Drug intelligence / Profile preview

MK-4830 + sacituzumab tirumotecan

Development stage
Preclinical
Lead developer
Merck
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

MK-4830 + sacituzumab tirumotecan is an investigational **combination therapy** composed of two experimental anticancer agents: MK-4830, a first-in-class human IgG4 monoclonal antibody targeting the immunoglobulin-like transcript 4 (ILT4) receptor, and sacituzumab tirumotecan, an investigational antibody-drug conjugate (ADC) derived from sacituzumab with a topoisomerase I inhibitor payload. MK-4830 is designed to inhibit immunosuppression mediated by myeloid cells in the tumor microenvironment by blocking ILT4, an inhibitory receptor on myeloid lineage cells, potentially enhancing T cell-mediated antitumor responses[1][7][11][12]. Sacituzumab tirumotecan, structurally related to sacituzumab govitecan, targets trophoblast cell-surface antigen 2 (Trop-2) highly expressed in several solid tumors and delivers a cytotoxic topoisomerase I inhibitor, aiming to kill Trop-2-expressing cancer cells directly. The rationale for combining these agents is to synergistically augment anticancer immune responses and direct tumor cell kill. The combination is under investigation for use in advanced solid tumors.

02

Targets

LILRB2 (Leukocyte immunoglobulin-like receptor subfamily B member 2)TACSTD2 (Tumor-associated calcium signal transducer 2)TOP1 (DNA Topoisomerase I)

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