Biological profile of cortexolone 17alpha-propionate (CB-03-01), a new topical and peripherally selective androgen antagonist

The aim of this study was to investigated the antiandrogenic activity of a new monoester of cortexolone, cortexolone 17-propionate (CAS 19608-29-8, CB-03-01). Although the compound displayed a strong local antiandrogenic activity in hamster's flank organ test, it did not affect gonadotropins hypersecretion when injected to parabiotic rats. As topical antiandrogen, the steroid resulted about 4 times more active than progesterone (CAS 57-83-0)and, when compared to known antiandrogen standards, it was 3 times more potent than flutamide (CAS 13311-84-7), about 2 times more effective than finasteride (CAS 98319-26-7) and approximatively as active as cyproterone acetate (CAS 427-51-0)Its pharmacologicalactivity seemed to be primarily related to its ability to antagonistically compete at androgen receptor level; nevertheless its primary pharmacological target needs to be further investigated. Its topical activity, along with the apparent absence of systemic effects, anticipates this compuond to have the potential of representing a novel and safe therapeutic approach for androgen-dependent skin disorders