Vimseltinib

Vimseltinib, sold under the brand name Romvimza, is an anti-cancer medication used for the treatment of tenosynovial giant cell tumor.^[1][2] Vimseltinib is a kinase inhibitor.^[1][2] Vimseltinib is a macrophage colony-stimulating factor receptor antagonist.^[3]

Vimseltinib

Clinical data
Trade names	Romvimza
License data	US DailyMed: Vimseltinib
Routes of administration	By mouth
Drug class	Antineoplastic
ATC code	None
Legal status
Legal status	US: ℞-only[1]
Identifiers
IUPAC name 3-methyl-5-[6-methyl-5-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxypyridin-2-yl]-2-(propan-2-ylamino)pyrimidin-4-one
CAS Number	1628606-05-2
PubChem CID	86267612
IUPHAR/BPS	11190
DrugBank	DB17520
ChemSpider	95499700
UNII	PX9FTM69BF
KEGG	D12238
ChEMBL	ChEMBL5095202
Chemical and physical data
Formula	C23H25N7O2
Molar mass	431.500 g·mol−1
3D model (JSmol)	Interactive image
SMILES CC1=C(C=CC(=N1)C2=CN=C(N(C2=O)C)NC(C)C)OC3=CC(=NC=C3)C4=CN(N=C4)C
InChI InChI=1S/C23H25N7O2/c1-14(2)27-23-25-12-18(22(31)30(23)5)19-6-7-21(15(3)28-19)32-17-8-9-24-20(10-17)16-11-26-29(4)13-16/h6-14H,1-5H3,(H,25,27) Key:TVGAHWWPABTBCX-UHFFFAOYSA-N

The most common adverse reactions, including laboratory abnormalities, include increased aspartate aminotransferase, periorbital edema, fatigue, rash, increased cholesterol, peripheral edema, face edema, decreased neutrophils, decreased leukocytes, pruritus, and increased alanine aminotransferase.^[2]

Vimseltinib was approved for medical use in the United States in February 2025.^[2][4]

Medical uses

Vimseltinib is indicated for the treatment of adults with symptomatic tenosynovial giant cell tumor for which surgical resection will potentially cause worsening functional limitation or severe morbidity.^[1][2]

History

The efficacy of vimseltinib was evaluated in MOTION (NCT05059262), a double-blind, multicenter, randomized (2:1), placebo-controlled trial in participants with tenosynovial giant cell tumor for whom surgical resection may cause worsening functional limitation or severe morbidity.^[2] Eligible participants had a confirmed diagnosis of tenosynovial giant cell tumor with measurable disease (RECIST v1.1) with at least one lesion having a minimum size of 2 cm.^[2] Participants were randomized to placebo or vimseltinib, 30 mg twice weekly administered for 24 weeks, during the double-blind period (part 1).^[2] During the open-label period (part 2), patients could continue vimseltinib and those receiving placebos could crossover to vimseltinib.^[2] Randomization was stratified by tumor location (lower limb versus all other) and region (United States versus Non-US).^[2] A total of 123 participants were randomized: 83 to the vimseltinib arm and 40 to placebo during part 1.^[2]

The US. Food and Drug Administration (FDA) granted the application for vimseltinib priority review designation.^[2]

Society and culture

Legal status

Vimseltinib was approved for medical use in the United States in February 2025.^[2][5]

Names

Vimseltinib is the international nonproprietary name.^[6]

Vimseltinib is sold under the brand name Romvimza.^[1][2]