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polfurmetinib
- Development stage
- Phase 1
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Polfurmetinib (PF-07799544) is a potent, brain-penetrant small molecule inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2) developed by Pfizer. It functions by blocking the MAPK/ERK signaling pathway, specifically inhibiting the phosphorylation of ERK1/2, which is frequently dysregulated in various cancers. A key differentiator for polfurmetinib is its ability to cross the blood-brain barrier, making it a potential candidate for treating central nervous system metastases. It is currently being investigated in Phase 1 clinical trials for advanced solid tumors, including BRAF-mutant melanoma, both as a monotherapy and in combination with the next-generation BRAF inhibitor claturafenib (PF-07799933).
- Other names
- ARRY-134ARRY134ARRY 134
02
Targets
MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)
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