Phase I Study of Mosperafenib, a Novel Paradox Breaker B-Raf Proto-Oncogene Serine/Threonine Kinase (BRAF) Inhibitor, in Patients With BRAF V600-Mutant Solid Tumors.

doi:10.1200/JCO-25-02444

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Phase I Study of Mosperafenib, a Novel Paradox Breaker B-Raf Proto-Oncogene Serine/Threonine Kinase (BRAF) Inhibitor, in Patients With BRAF V600-Mutant Solid Tumors.

Journal of clinical oncology : official journal of the American Society of Clinical Oncology - 10 May 2026

Vieito Maria, Fontana Elisa, Han Catherine H, Castanon Eduardo, Pinato David J, Bechter Oliver, Eefsen Rikke L, Moreno Irene, Prenen Hans, Dummer Reinhard, Plummer Ruth, Schnetzler Gabriel, Kornacker Martin, Pettazzoni Piergiorgio, Renner Florian, About Mahdi, Serrano-Serrano Martha L, Godfried Sie Christina, Keelara Abiraj, Roller Andreas, Dejardin David, Cinato Elisa, Fakolade Tomi, Guarin Ernesto, Flinn Nick, Kratochwil Nicole A, Keshelava Nino

Abstract excerpt

PURPOSE: BRAF V600 mutations are tumor-agnostic oncogenic drivers whose targeted inhibition is challenged by therapeutic resistance. Mosperafenib is a novel paradox breaker and brain-penetrant BRAF inhibitor (BRAFi), tested in this study for safety, maximum tolerated dose (MTD), pharmacokinetics (PK), and preliminary clinical activity. PATIENTS AND METHODS: This phase Ia/b study was conducted in patients with...

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PMID: 41894647
DOI: 10.1200/JCO-25-02444

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