Trastuzumab deruxtecan
Highest phase reached
Approved
Drug type
Antibody drug conjugate
First approval year
2019
- First approval year
- 2019
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Antibody drug conjugate
- Drug name
- Trastuzumab deruxtecan
- enhertu
- Enhertu
- ds 8201
- ds 8201a
- DS-8201
- Ds-8201a
- DS-8201a
- DS-8201a (DP)
- DS-8201a (DP1)
- DS-8201a (DP2)
- Enhertu
- fam trastuzumab deruxtecan nxki
- Fam-trastuzumab deruxtecan-nxki
- Fam-Trastuzumab Deruxtecan-Nxki
- fam-trastuzumab deruxtecan-nxki (T-DXd)
- Fam-Trastuzumab Deruxtecan-Nxki (TDxD)
- trastuzumab deruxtecan
- Trastuzumab deruxtecan
- Trastuzumab Deruxtecan
- Trastuzumab deruxtecan (DS-8201a)
- trastuzumab deruxtecan (T-DXd)
- Trastuzumab deruxtecan (T-DXd)
- Trastuzumab Deruxtecan (T-DXd)
- trastuzumab deruxtecan (T-DXd) (IV)
- trastuzumab deruxtecan [INN]
- TRASTUZUMAB DERUXTECAN [JAN]
- Trastuzumab deruxtecan [MI]
And 16 more, listed on the interactive page.
- ATC classification codes
- L01FD04
Sources for recorded values
- CAS registry numbers
- 1826843-81-5
- ChEMBL ID
- CHEMBL4297844
- RxNorm IDs (RxCUI)
- 2267582
- FDA ingredient codes (UNII)
- 5384HK7574
- Applicant
- DAIICHI SANKYO
- Approval date
- 20 Dec 2019
- Application number
- BLA761139
- Status
- Authorised
- Status date
- 18 Jan 2021
- Authorisation date
- 18 Jan 2021
- Approved indications
- 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. Other unresectable or metastatic solid tumours Enhertu as monotherapy is indicated for the treatment of adult patients with unresectable or metastatic HER2-positive (IHC3+) solid tumours who have received prior treatment and who have no satisfactory treatment options (see sections 4.4 and 5.1; for biomarker-based patient selection, see section 4.2).
- Product number
- EMEA/H/C/005124
- Authorisation holder
- Daiichi Sankyo Europe GmbH
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- Yes
- Additional monitoring
- Yes
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Breast Neoplasms
European medicines record
- Patents
- 0
- Designations
- 12
- Earliest recorded loss of exclusivity
- 15 Jan 2028
- First in class
- No
- Fast track
- Yes
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- Yes
- Availability
- Prescription only
- Boxed warning
- Yes
- Drug name stem
- -mab; -mab; -tecan
Administration routes
- Parenteral
- Mechanism
- Receptor protein-tyrosine kinase erbB-2 binding agent
- Action type
- BINDING_AGENT
- Target
- Receptor tyrosine-protein kinase erbB-2
- Protein identifier
- P04626
- Mechanism
- DNA topoisomerase I inhibitor
- Action type
- Inhibitor
- Target
- DNA topoisomerase 1
- Protein identifier
- P11387
- Mechanism
- Receptor protein-tyrosine kinase erbB-2 binding agent
- Action type
- BINDING AGENT
- Target
- Receptor tyrosine-protein kinase erbB-2
- Mechanism
- DNA topoisomerase I inhibitor
- Action type
- Inhibitor
- Target
- DNA topoisomerase 1
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000503
- Subject identifier
- D013274
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Osteosarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000637
- Subject identifier
- D012516
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003869
- Subject identifier
- D001943
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003897
- Subject identifier
- D013274
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0004142
- Subject identifier
- D015179
- Condition
- Triple Negative Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005537
- Subject identifier
- D064726
- Condition
- Digestive System Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0008549
- Subject identifier
- D004067
- Condition
- Neoplasm Metastasis
- Highest recorded phase
- 1
- Condition identifier
- EFO:0009708
- Subject identifier
- D009362
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:1000294
- Subject identifier
- D001943
- Condition
- Inflammatory Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000984
- Subject identifier
- D058922
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0001056
- Subject identifier
- D013274
- Condition
- Biliary Tract Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0003060
- Subject identifier
- D001661
- Condition
- Adenocarcinoma
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0003219
- Subject identifier
- D000230
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0005575
- Subject identifier
- D015179
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0007254
- Subject identifier
- D001943
- Condition
- Esophageal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0007576
- Subject identifier
- D004938
- Condition identifier
- EFO_0000305
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000503
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000637
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003869
- Condition identifier
- EFO_0004142
- Highest recorded phase
- 2
- Condition identifier
- EFO_0005537
- Highest recorded phase
- 2
- Condition identifier
- EFO_0008549
- Highest recorded phase
- 2
- Condition identifier
- EFO_0009708
- Highest recorded phase
- 1
- Condition identifier
- EFO_1000294
- Condition identifier
- EFO_1001012
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0000521
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001056
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0001475
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002087
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002158
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002280
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002974
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003060
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0003219
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003219
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0004669
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005028
- Highest recorded phase
- 2
And 23 more, listed on the interactive page.
- Warning
- Black Box Warning
- Effect
- gastrointestinal toxicity
- Warning
- Black Box Warning
- Effect
- teratogenicity
- Warning
- Black Box Warning
- Effect
- gastrointestinal toxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- teratogenicity
- Country
- United States
- Event
- administration site vasculitis
- Reports
- 1
- Reporting signal score
- 7.41182
- Event
- alopecia
- Reports
- 29
- Reporting signal score
- 34.6509
- Event
- arthralgia
- Reports
- 1
- Reporting signal score
- 7.86053
- Event
- ascites
- Reports
- 11
- Reporting signal score
- 15.442
- Event
- constipation
- Reports
- 19
- Reporting signal score
- 9.18719
- Event
- decreased appetite
- Reports
- 24
- Reporting signal score
- 16.216
- Event
- diarrhoea
- Reports
- 42
- Reporting signal score
- 10.0402
- Event
- disease progression
- Reports
- 50
- Reporting signal score
- 86.6126
- Event
- fatigue
- Reports
- 60
- Reporting signal score
- 25.4639
- Event
- gastrointestinal toxicity
- Reports
- 4
- Reporting signal score
- 8.13286
- Event
- interstitial lung disease
- Reports
- 59
- Reporting signal score
- 143.962
- Event
- lung opacity
- Reports
- 4
- Reporting signal score
- 13.8321
- Event
- metastases to central nervous system
- Reports
- 12
- Reporting signal score
- 29.2605
- Event
- metastases to lung
- Reports
- 5
- Reporting signal score
- 8.81826
- Event
- metastases to meninges
- Reports
- 3
- Reporting signal score
- 8.60573
- Event
- metastases to skin
- Reports
- 3
- Reporting signal score
- 9.70753
- Event
- myelosuppression
- Reports
- 8
- Reporting signal score
- 14.5186
- Event
- nail bed inflammation
- Reports
- 2
- Reporting signal score
- 8.4385
- Event
- nasal mucosal disorder
- Reports
- 2
- Reporting signal score
- 7.48989
- Event
- nausea
- Reports
- 121
- Reporting signal score
- 108.145
- Event
- neutrophil count decreased
- Reports
- 15
- Reporting signal score
- 19.1791
- Event
- pain
- Reports
- 2
- Reporting signal score
- 8.21349
- Event
- pleural effusion
- Reports
- 12
- Reporting signal score
- 9.75383
- Event
- pneumonitis
- Reports
- 33
- Reporting signal score
- 82.1028
- Event
- radiation necrosis
- Reports
- 2
- Reporting signal score
- 7.13502
And 3 more, listed on the interactive page.
- NCT02564900
- NCT04639219
- NCT05372614
- NCT06311214
- NCT03248492
- NCT03366428
- NCT03424005
- NCT03523585
- NCT03529110
- NCT03734029
- NCT04494425
- NCT04538742
- NCT04622319
- NCT04739761
- NCT04752059
- NCT04784715
- NCT05113251
- NCT05633979
- NCT05704829
- NCT05710666
- NCT05744375
- NCT05795101
- NCT05900206
- NCT05950945
- NCT06048718
And 31 more, listed on the interactive page.
- Dose
- 5.4 mg/kg
- Route
- Intravenous
- How often
- Every 3 weeks
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Natural product
- No
- Component
- Glycosylation sites (N)
- Sequence
- Asn-300 $ Asn-300''''
- Component
- Heavy chain
- Type
- Protein
- Sequence
- EVQLVESGGGLVQPGGSLRLSCAASGFNIKDTYIHWVRQAPGKGLEWVARIYPTNGYTRYADSVKGRFTISADTSKNTAYLQMNSLRAEDTAVYYCSRWGGDGFYAMDYWGQGTLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
- Component
- Disulfide bridges
- Sequence
- 22-96 $ 22''-96'' $ 23'-88' $ 23'''-88''' $ 134'-194' $ 134'''-194''' $ 147-203 $ 147''-203'' $ 214'-223 $ 214'''-223'' $ 229-229'' $ 232-232'' $ 264-324 $ 264''-324'' $ 370-428 $ 370''-428''
- Component
- Light chain
- Type
- Protein
- Sequence
- DIQMTQSPSSLSASVGDRVTITCRASQDVNTAVAWYQQKPGKAPKLLIYSASFLYSGVPSRFSGSRSGTDFTLTISSLQPEDFATYYCQQHYTTPPTFGQGTKVEIKRTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
- Component
- Glycosylation sites (N)
- Sequence
- Asn-300 $ Asn-300''
- 65597-406
Related records
Trials (173)
- A Clinical Study of Patritumab Deruxtecan to Treat Breast Cancer (MK-1022-016)
- A Phase 1 Trial of ZN-A-1041 Enteric Capsules or Combination in Participants With Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Advanced Solid Tumors
- A Phase 1b Study of T-DXd Combinations in HER2-low Advanced or Metastatic Breast Cancer
- A Phase 1b/2 Study of T-DXd Combinations in HER2-positive Metastatic Breast Cancer
- A Phase 2 Study of T-DXd in Patients With Selected HER2 Expressing Tumors
- A Phase II Study of HLX22 in Combination With Trastuzumab Deruxtecan in HER2-low, Hormone Receptor Positive Locally Advanced or Metastatic Breast Cancer Patients
- A Phase Ⅲ Study of Rilvegostomig in Combination With Fluoropyrimidine and Trastuzumab Deruxtecan as the First-line Treatment for HER2-positive Gastric Cancer
- A Randomised Trial Comparing Trastuzumab Deruxtecan to CDK4/6 Inhibitors in Non-luminal A, ER-positive/HER2-low Metastatic Breast Cancer
- A Randomized Secondary Adjuvant Treatment Intervention Study Comparing Trastuzumab-Deruxtecan to SOC Therapy in eBC Patients With Molecular Relapse
- A Real-world Clinical Study of T-DXd for the Treatment of Chinese Patients With HER2 Overexpressing and HER2 Underexpressing Advanced Breast Cancer
- A Safety and Activity Study of SBT6050 in Combination With Other HER2-directed Therapies for HER2-positive Cancers
- A Single Arm Phase 2 Study to Evaluate Efficacy and Safety of Trastuzumab Deruxtecan for Patients With HER2 Mutant NSCLC
- A Study Comparing BL-M07D1 With DS-8201 in Patients With HR-Positive, HER2-Low Expressing Recurrent/Metastatic Breast Cancer
- A Study Evaluating the Efficacy and Safety of De Trastuzumab (T-DXd) in Combination with Immunotherapy for the Neoadjuvant Treatment of HR-positive HER2 Low-expressing Chinese Patients with Early-stage Breast Cancer
- A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Patients With Metastatic or Locally Advanced Breast Cancer
- A Study of DS-1103a Combination Therapy in Participants With Advanced Solid Tumors
- A Study of DS-8201a in Metastatic Breast Cancer Previously Treated With Trastuzumab Emtansine (T-DM1)
- A Study of Novel Agents or Combinations as Perioperative Treatment in Participants With Locally Advanced Resectable Gastroesophageal Adenocarcinoma
- A Study of Novel Anti-cancer Agents in Patients With Metastatic Triple Negative Breast Cancer
- A Study of Patritumab Deruxtecan (HER3-DXd) in Combination With Trastuzumab Deruxtecan (T-DXd) in Participants With HR-Positive, HER2-Low or HER2-Ultralow Unresectable or Metastatic Breast Cancer
Approved for (6)
- Breast cancer
- Breast carcinoma
- Breast neoplasm
- Cancer
- HER2 positive breast carcinoma
- Neoplasm
In development for (13)
- Biliary tract cancer Phase 3
- Colorectal cancer Phase 2
- Colorectal neoplasm Phase 2
- Digestive system neoplasm Phase 2
- Esophageal cancer Phase 2
- Gastric adenocarcinoma Phase 2
- Gastric cancer Phase 2
- Gastric neoplasm Phase 2
- Gastroesophageal junction adenocarcinoma Phase 2
- Inflammatory breast carcinoma Phase 2
- Non-small cell lung carcinoma Phase 3
- Osteosarcoma Phase 2
- Triple-negative breast carcinoma Phase 2