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PF-07284892 + encorafenib + cetuximab
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
**PF-07284892 + encorafenib + cetuximab** is an investigational combination regimen for treatment-refractory advanced solid tumors, notably BRAF^V600E^-mutant colorectal cancer. PF-07284892 (ARRY-558) is a small molecule, highly potent, selective allosteric inhibitor of Src homology region 2 domain-containing phosphatase-2 (SHP2). SHP2 mediates bypass signaling that confers resistance to targeted therapies such as BRAF and EGFR inhibition. Encorafenib is a small molecule BRAF inhibitor, and cetuximab is an anti-EGFR monoclonal antibody. In phase I trials, this combination has shown the ability to overcome therapeutic resistance by simultaneously disrupting BRAF and EGFR signaling and eliminating compensatory SHP2-driven pathway activation[1][2][4]. The regimen is administered orally (PF-07284892, encorafenib) and intravenously (cetuximab), and is currently under development for BRAF^V600E^-mutant colorectal cancers and other solid tumors[1][4].
- Other names
- PF-07284892 + encorafenib + cetuximab
02
Targets
PTPN11 (Tyrosine-protein phosphatase non-receptor type 11)EGFR T790M (Epidermal growth factor receptor T790M mutant)BRAF V600ERAF1 (c-Raf-1 (Y340D/Y341D))
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