Abarelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist, which is used for prostate cancer treatment.

Abarelix (30 and 300 μg/mL) causes significantly increased histamine release[1]. Abarelix demonstrates to promptly and substantially reduce follicle-stimulating hormone levels to lower than LHRH agonist. Abarelix is the first GnRH antagonist to be developed which can produce rapid and sustained decreases in testosterone to castrate levels without the need for co-administration of an antiandrogen, and with a very low complication rate in the short term[2]. 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[3].

183552-38-7

C72H95ClN14O14

1416.06

R3827;阿巴瑞克;PPI 149;Abarelix

[1]Koechling W, et al. A novel GnRH antagonist, causes minimal histamine release compared with abarelix in an ex vivo model of human skin samples. Br J Clin Pharmacol. 2010 Oct;70(4):580-7.[2]Debruyne F, et al. Abarelix for injectable suspension: first-in-class releasing hormone antagonist for prostate cancer. Future Oncol. 2006 Dec;2(6):677-96.[3]Kirby RS, et al. Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4.

DMSO:14.2 mg/mL (10.03 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years