Drug intelligence / Profile preview

pf-07799544 + encorafenib

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

PF-07799544 + encorafenib is an investigational combination regimen of a next-generation, brain-penetrant MEK inhibitor (PF-07799544) and a BRAF inhibitor (encorafenib, marketed as BRAFTOVI) administered orally. PF-07799544 inhibits MEK, a key kinase in the MAPK signaling pathway implicated in tumor growth and progression, while encorafenib inhibits mutant BRAF kinase, targeting tumors harboring BRAF mutations. The combination is being studied in advanced solid tumors, particularly BRAF-mutant melanoma and other solid tumors with BRAF alterations, with the aim to suppress MAPK pathway signaling more effectively than either drug alone[1][3][4][5][7]. PF-07799544 is currently investigational and not FDA approved, while encorafenib is approved for certain cancer indications.

Brand names
BRAFTOVI
Other names
encorafenibBRAFTOVI
02

Targets

MAP2K4 (Mitogen-activated protein kinase kinase 4)STK36 (Serine/threonine-protein kinase 36)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)JNK (Mitogen-activated protein kinase kinase kinase family)LIMK2 (LIM domain kinase 2)LIMK1 (LIM domain kinase 1)MRP (Multidrug resistance-associated protein family)BRAF V600ERAF1 (c-Raf-1 (Y340D/Y341D))MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)

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