THE EFFECT OF P450 3A ACTIVITY ON THE PHARMACOKINETICS OF DOCETAXEL (TAXOTERE)

多西紫杉醇(Taxotere)是一种新的化疗药物，已显示 在治疗各种恶性肿瘤方面有希望，包括 乳房、肺、卵巢、胃、头颈部、膀胱软 组织肉瘤。多西紫杉醇通过细胞色素P450 3A代谢 在人类肝脏微粒体中。接受相同剂量的治疗的患者 多西紫杉醇每体表面积显示患者之间的差异 清除量和毒性程度。我们假设细胞色素P450 3A在多西紫杉醇的消除中是速率限制，并且在 P450 3A活性会导致患者间和患者内的差异 在多西紫杉醇的许可范围内。

Docetaxel (Taxotere) is a new chemotherapeutic agent which has shown promise in the treatment of various malignancies including cancers of the breast, lung, ovary, stomach, head and neck, bladder, and soft tissue sarcomas. Docetaxel undergoes metabolism by cytochrome P450 3A in human liver microsomes. Patients treated with the same dose of docetaxel per body surface area exhibit interpatient variation in clearance and degree of toxicity. We hypothesize that cytochrome P450 3A is rate limiting in the elimination of docetaxel and that changes in P450 3A activity will result in interpatient and intrapatient variation in docetaxel's clearance.