Vorozole is a triazole derivative which binds to the cytochrome P450 m
oiety of aromatase, thus causing reversible inhibition of the enzyme.
Plasma estradiol levels are reduced by about 90% in postmenopausal wom
en treated with vorozole. Phase II clinical studies found vorozole to
be an effective agent for the treatment of postmenopausal women with a
dvanced breast cancer, achieving objective responses in up to 35% of p
atients. In 2 large phase III studies, vorozole 2.5 mg/day demonstrate
d favourable clinical efficacy compared with aminoglutethimide and meg
estrol. Vorozole improved patients quality of life to a greater extent
thatn aminoglutethimide. Clinical trials to date indicate that the to
lerability of vorozole is better than that of aminoglutethimide. Voroz
ole also appears to be at least as well as tolerated megestrol (althou
gh inappropriate bodyweight gain is more common in me4gestrol recipien
ts). The most common adverse events with vorozole are hot flushes and
nausea which are generally mild in severity.