顺铂及顺铂载体研究进展.docVIP

顺铂及顺铂载体研究进展 　　[摘要] 本文探讨抗肿瘤药顺铂的临床特点及其研究进展，为临床应用提供参考。通过查阅国内外相关文献，系统地了解抗肿瘤药顺铂的临床作用，剂量限制性毒性及耐药性，并检索未获批准及正在进行临床研究的顺铂载体，以分析其临床发展趋势。在过去的10年间，药物研发转向注重药物运输靶向介质，这些新型载体在保留传统顺铂的活性的同时，在很大程度上减少了传统铂类药物的不良反应，提高疗效。 　　[关键词] 顺铂；剂量限制性毒性；耐药性；顺铂脂质体；纳米粒子 　　[中图分类号] R979.1[文献标识码]A [文章编号]1674-4721（2011）08（a）-０25－03 　　 　　Research evolution of cisplatin antitumor drugs and cisplatin-loaded 　　ZHANG Xiaochen1, ZHANG Lijin1, ZOU Yun2, ZHAO Yabin3* 　　1.China Medical University Public Health Preventive Medicine 07 grade, Liaoning Province, Shenyang 110001, China; 2. China Medical University Stomatology 08 grade, Liaoning Province, Shenyang 110001, China; 3.Respiratory Physicians, The First Hospital of China Medical University, Liaoning Province, Shenyang 110001, China 　　[Abstract] This article discussed the clinical features and research progress of cisplatin antitumor drugs for clinical references in drug application. The related literature both domestic and overseas was reviewed for a systematic understanding of the clinical effects and dose-limitted-toxicity and drug-resistance of cisplatin antitumor drugs. The cisplatin antitumor drugs，including those unapproved ones and those ongoing clinical trials were retrieved for analysis of their development tendency in the clinic. During the last decade, the focus of research and development on cisplatin has been shifted to targeted drug delivery system. These new cisplatin-loaded has the activity of cisplatin compound yet with greatly reduced side effects observed with traditional cisplatin drugs and enhance the efficiency. 　　[Key words] Cisplatin; Dose-limitted-toxicity; Drug-resistance; Lipoplatin; Nanoparticles 　　 　　顺铂（cisplatin，DDP）是第1个铂类药物，又名顺-双氯双氨络铂，是周期非特异性抗肿瘤药物，注射后广泛分布于肝、肾、前列腺、膀胱、卵巢，亦可到达胸、腹腔，极少通过血脑屏障。在人体内主要通过肾脏排泄。DDP是目前肿瘤化疗的主要药物，对睾丸癌、骨肉瘤、卵巢癌、乳腺癌、肺癌（小细胞肺癌和非小细胞肺癌）、头颈部癌、胃癌、膀胱癌、恶性淋巴瘤和软组织肉瘤有较好疗效[1]。但DDP在杀伤肿瘤细胞同时对人体正常细胞也造成很大伤害，毒性反应主要包括肾毒性、消化道毒性、骨髓抑制、神经毒性和耳毒性等，反应严重时导致中断治疗。本文对顺铂的作用机制，剂量限制性毒性和耐药性，临床应用及发展前景做以综述，为临床医务工作者提供参考。 　　1964年美国生理学家Rose