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sacituzumab tirumotecan + anlotinib
- Development stage
- Phase 2
- Lead developer
- Kelun-Biotech
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous, Oral
01
Overview
This combination therapy consists of sacituzumab tirumotecan (also known as SKB264 or MK-2870) and anlotinib. Sacituzumab tirumotecan is a trophoblast cell-surface antigen 2 (TROP2)-directed antibody-drug conjugate (ADC). It comprises a humanized monoclonal antibody targeting TROP2, conjugated via a carbonate-based linker to a cytotoxic payload, which is a derivative of the topoisomerase I inhibitor belotecan. Anlotinib is an orally active, multi-targeted small molecule tyrosine kinase inhibitor that primarily targets vascular endothelial growth factor receptors (VEGFR1, VEGFR2, and VEGFR3), fibroblast growth factor receptors (FGFR1-4), platelet-derived growth factor receptors (PDGFRα and PDGFRβ), and c-Kit. The combination is being evaluated for its synergistic potential in treating advanced malignancies, specifically unresectable, locally advanced, recurrent, or metastatic esophageal squamous cell carcinoma (ESCC), where the ADC provides targeted cytotoxicity and the kinase inhibitor disrupts angiogenesis and tumor signaling pathways.
- Other names
- SKB264 + anlotinibMK-2870 + anlotinib
02
Targets
FGFR1 (Fibroblast growth factor receptor 1)PDGFRB (Platelet-derived growth factor receptor beta)TACSTD2 (Tumor-associated calcium signal transducer 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)
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