Liarazole inhibits both aromatase and retinoid catabolism. The result of the latter effect is that retinoic acid accumulates in cells. Retinoic acid and other vitamin A derivatives have been identified as differentiating agents and inducers of apoptosis in many in vitro settings and are in clinical use as differentiating agents in acute promyelocytic leukemia.166,167 Early trials in hormone-refractory prostate cancer suggest the drug has limited activity in 18%-50% of patients failing castration and that most of its action may relate to its effects on retinoid metabolism rather than aromatase activity.168-170 The side effects are mainly cutaneous, with drying and exfoliation of the skin, hair, and nails, as well as nausea, fatigue, somnolence, and mild alopecia. The limited efficacy and profile of tox-icity have reduced its use in routine clinical practice.
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