Pharmacological Profile of 9,11-Dehydrocortexolone 17α-Butyrate (CB-03-04), a New Androgen Antagonist with Antigonadotropic Activity
December 2011
in “
Arzneimittelforschung
”
TLDR CB-03-04 shows promise as a treatment for prostate issues due to its strong anti-androgen effects.
The study investigated a series of cortexolone-related derivatives for anti-androgenic activity, identifying 9,11-dehydrocortexolone 17α-butyrate (CB-03-04) as the most promising candidate. CB-03-04 demonstrated strong local anti-androgenic activity in hamster flank organ tests and was effective in rats after subcutaneous injection. It showed a higher topical anti-androgenic activity compared to finasteride and flutamide, and was comparable to cyproterone acetate. Additionally, CB-03-04 exhibited selective antigonadotropic activity in parabiotic rats, similar to progesterone. Its mechanism involved competing with testosterone and dihydrotestosterone and inhibiting gonadotropin hypersecretion, suggesting potential clinical use in treating prostate cancer and benign prostate hypertrophy.