作者: Rafael Rosell , Santiago Viteri , Miguel Angel Molina , José Miguel Sánchez-Torres
DOI: 10.3978/J.ISSN.2218-6751.2013.04.01
关键词:
摘要: Inhibitors targeting active protein kinases, such as EGFR or ALK, have demonstrated significant efficacy in the treatment of lung cancer. Activating mutations MAPK pathway, which includes enzymes RAS, RAF, MEK, and ERK, result constitutive signalling, leading to oncogenic cell proliferation escape from apoptosis; therefore this pathway is a focus crucial interest for development cancer drugs. In melanoma, most commonly mutated gene BRAF, with usually occurring about 50% all tumours. The BRAF Val600Glu (V600E) mutation constitutes more than 90% melanoma. V600E shows great dependency on MEK activity, offers rational therapeutic strategy genetically defined tumour subtype. use vemurafenib dabrafenib, agents that block signaling patients melanoma mutation, has been associated prolonged survival progression-free survival. frequency adenocarcinoma 1.5% 2.8%. Treatment BRAF-mutant adenocarcinomas dabrafenib under evaluation phase 2 trial, could represent another milestone individualized therapy patients. next step will be combination inhibitor trametinib.