Drug intelligence / Profile preview

D3S-001 + cetuximab

Development stage
Unknown
Lead developer
D3 Bio
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
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Overview

D3S-001 + cetuximab is an investigational combination therapy for advanced solid tumors harboring the KRAS G12C mutation, notably in non-small cell lung cancer and colorectal cancer. **D3S-001** (elisrasib) is an orally available, next-generation small molecule inhibitor that targets the GDP-bound form of the mutant KRAS G12C protein with high covalent potency and rapid target engagement, aiming to suppress oncogenic signaling in tumors resistant to first-generation KRAS G12C inhibitors. **Cetuximab** is a chimeric monoclonal antibody that binds to the extracellular domain of the Epidermal Growth Factor Receptor (EGFR), preventing ligand-induced activation and downstream signaling involved in cell proliferation and survival. The combination is designed to overcome adaptive or intrinsic resistance mechanisms, leveraging the distinct and potentially synergistic inhibitory effects on the KRAS and EGFR pathways. Ongoing clinical trials (Phase 1/2) are investigating the safety and efficacy of this combination in patients with advanced/metastatic cancers carrying the KRAS G12C mutation[1][2][3][6].

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Targets

KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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