MEK inhibitors for the treatment of NRAS mutant melanoma

被引:41
作者
Sarkisian, Saro [1 ]
Davar, Diwakar [2 ,3 ]
机构
[1] Univ Pittsburgh, Div Gen Internal Med, Pittsburgh, PA 15232 USA
[2] Hillman Canc Ctr, Div Hematol Oncol, Pittsburgh, PA USA
[3] Univ Pittsburgh, Pittsburgh, PA 15232 USA
关键词
advanced; metastatic; melanoma; BRAF; MEK; NRAS; binimetinib; MAPK; ERK; DABRAFENIB PLUS TRAMETINIB; ADVANCED BRAF(V600)-MUTANT MELANOMA; CUTANEOUS MALIGNANT-MELANOMA; CELL LUNG-CANCER; PHASE-II TRIAL; OPEN-LABEL; SELUMETINIB AZD6244; ACQUIRED-RESISTANCE; RAF INHIBITORS; BRAF MUTATIONS;
D O I
10.2147/DDDT.S131721
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Melanoma is increasing rapidly in incidence and prevalence, especially in younger females and older males. Treatment options have expanded beyond high-dose interleukin 2 and adoptive T-cell therapy to include inhibitors of immune checkpoints programmed death 1 (PD-1) and cytotoxic T-lymphocyte-associated protein 4 (CTLA-4) and small molecular inhibitors of pathways activated in melanoma, in particular the mitogen-activated protein kinase (MAPK) pathway. PD-1/CTLA-4 inhibitors and inhibitors of MAPK such as BRAF/MEK inhibitors have significantly improved survival in both the metastatic and, more recently, adjuvant settings. In this review, we discuss the preclinical data, clinical development, and potential use of novel MEK inhibitor binemetinib, particularly in the setting of NRAS mutant melanoma.
引用
收藏
页码:2553 / 2565
页数:13
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