Drug intelligence / Profile preview

petosemtamab + FOLFOX

Development stage
Unknown
Lead developer
Merus
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

**petosemtamab + FOLFOX** is a combination therapy under clinical investigation for advanced solid tumors, especially metastatic colorectal cancer. Petosemtamab (MCLA-158) is a bispecific monoclonal antibody that targets both Epidermal growth factor receptor (EGFR) and Leucine-rich repeat-containing G-protein coupled receptor 5 (LGR5), designed to inhibit EGFR-dependent tumor growth and stemness in cancer cells. FOLFOX is an established chemotherapy regimen consisting of folinic acid (leucovorin), fluorouracil (5-FU), and oxaliplatin, primarily used to induce cytotoxicity in rapidly dividing tumor cells. This combination is being tested—most notably in Phase 1/2 clinical trials—for its tolerability and anti-tumor activity in patients with metastatic colorectal cancer (mCRC) who previously received certain chemotherapy regimens. Petosemtamab is developed by Merus, and FOLFOX is a generic regimen with no single developer. The combination leverages targeted inhibition of EGFR/LGR5 and standard chemotherapeutic cytotoxicity.

02

Targets

TS (Thymidylate synthase)LGR5 (Leucine-rich repeat-containing G-protein coupled receptor 5)DNAFcγR (Low affinity immunoglobulin gamma Fc region receptor II-c)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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