Datopotamab deruxtecan is an antibody-drug conjugate carrying a topoisomerase-I inhibitor payload for use in patients with previously treated HR+, HER2- breast cancer and EGFR+ non-small cell lung cancer. Datopotamab deruxtecan-dlnk (Datroway) was approved by the US FDA in January 2025 for the treatment of hormone receptor positive, HER2 negative unresectable or metastatic breast cancer.
- Mechanism
- Curator reviewed · 3 references
Datopotamab deruxtecan is an antibody-drug conjugate comprising three main components: datopotamab, DXd, and a cleavable linker between the two. Datopotamab is a monoclonal antibody directed against tumor-associated antigen (TAA) trophoblast cell surface protein 2 (Trop-2), which is a transmembrane protein overexpressed in various tumors with low and/or restricted expression in normal healthy tissues. Datopotamab binds to Trop-2 on the surface of tumor cells, after which the antibody-drug conjugate undergoes internalization and intracellular linker cleavage by lysosomal enzymes. Upon its release, DXd - a cytotoxic DNA topoisomerase I inhibitor - targets and binds to DNA topoisomerase I, thereby stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks, inhibition of DNA replication, and apoptosis.
- Primary indication
- Datopotamab deruxtecan is indicated for the treatment of adult patients with unresectable or metastatic, hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative (IHC 0, IHC 1+ or IHC 2+/ISH-) breast cancer who have...Curator reviewed · 6 structured indications
- First approval
- United States, 2025 · European Union, 2025
- Also known as
- Datopotamab deruxtecan-dlnk · Datopotamab-deruxtecan
- Code names
- DATO-DXD · DS-1062 · DS-1062a
- Brand names
Resolves to
What you can answer from here — as of June 25, 2026
Which drugs share a target with Datopotamab deruxtecan, and which of those have an active Phase 3 trial?
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