abarelix

Abarelix (PPI 149) 是一种促性腺激素释放激素 (GnRH) 拮抗剂，用于前列腺癌研究。

Abarelix (PPI 149; R 3827) Acetate is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer research.

Abarelix acetate is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist. It increases histamine release from rat peritoneal mast cells in vitro and from a human skin model ex vivo. In vivo, abarelix decreases plasma luteinizing hormone (LH) levels six hours post-treatment in castrated rats, with levels returning to baseline within 24 hours.3 Abarelix (2 mg kg) also transiently decreases plasma testosterone levels in intact rats, with levels returning to baseline within seven days post-treatment. Formulations containing abarelix have previously been used in the treatment of advanced prostate cancer.