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卡巴他赛:一种用于转移性去势抵抗性前列腺癌的新型紫杉烷类药物——当前影响及未来前景

Cabazitaxel: A novel taxane for metastatic castration-resistant prostate cancer-current implications and future prospects.

作者信息

Abidi Afroz

机构信息

Department of Pharmacology, Subharti Medical College, Subhartipuram, Meerut Bypass, Meerut, Uttar Pradesh, India.

出版信息

J Pharmacol Pharmacother. 2013 Oct;4(4):230-7. doi: 10.4103/0976-500X.119704.

Abstract

Recent advances in the management of prostate cancer have shown considerable development with time and many novel therapeutic agents have been approved over the past years. For patients with metastatic castration-resistant prostate cancer (mCRPC), initially docetaxel was the standard chemotherapy but once they became refractory to docetaxel, no treatment improved survival. This scenario changed in June 2010 when the US Food and Drug Administration (FDA) approved Cabazitaxel as a new therapeutic option for patients with mCRPC resistant to docetaxel. Cabazitaxel, being a novel tubulin-binding taxane with poor affinity for P-glycoprotein, decreases the chances of resistance. It has shown antitumor activity in preclinical, phase I, II and III clinical studies in docetaxel-resistant tumors. This article summarises the background, pharmacodynamic, kinetics and clinical development of cabazitaxel for the treatment of castration-resistant prostate cancer. Future development and rational use of this drug in other tumors is under therapeutic investigation.

摘要

前列腺癌治疗的最新进展随着时间推移有了显著发展,过去几年有许多新型治疗药物获批。对于转移性去势抵抗性前列腺癌(mCRPC)患者,最初多西他赛是标准化疗药物,但一旦患者对多西他赛产生耐药,就没有治疗方法能改善生存期。2010年6月这种情况发生了改变,当时美国食品药品监督管理局(FDA)批准卡巴他赛作为对多西他赛耐药的mCRPC患者的一种新治疗选择。卡巴他赛是一种新型微管结合紫杉烷,对P-糖蛋白亲和力低,降低了耐药的可能性。它在多西他赛耐药肿瘤的临床前、I期、II期和III期临床研究中均显示出抗肿瘤活性。本文总结了卡巴他赛治疗去势抵抗性前列腺癌的背景、药效学、药代动力学及临床进展。该药物在其他肿瘤中的未来发展及合理应用正在进行治疗研究。

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