Pharmacodynamics<unk>  is a steroidal antiandrogen, or antagonist of the androgen receptor (AR), the biological target of androgens such as testosterone and dihydrotestosterone (DHT). In a bioassay, the topical potency of the medication was greater than that of progesterone, flutamide, and finasteride and was equivalent to that of cyproterone acetate. Likewise, it is significantly more efficacious as an antiandrogen than other AR antagonists such as enzalutamide and spironolactone in scalp dermal papilla cells and sebocytes in vitro. Pharmacokinetics Steady-state levels of<unk>  occur within 5 days of twice daily administration. At a dosage of 6 g<unk>  cream applied twice daily, maximal circulating levels of<unk>  were 4.5 ± 2.9 ng/mL, area-under-the-curve levels over the dosing interval were 37.1 ± 22.3 h*ng/mL, and average circulating levels of<unk>  were 3.1 ± 1.9 ng/mL. In rodents,<unk>  has been found to possess strong local antiandrogenic activity, but negligible systemic antiandrogenic activity when administered via subcutaneous injection. Along these lines, the medication is not progonadotropic in animals. The plasma protein binding of<unk>  is 84 to 89% regardless of concentration.<unk>  is rapidly hydrolyzed into cortexolone (11-deoxycortisol) and this compound is a possible primary metabolite of<unk>  based on in-vitro studies in human liver cells. During treatment with<unk> , cortexolone levels were detectable and generally below or near the low limit of quantification (0.5 ng/mL).<unk>  may also produce other metabolites, including conjugates. The elimination of<unk>  has not been fully characterized in humans.
Clascoterone
Silodosin
Doxazosin
Spirorenone
Canrenone
Acebutolol
Azaperone
Finerenone