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sacituzumab tritumotecan
- Development stage
- Unknown
- Lead developer
- Kelun-Biotech
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Sacituzumab tritumotecan (SKB264/MK-2870) is a trophoblast cell-surface antigen 2 (TROP2)-directed antibody-drug conjugate (ADC) developed by Kelun-Biotech and licensed to Merck & Co. (MSD) for global development. The molecule consists of a humanized monoclonal antibody targeting TROP2 conjugated to a proprietary topoisomerase I inhibitor payload, tritumotecan (a belotecan derivative), via a novel pH-sensitive linker. By targeting TROP2, which is highly expressed in various epithelial tumors, the ADC delivers the cytotoxic payload directly to cancer cells, inducing DNA damage and apoptosis. It is currently under investigation in multiple Phase 3 clinical trials for indications such as triple-negative breast cancer (TNBC) and non-small cell lung cancer (NSCLC), and is being explored in combination with immune checkpoint inhibitors like iparomlimab and tuvonralimab for rare indications such as gastric-type adenocarcinoma of the cervix.
- Other names
- sacituzumab tritumotecanSKB264 ADCSKB-264 ADCSKB 264 ADC
02
Targets
TACSTD2 (Tumor-associated calcium signal transducer 2)TOP1 (DNA Topoisomerase I)
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