Drug intelligence / Profile preview

petosemtamab + FOLFIRI

Development stage
Unknown
Lead developer
Merus
Modality
Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

This is a combination therapy consisting of **petosemtamab** (also known as MCLA-158), a bispecific monoclonal antibody targeting epidermal growth factor receptor (EGFR) and leucine-rich repeat-containing G-protein coupled receptor 5 (LGR5)[1][3], used together with **FOLFIRI**, a standard chemotherapy regimen containing folinic acid (leucovorin), fluorouracil (5-FU), and irinotecan[2][4][6]. - Petosemtamab is designed to block EGFR and selectively target LGR5-positive cancer stem cells, inducing dual blockade of tumor cell growth and stemness in EGFR-dependent solid tumors, such as metastatic colorectal cancer (mCRC)[1][3][5]. - FOLFIRI works by disrupting DNA synthesis and replication in rapidly dividing cancer cells, contributing to cytotoxic effects and cell death[2][4][6]. This combination is under investigation for second-line treatment of metastatic colorectal cancer (mCRC), particularly in RAS/RAF wild-type, microsatellite stable (MSS) tumors[3][5]. Petosemtamab was developed by Merus[3]. The FOLFIRI regimen uses established generic drugs.

Other names
petosemtamab + FOLFIRIpetosemtamab and FOLFIRIMCLA-158 + FOLFIRI
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)LGR5 (Leucine-rich repeat-containing G-protein coupled receptor 5)

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