vimseltinib

{{Infobox drug

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| tradename = Romvimza

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| DailyMedID = Vimseltinib

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| routes_of_administration = By mouth

| class = Antineoplastic

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| CAS_number = 1628606-05-2

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| PubChem = 86267612

| IUPHAR_ligand = 11190

| DrugBank = DB17520

| ChemSpiderID = 95499700

| UNII = PX9FTM69BF

| KEGG = D12238

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| ChEMBL = 5095202

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| 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

| C=23 | H=25 | N=7 | O=2

| 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

| StdInChI = 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)

| StdInChIKey = TVGAHWWPABTBCX-UHFFFAOYSA-N

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Vimseltinib, sold under the brand name Romvimza, is an anti-cancer medication used for the treatment of tenosynovial giant cell tumor.{{cite web | title=Romvimza- vimseltinib capsule | website=DailyMed | date=18 February 2025 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f73c7a62-9601-4df0-810f-100f515d79ea | access-date=3 March 2025}} Vimseltinib is a kinase inhibitor. Vimseltinib is a macrophage colony-stimulating factor receptor antagonist.{{cite journal | vauthors = Caldwell TM, Ahn YM, Bulfer SL, Leary CB, Hood MM, Lu WP, Vogeti L, Vogeti S, Kaufman MD, Wise SC, Le Bourdonnec B, Smith BD, Flynn DL | title = Discovery of vimseltinib (DCC-3014), a highly selective CSF1R switch-control kinase inhibitor, in clinical development for the treatment of Tenosynovial Giant Cell Tumor (TGCT) | journal = Bioorganic & Medicinal Chemistry Letters | volume = 74 | issue = | pages = 128928 | date = October 2022 | pmid = 35961460 | doi = 10.1016/j.bmcl.2022.128928 | doi-access = free }}

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.

Vimseltinib was approved for medical use in the United States in February 2025.{{cite web | title=FDA approves vimseltinib for symptomatic tenosynovial giant cell tumor | website=U.S. Food and Drug Administration (FDA) | date=14 February 2025 | url=https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-vimseltinib-symptomatic-tenosynovial-giant-cell-tumor | access-date=16 February 2025}} {{PD-notice}}{{cite web | title=Novel Drug Approvals for 2025 | website=U.S. Food and Drug Administration (FDA) | date=21 February 2025 | url=https://www.fda.gov/drugs/novel-drug-approvals-fda/novel-drug-approvals-2025 | access-date=9 March 2025}}

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.

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. 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. Participants were randomized to placebo or vimseltinib, 30 mg twice weekly administered for 24 weeks, during the double-blind period (part 1). During the open-label period (part 2), patients could continue vimseltinib and those receiving placebos could crossover to vimseltinib. Randomization was stratified by tumor location (lower limb versus all other) and region (United States versus Non-US). A total of 123 participants were randomized: 83 to the vimseltinib arm and 40 to placebo during part 1.

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

Society and culture

= Legal status =

Vimseltinib was approved for medical use in the United States in February 2025.{{cite press release | title=U.S. FDA Grants Full Approval of Deciphera's Romvimza (vimseltinib) for the Treatment of Symptomatic Tenosynovial Giant Cell Tumor (TGCT) | publisher=Deciphera Pharmaceuticals | via=Business Wire | date=14 February 2025 | url=https://www.businesswire.com/news/home/20250214768549/en/U.S.-FDA-Grants-Full-Approval-of-Deciphera%E2%80%99s-ROMVIMZA%E2%84%A2-vimseltinib-for-the-Treatment-of-Symptomatic-Tenosynovial-Giant-Cell-Tumor-TGCT | access-date=16 February 2025}}

= Names =

Vimseltinib is the international nonproprietary name.{{cite journal | vauthors = ((World Health Organization)) | year = 2021 | title = International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 85 | journal = WHO Drug Information | volume = 35 | issue = 1 | hdl = 10665/340684 | hdl-access = free | author-link = World Health Organization }}

Vimseltinib is sold under the brand name Romvimza.

References

External links

{{ClinicalTrialsGov|NCT05059262|Study of Vimseltinib for Tenosynovial Giant Cell Tumor (MOTION)}}

Category:Antineoplastic drugs

Category:Pyrazoles

Category:Pyridines

Category:Pyrimidones