Drug intelligence / Profile preview

gdc-1971 + cetuximab

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

**GDC-1971 + cetuximab** is an experimental combination therapy evaluated in oncology clinical trials. GDC-1971 is a small molecule, orally bioavailable, allosteric inhibitor of SHP2 (Src homology phosphotyrosyl phosphatase 2), a non-receptor tyrosine phosphatase that regulates signaling cascades including RAS/MAPK, PI3K/AKT, and JAK/STAT. Inhibition of SHP2 is being explored to overcome resistance in tumors driven by aberrant RAS signaling, particularly in the presence of activating KRAS mutations. Cetuximab is a monoclonal antibody targeting the Epidermal growth factor receptor (EGFR), acting as an antagonist and blocking ligand binding and downstream signaling, used in the treatment of colorectal, head and neck, and non-small cell lung cancers. The combination is designed to synergistically disrupt cancer cell proliferation and survival pathways, especially in solid tumors that are resistant to EGFR blockade alone. Development of this combination is led by Relay Therapeutics (originator of GDC-1971) and Genentech/Roche (cetuximab manufacturer)[1][3][5][7][8][9].

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Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)PTPN11 (Tyrosine-protein phosphatase non-receptor type 11)

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