Datopotamab Deruxtecan

Summary

Datopotamab Deruxtecan (CHEMBL4297939) is a phase-3 clinical-stage antibody drug conjugate (ATC L01FX35) targeting TACSTD2; indicated across 8 conditions including non-small cell lung carcinoma and breast neoplasm; with CIViC clinical evidence for 1 variant-indication association (e.g. EGFR Mutation in lung non-small cell carcinoma).

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Antibody drug conjugate
• ATC class: L01FX35
• Targets: 1 (TACSTD2)
• Indications: 8 conditions
• Clinical trials: 37
• Precision-oncology evidence (CIViC): 1 variant–indication association

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4297939
Name	Datopotamab Deruxtecan
Type	Antibody drug conjugate
Max phase	3
ATC	L01FX35

Also known as: ADC DS-1062A, Datopotamab deruxtecan, Ds-1062, DS-1062, Ds-1062a, DS-1062a, DS1062, Dato-DXd, DATOPOTAMAB DERUXTECAN

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
TACSTD2	tumor associated calcium signal transducer 2	Binding		0.7%	P09758

Bioactivity

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

Target pathways

Aggregated over 1 target gene(s): TACSTD2.

Dominant GO biological processes

GO term	Targets
visual perception	1
negative regulation of epithelial cell migration	1
regulation of epithelial cell proliferation	1
negative regulation of stress fiber assembly	1
ureteric bud morphogenesis	1
negative regulation of branching involved in ureteric bud morphogenesis	1
negative regulation of substrate adhesion-dependent cell spreading	1
negative regulation of ruffle assembly	1
negative regulation of cell motility	1
positive regulation of stem cell differentiation	1

Indications & clinical

Indications

8 indications (0 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
non-small cell lung carcinoma	3	MONDO:0005233	EFO:0003060
breast neoplasm	3	MONDO:0021100	MONDO:0007254
neoplasm	3	MONDO:0005070	EFO:0000616
lung neoplasm	2	MONDO:0021117	MONDO:0008903
angiosarcoma	2	MONDO:0016982	EFO:0003968
triple-negative breast carcinoma	2	MONDO:0005494	EFO:0005537

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

Clinical trials

Total trials: 37.

Phase distribution

Phase	Trials
PHASE3	14
PHASE2	12
PHASE1/PHASE2	5
PHASE1	3
Not specified	2
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04656652	PHASE3	ACTIVE_NOT_RECRUITING	Study of DS-1062a Versus Docetaxel in Previously Treated Advanced or Metastatic Non-small Cell Lung Cancer With or Without Actionable Genomic Alterations (TROPION-LUNG01)
NCT05104866	PHASE3	ACTIVE_NOT_RECRUITING	A Phase-3, Open-Label, Randomized Study of Dato-DXd Versus Investigator’s Choice of Chemotherapy (ICC) in Participants With Inoperable or Metastatic HR-Positive, HER2-Negative Breast Cancer Who Have Been Treated With One or Two Prior Lines of Systemic Chemotherapy (TROPION-Breast01)
NCT05215340	PHASE3	RECRUITING	Study of Dato-DXd Plus Pembrolizumab vs Pembrolizumab Alone in the First-line Treatment of Subjects With Advanced or Metastatic NSCLC Without Actionable Genomic Alterations
NCT05374512	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Dato-DXd Versus Investigator’s Choice Chemotherapy in Patients With Locally Recurrent Inoperable or Metastatic Triple-negative Breast Cancer, Who Are Not Candidates for PD-1/PD-L1 Inhibitor Therapy (TROPION-Breast02)
NCT05555732	PHASE3	ACTIVE_NOT_RECRUITING	Datopotamab Deruxtecan (Dato-DXd) and Pembrolizumab With or Without Platinum Chemotherapy in 1L Non-Small Cell Lung Cancer (TROPION-Lung07)
NCT05629585	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Dato-DXd With or Without Durvalumab Versus Investigator’s Choice of Therapy in Patients With Stage I-III Triple-negative Breast Cancer Without Pathological Complete Response Following Neoadjuvant Therapy (TROPION-Breast03)
NCT05687266	PHASE3	ACTIVE_NOT_RECRUITING	Phase III, Open-label, First-line Study of Dato-DXd in Combination With Durvalumab and Carboplatin for Advanced NSCLC Without Actionable Genomic Alterations
NCT06103864	PHASE3	RECRUITING	A Phase III Study of Dato-DXd With or Without Durvalumab Compared With Investigator’s Choice of Chemotherapy in Combination With Pembrolizumab in Patients With PD-L1 Positive Locally Recurrent Inoperable or Metastatic Triple-negative Breast Cancer
NCT06112379	PHASE3	ACTIVE_NOT_RECRUITING	A Phase III Randomised Study to Evaluate Dato-DXd and Durvalumab for Neoadjuvant/Adjuvant Treatment of Triple-Negative or Hormone Receptor-low/HER2-negative Breast Cancer
NCT06350097	PHASE3	RECRUITING	Phase III, Open-label Study of First-line Osimertinib With or Without Datopotamab Deruxtecan for EGFRm Locally Advanced or Metastatic Non-small Cell Lung Cancer
NCT06357533	PHASE3	RECRUITING	Phase III, Open-label, Study of First-line Dato-DXd in Combination With Rilvegostomig for Advanced Non-squamous NSCLC With High PD-L1 Expression (TC ≥ 50%) and Without Actionable Genomic Alterations
NCT06417814	PHASE3	RECRUITING	A Study to Investigate the Efficacy and Safety of Dato-DXd With or Without Osimertinib Compared With Platinum Based Doublet Chemotherapy in Participants With EGFR-Mutated Locally Advanced or Metastatic Non-Small Cell Lung Cancer
NCT06564844	PHASE3	ACTIVE_NOT_RECRUITING	A Phase III, Randomised Study of Adjuvant Dato-DXd in Combination With Rilvegostomig or Rilvegostomig Monotherapy Versus Standard of Care, Following Complete Tumour Resection, in Participants With Stage I Adenocarcinoma NSCLC Who Are ctDNA-positive or Have High-risk Pathological Features
NCT07129993	PHASE2/PHASE3	RECRUITING	Study of Datopotamab Deruxtecan Plus Carboplatin or Cisplatin Versus Gemcitabine Plus Carboplatin or Cisplatin in Participants With Locally Advanced or Metastatic Urothelial Carcinoma
NCT07205822	PHASE3	RECRUITING	A Study of Dato-DXd in Inoperable or Metastatic Hormone Receptor-positive, HER2 IHC 0 Breast Cancer
NCT01042379	PHASE2	RECRUITING	I-SPY TRIAL: Neoadjuvant and Personalized Adaptive Novel Agents to Treat Breast Cancer
NCT03742102	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	A Study of Novel Anti-cancer Agents in Patients With Metastatic Triple Negative Breast Cancer
NCT03944772	PHASE2	ACTIVE_NOT_RECRUITING	Phase 2 Platform Study in Patients With Advanced Non-Small Lung Cancer Who Progressed on First-Line Osimertinib Therapy (ORCHARD)
NCT04644068	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Study of AZD5305 as Monotherapy and in Combination With Anti-cancer Agents in Patients With Advanced Solid Malignancies
NCT04940325	PHASE2	ACTIVE_NOT_RECRUITING	Datopotamab Deruxtecan (Dato-DXd, DS-1062a) in Advanced and/or Unresectable Non-Small Cell Lung Cancer
NCT05061550	PHASE2	RECRUITING	Neoadjuvant and Adjuvant Treatment in Resectable Non-small Cell Lung Cancer
NCT05866432	PHASE2	RECRUITING	Phase II Study of Dato-DXd in Triple-negative Breast Cancer Patients With Newly Diagnosed or Progressing Brain Metastases
NCT06130553	PHASE1/PHASE2	RECRUITING	A Study of AZD3470, a PRMT5 Inhibitor, Given as Monotherapy and in Combination in Patients With MTAP Deficient Advanced/Metastatic Solid Tumors
NCT06176261	PHASE2	RECRUITING	DATO-BASE: DATOpotamab-deruxtecan for Breast Cancer Brain metAstaSEs
NCT06508216	PHASE1/PHASE2	RECRUITING	A Study to Explore Safety, Tolerability, Pharmacokinetics, and Anti-tumor Activity of Novel Therapeutics in Patients With Early Relapsed Metastatic Triple-negative Breast Cancer
NCT06533826	PHASE2	RECRUITING	TReatment of ADC-Refractory Breast CancEr With Dato-DXd or T-DXd: TRADE DXd
NCT06822543	PHASE2	RECRUITING	A Single Arm, Phase 2 Study of Datopotamab Deruxtecan, Carboplatin, and Pembrolizumab for Treatment-naive Brain Metastases From NSCLC (Non-small Cell Lung Cancer)
NCT07069595	PHASE2	RECRUITING	PREDICT-RD: ctDNA Surveillance in TNBC With Residual Disease
NCT07098338	PHASE2	RECRUITING	A Study of Novel Combinations in Non-Small Cell Lung Cancer (NSCLC)
NCT07535437	PHASE1/PHASE2	RECRUITING	A Study of Ivonescimab in Combination With Dato-DXd or Osimertinib in People With Non-Small Cell Lung Cancer
NCT04484142	PHASE2	COMPLETED	Study of DS-1062a in Advanced or Metastatic Non-small Cell Lung Cancer With Actionable Genomic Alterations (TROPION-Lung05)
NCT06676917	PHASE2	WITHDRAWN	Datopotamab Deruxtecan (Dato-DXd) for Non-Small Cell Lung Cancer (NSCLC) Patients With Active Brain Metastases
NCT04526691	PHASE1	ACTIVE_NOT_RECRUITING	Datopotamab Deruxtecan (Dato-DXd) in Combination With Pembrolizumab With or Without Platinum Chemotherapy in Subjects With Advanced or Metastatic Non-Small Cell Lung Cancer (TROPION-Lung02)
NCT04612751	PHASE1	ACTIVE_NOT_RECRUITING	Phase 1b Study of Dato-DXd in Combination With Immunotherapy With or Without Carboplatin in Advanced or Metastatic Non-Small Cell Lung Cancer
NCT06244485	PHASE1	RECRUITING	A Study of Valemetostat Tosylate in Combination With DXd ADCs in Subjects With Solid Tumors
NCT07582887	Not specified	RECRUITING	Impact of Genetic Variants on the Toxicity of Antibody-Drug Conjugates in Locally Advanced or Metastatic Breast Cancer: The Role of the UGT1A1 Gene as a Predictive Biomarker of Therapeutic Response
NCT06279728	Not specified	APPROVED_FOR_MARKETING	Medical Access Program for Datopotamab Deruxtecan in EGFRm NSCLC Patients

Clinical evidence (CIViC)

Variant × indication × effect (1 predictive associations from 1 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
EGFR Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Datopotamab Deruxtecan	CIViC A	EID12523

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).