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sacituzumab tirumotecan + KL-A167 + fruquintinib

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

Overview

This combination therapy consists of the Trop2-directed antibody-drug conjugate (ADC) sacituzumab tirumotecan (SKB264), the PD-L1 monoclonal antibody KL-A167, and the selective VEGFR inhibitor fruquintinib. Sacituzumab tirumotecan targets Trop2-expressing cancer cells to deliver a cytotoxic topoisomerase I inhibitor payload (KL610023), while KL-A167 inhibits the PD-1/PD-L1 pathway to enhance the anti-tumor immune response. Fruquintinib selectively inhibits VEGFR-1, -2, and -3, thereby suppressing tumor angiogenesis and potentially normalizing the tumor vasculature to improve drug delivery. This triplet regimen is being evaluated by Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University in a randomized Phase 2 study for the treatment of advanced or metastatic triple-negative breast cancer (mTNBC), aiming to leverage the synergistic effects of cytotoxic cell killing, immune checkpoint blockade, and anti-angiogenesis.

Brand names: Elunate
Other names: sacituzumab tirumotecan + KL-A167 + fruquintinibSKB264 + KL-A167 + fruquintinibTrop2-ADC + PD-L1 inhibitor + VEGFR inhibitor

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)TACSTD2 (Tumor-associated calcium signal transducer 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)CD274 (Programmed cell death protein 1 ligand 1)TOP1 (DNA Topoisomerase I)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)FGFR1 (Fibroblast growth factor receptor 1)

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