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datopotamab deruxtecan + pembrolizumab
- Development stage
- Unknown
- Lead developer
- Daiichi Sankyo
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Datopotamab deruxtecan + pembrolizumab is an investigational combination therapy consisting of an antibody-drug conjugate (datopotamab deruxtecan) and an immune checkpoint inhibitor (pembrolizumab). Datopotamab deruxtecan (Dato-DXd) is composed of a humanized anti-TROP2 monoclonal antibody linked to a potent topoisomerase I inhibitor payload via a tetrapeptide-based linker. Once bound to TROP2 on cancer cells, the conjugate is internalized, and the payload is released in lysosomal compartments, causing DNA damage and triggering cellular apoptosis. Pembrolizumab is an anti-PD-1 monoclonal antibody that enhances T-cell immune responses against tumor cells. The combination is being evaluated in several Phase 3 clinical trials for non-small cell lung cancer (NSCLC), with early data showing promising efficacy and manageable safety profile.
- Other names
- Datopotamab deruxtecan plus pembrolizumab
02
Targets
TACSTD2 (Tumor-associated calcium signal transducer 2)PDCD1 (Programmed cell death protein 1 receptor)TOP1 (DNA Topoisomerase I)
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