Drug intelligence / Profile preview

sacituzumab tirumotecan + immune checkpoint inhibitor

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

Overview

Sacituzumab tirumotecan (MK-2870/SKB264) is a trophoblast cell-surface antigen 2 (Trop-2)-directed antibody-drug conjugate (ADC) consisting of a humanized anti-Trop-2 monoclonal antibody conjugated to a topoisomerase I inhibitor payload (tirumotecan, a camptothecin derivative). This combination therapy pairs the ADC with an immune checkpoint inhibitor (ICI), typically targeting the PD-1/PD-L1 pathway, to enhance anti-tumor activity through synergistic mechanisms: the ADC induces direct tumor cell death and potentially promotes immunogenic cell death, while the ICI reinvigorates the T-cell-mediated immune response. This specific combination is being investigated in a Phase 2 clinical trial for patients with recurrent or metastatic head and neck squamous cell carcinoma (R/M HNSCC) who have progressed on prior therapies.

Other names
sacituzumab tirumotecan plus immune checkpoint inhibitor
02

Targets

TACSTD2 (Tumor-associated calcium signal transducer 2)TOP1 (DNA Topoisomerase I)CD274 (Programmed cell death protein 1 ligand 1)PDCD1 (Programmed cell death protein 1 receptor)

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