Drug intelligence / Profile preview

vorozole

Development stage
Discontinued
Lead developer
Janssen Pharmaceutical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Vorozole is a non-steroidal, triazole-based small molecule that acts as a competitive inhibitor of the aromatase enzyme (CYP19A1), which catalyzes the final step in estrogen biosynthesis. By binding to the cytochrome P450 moiety of aromatase, vorozole causes reversible inhibition and significantly reduces plasma estradiol levels in postmenopausal women. It was developed for use as an antineoplastic agent, particularly for advanced breast cancer in postmenopausal women. Clinical trials demonstrated efficacy comparable to megestrol acetate and aminoglutethimide with generally better tolerability; however, development was discontinued after phase III trials due to lack of survival benefit over existing therapies[1][5][7][8][10].

Brand names
RivizorRizivor
Other names
vorozoleVorozolumVorozol129731-10-8UNII-1E2S9YXV2AUNII1E2S9YXV2AUNII 1E2S9YXV2A
02

Targets

CYP19A1 (Aromatase)

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