Last reviewed · How we verify
trastuzumab deruxtecan (T-DXd)
Trastuzumab deruxtecan (T-DXd) is a HER2-targeting antibody-drug conjugate that delivers a DNA crosslinking agent to cancer cells.
Trastuzumab deruxtecan (T-DXd) is a HER2-targeting antibody-drug conjugate that delivers a DNA crosslinking agent to cancer cells. Used for Locally advanced or metastatic HER2-positive breast cancer, Locally advanced or metastatic HER2-positive gastric or gastroesophageal junction adenocarcinoma.
At a glance
| Generic name | trastuzumab deruxtecan (T-DXd) |
|---|---|
| Also known as | ENHERTU®, Enhertu, DS-8201a, DS8201 |
| Sponsor | GI Innovation, Inc. |
| Drug class | HER2-targeting antibody-drug conjugate |
| Target | HER2 |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
T-DXd works by binding to the HER2 protein on the surface of cancer cells, which then internalizes the conjugate and releases the DNA crosslinking agent, causing DNA damage and cell death. This mechanism is specific to cancer cells that overexpress HER2, making it a targeted therapy for HER2-positive cancers.
Approved indications
- Locally advanced or metastatic HER2-positive breast cancer
- Locally advanced or metastatic HER2-positive gastric or gastroesophageal junction adenocarcinoma
Common side effects
- Fatigue
- Nausea
- Diarrhea
- Vomiting
- Neutropenia
- Thrombocytopenia
- Anemia
- Increased alanine aminotransferase
- Increased aspartate aminotransferase
- Increased gamma-glutamyltransferase
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)
- Trastuzumab Deruxtecan in First-Line HER2-Positive Metastatic Breast Cancer With Proactive Toxicity Management (PHASE2)
- 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)
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:
- trastuzumab deruxtecan (T-DXd) CI brief — competitive landscape report
- trastuzumab deruxtecan (T-DXd) updates RSS · CI watch RSS
- GI Innovation, Inc. portfolio CI