产品描述:
Abarelix is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist (IC50 = 3.5 nM in HEK293 cells expressing the human receptor).{48583,39553} In vivo, abarelix (200 μg/kg) decreases plasma luteinizing hormone (LH) levels six hours post-treatment in castrated rats, with levels returning to baseline within 24 hours.{48584} 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.