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Trastuzumab deruxtecan-nxki
Trastuzumab deruxtecan-nxki is an antibody-drug conjugate that binds HER2-positive cancer cells and delivers a topoisomerase I inhibitor payload to kill them.
Trastuzumab deruxtecan-nxki is an antibody-drug conjugate that binds HER2-positive cancer cells and delivers a topoisomerase I inhibitor payload to kill them. Used for HER2-positive metastatic breast cancer, HER2-positive gastric or gastroesophageal junction adenocarcinoma, HER2-low metastatic breast cancer.
At a glance
| Generic name | Trastuzumab deruxtecan-nxki |
|---|---|
| Sponsor | Memorial Sloan Kettering Cancer Center |
| Drug class | HER2-targeted antibody-drug conjugate (ADC) |
| Target | HER2 (human epidermal growth factor receptor 2) |
| Modality | Biologic |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
Mechanism of action
This drug combines trastuzumab, a monoclonal antibody targeting HER2, with deruxtecan, a potent topoisomerase I inhibitor, linked via a cleavable linker. The antibody portion recognizes and binds to HER2 on cancer cell surfaces, allowing internalization and release of the cytotoxic payload inside the cell. The topoisomerase I inhibitor then causes DNA damage and cell death, with potential bystander killing of nearby HER2-low or HER2-negative cells.
Approved indications
- HER2-positive metastatic breast cancer
- HER2-positive gastric or gastroesophageal junction adenocarcinoma
- HER2-low metastatic breast cancer
Common side effects
- Nausea
- Fatigue
- Vomiting
- Diarrhea
- Decreased hemoglobin/anemia
- Interstitial lung disease
- Left ventricular dysfunction
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)
- 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)
- TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer (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-nxki CI brief — competitive landscape report
- Trastuzumab deruxtecan-nxki updates RSS · CI watch RSS
- Memorial Sloan Kettering Cancer Center portfolio CI