vimseltinib

Vimseltinib is an oral, highly selective small molecule kinase inhibitor that targets the colony-stimulating factor 1 receptor (CSF1R), a type III receptor tyrosine kinase crucial for the survival, proliferation, and differentiation of myeloid lineage cells such as macrophages and osteoclasts. By binding to a unique switch-control region of CSF1R, vimseltinib stabilizes the receptor in its inactive state and prevents autophosphorylation and downstream signaling induced by its ligands (CSF1 and interleukin-34). This mechanism blocks tumor-associated macrophage activity in the tumor microenvironment, reduces inflammation, inhibits tumor growth, and enhances anti-tumor immune responses. Vimseltinib is indicated for adults with symptomatic tenosynovial giant cell tumor (TGCT) when surgical resection would likely cause worsening functional limitation or severe morbidity. It was developed by Deciphera Pharmaceuticals (now part of Ono Pharmaceutical) and approved by the FDA in February 2025[2][3][4][5][7].

Brand names

Romvimza

Other names

vimseltinib [INN]vimseltinib [USAN]