Department of Dermatology, University Hospital of Zurich, Zurich, Switzerland.
Department of Dermatology, Paracelsus Medical University, Salzburg, Austria.
Future Oncol. 2017 Aug;13(20):1755-1766. doi: 10.2217/fon-2017-0170. Epub 2017 Jun 7.
Although significant progress has been made in the treatment of unresectable or metastatic melanoma, at least half of all advanced melanoma patients eventually progress and pass away due to their disease. In particular, patients with NRAS-mutated melanoma still face limited therapeutic options, with immunotherapy being the current treatment type of choice. Binimetinib is a selective inhibitor of MEK, a central kinase in the tumor-promoting MAPK pathway. The results of a recent Phase III trial rendered binimetinib the first targeted therapy agent to significantly improve progression-free survival in NRAS-mutated melanoma. This review will summarize the development and clinical data of binimetinib in melanoma in general and also explore the potential future role of this substance as single agent or combination therapy.
尽管在治疗不可切除或转移性黑色素瘤方面取得了重大进展，但至少一半的晚期黑色素瘤患者最终仍因疾病而进展和死亡。特别是NRAS 突变型黑色素瘤患者仍然面临有限的治疗选择，免疫疗法是目前首选的治疗类型。Binimetinib 是 MEK 的选择性抑制剂，MEK 是促进 MAPK 通路的中央激酶。最近的一项 III 期试验结果使 binimetinib 成为首个显著改善NRAS 突变黑色素瘤无进展生存期的靶向治疗药物。这篇综述将总结 binimetinib 在黑色素瘤中的开发和临床数据，并探讨该物质作为单一药物或联合治疗的潜在未来作用。
