Trastuzumab Deruxtecan

Summary

Trastuzumab Deruxtecan (CHEMBL4297844) is an approved antibody drug conjugate (ATC L01FD04); indicated across 20 conditions including neoplasm and breast neoplasm; with CIViC clinical evidence for 26 variant-indication associations (e.g. ERBB2 Exon 20 Insertion in lung non-small cell carcinoma).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Antibody drug conjugate
• ATC class: L01FD04
• Indications: 20 conditions
• Clinical trials: 120
• Precision-oncology evidence (CIViC): 26 variant–indication associations

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4297844
Name	Trastuzumab Deruxtecan
Type	Antibody drug conjugate
Max phase	4
ATC	L01FD04

Also known as: DS-8201, Ds-8201a, DS-8201a, Enhertu, Fam-trastuzumab deruxtecan-nxki, Trastuzumab deruxtecan, Trastuzumab deruxtecan nxki, Trastuzumab deruxtecan-nxki, TRASTUZUMAB DERUXTECAN

Targets

Targets

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

20 indications (6 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
neoplasm	4	MONDO:0005070	EFO:0000616
breast neoplasm	4	MONDO:0021100	EFO:0003869
breast carcinoma	4	MONDO:0004989	EFO:0000305
HER2 positive breast carcinoma	4	MONDO:0006244	EFO:1000294
non-small cell lung carcinoma	3	MONDO:0005233	EFO:0003060
colorectal neoplasm	2	MONDO:0005335	EFO:0004142
digestive system neoplasm	2	MONDO:0021223	EFO:0008549
osteosarcoma	2	MONDO:0009807	EFO:0000637
gastric neoplasm	2	MONDO:0021085	MONDO:0001056
gastric adenocarcinoma	2	MONDO:0005036	EFO:0000503
inflammatory breast carcinoma	2	MONDO:0006804	EFO:1000984
triple-negative breast carcinoma	2	MONDO:0005494	EFO:0005537
adenocarcinoma	2	MONDO:0004970	MONDO:0003219

7 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 120.

Phase distribution

Phase	Trials
PHASE2	52
PHASE3	20
PHASE1	20
Not specified	13
PHASE1/PHASE2	12
PHASE4	2
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05376878	PHASE4	RECRUITING	An Investigational Scan (64Cu-DOTA-Trastuzumab PET/MRI) in Imaging Patients With HER2+ Breast Cancer With Brain Metastasis
NCT06429761	PHASE4	RECRUITING	Phase 4 Study to Assess the Safety of Trastuzumab Deruxtecan, in Indian Patients
NCT03734029	PHASE3	ACTIVE_NOT_RECRUITING	Trastuzumab Deruxtecan (DS-8201a) Versus Investigator’s Choice for HER2-low Breast Cancer That Has Spread or Cannot be Surgically Removed [DESTINY-Breast04]
NCT04494425	PHASE3	ACTIVE_NOT_RECRUITING	Study of Trastuzumab Deruxtecan (T-DXd) vs Investigator’s Choice Chemotherapy in HER2-low, Hormone Receptor Positive, Metastatic Breast Cancer
NCT04622319	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Trastuzumab Deruxtecan (T-DXd) Versus Trastuzumab Emtansine (T-DM1) in High-risk HER2-positive Participants With Residual Invasive Breast Cancer Following Neoadjuvant Therapy (DESTINY-Breast05)
NCT04704934	PHASE3	ACTIVE_NOT_RECRUITING	Trastuzumab Deruxtecan for Subjects With HER2-Positive Gastric Cancer or Gastro-Esophageal Junction Adenocarcinoma After Progression on or After a Trastuzumab-Containing Regimen (DESTINY-Gastric04)
NCT04739761	PHASE3	ACTIVE_NOT_RECRUITING	A Study of T-DXd in Participants With or Without Brain Metastasis Who Have Previously Treated Advanced or Metastatic HER2 Positive Breast Cancer
NCT04784715	PHASE3	ACTIVE_NOT_RECRUITING	Trastuzumab Deruxtecan (T-DXd) With or Without Pertuzumab Versus Taxane, Trastuzumab and Pertuzumab in HER2-positive Metastatic Breast Cancer (DESTINY-Breast09)
NCT05048797	PHASE3	ACTIVE_NOT_RECRUITING	A Study to Investigate the Efficacy and Safety of Trastuzumab Deruxtecan as the First Treatment Option for Unresectable, Locally Advanced/Metastatic Non-Small Cell Lung Cancer With HER2 Mutations
NCT05113251	PHASE3	ACTIVE_NOT_RECRUITING	Trastuzumab Deruxtecan (T-DXd) Alone or in Sequence With THP, Versus Standard Treatment (ddAC-THP), in HER2-positive Early Breast Cancer
NCT05950945	PHASE3	RECRUITING	Trastuzumab Deruxtecan (T-DXd) in Patients Who Have Hormone Receptor-negative and Hormone Receptor-positive HER2-low or HER2 IHC 0 Metastatic Breast Cancer
NCT06467357	PHASE3	RECRUITING	Phase 3 Study of T-DXd and Rilvegostomig Versus SoC in Advanced HER2-expressing Biliary Tract Cancer
NCT06731478	PHASE3	RECRUITING	Study of TDXd, Chemotherapy, Pembrolizumab, and Trastuzumab in First-Line Metastatic HER2-Positive Gastric or Gastroesophageal Junction Cancer
NCT06764875	PHASE3	RECRUITING	A Phase Ⅲ Study of Rilvegostomig in Combination With Fluoropyrimidine and Trastuzumab Deruxtecan as the First-line Treatment for HER2-positive Gastric Cancer
NCT06819007	PHASE3	RECRUITING	Study of Trastuzumab Deruxtecan With Bevacizumab Versus Bevacizumab Monotherapy for First-line Maintenance in HER2-Expressing Ovarian Cancer (DESTINY-Ovarian01)
NCT06899126	PHASE3	RECRUITING	Study of Trastuzumab Deruxtecan, Pembrolizumab, and Platinum-based Chemotherapy in First-line HER2 Overexpressing Non-small Cell Lung Cancer
NCT06989112	PHASE3	RECRUITING	DESTINY-Endometrial01: A Phase III Study of Trastuzumab Deruxtecan Plus Rilvegostomig or Pembrolizumab as First-Line Treatment of HER2-Expressing (IHC 3+/2+), Mismatch Repair Proficient (pMMR) Endometrial Cancer
NCT07022483	PHASE3	RECRUITING	Study of Trastuzumab Deruxtecan Versus Standard of Care Chemotherapy for HER2-Expressing (IHC 3+/2+) Endometrial Cancer
NCT07060807	PHASE3	RECRUITING	A Clinical Study of Patritumab Deruxtecan to Treat Breast Cancer (MK-1022-016)
NCT07543536	PHASE3	NOT_YET_RECRUITING	Megestrol Acetate for Fatigue Management in T-DXd Treated Breast Cancer
NCT07578116	PHASE3	NOT_YET_RECRUITING	Adding Surgery and Radiation to the Usual Treatment for HER2-Positive Breast Cancer That Had Already Spread at Diagnosis
NCT03523585	PHASE3	COMPLETED	DS-8201a in Pre-treated HER2 Breast Cancer That Cannot be Surgically Removed or Has Spread [DESTINY-Breast02]
NCT03334617	PHASE2	ACTIVE_NOT_RECRUITING	Phase II Umbrella Study of Novel Anti-cancer Agents in Participants With NSCLC Who Progressed on an Anti-PD-1/PD-L1 Containing Therapy
NCT03424005	PHASE1/PHASE2	RECRUITING	A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Patients With Metastatic or Locally Advanced Breast Cancer
NCT03742102	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	A Study of Novel Anti-cancer Agents in Patients With Metastatic Triple Negative Breast Cancer
NCT04379596	PHASE2	RECRUITING	Ph1b/2 Study of the Safety and Efficacy of T-DXd Combinations in Advanced HER2-expressing Gastric Cancer (DESTINY-Gastric03)
NCT04482309	PHASE2	ACTIVE_NOT_RECRUITING	A Phase 2 Study of T-DXd in Patients With Selected HER2 Expressing Tumors
NCT04538742	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	A Phase 1b/2 Study of T-DXd Combinations in HER2-positive Metastatic Breast Cancer
NCT04553770	PHASE2	RECRUITING	Trastuzumab Deruxtecan Alone or in Combination With Anastrozole for the Treatment of Early Stage HER2 Low, Hormone Receptor Positive Breast Cancer
NCT04639219	PHASE2	ACTIVE_NOT_RECRUITING	A Study of T-DXd for the Treatment of Solid Tumors Harboring HER2 Activating Mutations
NCT04986579	PHASE2	RECRUITING	Scalp Cooling in MBC
NCT05246514	PHASE2	ACTIVE_NOT_RECRUITING	A Single Arm Phase 2 Study to Evaluate Efficacy and Safety of Trastuzumab Deruxtecan for Patients With HER2 Mutant NSCLC
NCT05408845	PHASE2	RECRUITING	Testing the Use of Ado-Trastuzumab Emtansine Compared to the Usual Treatment (Chemotherapy With Docetaxel Plus Trastuzumab) or Trastuzumab Deruxtecan for Recurrent, Metastatic, or Unresectable HER2-Expressing Salivary Gland Cancers
NCT05480384	PHASE2	ACTIVE_NOT_RECRUITING	Adjuvant Trastuzumab Deruxtecan (Enhertu) & Nivolumab For Patients Who Are Disease Free After Completion of Trimodality Treatment For HER-2+ Cancers of Esophagus & Gastroesophageal Junction
NCT05704829	PHASE2	ACTIVE_NOT_RECRUITING	NeoAdjuvant Therapy With Trastuzumab-deruxtecan Versus Chemotherapy+Trastuzumab+Pertuzumab in HER2+ Early Breast Cancer
NCT05795101	PHASE2	RECRUITING	TRUDI: TDXD+Durva in HER2+/Low IBC
NCT05845450	PHASE2	RECRUITING	Pre-operative Targeted Treatments in Molecularly Selected Resectable Colorectal Cancer (UNICORN)
NCT05900206	PHASE2	RECRUITING	Trastuzumab Deruxtecan Versus Standard Neoadjuvant Treatment for HER2-positive Breast Cancer
NCT05953168	PHASE2	NOT_YET_RECRUITING	T-DXd in the First-Line Treatment of Locally Advanced or Metastatic TNBC-LAR HER2-low Patients
NCT05965479	PHASE2	RECRUITING	Developing ctDNA Guided Adjuvant Therapy for Gastrooesophageal Cancer

Clinical evidence (CIViC)

Variant × indication × effect (26 predictive associations from 27 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
ERBB2 Exon 20 Insertion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11765 +1
ERBB2 A775_G776insTVMA	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11755
ERBB2 A775_G776insV	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11756
ERBB2 A775_G776insVVMA	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11757
ERBB2 G776_V777delinsVCD	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11758
ERBB2 G776delinsLC	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11760
ERBB2 G776delinsVC	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11761
ERBB2 G778_P780dup	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11762
ERBB2 G778_S779insLPS	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11763
ERBB2 L755A	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11752
ERBB2 L755M	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11753
ERBB2 L755P	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11754
ERBB2 L755S	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID12233
ERBB2 L755W	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID12234
ERBB2 Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11731
ERBB2 Overexpression	Solid Tumor	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID12013
ERBB2 S310F	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11751
ERBB2 S310Y	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID12232
ERBB2 Y772_A775DUP	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC A	EID11764
ERBB2 Amplification	Colorectal Cancer	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC B	EID11321
ERBB2 Amplification	Stomach Cancer	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC B	EID7647
ERBB2 Amplification	Breast Cancer	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC B	EID7648
EGFR::ERBB4 Fusion	Lung Adenocarcinoma	Sensitivity/Response	Osimertinib + Mobocertinib + Trastuzumab Deruxtecan + Tarloxotinib	CIViC C	EID12373
ERBB2 G776delinsCV	Lung Non-small Cell Carcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC C	EID11759
ERBB2 H878Y	Lung Adenocarcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC C	EID12529
ERBB2 V659E	Lung Adenocarcinoma	Sensitivity/Response	Trastuzumab Deruxtecan	CIViC C	EID12528

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).