liarozole fumarate
The orally active fumarate salt of the benzimidazole derivative liarozole with potential antineoplastic activity. As a retinoic acid metabolism blocking agent (RAMBA), liarozole inhibits cytochrome P450-dependent all-trans-retinoic acid (ATRA)-4-hydroxylase, resulting in an increase in endogenous ATRA production, inhibition of cell proliferation, and induction of cell differentiation. This agent also inhibits aromatase, the enzyme that catalyzes the final, rate-limiting step in estrogen biosynthesis.
Code name: | R85246 |
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Chemical structure: | (+-)-5-(m-chloro-alpha-imidazol-1-ylbenzyl)benzimidazole fumarate (2:3) 1H-benzimidazole, 5-((3-chlorophenyl)-1H-imidazol-1-ylmethyl)-, (+-)-, (E)-2-butenedioate (2:3) |