Description
Abarelix is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist (IC50 = 3.5 nM in HEK293 cells expressing the human receptor).1,2 It increases histamine release from rat peritoneal mast cells in vitro and from a human skin model ex vivo.3,4 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.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.WARNING This product is not for human or veterinary use.
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