Drug intelligence / Profile preview

sacituzumab tirumotecan + bevacizumab

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

**Sacituzumab tirumotecan + bevacizumab** is an investigational combination therapy composed of two distinct agents: - **Sacituzumab tirumotecan**: an antibody-drug conjugate (ADC) targeting TROP2 (trophoblast cell-surface antigen 2), constructed using the same anti-TROP2 antibody as sacituzumab govitecan, but conjugated to a novel payload—a belotecan-derived topoisomerase I inhibitor—via a methyl sulfonyl pyrimidine linker. The linker allows selective payload release under the acidic and enzymatic conditions found in the tumor microenvironment. Sacituzumab tirumotecan destroys tumor cells expressing TROP2 through targeted cytotoxicity by delivering the payload intracellularly, causing DNA damage and apoptosis[2]. - **Bevacizumab**: a recombinant humanized monoclonal antibody that inhibits vascular endothelial growth factor A (VEGF-A), blocking angiogenesis required for tumor growth and maintenance. This combination is currently undergoing phase 3 clinical investigation for the treatment of advanced gynecologic malignancies, specifically fallopian tube cancer, ovarian cancer, and primary peritoneal cancer. The combination aims to leverage both targeted cytotoxicity (via TROP2-directed ADC) and inhibition of tumor-associated angiogenesis[3][4][6][10].

Brand names
Avastin
Other names
sacituzumab tirumotecan + bevacizumab
02

Targets

TOP1 (DNA Topoisomerase I)TACSTD2 (Tumor-associated calcium signal transducer 2)VEGFA (Vascular endothelial growth factor A)

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