Drug intelligence / Profile preview

Liarozole

Development stage
Phase 3
Lead developer
Stiefel
Modality
Small Molecules
Administration
Oral
01

Overview

Liarozole is an orally active benzimidazole derivative and imidazole-containing small molecule that acts as a retinoic acid metabolism blocking agent (RAMBA). Its primary mechanism of action is the inhibition of cytochrome P450-dependent all-trans-retinoic acid (ATRA)-4-hydroxylase, leading to increased endogenous ATRA levels, which results in inhibition of cell proliferation and induction of cell differentiation. Liarozole also inhibits aromatase, thereby reducing estrogen biosynthesis. It has demonstrated antineoplastic activity in preclinical models and was investigated for use in conditions such as lamellar ichthyosis, prostate cancer, breast cancer, bladder cancer, and psoriasis. Liarozole was granted orphan drug designation for congenital ichthyosis but its development has been discontinued following mixed clinical trial results[1][2][3][4][5].

Brand names
Liazal
Other names
liarozolliarozolum
02

Targets

CYP19A1 (Aromatase)CYP2S1 (Cytochrome P450 2S1)CYP26A1 (Cytochrome P450 26A1)

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