly converted to its active trans-alcohol metabolite following oral administration, and reaches its peak plasma concentration within 30 to 50 minutes.

Mechanism of action

As most NSAIDs, loxoprofen is a non-selective cyclooxygenase inhibitor, and works by reducing the synthesis of prostaglandins from arachidonic acid.

Interactions

Loxoprofen should not be administered at the same time as second-generation quinolone antibiotics such as ciprofloxacin and norfloxacin, as it increases their inhibition of GABA and this may cause seizures.^[2] It may also increase the plasma concentration of warfarin, methotrexate, sulfonylurea derivatives and lithium salts, so care should be taken when loxoprofen is administered to patients taking any of these drugs.^[2]

synthesis

Ethyl 2-oxocyclopentanecarboxylate (I) reacts with ethyl 2-(4-chloromethylphenyl)propionate (II) in the presence of KOH in hot DMF to afford ethyl 2-[4-(1-ethoxycarbonyl-2-oxocyclopentan-1-ylmethyl)phenyl]propionate (III), which is then hydrolyzed and decarboxylated by treatment with 47% HBr in refluxing dioxane.

http://zhou.nankai.edu.cn/index.php/highlights

…………….

WO-2014065577

Method for the preparation of loxoprofen (2S,1’R,2’S) trans-alcohol. Appears to be the first filing from the assignee. Sankyo (now Daiichi Sankyo) has developed and launched oral loxoprofen (Loxonin), an NSAID, is indicated for the symptom relief of inflammation and pain associated with eg rheumatoid arthritis, osteoarthritis and low back pain. Regional and national filings based on the product patent, WO03059880 start expiring from Jan 2023.

References

Daiichi Sankyo Co. (January 24, 2006). “Percutaneous Absorption-Type Analgesic and Anti-inflammatory Drug Loxonin Poultice 100mg Receives Approval for Manufacture” (Press release). Doctor’s Guide Global Edition. Retrieved 2007-04-19.
(Portuguese) “LOXONIN – Bula do Medicamento [Label Information]”. Centralx. 2007. Retrieved 2007-04-19.

US4683325	7-29-1987	Leukotriene antagonists
US4666907	5-20-1987	Phenothiazine and derivatives and analogs and use as leukotriene biosynthesis inhibitors
US4666928	5-20-1987	Propylphenoxy pyridine carboxylates as leukotriene antagonists
US4667032	5-20-1987	Phenothiazone derivatives and analogs
US4667055	5-20-1987	Leukotriene antagonists
US4663347	5-6-1987	Benzofuran 2-carboxylic acid esters useful as inhibitors of leukotriene biosynthesis
US4634766	1-7-1987	1,4-diaza-phenothiazines
US4617407	10-15-1986	Leukotriene antagonists
US4611056	9-10-1986	Benzo[A]phenothiazines and hydro-derivatives
US4609744	9-3-1986	4-oxo-benzopyran carboxylic acids

US4599360	7-9-1986	Ophthalmic anti-inflammatory agents
EP0055588	10-27-1983	ANALGESIC AND ANTI-INFLAMMATORY AGENTS
US4400534	8-24-1983	Analgesic and anti-inflammatory agents
US4161538	7-18-1979	Substituted phenylacetic acid derivatives and process for the preparation thereof

Fulvestrant… For the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy.

May 3, 2014 3:40 am / Leave a comment

fulvestrant

Fibrosis; Breast tumor; Female genital tract tumor; Uterus tumor

Estrogen receptor antagonist

(7α,17β)-7-{9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl}estra-1,3,5(10)-triene-3,17-diol

129453-61-8 CAS

C₃₂H₄₇F₅O₃S

606.771

Fulvestrant is a drug treatment of hormone receptor-positive metastatic breast cancer in post-menopausal women with disease progression following anti-estrogen therapy. It is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor.

Canada	2351004	2003-02-18	EXPIRY 2021-01-08
United States	6774122	2001-01-09	EXPIRY 2021-01-09

Fulvestrant (Faslodex, AstraZeneca) is a drug treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy. It is an estrogen receptor antagonist with no agonist effects, which works by down-regulating the estrogen receptor.^[1] It is administered as a once-monthly injection.

Clinical uses

Fulvestrant is a selective estrogen receptor down-regulator (SERD). Fulvestrant is indicated for the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy. The dosing schedule for fulvestrant remains under investigation in an attempt to optimize its effectiveness.^[2]

Clinical trials

Metastatic or locally advanced breast cancer

Fulvestrant provided effective second-line therapy in this setting for postmenopausal women who had relapsed or progressed after previous endocrine therapy.^[3]

In particular 4 clinical trials in this setting did show similar efficacy to the other hormonal agents (aromatase inhibitors and tamoxifen) with good tolerability profile. Fulvestrant had a lower incidence of joint disorders.^[4]^[5]

NICE evaluation

The U.K. National Institute for Health and Clinical Excellence (NICE) said in 2011 that it found no evidence Faslodex was significantly better than existing treatments, so its widespread use would not be a good use of resources for the country’s National Health Service

The first month’s treatment of Faslodex, which starts with a loading dose, costs £1,044.82 ($1,666), and subsequent treatments cost £522.41 a month.

A month’s supply of anastrozole (Arimidex), which is off patent, costs £5.99, and letrozole (Femara) costs £84.86.^[6]^[7]^[8]

Patent extension

The original patent for Faslodex expired in October 2004. Drugs subject to pre-marketing regulatory review are eligible for patent extension, and for this reason AstraZeneca got an extension of the patent to December 2011.^[9]^[10]

AstraZeneca has filed later patents. There is no generic Faslodex available.^[11] A later patent for Faslodex expires in January 2021.^[12]

FASLODEX® (fulvestrant) injection for intramuscular administration is an estrogen receptor antagonist. The chemical name is 7-alpha-[9-(4,4,5,5,5-penta fluoropentylsulphinyl) nonyl]estra-1,3,5-(10)- triene-3,17beta-diol. The molecular formula is C₃₂H₄₇F₅O₃S and its structural formula is:

FASLODEX® (fulvestrant) Structural Formula Illustration

Fulvestrant is a white powder with a molecular weight of 606.77. The solution for injection is a clear, colorless to yellow, viscous liquid.

Each injection contains as inactive ingredients: 10% w/v Alcohol, USP, 10% w/v Benzyl Alcohol, NF, and 15% w/v Benzyl Benzoate, USP, as co-solvents, and made up to 100% w/v with Castor Oil, USP as a co-solvent and release rate modifier.

Fulvestrant is a pure antiestrogen that represent a significant breakthrough in the treatment of breast cancer. Despite its pure antagonist activity, studies on ovariectomized rats have confirmed that fulvestrant, in contrast to Tamoxifen which acts like estrogen to reduce periosteal bone formation, does not alter estrogen-like or antiestrogenic effects. Fulvestrant also has some distinct advantages on target organs other than breast tissue.
Fulvestrant is a steroidal pure antiestrogen with a chemical structure similar to estradiol. Studies of etrogen receptor (ER) function have demonstrated that estradiol binding to the ER initiate a sequence of events. Fulvestrant antagonizes estrogen action by occupying the ER and preventing estrogen-stimulated gene activation, thus interfering with the estrogen related processes essential for cell-cycle competion.
Fulvestrant, 7-alpha- [9-(4,4,5,5,5pentafluoropentylsulphinyl) nonyl]-estra-1,3,5 (10)-triene-3,17β-diol, has the following formula:
WO Patent application No. 02/32922 describes a process for preparing an intermediate compound useful for preparing, e.g. fulvestrant, which process comprises aromatization of a compoud, and thereafter if necessary or desired, carrying out one or more of the following steps: (i) removing any hydroxy protecting group; (ii) converting a precursor group to a different such group.
EP Patent No. 0138504 relates to certain 7α-substituted derivatives of oestradiol and related steroids which possess antioestrogenic activity. US Patent No. 4659516 , EP Patent No. 0138504 and Bowler, Steroids 1989, 54, 71 describe a process for making steroids such as fulvestrant, by which 1,6-conjugate addition of an alkyl group to an estra-4,6-diene-3-one gave a ratio of 7α- to 7β-epimer of 1.2 : 1 (isolated). In WO 02/32922 it is stated that the ratio of epimers obtained using this process on an industrial scale is 1.9: 1.
US patent No 6288051 describes 7α-(5 -methylaminopentyl)-estratrienes.
There remains a need in the art for improved methods of preparing fluvestrant and other 7α-alkylated 19-norsteroids.

PATENT

http://www.google.com/patents/EP1771462B1?cl=en

Preparative Example 16: Preparation of fulvestrant (Cp 9305) from Cp 9363 – indirect process (depicted in Figure 12)

A solution of 40.5 grams of Cp 9363 in 320 grams tetrahydrofuran and 81 grams methanol was cooled to 5°C and treated with a warm solution of 27 grams sodium (meta) periodate in 183 grams water. The mixture was allowed to stand at room temperature overnight, concentrated under vacuum and then dissolved in dichloromethane, extracted with water and evaporated to give 40 grams of Cp 9368 (fulvestrant 17-acetate).
The oily residue of Cp 9368 (40 grams) was dissolved in 320 grams of methanol under nitrogen and treated for 3 hours at room temperature with a solution of 20 grams of potassium hydroxide in 128 grams methanol. After neutralisation with 30 grams of acetic acid, the reaction mixture was concentrated under vacuum and then dissolved in dichloromethane, extracted with water and evaporated. The oily residue was crystallised from 400 grams of toluene, then dried under vacuum to constant weight. 26.6 grams of fulvestrant were obtained.

Example 17: Preparation of fulvestrant (Cp 9305) from Cp 9304 – direct process (depicted in Figure 9)

A solution of 41 grams of Cp 9304 in 328 grams tetrahydrofuran and 82 grams methanol was cooled to 5°C and treated with a warm solution of 27 grams sodium (meta)periodate in 185 grams water. The mixture was allowed to stand at room temperature overnight, concentrated under vacuum and then dissolved in dichloromethane, extracted with water, evaporated, and crystallised from toluene to give 28 grams of Cp 9305 (fulvestrant). Further purification can be effected by recrystallisation from ethyl acetate.

PAPER

Org. Process Res. Dev., 2010, 14 (3), pp 544–552

DOI: 10.1021/op900315j

http://pubs.acs.org/doi/abs/10.1021/op900315j

Org. Process Res. Dev., 2010, 14 (3), pp 544–552

DOI: 10.1021/op900315j

The development of a commercial manufacturing process for fulvestrant (the active ingredient in ‘Faslodex’) is described. Key steps in the synthesis are stereoselective 1,6-addition of an organocuprate to a steroidal dienone followed by copper-mediated aromatisation of the A-ring. The strategy for dealing with noncrystalline intermediates is outlined. The production of drug substance of acceptable quality is critically dependent on limiting the formation of key impurities. The origin of these impurities is discussed, and measures to prevent or control their formation are described.

7α-[9-(4,4,5,5,5-Pentafluoropentylsulfinyl)nonyl]estra-1,3,5-(10)-triene-3,17β-diol (Fulvestrant) (6)

An approximately 50% w/w solution of 26 (assumed content 308 kg, 521 mol as a mixture of 7α- and 7β-isomers) in EtOAc was diluted with more EtOAc (695 kg) and glacial acetic acid (188 kg, 3131 mol). Aqueous hydrogen peroxide (17.5% w/v, 203 kg, 1045 mol) was added, ………………….DELETED………….. to another crystallisation cycle. In total, four crystallisations were carried out to achieve the required purity (<0.1% 7β-isomer). With each successive crystallisation, the EtOAc solution was concentrated to a predetermined volume that decreased in proportion to the estimated weight of product present (based on laboratory experiments and HPLC analysis). After the final crystallisation the product was dried in a stream of nitrogen at 60 °C. The yield of pure fulvestrant at 100% w/w strength was 88.4 kg (mean of five batches) which represents 28% overall yield from dienone 2. Ratio of sulfoxide A to sulfoxide B = 46:54 by HPLC analysis (the retention times of sulfoxide A and sulfoxide B are approximately 20.0 and 23.5 min); mp 104−112 °C by DSC analysis (sulfoxide A and sulfoxide B have mp 102 and 117 °C).

¹H NMR (400 MHz, 300 K, CDCl₃) δ 0.78 (3H, s), 0.95−1.82 (23H, m), 1.91 (1H, ddd, J = 12.2, 2.9, 2.7 Hz), 2.03−2.40 (8H, m), 2.56−2.90 (6H, m), 3.75 (1H, m), 6.56 (1H, d, J = 2.37 Hz), 6.60−6.66 (1H, m), 6.61 (1H, s), 6.76 (1H, s), 7.12 (1H, d, J = 8.62 Hz); ¹³C NMR (100 MHz, CDCl₃) δ 11.1, 14.7, 22.6, 22.7, 25.1, 27.3, 27.4, 28.6, 28.8, 29.0, 29.3, 29.4, 29.6 (t, J_CF = 21.9 Hz), 30.6, 33.3, 34.7, 37.0, 38.3, 42.1, 43.4, 46.5, 50.9, 52.5, 82.0, 113.1, 115.4 (tq, J_CF = 253 Hz, 38 Hz), 116.2, 118.9 (qt, J_CF = 285 Hz, 36 Hz), 127.0, 131.2, 136.9, 154.1.

Image result for Fulvestrant

7α-[9-(4,4,5,5,5-Pentafluoropentylsulfinyl)nonyl]estra-1,3,5-(10)-triene-3,17β-diol (Fulvestrant)

References

S. Kansra, S. Yamagata, L. Sneade, L. Foster & N. Ben-Jonathan (2005). “Differential effects of estrogen receptor antagonists on pituitary lactotroph proliferation and prolactin release”. Mol Cell Endocrinol 239 (1-2): 27–36. doi:10.1016/j.mce.2005.04.008. PMID 15950373.
Angela Mae Obermiller, PharmD; and Mehmet Sitki Copur, MD (2011). “The Longstanding Quest for a Better Endocrine Therapy Continues High-Dose Fulvestrant: Have We Found Its Effective Dose, Combination, Setting, or Sequence?”. Contemporary Oncology 3 (1).
Croxtall, J. D.; McKeage, K. (2011). “Fulvestrant”. Drugs 71 (3): 363–380. doi:10.2165/11204810-000000000-00000. PMID 21319872. edit
Fulvestrant in the treatment of advanced breast cancer: a systematic review and meta-analysis of randomized controlled trials. Valachis A, Mauri D, Polyzos NP, Mavroudis D, Georgoulias V, Casazza G. Crit Rev Oncol Hematol. 2010 Mar;73(3):220-7. Epub 2009 Apr 14. Review. PMID:19369092
Fulvestrant for systemic therapy of locally advanced or metastatic breast cancer in postmenopausal women: a systematic review. Flemming J, Madarnas Y, Franek JA. Breast Cancer Res Treat. 2009 May;115(2):255-68. Epub 2008 Aug 6. Review. PMID:18683044
UK cost body rules against AstraZeneca cancer drug, Reuters, Nov 9, 2011
UK’s NICE says no to AstraZeneca breast cancer drug Faslodex, The Pharma Letter, 10 November 2011
National Institute for Health and Clinical Excellence Guidance Breast cancer (metastatic) – fulvestrant
Patent Term Extensions The United States Patent and Trademark Office.
Determination of Regulatory Review Period for Purposes of Patent Extension; FASLODEX A Notice by the Food and Drug Administration on 04/17/2003
Generic Faslodex Availability, Drugs.COM
Pink Ribbon Blues: How Breast Cancer Culture Undermines Women’s Health By Gayle A. Sulik, Oxford University Press (Oct. 2010)

VERY New patent

WO-2014064712

Process for the preparation of fulvestrant and its intermediates. Appears to be the first filing from Intas Pharmaceuticals on this API. Family members of the product patent, WO0151056 (assigned to AstraZeneca), expire in the EU states and in the US in 2021

Fulvestrant
Clinical data

Trade names	Faslodex
AHFS/Drugs.com	Monograph
Pregnancy category	D
Routes of administration	Intramuscular injection
ATC code	L02BA03 (WHO)
Legal status
Legal status	℞ (Prescription only)
Pharmacokinetic data
Protein binding	99%
Biological half-life	40 days
Identifiers
IUPAC name [show]
Synonyms	ICI-182,780
CAS Number	129453-61-8
PubChem (CID)	104741
IUPHAR/BPS	1015
DrugBank	DB00947
ChemSpider	94553
UNII	22X328QOC4
KEGG	D01161
ChEBI	CHEBI:31638
ChEMBL	CHEMBL1358
ECHA InfoCard	100.170.955
Chemical and physical data
Formula	C₃₂H₄₇F₅O₃S
Molar mass	606.772 g/mol
3D model (Jmol)	Interactive image
SMILES FC(F)(F)C(F)(F)CCCS(=O)CCCCCCCCCC3Cc1c(ccc(O)c1)[C@H]2CC[C@]4([C@H]([C@@H]23)CC[C@@H]4O)C

//////////

Researchers create protein with potential for weight loss, diabetes treatment

May 3, 2014 1:15 am / Leave a comment

Lyra Nara Blog

It sounds like a magic bullet: Administer a protein, watch the subject lose weight. But that’s exactly what University of Florida scientists found when they discovered a new way to deliver a protein that helps develop cells that convert fat into energy.

The study builds upon on a discovery by Bruce Spiegelman, a cell biologist at the Boston-based Dana-Farber Cancer Institute, who found that human muscles release a hormone he called irisin during exercise. Spiegelman also found that mice lost a small amount of weight when given the irisin gene using a virus to ferry it into cells.

Now the UF team—including researcher Dr. Li-Jun Yang, Shi-Wu Li, and postdoctoral researcher William Donelan—has for the first time created a stable protein form of irisin, opening the door to human studies that weren’t previously possible because the virus has not been approved for use in people.

“We found that if you…

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Cancer: Health Care In India In A Nutshell

May 2, 2014 10:38 am / Leave a comment

TGI: Thrive Health

Since independence several measures have been undertaken by the National Government to improve the health of the people. Several National Health Programs have been launched by the Government including programs on Non-communicable diseases (NCD) along with the communicable diseases which are prevalent in India. Now India is experiencing a rapid health transition with rising burden of chronic NCDs especially CVD, Diabetes, Cancer, Stroke and lung diseases. In 2005 NCDs accounted for 53 % of deaths and NCDs are surpassing the burden of communicable diseases in India.

In 2010 the Cancer program was integrated with the then existing program and the new program is NPCDCS (National Program for Prevention and Control of Cancer, Diabetes, Cardiovascular Diseases and Stroke). There are two programs under NPCDCS:

DCS – Diabetes, Cardiovascular Disease and Stroke – under NPCDCS
Cancer component under NPCDCS

The objectives of the new cancer program under NPCDCS are:

Primary prevention: Health education
Secondary…

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Pharmaceutical Packaging – New USP Proposal for Optimised Method of Measuring Moisture Vapour Permeation

May 2, 2014 3:38 am / Leave a comment

DRUG REGULATORY AFFAIRS INTERNATIONAL

Pharmaceutical Packaging – New USP Proposal for Optimised Method of Measuring Moisture Vapour Permeation

An improved method of measuring water vapour permeation for solid oral dosage forms like tablets or capsules has been discussed during a USP – PQRI Workshop and presented in the Pharmacopeial Forum. See the detailed information.

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Revision of the USP Chapter on Spectroscopic Methods

May 2, 2014 3:38 am / Leave a comment

DRUG REGULATORY AFFAIRS INTERNATIONAL

Revision of the USP Chapter on Spectroscopic Methods

A new concept for the representation of different analytical and spectroscopic methods (AAS, IR, UV, etc.) has been presented as general chapter in the USP. In the future, there should be two general chapters for each method. The concrete implementation is planned in the USP38/NF33. Read more here in the News.

GMP News: Revision of the USP Chapter on Spectroscopic Methods

In the USP Pharmacopeial Forum 40(1), a “Stimuli to the Revision Process” article states that the responsible working group of the USP has conducted a review of the existing general chapters on spectroscopic methods.

The goal of this review was to establish a uniform concept for all the spectroscopic methods and generate a common format. As a result, consistency in the overall approach and ease of use in the future should also be enabled for the user. The general chapters smaller…

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Resveratrol remains effective against cancer after the body converts it

May 2, 2014 1:12 am / Leave a comment

Lyra Nara Blog

A chemical found in red wine remains effective at fighting cancer even after the body’s metabolism has converted it into other compounds. This is an important finding in a new paper published in the journal Science Translational Medicine by Cancer Research UK-funded researchers at the University of Leicester’s Department of Cancer Studies and Molecular Medicine.

The paper reveals that resveratrol – a compound extracted from the skins of red grapes – is not rendered ineffective once it is metabolised by the body.

This is an important development, as resveratrol is metabolised very quickly – and it had previously been thought that levels of the extracted chemical drop too quickly to make it usable in clinical trials.

The new research shows that the chemical can still be taken into cells after it has been metabolised into resveratrol sulfates.

Enzymes within cells are then able to break it down into resveratrol…

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Stem cell therapy regenerates heart muscle damaged from heart attacks in primates

May 2, 2014 1:11 am / Leave a comment

Lyra Nara Blog

Heart cells created from human embryonic stem cells successfully restored damaged heart muscles in monkeys. The results of the experiment appear in the April 30 advanced online edition of the journal Nature in a paper titled, “Human embryonic-stem cell derived cardiomyocytes regenerate non-human primate hearts.”

The findings suggest that the approach should be feasible in humans, the researchers said.

“Before this study, it was not known if it is possible to produce sufficient numbers of these cells and successfully use them to remuscularize damaged hearts in a large animal whose heart size and physiology is similar to that of the human heart,” said Dr. Charles Murry, UW professor of pathology and bioengineering, who led the research team that conducted the experiment.

A physician/scientist, Murry directs the UW Center for Cardiovascular Biology and is a UW Medicine pathologist.

Murry said he expected the approach could be ready for clinical trials in…

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Sanfilippo Syndrome: FDA Orphan Designations For Gene Therapy

May 1, 2014 6:57 am / Leave a comment

Orphan Druganaut Blog

Abeona Therapeutics , a Cleveland-based biotechnology start-up, is created in March 2013 as a spinoff of Nationwide Children’s Hospital , with the goal of developing therapies for patients with the rare Lysosomal Storage Disorder (LSD), Sanfilippo (SF) Syndrome or Mucopolysaccharidosis III (MPS III). Abeona in Roman Mythology is the Goddess of Departures. She protects children as they step away from home for the first time, keeping them safe as they venture into the world. Her name comes from the Latin verb abeo, “to depart, go away, or go forth”.

SF is a genetic metabolism disorder that prohibits the proper breakdown of the body’s sugar molecules. There are 4 types of MPS III (MPS III A, MPS III B, MPS III C, and MPS III D), each with a deficiency in one of four lysosomal enzymes. The disease first affects the central nervous system, causing severe brain damage, and typically results in hearing loss, vision loss…

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Anvumetostat CAS 2790567-82-5 MF C22H19F3N4O3 MW444.4 g/mol (4-amino-1,3-dihydrofuro[3,4-c][1,7]naphthyridin-8-yl)-[(3S)-3-[4-(trifluoromethyl)phenyl]morpholin-4-yl]methanone (4-amino-1,3-dihydrofuro[3,4-c][1,7]naphthyridin-8-yl){(3S)-3-[4-(trifluoromethyl)phenyl]morpholin-4-yl}methanoneantineoplastic, AMG 193, QAT649EJ5E, PRMT5-IN-27, Anvumetostat (also known as AMG 193) is an orally available, small-molecule inhibitor of protein arginine methyltransferase…
Andamertinib
Andamertinib CAS 2254145-43-0 MF C31H36N8O3 MW568.7 g/mol N-[4-methoxy-2-[4-(3-methoxyazetidin-1-yl)piperidin-1-yl]-5-[[6-(1-methylindazol-5-yl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide N-(4-methoxy-2-[4-(3-methoxyazetidin-1-yl)piperidin-1-yl]-5-{[6-(1-methyl-1H-indazol-5-yl)pyrimidin-4-yl]amino}phenyl)prop-2-enamideepidermal growth factor receptor tyrosine kinase inhibitor, antineoplastic, PLB 1004, 5X3KAG7ZBW Andamertinib (also known as PLB1004) is an investigational, orally…
Amsulostat
Amsulostat CAS 2409963-83-1 MF C13H13FN2O2S MW280.32 2-Buten-1-amine, 3-fluoro-4-(8-quinolinylsulfonyl)-, (2Z)- (2Z)-3-fluoro-4-(quinolin-8-ylsulfonyl)but-2-en-1-amine (Z)-3-fluoro-4-quinolin-8-ylsulfonylbut-2-en-1-amine (2Z)-3-fluoro-4-(quinolin-8-ylsulfonyl)but-2-en-1-amineprotein-lysine-oxidase (LOX) inhibitor, antifibrotic, PXS 5505, LOX inhibitor PXS-5505, LOX-IN-3, pan-LOX inhibitor PXS-5505, DO94E28WYW,…
Amezalpat
Amezalpat CAS 1616372-41-8 MF C34H41N3O4 MW555.7 g/mol 2-[5-[3-[3-[1-[(4-tert-butylphenyl)methyl]-4-ethyl-5-oxo-1,2,4-triazol-3-yl]propyl]phenyl]-2-ethoxyphenyl]acetic acid peroxisome proliferator-activated receptor alpha (PPARα) antagonist, antineoplastic, TPST 1120, FDA Fast Track, Orphan Drug, 1EQ4LQN9N3 Amezalpat (formerly…
Alnodesertib
Alnodesertib CAS 2267316-76-5 MF C18H24N6O2S MW388.49 4-[4-[(cyclopropyl-methyl-oxo-λ6-sulfanylidene)amino]-6-[(3R)-3-methylmorpholin-4-yl]pyrimidin-2-yl]pyridin-2-amine 4-[4-[(cyclopropyl-methyl-oxo-lambda6-sulfanylidene)amino]-6-[(3R)-3-methylmorpholin-4-yl]pyrimidin-2-yl]pyridin-2-amine (S)-({2-(2-aminopyridin-4-yl)-6-[(3R)-3-methylmorpholin-4-yl]pyrimidin-4-yl}imino)(cyclopropyl)(methyl)-λ6-sulfanoneserine/threonine kinase inhibitor, antineoplastic, ART 0380, EX-A9085 Alnodesertib (formerly known as ART0380) is an investigational, orally administered drug designed to…
Alixorexton
Alixorexton CAS 2648347-56-0 MF C21H30N2O5S MW 422.5 g/mol N-((21S,24S,52R,53S)-6-oxo-3,8-dioxa-5(2,1)-piperidina-1(1,2)-benzena-2(1,4)-cyclohexanacyclooctaphane-53-yl)methanesulfonamide N-[(15S,16R)-10-oxo-8,18-dioxa-11-azatetracyclo[17.2.2.02,7.011,16]tricosa-2,4,6-trien-15-yl]methanesulfonamide N-[7,10-cis-(4S,4aR)-17-oxo-1,2,3,4,4a,5,7,8,9,10,16,17-dodecahydro-7,10-ethanopyrido[1,2-d][1,7,4]benzodioxaazacyclotridecin-4-yl]methanesulfonamideorexin-2 receptor agonist, ALKS 2680, Breakthrough Therapy designation, 3BRW4ARU66, TAK 994, firazorexton Alixorexton (formerly ALKS 2680)…
Zeprumetostat
Zeprumetostat CAS 2098545-98-1 MF C32H44N4O4 MW 548.7 g/mol CHINA 2025, APPROVALS 2025 N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-5-ethyl-6-[ethyl(oxan-4-yl)amino]-2-(piperidin-1-ylmethyl)-1-benzofuran-4-carboxamide N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-5-ethyl-6-[ethyl(oxan-4-yl)amino]-2-[(piperidin-1-yl)methyl]-1-benzofuran-4-carboxamideenhancer of zeste homolog 2 (EZH2) inhibitor, antineoplastic, Airijing® (China), EZH2-IN-15, SHR 2554…
Zelebrudomide
Zelebrudomide CAS 2416131-46-7 MF C39H45N9O5 MW 719.8 g/mol 3-[4-[1-[[(3S)-1-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]pyrrolidin-3-yl]methyl]piperidin-4-yl]anilino]-5-piperidin-1-ylpyrazine-2-carboxamide 3-[[4-[1-[[(3S)-1-[2-(2,6-Dioxo-3-piperidyl)-1,3-dioxo-5-isoindolinyl]-3-pyrrolidinyl]methyl]-4-piperidyl]phenyl]amino]-5-(1-piperidyl)pyrazine-2-carboxamide protein degrader, antineoplastic, NX 2127, LSC67HA8DE, NX-2127, BTK Degrader NX-2127 Zelebrudomide (NX-2127) is an investigational new drug that is…
Zanvipixant
Zanvipixant CAS 2166558-11-6 MF C17H12F5N7O MW 425.3 g/mol [(6S)-1-(5-fluoropyrimidin-2-yl)-6-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]-[3-fluoro-2-(trifluoromethyl)-4-pyridinyl]methanone METHANONE, ((6S)-1-(5-FLUORO-2-PYRIMIDINYL)-1,4,6,7-TETRAHYDRO-6-METHYL-5H-1,2,3-TRIAZOLO(4,5-C)PYRIDIN-5-YL)(3-FLUORO-2-(TRIFLUOROMETHYL)-4-PYRIDINYL)- [(6S)-1-(5-fluoropyrimidin-2-yl)-6-methyl-1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridin-5-yl][3-fluoro-2-(trifluoromethyl)pyridin-4-yl]methanonepurinoreceptor (P2X) antagonist, JNJ-55308942, JNJ 55308942, B7YN3CQ7S7, JNJ-55308942 is under investigation in clinical trial NCT05328297…

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