ripretinib + binimetinib

**Ripretinib + binimetinib** is an investigational combination of two small molecule drugs: ripretinib, a switch-control tyrosine kinase inhibitor, and binimetinib, a MEK inhibitor. Ripretinib broadly inhibits KIT and PDGFRA kinases by stabilizing their inactive forms, targeting drug-resistant mutations associated with gastrointestinal stromal tumors (GIST). Binimetinib inhibits MEK1/2 kinase, a downstream effector in the MAPK pathway. The combination is being explored as a late-line or alternative therapy in refractory GIST, especially post-progression on standard treatments, with the goal of overcoming resistance by dual blockade of upstream (KIT/PDGFRA) and downstream (MEK) signaling[1]. There is preclinical and clinical rationale that combining a tyrosine kinase inhibitor with a MAPK pathway inhibitor can improve disease control, but this regimen remains experimental in GIST[1].

Brand names

None known for the combination.QINLOCK (ripretinib)MEKTOVI (binimetinib)

Other names

ripretinib + binimetinib