US clinical-stage biopharma firm Day One Biopharmaceuticals has entered into a global licensing agreement with Germany’s Merck KGaA (MRK: DE), for an exclusive license to develop and commercialize pimasertib as well as a second compound, MSC2015103B.
Pimasertib and MSC2015103B are oral, highly-selective small molecule allosteric inhibitors of MEK 1/2, a key enzyme in the MAPK signaling pathway. Dysregulation of the MAPK pathway has been shown to occur in many cancers.
Pimasertib has been studied in more than 10 Phase I/II clinical trials in around 900 patients with various tumor types. Day One plans to initiate a Phase I/II study to evaluate the safety, tolerability, and preliminary efficacy of combining pimasertib with DAY101, the company’s potential first-in-class, oral, brain-penetrant, highly selective type II pan-RAF kinase inhibitor, in patients ≥12 years of age with recurrent, progressive, or refractory solid tumors with MAPK pathway aberrations.
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