Drug intelligence / Profile preview

pembrolizumab + MK-4830 + irinotecan

Development stage
Phase 2
Lead developer
Merck
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

A three-drug combination consisting of pembrolizumab (a humanized monoclonal antibody targeting PD-1), MK-4830 (a monoclonal antibody targeting immunoglobulin-like transcript 4, ILT4), and irinotecan (a topoisomerase I inhibitor). **Pembrolizumab** is an immune checkpoint inhibitor that blocks PD-1, enhancing anti-tumor T-cell activity. **MK-4830** targets and inhibits ILT4, a myeloid-associated immunosuppressive receptor, aiming to relieve myeloid-driven suppression in the tumor microenvironment and potentiate the anti-tumor immune response. **Irinotecan** is a cytotoxic chemotherapy drug that inhibits topoisomerase I, leading to DNA damage and cell death, primarily used in various solid tumors such as colorectal cancer. This combination is being clinically investigated for efficacy and safety in advanced solid tumors, including esophageal cancer, typically via intravenous administration[5][6][8]. The rationale is to synergistically integrate immune checkpoint inhibition, myeloid suppression blockade, and cytotoxic chemotherapy for enhanced anti-tumor activity.

Brand names
Keytruda (for pembrolizumab)Camptosar (for irinotecan; specify if Camptosar formulation)no unique brand name for the three-drug combination
Other names
pembrolizumab + MK-4830 + irinotecan
02

Targets

TOP1 (DNA Topoisomerase I)LILRB2 (Leukocyte immunoglobulin-like receptor subfamily B member 2)PDCD1 (Programmed cell death protein 1 receptor)

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