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Drug

Trastuzumab deruxtecan

Approved · EMA
ClassReceptor protein-tyrosine kinase erbB-2 binding agentActively researchedLate-stage developmentRising momentum

Also known as Trastuzumab-deruxtecan.

25
Research papers
92
Active clinical trials
2
Protein targets
1
Regulatory events
Latest activity
beta

Recent clinical, regulatory, research and industry developments relating to this drug.

Phase 1b Study of Pidnarulex and Trastuzumab Deruxtecan in Patients With HER2 Expressing Solid Tumors

Clinical trial2026-07-13Results expected Q1 2028 · ClinicalTrials.gov

Trastuzumab Deruxtecan with Nivolumab in HER2-Expressing Metastatic Breast or Urothelial Cancer: Analysis of the Phase Ib DS8201-A-U105 Study.

Research2024-12-01Clinical cancer research : an official journal of the American Association for Cancer Research

Approval: Enhertu (EMA)

Regulatory2021-01-18EMA

Profile

Identifiers & mechanism

Canonical identifiers, marketed brand names and mechanism, resolved across RxNorm, ChEMBL and ATC.

Canonical name
Trastuzumab deruxtecan
Aliases & brands
Trastuzumab-deruxtecan
RxNorm CUI
2267582
ChEMBL ID
CHEMBL4297844
ATC codes
L01FD04
UNII
5384HK7574
Primary mechanism
Receptor protein-tyrosine kinase erbB-2 binding agent
Regulatory jurisdictions
ema

Pharmacology & targets

2 targets

Known molecular targets and mechanisms supported by curated pharmacology databases.

BINDING AGENTReceptor protein-tyrosine kinase erbB-2 binding agent
DNA topoisomerase 1
TOP1 · P11387
INHIBITORDNA topoisomerase I inhibitor

Regulatory timeline

1 event

The complete regulatory record, grouped by authority — approvals, safety advisories and label changes. Each authority shows its most recent events; expand one to read its full history.

Earliest approval
2021-01-18
Latest approval
2021-01-18
Authorities
EMA
Total events
1
emaEuropean Medicines Agency· 1 event
2021-01-18Approval
Approval: Enhertu (EMA)
Indication: Breast cancerHER2-positive breast cancerEnhertu as monotherapy is indicated for the treatment of adult patients with unresectable or metastatic HER2-positive breast cancer whoShow full indication

Breast cancerHER2-positive breast cancerEnhertu as monotherapy is indicated for the treatment of adult patients with unresectable or metastatic HER2-positive breast cancer who have received one or more prior anti-HER2-based regimens.HER2-low and HER2-ultralow breast cancerEnhertu as monotherapy is indicated for the treatment of adult patients with unresectable or metastatic  hormone receptor (HR)-positive, HER2-low or HER2-ultralow breast cancer who have received at least one endocrine therapy in the metastatic setting and who are not considered suitable for endocrine therapy as the next line of treatment (see sections 4.2 and 5.1). HER2-low breast cancer who have received prior chemotherapy in the metastatic setting or developed disease recurrence during or within 6 months of completing adjuvant chemotherapy (see section 4.2). Non-small cell lung cancer (NSCLC)Enhertu as monotherapy is indicated for the treatment of adult patients with advanced NSCLC whose tumours have an activating HER2 (ERBB2) mutation and who require systemic therapy following platinum-based chemotherapy with or without immunotherapy.Gastric cancer Enhertu as monotherapy is indicated for the treatment of adult patients with advanced HER2-positive gastric or gastroesophageal junction (GEJ) adenocarcinoma who have received a prior trastuzumab-based regimen.

Evidence ↗

Contains information from the European Medicines Agency (European Medicines Agency), © EMA, reused under CC BY 4.0.

Clinical trials

106 trials

The current development programme across all trial phases — status mix, phase distribution and the late-stage studies shaping the evidence base.

Development programme
CLINICALTRIALS.GOV · LIVE REGISTRY
106
registered trials across all phases
LATEST COMPLETION 2025
92
Active studies
66
Recruiting
24
Late-stage (III+)
8
Completed
6
Discontinued
PHASE DISTRIBUTIONn = 106
Early Phase 11Phase 115Phase 1 / 215Phase 251Phase 322Phase 42

Late-stage studies

Phase III+ trials still open or recently active — where late-stage evidence is being generated.

Recent completions

Trials that read out recently, adding to the completed evidence base.

Research activity

25 papers

Key research shaping understanding of this drug, combining the latest publications with the most influential evidence.

Publications over time
20192025
Most influential

Trastuzumab Deruxtecan in Previously Treated HER2-Low Advanced Breast Cancer.

The New England journal of medicine · 2022 · 1,982 cites

Trastuzumab Deruxtecan in Previously Treated HER2-Positive Breast Cancer.

The New England journal of medicine · 2020 · 1,483 cites

Trastuzumab Deruxtecan in Previously Treated HER2-Positive Gastric Cancer.

The New England journal of medicine · 2020 · 983 cites

Trastuzumab Deruxtecan versus Trastuzumab Emtansine for Breast Cancer.

The New England journal of medicine · 2022 · 893 cites

Trastuzumab Deruxtecan in <i>HER2</i>-Mutant Non-Small-Cell Lung Cancer.

The New England journal of medicine · 2022 · 751 cites

Efficacy and Safety of Trastuzumab Deruxtecan in Patients With HER2-Expressing Solid Tumors: Primary Results From the DESTINY-PanTumor02 Phase II Trial.

Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2024 · 717 cites
Recent papers
Major research themes8
Breast Neoplasms13Immunoconjugates11Trastuzumab8Erb-b2 Receptor Tyrosine Kinases7Brain Neoplasms3Camptothecin3Carcinoma, Non-Small-Cell Lung3Lung Diseases, Interstitial3
Journals, researchers & institutions
Top journals
  • The New England journal of medicine5
  • Nature medicine4
  • ESMO open3
  • Journal of clinical oncology : official journal of the American Society of Clinical Oncology3
  • Clinical cancer research : an official journal of the American Association for Cancer Research2
  • The oncologist2
Leading researchers
  • Iwata H7
  • Kim SB6
  • Tsurutani J6
  • Curigliano G5
  • Im SA5
  • Park YH5
  • Hamilton E4
  • Hurvitz SA4
Leading institutions
free-text, unnormalised
  • Aichi Cancer Center Hospital6
  • Asan Medical Center5
  • Dana-Farber Cancer Institute5
  • Memorial Sloan Kettering Cancer Center5
  • Advanced Cancer Translational Research Institute4
  • National Cancer Center Hospital4

Related diseases

8 conditions

Regulator-approved indications and conditions co-mentioned with this drug across the research literature. Number shows shared papers.

Related drugs

4 matches

Drugs sharing diseases, protein targets and literature with this one. Ranked by graph evidence (shared targets + diseases weighted above co-mentions).

Studied across 15 of the same disease areas as Trastuzumab deruxtecan in the shared literature.

25 shared papers15 shared diseases

Studied across 11 of the same disease areas as Trastuzumab deruxtecan in the shared literature.

11 shared diseases1 shared paper

Studied across 11 of the same disease areas as Trastuzumab deruxtecan in the shared literature.

11 shared diseases1 shared paper

Studied across 3 of the same disease areas as Trastuzumab deruxtecan in the shared literature.

3 shared diseases1 shared paper
References & data sources
  • RxNorm (U.S. National Library of Medicine) — drug identity
  • ChEMBL (EMBL-EBI) & UniProt — pharmacology and targets
  • Europe PMC — research literature
  • ClinicalTrials.gov — clinical trials
  • Regulatory event sources are credited in the Regulatory Timeline above.