PF-07799544 + PF-07799933

PF-07799544 + PF-07799933 is an investigational, oral, dual small-molecule combination therapy under development for the treatment of BRAF-mutant melanoma and other solid tumors with MAPK pathway alterations. PF-07799544 is a selective, reversible, and fully brain-penetrant inhibitor of mitogen-activated protein kinase kinases 1 and 2 (MEK1/2), key regulators in the MAPK/ERK signaling pathway. PF-07799933 is a selective ATP-competitive BRAF kinase inhibitor with activity against BRAF V600 and non-V600 mutations; it is designed to show minimal paradoxical activation and sparing of wild-type RAF dimers, thus potentially minimizing some of the liabilities seen with earlier BRAF inhibitors. The combination is under clinical investigation to address resistance to BRAF/MEK inhibitors and improve efficacy, including in patients with brain metastases. Pfizer is the developer of both compounds, and all clinical studies to date have been sponsored by Pfizer. The combination is being tested as an oral therapy in ongoing phase 1 trials in participants with advanced solid tumors with BRAF mutations, in particular melanoma and other solid tumors.

Other names

claturafenib + PF-07799544