2-Chloro-4-(1R,2R)-2-hydroxy-2-methyl-cyclopentylamino-3-methyl-benzonitrile: A Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy

摘要

A transdermal SARM has a potential to have therapeutic benefit through anabolic activity in muscle, while sparing undesired effects of benign prostate hyperplasia (BPH) and liver-mediated decrease in HDL-C. 2-Chloro-4-(2-hydroxy-2-methyl-cyclopentyl)amino-3-methyl-benzonitrile 6 showed the desired muscle and prostate effects in a preclinical ORX rat model. Compound 6 had minimal effect on HDL-C levels in cynomolgus monkeys and showed human cadaver skin permeability, thus making it an effective tool for proof of concept studies in a clinical setting.