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Pimasertib is an investigational, highly selective, oral, small molecule inhibitor of mitogen‐activated protein kinases 1 and 2 (MEK) within the MAPK signaling pathway.

To date, pimasertib has been dosed in hundreds of patients across multiple Phase 1/2 clinical trials for various tumor types. Preclinical data has indicated that the combination of a MEK inhibitor, such as pimasertib, and a type II RAF inhibitor may have synergistic anti-tumor activity.

A Phase 1/2 trial (FIRELIGHT-1) is evaluating the safety, tolerability, and preliminary efficacy of combining pimasertib with tovorafenib in adolescent (≥12 years of age) and adult patients with recurrent, progressive or refractory solid tumors with MAPK pathway aberrations.

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