DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Nirsevimab
(Heavy chain)
QVQLVQSGAE VKKPGSSVMV SCQASGGLLE DYIINWVRQA PGQGPEWMGG IIPVLGTVHY
GPKFQGRVTI TADESTDTAY MELSSLRSED TAMYYCATET ALVVSETYLP HYFDNWGQGT
LVTVSSASTK GPSVFPLAPS SKSTSGGTAA LGCLVKDYFP EPVTVSWNSG ALTSGVHTFP
AVLQSSGLYS LSSVVTVPSS SLGTQTYICN VNHKPSNTKV DKRVEPKSCD KTHTCPPCPA
PELLGGPSVF LFPPKPKDTL YITREPEVTC VVVDVSHEDP EVKFNWYVDG VEVHNAKTKP
REEQYNSTYR VVSVLTVLHQ DWLNGKEYKC KVSNKALPAP IEKTISKAKG QPREPQVYTL
PPSREEMTKN QVSLTCLVKG FYPSDIAVEW ESNGQPENNY KTTPPVLDSD GSFFLYSKLT
VDKSRWQQGN VFSCSVMHEA LHNHYTQKSL SLSPGK
(Light chain)
DIQMTQSPSS LSAAVGDRVT ITCQASQDIV NYLNWYQQKP GKAPKLLIYV ASNLETGVPS
RFSGSGSGTD FSLTISSLQP EDVATYYCQQ YDNLPLTFGG GTKVEIKRTV AAPSVFIFPP
SDEQLKSGTA SVVCLLNNFY PREAKVQWKV DNALQSGNSQ ESVTEQDSKD STYSLSSTLT
LSKADYEKHK VYACEVTHQG LSSPVTKSFN RGEC
(Disulfide bridge: H22-H96, H153-H209, H229-L214, H235-H’235, H238-H’238, H270-H330, H376-H434, H’22-H’96, H’153-H’209, H’229-L’214, H’270-H’330, H’376-H’434, L23-L88, L’23-L’88, L134-L194, L’134-L’194)
>Heavy_chain QVQLVQSGAEVKKPGSSVMVSCQASGGLLEDYIINWVRQAPGQGPEWMGGIIPVLGTVHY GPKFQGRVTITADESTDTAYMELSSLRSEDTAMYYCATETALVVSETYLPHYFDNWGQGT LVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFP AVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCPA PELLGGPSVFLFPPKPKDTLYITREPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKP REEQYNSTYRVVSVLTVLHQDWLEGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTL PPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLT VDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
>Light_chain DIQMTQSPSSLSAAVGDRVTITCQASQDIVNYLNWYQQKPGKAPKLLIYVASNLETGVPS RFSGSGSGTDFSLTISSLQPEDVATYYCQQYDNLPLTFGGGTKVEIKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Nirsevimab
EMS APPROVED 2022/10/31, Beyfortus, AstraZeneca AB
| Formula | C6494H10060N1708O2050S46 |
|---|---|
| CAS | 1989556-22-0 |
| Mol weight | 146334.5658 |
Monoclonal antibody
Prevention of respiratory syncytial virus infection
- Immunoglobulin g1-kappa, anti-(human respiratory syncytial virus fusion glycoprotein f0 (protein f))human monoclonal antibody.gamma.1 heavy chain (1-456) (human vh (homo sapiens ighv1-69*01(ighd)-ighj4*01 (90.1%)) (8.8.19) (1-126) -homo sapiens ighg1*03
- Immunoglobulin g1, anti-(human respiratory syncytial virus fusion protein)(human monoclonal med18897 .gamma.1-chain), disulfide with monoclonal med18897 .kappa.-chain, dimer
Synthesis Reference
Khan, AA et al. (2020) Dosage regimens for and compositions including anti-rsv antibodies. (U.S. Patent No. 2020/0347120 A1). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/6b/d2/10/a841b66e0c90cf/US20200347120A1.pdf
Nirsevimab, sold under the brand name Beyfortus, is a human recombinant monoclonal antibody with activity against respiratory syncytial virus, or RSV for infants.[2][3] It is under development by AstraZeneca and Sanofi.[2][3] Nirsevimab is designed to bind to the fusion protein on the surface of the RSV virus.[4][5]
The most common side effects reported for nirsevimab are rash, pyrexia (fever) and injection site reactions (such as redness, swelling and pain where the injection is given).[6]
Nirsevimab was approved for medical use in the European Union in November 2022.[1][7]
Nirsevimab (MEDI8897) is a recombinant human immunoglobulin G1 kappa (IgG1ĸ) monoclonal antibody used to prevent respiratory syncytial virus (RSV) lower respiratory tract disease in neonates and infants.6 It binds to the prefusion conformation of the RSV F protein, a glycoprotein involved in the membrane fusion step of the viral entry process, and neutralizes several RSV A and B strains.6,1 Compared to palivizumab, another anti-RSV antibody, nirsevimab shows greater potency at reducing pulmonary viral loads in animal models. In addition, nirsevimab was developed as a single-dose treatment for all infants experiencing their first RSV season, whereas palivizumab requires five monthly doses to cover an RSV season.5 This is due to a modification in the Fc region of nirsevimab that grants it a longer half-time compared to typical monoclonal antibodies.1,6
On November 2022, nirsevimab was approved by the EMA for the prevention of RSV lower respiratory tract disease in newborns and infants during their first RSV season.6
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| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Human |
| Target | F protein of RSV |
| Clinical data | |
| Trade names | Beyfortus |
| Other names | MED-18897, MEDI8897 |
| Routes of administration | Intramuscular |
| ATC code | None |
| Legal status | |
| Legal status | EU: Rx-only [1] |
| Identifiers | |
| CAS Number | 1989556-22-0 |
| PubChem SID | 384585358 |
| DrugBank | DB16258 |
| UNII | VRN8S9CW5V |
| KEGG | D11380 |
| ChEMBL | ChEMBL4297575 |
| Chemical and physical data | |
| Formula | C6494H10060N1708O2050S46 |
| Molar mass | 146336.58 g·mol−1 |
Adverse effects
No major hypersensitivity reactions have been reported, and adverse events of grade 3 or higher were only reported in 8% (77 of 968) of participants in clinical trial NCT02878330.[8][4]
Pharmacology
Mechanism of action
Nirsevimab binds to the prefusion conformation of the RSV fusion protein, i.e. it binds to the site at which the virus would attach to a cell; effectively rendering it useless. It has a modified Fc region, extending the half-life of the drug in order for it to last the whole RSV season.[4]
History
The opinion by the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) is based on data from two randomized, double-blind, placebo-controlled multicenter clinical trials that investigated the efficacy and safety of nirsevimab in healthy preterm (premature) and full-term infants entering their first respiratory syncytial virus (RSV) season.[6] These studies demonstrated that nirsevimab prevents lower respiratory tract infection caused by RSV requiring medical attention (such as bronchiolitis and pneumonia) in term and preterm infants during their first RSV season.[6]
The safety of nirsevimab was also evaluated in a phase II/III, randomized, double‑blind, multicenter trial in infants who were born five or more weeks prematurely (less than 35 weeks gestation) at higher risk for severe RSV disease and infants with chronic lung disease of prematurity (i.e. long-term respiratory problems faced by babies born prematurely) or congenital heart disease.[6] The results of this study showed that nirsevimab had a similar safety profile compared to palivizumab (Synagis).[6]
Society and culture
Legal status
On 15 September 2022, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Beyfortus, intended for the prevention of respiratory syncytial virus (RSV) lower respiratory tract disease in newborns and infants.[9][6] Beyfortus was reviewed under EMA’s accelerated assessment program.[9] The applicant for this medicinal product is AstraZeneca AB.[9] Nirsevimab was approved for medical use in the European Union in November 2022.[1][7]
Research
Nirsevimab is being investigated as an experimental vaccine against respiratory syncytial virus, RSV, in the general infant population.[2][3] The MELODY study is an ongoing, randomized, double-blind, placebo-controlled to evaluate the safety and efficacy of nirsevimab in late preterm and term infants. Initial results have been promising, with nirsevimab reducing LRTI (lower respiratory tract infections) by 74.5% compared to placebo in infants born at term or late preterm.[5][10][11]
Ongoing trials for nirsevimab are:
- “Evaluate the Safety and Efficacy of Nirsevimab in Healthy Preterm and Term Infants in China (CHIMES)”.
- “A Study to Evaluate the Safety and Efficacy of MEDI8897 for the Prevention of Medically Attended Lower Respiratory Tract Infection Due to Respiratory Syncytial Virus in Healthy Late Preterm and Term Infants (MELODY)”.
- “Evaluate the Safety and Tolerability, for Nirsevimab in Immunocompromised Children (MUSIC)”.
References
- ^ Jump up to:a b c “Beyfortus”. Union Register of medicinal products. 3 November 2022. Retrieved 6 November 2022.
- ^ Jump up to:a b c “Nirsevimab demonstrated protection against respiratory syncytial virus disease in healthy infants in Phase 3 trial” (Press release). Sanofi. 26 April 2021. Archived from the original on 27 December 2021. Retrieved 27 December 2021.
- ^ Jump up to:a b c “Nirsevimab MELODY Phase III trial met primary endpoint of reducing RSV lower respiratory tract infections in healthy infants” (Press release). AstraZeneca. 26 April 2021. Archived from the original on 26 December 2021. Retrieved 27 December 2021.
- ^ Jump up to:a b c Griffin MP, Yuan Y, Takas T, Domachowske JB, Madhi SA, Manzoni P, et al. (Nirsevimab Study Group) (July 2020). “Single-Dose Nirsevimab for Prevention of RSV in Preterm Infants”. The New England Journal of Medicine. 383 (5): 415–425. doi:10.1056/NEJMoa1913556. PMID 32726528. S2CID 220876651.
- ^ Jump up to:a b Hammitt LL, Dagan R, Yuan Y, Baca Cots M, Bosheva M, Madhi SA, et al. (March 2022). “Nirsevimab for Prevention of RSV in Healthy Late-Preterm and Term Infants”. The New England Journal of Medicine. 386 (9): 837–846. doi:10.1056/NEJMoa2110275. PMID 35235726. S2CID 247220023.
- ^ Jump up to:a b c d e f “New medicine to protect babies and infants from respiratory syncytial virus (RSV) infection”. European Medicines Agency (EMA) (Press release). 16 September 2022. Archived from the original on 19 September 2022. Retrieved 18 September 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
- ^ Jump up to:a b “Beyfortus approved in the EU for the prevention of RSV lower respiratory tract disease in infants”. AstraZeneca (Press release). 4 November 2022. Retrieved 6 November 2022.
- ^ Clinical trial number NCT02878330 at ClinicalTrials.gov
- ^ Jump up to:a b c “Beyfortus: Pending EC decision”. European Medicines Agency (EMA). 15 September 2022. Archived from the original on 19 September 2022. Retrieved 18 September 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
- ^ Zacks Equity Research (25 March 2022). “Pfizer’s (PFE) RSV Jab Gets Another Breakthrough Therapy Tag”. Nasdaq. Archived from the original on 8 April 2022. Retrieved 8 April 2022.
- ^ “Nirsevimab significantly protected infants against RSV disease in Phase III MELODY trial”. AstraZeneca (Press release). 3 March 2022. Retrieved 6 November 2022.
////////////Nirsevimab, EU 2022, APPROVALS 2022, PEPTIDE, Monoclonal antibody, respiratory syncytial virus infection, ANTIVIRAL, 1989556-22-0, MED-18897, MEDI8897, AstraZeneca AB
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Olutasidenib
Olutasidenib
- FT-2102
- FT2102
C18H15ClN4O2
354.79
CAS1887014-12-1
Rezlidhia (Forma Therapeutics)
SYN Caravella JA, et al. Structure-Based Design and Identification of FT-2102 (Olutasidenib), a Potent Mutant-Selective IDH1 Inhibitor. J Med Chem. 2020 Feb 27;63(4):1612-1623. doi: 10.1021/acs.jmedchem.9b01423. Epub 2020 Feb 12.
FDA 12/1/2022, To treat adults with relapsed or refractory acute myeloid leukemia with a susceptible isocitrate dehydrogenase-1 (IDH1) mutation, Rezlidhia
Olutasidenib, sold under the brand name Rezlidhia, is an anticancer medication used to treat relapsed or refractory acute myeloid leukemia.[1][2] Olutasidenib is an isocitrate dehydrogenase-1 (IDH1) inhibitor.[1] It is taken by mouth.[1]
Olutasidenib was approved for medical use in the United States in December 2022.[1][2][3][4]
Medical uses
Olutasidenib is indicated for the treatment of adults with relapsed or refractory acute myeloid leukemia with a susceptible isocitrate dehydrogenase-1 (IDH1) mutation as detected by an FDA-approved test.[1][2]
Society and culture
Names
Olutasidenib is the international nonproprietary name.[5]
Olutasidenib is an isocitrate dehydrogenase-1 (IDH1) inhibitor indicated for the treatment of patients with relapsed or refractory acute myeloid leukemia with a susceptible IDH1 mutation as detected by an FDA-approved test.
Olutasidenib (FT-2102) is a selective and potent isocitrate dehydrogenase-1 (IDH1) inhibitor approved by the FDA in December 2022.5,6 It is indicated for the treatment of relapsed or refractory acute myeloid leukemia (AML) in patients with a susceptible IDH1 mutation as determined by an FDA-approved test.5 IDH1 mutations are common in different types of cancer, such as gliomas, AML, intrahepatic cholangiocarcinoma, chondrosarcoma, and myelodysplastic syndromes (MDS), and they lead to an increase in 2-hydroxyglutarate (2-HG), a metabolite that participates in tumerogenesis.1,2 Olutasidenib inhibits the mutated IDH1 specifically, and provides a therapeutic benefit in IDH1-mutated cancers.1,5
Other IDH1 inhibitors, such as ivosidenib, have also been approved for the treatment of relapsed or refractory AML.3,4 Olutasidenib is orally bioavailable and capable of penetrating the blood-brain barrier, and is also being evaluated for the treatment of myelodysplastic syndrome (MDS), as well as solid tumors and gliomas (NCT03684811).4
SYN
https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b01423
a Reagents and conditions: (a) DIEA, DMSO, 80−110 °C, 16 h, 67%; (b) (R)-2-methylpropane-2-sulfinamide, CuSO4, 55 °C, DCE, 16 h, 81%; (c) MeMgBr, DCM, −50 to −60 °C, 3 h, 63%; (d) 1 N HCl, dioxane, reflux, 16 h, >98%, 98.4% ee; (e) m-CPBA, CHCl3, reflux, 4 days, 52%; (f) Ac2O, reflux, 3 days, 60%; (g) K2CO3, MeOH, 4 h, 92%; (h) MeI, K2CO3, DMF, 45 min, 67%.
1H NMR (300 MHz,
DMSO-d6) δ 12.07 (s, 1 H), 7.71−7.76 (m, 2 H), 7.51 (dd, J = 8.79,
2.35 Hz, 1 H), 7.31 (d, J = 8.79 Hz, 1 H), 6.97 (d, J = 7.92 Hz, 1 H),
6.93 (d, J = 7.92 Hz, 1 H), 5.95 (d, J = 7.92 Hz, 1 H), 4.62−4.75 (m,
1 H), 3.58 (s, 3 H), 1.50 (d, J = 6.74 Hz, 3 H); 13C NMR (75 MHz,
DMSO-d6) δ 161.0, 155.9, 141.4, 136.6, 135.0, 133.4, 129.8, 126.7,
125.8, 120.1, 119.4, 116.7, 115.1, 104.5, 103.7, 47.4, 34.0, 20.3; LCMS
(method 2) >95% purity; tR 10.18 min; m/z 355, 357 [M + H]+
;
HRMS (ESI) calcd for C18H16ClN4O2 [M + H]+ 355.0962 found
356.0956.
////////
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/////////////////////////////////////////////////////////////////////////////
| Clinical data | |
|---|---|
| Trade names | Rezlidhia |
| Other names | FT-2102 |
| License data | US DailyMed: Olutasidenib |
| Routes of administration | By mouth |
| ATC code | None |
| Legal status | |
| Legal status | US: ℞-only [1][2] |
| Identifiers | |
| CAS Number | 1887014-12-1 |
| PubChem CID | 118955396 |
| IUPHAR/BPS | 10319 |
| DrugBank | DB16267 |
| ChemSpider | 72380144 |
| UNII | 0T4IMT8S5Z |
| KEGG | D12483 |
| ChEMBL | ChEMBL4297610 |
| PDB ligand | PWV (PDBe, RCSB PDB) |
| Chemical and physical data | |
| Formula | C18H15ClN4O2 |
| Molar mass | 354.79 g·mol−1 |
| 3D model (JSmol) | Interactive image |
| showSMILES | |
References
- ^ Jump up to:a b c d e f https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/215814s000lbl.pdf
- ^ Jump up to:a b c d https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2022/215814Orig1s000ltr.pdf
This article incorporates text from this source, which is in the public domain. - ^ “Rigel Announces U.S. FDA Approval of Rezlidhia (olutasidenib) for the Treatment of Adult Patients with Relapsed or Refractory Acute Myeloid Leukemia with a Susceptible IDH1 Mutation”. Rigel Pharmaceuticals, Inc. (Press release). 1 December 2022. Retrieved 2 December 2022.
- ^ “Rigel Announces U.S. FDA Approval of Rezlidhia (olutasidenib) for the Treatment of Adult Patients with Relapsed or Refractory Acute Myeloid Leukemia with a Susceptible IDH1 Mutation” (Press release). Rigel Pharmaceuticals. 1 December 2022. Retrieved 2 December 2022 – via PR Newswire.
- ^ World Health Organization (2019). “International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 82”. WHO Drug Information. 33 (3). hdl:10665/330879.
Further reading
- Liu X, Gong Y (2019). “Isocitrate dehydrogenase inhibitors in acute myeloid leukemia”. Biomarker Research. 7: 22. doi:10.1186/s40364-019-0173-z. PMC 6806510. PMID 31660152.
- Watts JM, Baer MR, Yang J, Prebet T, Lee S, Schiller GJ, et al. (November 2022). “Olutasidenib alone or with azacitidine in IDH1-mutated acute myeloid leukaemia and myelodysplastic syndrome: phase 1 results of a phase 1/2 trial”. The Lancet Haematology. doi:10.1016/S2352-3026(22)00292-7. PMID 36370742. S2CID 253471380.
External links
- “Olutasidenib”. Drug Information Portal. U.S. National Library of Medicine.
- Clinical trial number NCT02719574 for “Open-label Study of FT-2102 With or Without Azacitidine or Cytarabine in Patients With AML or MDS With an IDH1 Mutation” at ClinicalTrials.gov
/////////////Olutasidenib, FDA 2022, APPROVALS 2022, Rezlidhia, FT-2102, FT 2102
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ABY 737
ABT-737
| Molecular Weight | 813.43 |
|---|---|
| Formula | C42H45ClN6O5S2 |
| CAS No. | 852808-04-9 |
ABT-737 is a small molecule drug that inhibits Bcl-2 and Bcl-xL, two members of the Bcl-2 family of evolutionarily-conserved proteins that share Bcl-2 Homology (BH) domains. First developed as a potential cancer chemotherapy,[1] it was subsequently identified as a senolytic (a drug that selectively induces cell death in senescent cells).[2]
The Bcl-2 family is most notable for their regulation of apoptosis, a form of programmed cell death, at the mitochondrion; Bcl-2 and Bcl-xL are anti-apoptotic proteins. Because many cancers have mutations in these genes that allow them to survive, scientists began working to develop drugs that would inhibit this pathway in the 1990s.[1] ABT-737 was one of the earliest of a series of drugs developed by Abbott Laboratories (now Abbvie) to target this pathway, based on their resolution of the 3D structure of Bcl-xL and studies using high-field solution nuclear magnetic resonance (NMR) that revealed how the BH domains of these proteins interacted with their targets.[1]
ABT-737 was superior to previous BCL-2 inhibitors given its higher affinity for Bcl-2, Bcl-xL and Bcl-w. In vitro studies showed that primary cells from patients with B-cell malignancies are sensitive to ABT-737.[3] In animal models, it improved survival, caused tumor regression, and cured a high percentage of mice.[4] In preclinical studies utilizing patient xenografts, ABT-737 showed efficacy for treating lymphoma and other blood cancers.[5]
Unfortunately, ABT-737 is not bioavailable after oral administration, leading to the development of navitoclax (ABT-263) as an orally-available derivative with similar activity on small cell lung cancer (SCLC) cell lines.[1][6] Navitoclax entered clinical trials,[1][6] and showed promise in haematologic cancers, but was stalled when it was found to cause thrombocytopenia (severe loss of platelets), which was discovered to be caused by the platelets’ requirement for Bcl-xL for survival.[1]
Subsequently, it was reported that ABT-737 specifically induces apoptosis in senescent cells in vitro and in mouse models.[2]
ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research.
PATENT
PATENT
CN113248415
PATENT
US20070015787
Journal of Medicinal Chemistry (2007), 50(4), 641-662
https://pubs.acs.org/doi/10.1021/jm061152t
////////
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/////////////////////////////////////////////////////////////////////////////
| Names | |
|---|---|
| Preferred IUPAC name4-{4-[(4′-Chloro[1,1′-biphenyl]-2-yl)methyl]piperazin-1-yl}-N-(4-{[(2R)-4-(dimethylamino)-1-(phenylsulfanyl)butan-2-yl]amino}-3-nitrobenzene-1-sulfonyl)benzamide | |
| Identifiers | |
| CAS Number | 852808-04-9 |
| 3D model (JSmol) | Interactive image |
| ChEBI | CHEBI:47575 |
| ChemSpider | 9403232 |
| PubChemCID | 11228183 |
| UNII | Z5NFR173NV |
| CompTox Dashboard (EPA) | DTXSID7042641 |
| showInChI | |
| showSMILES | |
| Properties | |
| Chemical formula | C42H45ClN6O5S2 |
| Molar mass | 813.43 g·mol−1 |
| Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). |
References
- ^ Jump up to:a b c d e f Croce, Carlo M; Reed, John C (October 2016). “Finally, An Apoptosis-Targeting Therapeutic for Cancer”. Cancer Research. 76 (20): 5914–5920. doi:10.1158/0008-5472.CAN-16-1248. PMC 5117672. PMID 27694602.
- ^ Jump up to:a b Yosef, Reut; Pilpel, Noam; Tokarsky-Amiel, Ronit; Biran, Anat; Ovadya, Yossi; Cohen, Snir; Vadai, Ezra; Dassa, Liat; Shahar, Elisheva; Condiotti, Reba; Ben-Porath, Ittai; Krizhanovsky, Valery (2016). “Directed elimination of senescent cells by inhibition of BCL-W and BCL-XL”. Nature Communications. 7: 11190. Bibcode:2016NatCo…711190Y. doi:10.1038/ncomms11190. PMC 4823827. PMID 27048913.
- ^ Vogler, Meike, et al. “Bcl-2 inhibitors: small molecules with a big impact on cancer therapy.” Cell Death & Differentiation 16.3 (2008): 360–367.
- ^ Oltersdorf, Tilman; Elmore, Steven W.; Shoemaker, Alexander R.; Armstrong, Robert C.; Augeri, David J.; Belli, Barbara A.; Bruncko, Milan; Deckwerth, Thomas L.; Dinges, Jurgen; Hajduk, Philip J.; Joseph, Mary K.; Kitada, Shinichi; Korsmeyer, Stanley J.; Kunzer, Aaron R.; Letai, Anthony; Li, Chi; Mitten, Michael J.; Nettesheim, David G.; Ng, ShiChung; Nimmer, Paul M.; O’Connor, Jacqueline M.; Oleksijew, Anatol; Petros, Andrew M.; Reed, John C.; Shen, Wang; Tahir, Stephen K.; Thompson, Craig B.; Tomaselli, Kevin J.; Wang, Baole; Wendt, Michael D.; Zhang, Haichao; Fesik, Stephen W.; Rosenberg, Saul H. (2005). “An inhibitor of Bcl-2 family proteins induces regression of solid tumours”. Nature. 435 (7042): 677–81. Bibcode:2005Natur.435..677O. doi:10.1038/nature03579. PMID 15902208. S2CID 4335635.
- ^ Hann CL, Daniel VC, Sugar EA, Dobromilskaya I, Murphy SC, Cope L, Lin X, Hierman JS, Wilburn DL, Watkins DN, Rudin CM (April 2008). “Therapeutic efficacy of ABT-737, a selective inhibitor of BCL-2, in small cell lung cancer”. Cancer Research. 68 (7): 2321–8. doi:10.1158/0008-5472.can-07-5031. PMC 3159963. PMID 18381439.
- ^ Jump up to:a b Hauck P, Chao BH, Litz J, Krystal GW (April 2009). “Alterations in the Noxa/Mcl-1 axis determine sensitivity of small cell lung cancer to the BH3 mimetic ABT-737”. Mol Cancer Ther. 8 (4): 883–92. doi:10.1158/1535-7163.MCT-08-1118. PMID 19372561. Retrieved 9 September 2019.
///////////ABT-737, ABT 737
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