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DS-1062a
DS-1062a is an antibody-drug conjugate that targets TROP-2 on cancer cells and delivers a topoisomerase I inhibitor payload to induce cell death.
DS-1062a is an antibody-drug conjugate that targets TROP-2 on cancer cells and delivers a topoisomerase I inhibitor payload to induce cell death. Used for Advanced or metastatic non-small cell lung cancer, Advanced gastric or gastroesophageal junction cancer.
At a glance
| Generic name | DS-1062a |
|---|---|
| Also known as | Datopotamab deruxtecan (Dato-DXd), Datopotamab Deruxtecan |
| Sponsor | Gustave Roussy, Cancer Campus, Grand Paris |
| Drug class | Antibody-drug conjugate (ADC) |
| Target | TROP-2 (Trophoblast cell surface antigen 2) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
DS-1062a combines a humanized anti-TROP-2 monoclonal antibody with a topoisomerase I inhibitor (SN-38 derivative) linked via a cleavable linker. Upon binding to TROP-2 expressed on tumor cells, the conjugate is internalized and the payload is released intracellularly, leading to DNA damage and apoptosis. This targeted approach aims to maximize efficacy while minimizing systemic toxicity.
Approved indications
- Advanced or metastatic non-small cell lung cancer
- Advanced gastric or gastroesophageal junction cancer
Common side effects
- Neutropenia
- Anemia
- Nausea
- Fatigue
- Diarrhea
Key clinical trials
- Study of DS-1062a in Advanced or Metastatic Non-small Cell Lung Cancer With Actionable Genomic Alterations (TROPION-Lung05) (PHASE2)
- Study of DS-1062a Versus Docetaxel in Previously Treated Advanced or Metastatic Non-small Cell Lung Cancer With or Without Actionable Genomic Alterations (TROPION-LUNG01) (PHASE3)
- Phase III Study of Datopotamab Deruxtecan Versus Docetaxel in Previously Treated TROP2-positive Advanced or Metastatic Non-squamous NSCLC Without Actionable Genomic Alterations (PHASE3)
- Study of Dato-DXd as Monotherapy and in Combination With Anti-cancer Agents in Patients With Advanced Solid Tumours (TROPION-PanTumor03) (PHASE2)
- Study of Datopotamab Deruxtecan Plus Carboplatin or Cisplatin Versus Gemcitabine Plus Carboplatin or Cisplatin in Participants With Locally Advanced or Metastatic Urothelial Carcinoma (PHASE2, PHASE3)
- 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) (PHASE3)
- 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) (PHASE1, PHASE2)
- A Study to Investigate the Efficacy and Safety of Dato-DXd With or Without Osimertinib Compared With Platinum Based Doublet Chemotherapy in Participants With EGFR-Mutated Locally Advanced or Metastatic Non-Small Cell Lung Cancer (PHASE3)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |