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曲美替尼是一种丝裂原活化细胞外信号调节激酶1/2可逆性抑制剂,主要通过对MEK蛋白(胞外信号相关激酶(ERK)通路的上游调节器)的作用,影响MAPK通路,抑制细胞增殖;在体内、体外均可抑制BRAF V600突变阳性的黑色素瘤细胞的生长。美国FDA于2013年5月批准其用于治疗BRAF V600E或V600K基因突变的不可切除或转移性黑色素瘤。本品在早期的试验中显示了很好的临床疗效,特别是对于BRAF V600突变的黑色素瘤,在近期的III期临床研究中,相比于其他细胞毒的化疗药物,显示了无进展生存期和总生存期更长的优势。本文以曲美替尼为关键词进行文献检索,并对其作用机制、药动学、临床评价,剂量及安全性等进行综述。
Trametinib, a mitogen-activated extracellular signal-regulated kinase 1/2 reversible inhibitor, affects the MAPK pathway primarily through the action of the MEK protein, an upstream regulator of the extracellular signal-related kinase (ERK) pathway , Inhibits cell proliferation; inhibits the growth of BRAF V600 mutation-positive melanoma cells both in vitro and in vivo. The US FDA approved in May 2013 its non-resectable or metastatic melanoma for the treatment of BRAF V600E or V600K mutations. This product has shown good clinical efficacy in early trials, especially for BRAF V600 mutant melanoma, which shows progression-free survival in recent phase III clinical studies compared to other cytotoxic chemotherapeutic agents And longer overall survival advantage. In this paper, trimetidibidine as the key word for literature search, and its mechanism of action, pharmacokinetics, clinical evaluation, dose and safety are reviewed.