rociletinib + trametinib

**rociletinib + trametinib** is an investigational, orally administered combination of two small molecule kinase inhibitors used in clinical trials for advanced or metastatic non-small cell lung cancer (NSCLC) bearing EGFR mutations. **Rociletinib** is a third-generation, irreversible EGFR tyrosine kinase inhibitor that selectively targets both common activating EGFR mutations (such as L858R, exon 19 deletions) and the resistance-associated T790M mutation, with minimal activity toward wild-type EGFR. **Trametinib** is a reversible, highly selective allosteric inhibitor of MEK1 and MEK2 kinases, acting downstream of EGFR in the MAPK signaling pathway. The combination aims to inhibit multiple nodes in the EGFR/MAPK pathway to overcome resistance to EGFR inhibitors in EGFR-mutated NSCLC[1][3][4].

Other names

rociletinib + trametinibCO-1686 + GSK1120212rociletinib + MekinistCO-1686 + trametinib