In vitro and in vivo evaluation of a 3β-androsterone derivative as inhibitor of 17β-hydroxysteroid dehydrogenase type 3.

Highlights: [•] 17β-HSD3 is involved in the formation of androgenic hormone testosterone (T). [•] RM-532-105 is an androsterone derivative inhibiting 17β-HSD3. [•] RM-532-105 inhibits the formation of T in homogenized and whole HEK-293 cells overexpressing 17β-HSD3. [•] RM-532-105 (10mg/kg, s.c.) reached a plasma concentration of 250ng/mL at 7h in rat. [Copyright &y& Elsevier]