tunlametinib

Tunlametinib is an orally bioavailable, highly selective small molecule inhibitor of mitogen‑activated protein kinase kinase (MEK1 and MEK2), key components of the MAPK/ERK signaling pathway. It is developed primarily for the treatment of solid tumors harboring RAS or RAF mutations, including melanoma, non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and neurofibromatosis type 1 (NF1) plexiform neurofibromas. Tunlametinib has demonstrated high potency and selectivity in preclinical studies, with significant tumor suppression and inhibition of ERK phosphorylation. In March 2024, it received conditional approval in China for use in patients with NRAS-mutated advanced melanoma who have failed anti-PD‑1/PD‑L1 therapy[1][2][5][6].

Brand names

tunlametinib

Other names

4-fluoro-5-((2-fluoro-4-iodophenyl)amino)-n-(2-hydroxyethoxy)-6-benzothiazolecarboxamide6-benzothiazolecarboxamide, 4-fluoro-5-((2-fluoro-4-iodophenyl)amino)-n-(2-hydroxyethoxy)-