dabrafenib + LTT462 + LXH254

A combination regimen comprising three small molecule inhibitors: **dabrafenib** (a BRAF inhibitor), **LTT462** (an ERK1/2 inhibitor), and **LXH254** (a type II RAF inhibitor with selectivity for BRAF and CRAF). This regimen is being investigated in clinical trials for patients with advanced or metastatic cancers harboring BRAF V600 mutations, especially colorectal cancer and melanoma. Dabrafenib directly inhibits mutated BRAF kinase activity. LXH254 inhibits BRAF and CRAF kinases, including dimerized forms, and is designed to overcome resistance mechanisms in RAS/RAF pathway-driven tumors. LTT462 targets ERK1/2, acting downstream of RAF and MEK, to further suppress MAPK pathway signaling. Developed to target multiple nodes in the MAPK pathway, this regimen aims to overcome resistance seen with single-agent BRAF or MEK inhibition.

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