refametinib
Overview
Refametinib is an oral, selective MEK1/2 inhibitor (MAP2K1/MAP2K2) investigated in RAS-mutant solid tumors. It targets the RAS/RAF/MAPK pathway, which is universally activated in advanced HCC despite a low somatic RAS/RAF mutation rate (<5%).
Evidence in the corpus
- Proposed as a biomarker-enriched targeted therapy for advanced HCC: RAS mutations cited as the enrollment criterion for an ongoing MEK inhibitor (refametinib) trial (NCT01915602) in a 2014 genomic review; the RAS/RAF/MAPK pathway is universally activated in advanced HCC even though somatic mutations are rare (<5%) PMID:24735922
- MEK inhibitor refametinib + sorafenib in RAS-mutant HCC: biomarker-enriched phase II in 16 RAS-mutant patients reported median OS 12.7 months; KRAS/NRAS mutations are rare in HCC (~1% each, only 4.4% of 1,318 ctDNA samples by BEAMing) PMID:24798001
Resistance mechanisms
Cancer types (linked)
- HCC — RAS-pathway activation rationale; ongoing trial NCT01915602
Sources
This page was processed by entity-page-writer on 2026-05-11. - PMID:24798001
This page was processed by wiki-cli on 2026-05-11.