CH7057288 / Roche - LARVOL DELTA

Discovery of CH7057288 as an Orally Bioavailable, Selective, and Potent pan-TRK Inhibitor. (PubMed, J Med Chem) - "Compound 1 showed high TRK selectivity but moderate cell growth inhibitory activity as well as a potential risk of inducing CYP3A4. In this report, chemical modification intended to improve TRK inhibition and avoid CYP3A4 induction enabled us to identify an orally bioavailable, selective, and potent TRK inhibitor 7."

Journal • Oncology • CYP3A4

Selective TRK inhibitor CH7057288 against TRK fusion-driven cancer. (PubMed, Mol Cancer Ther) - "Additionally, gene expression analysis revealed that CH7057288 suppressed mitogen-activated protein kinase (MAPK) and E2F pathways as downstream signaling of TRK fusion. Therefore, CH7057288 could be a promising therapeutic agent for TRK fusion-positive cancer."

Journal