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

多西他赛（泰索帝）是一种新的化疗药物， 在治疗各种恶性肿瘤，包括癌症， 乳房、肺、卵巢、胃、头颈部、膀胱和软组织 组织肉瘤 多西紫杉醇通过细胞色素P450 3A代谢 在人类肝微粒体中。 接受相同剂量的 多西他赛/体表面积显示患者间差异 清除率和毒性程度。 我们假设细胞色素P450 3A是多西他赛消除的速率限制， P450 3A活性将导致患者间和患者内变异 多西他赛的清除率

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.