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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].
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