Daisuke Kotani, GI Medical Oncologist, Chief Physician at the Department of Gastrointestinal Oncology at the National Cancer Center Hospital East, Japan, shared a post on X:
” Ph1 Mosperafenib: A Next-Gen “BRAF Paradox Breaker” Mosperafenib
BRAFi-naive mCRC: ORR 24%, PFS 7.3 mo
Target inhibition: ≥90% pERK inhibition sustained for 18h at 1,200mg TID
Dimer Breaker vs. Monomer Inhibitor:
- High-dose potential without increasing class-specific skin toxicities
- Deeper pERK suppression
- CNS activity via brain penetration
- Meaningful single-agent activity in both BRAFi-naive and exposed patients.”
Title: 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
Authors: Maria Vieito, Elisa Fontana, Catherine H. Han, Eduardo Castanon, David J. Pinato, Oliver Bechter, Rikke L. Eefsen, Irene Moreno, Hans Prenen, Reinhard Dummer, Ruth Plummer, Gabriel Schnetzler, Martin Kornacker, Piergiorgio Pettazzoni, Florian Renner, Mahdi About, Martha L. Serrano-Serrano, Christina Godfried Sie, Abiraj Keelara, Andreas Roller, David Dejardin, Elisa Cinato, Tomi Fakolade, Ernesto Guarin, Nick Flinn, Nicole A. Kratochwil, Nino Keshelava
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