目的 :研究前列腺癌的导向酶 前体药物疗法 (ADEPT) ,在体内观察前体药物甲氨喋呤 α 肽对前列腺癌的作用。方法 :用前体药物甲氨喋呤 α 苯丙氨酸 (MTX α Phe )和甲氨喋呤 α 精氨酸 (MTX α Arg)对前列腺癌荷瘤裸鼠模型行肿瘤生长抑制及药物动力学的观察。结果 :经抗人精浆蛋白单克隆抗体导向的羧肽酶 A MTX α Phe动物模型体内试验 ,ADEPT治疗组肿瘤生长明显抑制 ,裸鼠生存时间延长 ,生活质量优于单用MTX组。药物动力学显示 ,抗人精浆蛋白单克隆抗体 羧肽酶A注入72h后 ,给于MTX α Phe治疗效果最佳。结论 :MTX α Phe +CP A是一理想的前列腺癌的ADEPT对 OBJECTIVE: To study the effect of prodrug-mediated prodrug therapy (ADEPT) on prostate cancer in vivo. Methods: The tumor growth inhibition and pharmacokinetics of prostatic cancer in nude mice model were induced by using the prodrugs MTX α Phe and MTX α Arg Observation. Results: The in vivo experiments of carboxypeptidase A MTX α Phe animal model induced by anti-human seminal plasma monoclonal antibody showed that the tumor growth of ADEPT treatment group was significantly inhibited, the survival time of nude mice was prolonged, and the quality of life was better than that of MTX alone group. Pharmacokinetics showed that the anti-human seminal plasma monoclonal antibody carboxypeptidase A injection for 72h, the best for MTX α Phe treatment. Conclusion: MTX α Phe + CP A is an ideal ADEPT pair for prostate cancer