liarozole hydrochloride

Liarozole HCl is a benzimidazole derivative with antineoplastic activity. As a retinoic acid metabolism blocking agent, liarozole inhibits CYP450-dependent all-trans-retinoic acid (ATRA)-4-hydroxylase, leading to an increase in endogenous ATRA production,

Liarozole fumarate is used as a retinoic acid metabolism blocking agent (RAMBA) and an aromatase inhibitor.

Liarozole dihydrochloride is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.

Liarozole (R75251 dihydrochloride) 是一种咪唑衍生物，是一种具有口服活性的维甲酸 (RA) 代谢阻断剂(RAMBA)，具有抗肿瘤作用。它能够抑制维甲酸依赖的细胞色素P450(CYP26) 4- 羟基化 (IC50=7 μM)，导致组织维甲酸水平增加。