Drug intelligence / Profile preview

CGX1321 + encorafenib + cetuximab

Development stage
Unknown
Lead developer
Curegenix
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

CGX1321 + encorafenib + cetuximab is a combination of three agents being investigated for the treatment of metastatic colorectal cancer (mCRC), particularly those harboring BRAF V600E or other BRAF mutations. - **CGX1321** is a small molecule inhibitor targeting the Wnt/β-catenin pathway, developed to inhibit tumor growth driven by abnormal Wnt signaling. - **Encorafenib** is a small molecule BRAF inhibitor that targets the BRAF V600E-mutated protein, suppressing MAPK pathway-driven tumor growth. - **Cetuximab** is a monoclonal antibody targeting the epidermal growth factor receptor (EGFR), blocking ligand-induced signaling that promotes tumor cell proliferation. The combination aims to block key oncogenic pathways (Wnt/β-catenin, BRAF-MEK-ERK, EGFR) implicated in mCRC pathogenesis and treatment resistance, maximizing tumor growth inhibition and overcoming resistance seen with single-agent or doublet regimens. The combination has been evaluated in clinical trials for safety and efficacy, with encorafenib + cetuximab having established efficacy as standard of care in previously treated BRAF V600E-mutant mCRC, and triplet or quadruple regimens (including agents like binimetinib or CGX1321) being studied in advanced phases for greater benefit[1][2].

Other names
CGX1321 + encorafenib + cetuximab
02

Targets

PORCN (Porcupine protein)RAF1 (c-Raf-1 (Y340D/Y341D))BRAF V600EEGFR T790M (Epidermal growth factor receptor T790M mutant)

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