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DS-8201a
DS-8201a is an anti-HER2 antibody-drug conjugate that delivers a cytotoxic payload directly to HER2-expressing cancer cells.
DS-8201a is an anti-HER2 antibody-drug conjugate that delivers a cytotoxic payload directly to HER2-expressing cancer cells. Used for HER2-positive metastatic breast cancer, HER2-low metastatic breast cancer, HER2-positive gastric cancer.
At a glance
| Generic name | DS-8201a |
|---|---|
| Also known as | Trastuzumab deruxtecan, Trastuzumab deruxtecan (T-DXd), Experimental product |
| Sponsor | Daiichi Sankyo Co., Ltd. |
| Drug class | HER2-targeted antibody-drug conjugate |
| Target | HER2 (human epidermal growth factor receptor 2) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
DS-8201a (trastuzumab deruxtecan) combines a humanized anti-HER2 monoclonal antibody with a topoisomerase I inhibitor payload linked via a cleavable linker. The antibody binds to HER2 on cancer cells, enabling internalization and release of the cytotoxic agent intracellularly, which causes DNA damage and cell death. This design allows for potent tumor killing while potentially reducing systemic toxicity compared to conventional chemotherapy.
Approved indications
- HER2-positive metastatic breast cancer
- HER2-low metastatic breast cancer
- HER2-positive gastric cancer
Common side effects
- Nausea
- Fatigue
- Vomiting
- Decreased hemoglobin
- Interstitial lung disease
Key clinical trials
- Testing the Combination of Two Anti-cancer Drugs, DS-8201a and AZD6738, for The Treatment of Advanced Solid Tumors Expressing the HER2 Protein or Gene, The DASH Trial (PHASE1)
- Testing the Combination of DS-8201a and Olaparib in HER2-Expressing Cancers With Expansion in Patients With Platinum Resistant Ovarian Cancer (PHASE1)
- Testing the Safety of the Combination of Anti-Cancer Drugs CX-5461 (Pidnarulex) and Trastuzumab Deruxtecan (T-DXd) for Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Solid Tumors and Breast Cancer (PHASE1)
- Testing the Safety and Tolerability of the Anti-cancer Drugs Trastuzumab Deruxtecan and Neratinib for Cancers With Changes in the HER2 Gene (PHASE1)
- Sotorasib in Combination With Trastuzumab Deruxtecan for the Treatment of Locally Advanced and Metastatic Non-small Cell Lung Cancer With a KRAS G12C Mutation (PHASE1, PHASE2)
- Trastuzumab Deruxtecan for the Treatment of HER2+ Newly Diagnosed or Recurrent Osteosarcoma (PHASE2)
- A Phase 2 Study of T-DXd in Patients With Selected HER2 Expressing Tumors (PHASE2)
- Personalized Antibody-Drug Conjugate Therapy Based on RNA and Protein Testing for the Treatment of Advanced or Metastatic Solid Tumors (The ADC MATCH Screening and Treatment Trial) (PHASE2)
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 |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- DS-8201a CI brief — competitive landscape report
- DS-8201a updates RSS · CI watch RSS
- Daiichi Sankyo Co., Ltd. portfolio CI