sacituzumab tirumotecan + fruquintinib

Sacituzumab tirumotecan + fruquintinib is a combination therapy being investigated for the treatment of advanced gastrointestinal malignancies. **Sacituzumab tirumotecan** (also known as SKB264 or MK-2870) is a trophoblast cell-surface antigen 2 (TROP-2)-directed antibody-drug conjugate (ADC). It consists of a humanized monoclonal antibody targeting TROP-2, which is highly expressed in various epithelial tumors, conjugated via a pH-sensitive linker to a novel topoisomerase I inhibitor payload (a belotecan derivative). **Fruquintinib** is a highly selective and potent oral small-molecule inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3. By inhibiting these receptors, fruquintinib blocks VEGF-induced tyrosine kinase phosphorylation and subsequent downstream signaling, thereby inhibiting endothelial cell proliferation, migration, and tubule formation, which leads to the suppression of tumor angiogenesis. The combination aims to provide synergistic anti-tumor activity by combining the targeted cytotoxic delivery of the ADC with the anti-angiogenic effects of the VEGFR inhibitor, specifically as a second-line therapy for advanced gastric or gastroesophageal junction (GEJ) adenocarcinoma.

Other names

Sacituzumab Tirumotecan + FruquintinibSKB264 + FruquintinibMK-2870 + Fruquintinib