Abarelix

• CAT Number: I002380
• CAS Number: 183552-38-7
• Molecular Formula: C72H95ClN14O14
• Molecular Weight: 1416.06
• Purity: ≥95%
• Solubility: DMSO: ≥ 14.2 mg/mL
• Storage: 3 years -20C powder
• InChI: InChI=1S/C72H95ClN14O14/c1-41(2)32-54(64(93)80-53(17-10-11-30-77-42(3)4)72(101)87-31-13-18-60(87)69(98)78-43(5)63(75)92)81-68(97)58(38-62(74)91)84-70(99)61(37-46-22-27-52(90)28-23-46)86(7)71(100)59(40-88)85-67(96)57(36-48-14-12-29-76-39-48)83-66(95)56(34-
• InChIKey: AIWRTTMUVOZGPW-HSPKUQOVSA-N
• SMILES: O=C(N[C@@H](CC(C)C)C(N[C@@H](CCCCNC(C)C)C(N1[C@H](C(N[C@H](C)C(N)=O)=O)CCC1)=O)=O)[C@H](NC([C@@H](N(C([C@@H](NC([C@H](NC([C@H](NC([C@H](NC(C)=O)CC2=CC=C3C=CC=CC3=C2)=O)CC4=CC=C(Cl)C=C4)=O)CC5=CC=CN=C5)=O)CO)=O)C)CC6=CC=C(O)C=C6)=O)CC(N)=O

Abarelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.IC50 value:Target:In vitro: Abarelix (30 and 300 μg/ml) and cetrorelix cause significantly increased histamine release. Abarelix demonstrates to promptly and substantially reduce follicle-stimulating hormone levels to lower than LHRH agonist. Abarelix does not cause a surge in serum testosterone that can precipitate a flare phenomenon or worsening of disease, particularly dangerous for patients with metastatic, symptomatic disease, and produces medical castration more quickly

Reference

1:New treatment paradigm for prostate cancer: abarelix initiation therapy for immediate testosterone suppression followed by a luteinizing hormone-releasing hormone agonist. Tombal B.BJU Int. 2012 Mar;109(6):E16; author reply E16-7. doi: 10.1111/j.1464-410X.2012.10983.x. No abstract available. PMID: 22360806 Free Article2:New treatment paradigm for prostate cancer: abarelix initiation therapy for immediate testosterone suppression followed by a luteinizing hormone-releasing hormone agonist. Garnick MB, Mottet N.BJU Int. 2012 Aug;110(4):499-504. doi: 10.1111/j.1464-410X.2011.10708.x. Epub 2011 Nov 16. PMID: 22093775 Free Article3:Degarelix, a novel GnRH antagonist, causes minimal histamine release compared with cetrorelix, abarelix and ganirelix in an ex vivo model of human skin samples. Koechling W, Hjortkjaer R, Tankó LB.Br J Clin Pharmacol. 2010 Oct;70(4):580-7. doi: 10.1111/j.1365-2125.2010.03730.x. PMID: 20840449 Free PMC Article4:Retraction statement: Reconstitution of Plenaxis® (Abarelix) 100 mg for injection is more effective with a vortex-like mixer than when performed manually. [No authors listed]J Pharm Pract. 2010 Feb;23(1):78. doi: 10.1177/0897190009360369. PMID: 21507797 5:Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. Kirby RS, Fitzpatrick JM, Clarke N.BJU Int. 2009 Dec;104(11):1580-4. doi: 10.1111/j.1464-410X.2009.08924.x. Review. PMID: 20053189 Free Article6:Abarelix for injectable suspension: first-in-class gonadotropin-releasing hormone antagonist for prostate cancer. Debruyne F, Bhat G, Garnick MB.Future Oncol. 2006 Dec;2(6):677-96. Review. PMID: 17155895 7:Dose-escalated abarelix in androgen-independent prostate cancer: a phase I study. Beer TM, Ryan C, Bhat G, Garnick M; Abarelix Study Group..Anticancer Drugs. 2006 Oct;17(9):1075-9. PMID: 17001181 8:Abarelix (plenaxis). Hogle WP.Clin J Oncol Nurs. 2004 Dec;8(6):663-5. No abstract available. PMID: 15637961 9:Abarelix: the first gonadotrophin-releasing hormone antagonist for the treatment of prostate cancer. Mongiat-Artus P, Teillac P.Expert Opin Pharmacother. 2004 Oct;5(10):2171-9. Review. PMID: 15461552 10:Pharmacokinetics and pharmacodynamics of a novel depot formulation of abarelix, a gonadotropin-releasing hormone (GnRH) antagonist, in healthy men ages 50 to 75. Wong SL, Lau DT, Baughman SA, Fotheringham N, Menchaca D, Garnick MB.J Clin Pharmacol. 2004 May;44(5):495-502. PMID: 15102870