pexacerfont

Pexacerfont is a potent and selective small molecule antagonist of the corticotropin-releasing factor 1 (CRF1) receptor. Developed by Bristol-Myers Squibb, it was investigated for the treatment of anxiety disorders, alcohol dependence, alcoholism, irritable bowel syndrome, depression, and withdrawal symptoms from drug dependence[2][1][4][5][6]. Pexacerfont acts by blocking CRF1 receptors in the brain; these receptors mediate stress responses via corticotropin-releasing hormone (CRH), which triggers adrenocorticotropic hormone (ACTH) release and subsequent physiological stress effects[2][3]. Preclinical studies demonstrated anxiolytic effects in animal models and high selectivity for CRF1 over CRF2 receptors[6][8]. However, clinical trials did not show significant efficacy compared to placebo in generalized anxiety disorder or alcohol craving reduction in humans[5]. The drug remains investigational.