datopotamab deruxtecan   Click here for help

GtoPdb Ligand ID: 13304

Synonyms: Dato-DXd | datopotamab deruxtecan-dlnk | Datroway® | DS-1062 | DS-1062a
Approved drug
datopotamab deruxtecan is an approved drug (FDA (2025))
Compound class: Antibody
Comment: Datopotamab deruxtecan is an anti-TROP2 (TACSTD2) antibody drug conjugate (ADC). The cytotoxic payload is an exatecan-derived topoisomerase I inhibitor known as deruxtecan (DXd/MAAA1181a; PubChem CID 118305111). The ADC is highly stable in circulation and the DXd is only cleaved once inside cells where it induces DNA damage and apoptosis.

Overexpression of TROP2 is oncogenic and drives proliferation in cancer cells.
No information available.
Summary of Clinical Use Click here for help
Datopotamab deruxtecan was progressed as a clinical candidate for the treatment of advanced non-small cell lung cancer and triple-negative breast cancer [1]. It was granted first approval by the FDA in January 2025 to treat unresectable or metastatic hormone receptor (HR)-positive, HER2-negative breast cancer.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT05460273 A Study of Dato-DXd in Chinese Patients With Advanced Non-Small Cell Lung Cancer, Triple-negative Breast Cancer and Other Solid Tumors (TROPION-PanTumor02) Phase 1/Phase 2 Interventional AstraZeneca
NCT05104866 A Phase-3, Open-Label, Randomized Study of Dato-DXd Versus Investigator's Choice of Chemotherapy (ICC) in Participants With Inoperable or Metastatic HR-Positive, HER2-Negative Breast Cancer Who Have Been Treated With One or Two Prior Lines of Systemic Chemotherapy (TROPION-Breast01) Phase 3 Interventional AstraZeneca
NCT05629585 A Study of Dato-DXd With or Without Durvalumab Versus Investigator's Choice of Therapy in Patients With Stage I-III Triple-negative Breast Cancer Without Pathological Complete Response Following Neoadjuvant Therapy (TROPION-Breast03) Phase 3 Interventional AstraZeneca