Dabrafenib: a new opportunity for the treatment of BRAF V600-positive melanoma.
Dabrafenib: a new opportunity for the treatment of BRAF V600-positive melanoma.
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DOI：
10.2147/ott.s75104
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发表时间：
2016
影响因子：
4
通讯作者：
Argenziano G
中科院分区：
文献类型：
--
作者：
Banzi M;De Blasio S;Lallas A;Longo C;Moscarella E;Alfano R;Argenziano G
在2011年之前，晚期或转移性黑色素瘤患者的1年生存率低至33%，中位总生存期约为9个月。已经应用了几种化疗方案，无论是作为单药化疗还是作为多药化疗，总体上没有导致无进展生存期或总生存期的改善。对黑色素瘤流行病学和生物学的新见解允许开发更新的疗法。BRAF（促分裂原活化蛋白激酶的一部分）突变的发现使得两种BRAF抑制剂vemurafenib和dabrafenib的开发成为可能，这两种抑制剂显著改善了转移性黑色素瘤治疗的结果。本文综述了达拉非尼的作用机制、疗效和安全性。对这种药物的深入了解将鼓励临床医生为每位患者选择适当的治疗策略，以及预防或充分管理副作用，从而优化药物的适用性。
Prior to 2011, the 1-year survival rates for patients suffering from advanced or metastatic melanoma was as low as 33%, with a median overall survival of about 9 months. Several chemotherapeutic regimens have been applied, either as monochemotherapy or as polychemotherapy, overall not resulting in an improvement of progression-free or overall survival. Novel insights into the epidemiology and biology of melanoma allowed the development of newer therapies. The discovery of mutations in BRAF, a part of the mitogen-activated protein kinase, allowed the development of two BRAF inhibitors, vemurafenib and dabrafenib, which significantly improved the outcome of metastatic melanoma treatment. This article reviews the mechanism of action, efficacy, and safety profile of dabrafenib. An in-depth knowledge of this medication will encourage clinicians to select the appropriate therapeutic strategy for each patient, as well as to prevent or adequately manage side effects, optimizing, thus, the drug’s applicability.