ADC ID	DRG0ZOYQV
ADC Name	Datopotamab deruxtecan
Brand Name	Datroway
Synonyms	datopotamab deruxtecan; DS-1062; DS-1062a; Dato-DXd; Datroway; datopotamab deruxtecan-dlnk    Click to Show/Hide
Organization	Daiichi Sankyo (Originator);AstraZeneca (Top20 MNC)
Drug Status	Approved in 2025
Drug-to-Antibody Ratio	4
Structure
	3D MOL			2D MOL
Antibody Name	Datopotamab					Antibody Info
Antigen Name	Tumor-associated calcium signal transducer 2 (TACSTD2)					Antigen Info
Payload Name	DXd					Payload Info
Payload Target	DNA topoisomerase 1 (TOP1)					Target Info
Linker Name	Mc-Gly-Gly-Phe-Gly					Linker Info
Conjugate Type	Random Cysteines
Combination Type	deruxtecan
Absorption	Following the first dose at the approved recommended dosage, the mean Cmax and AUC of datopotamab deruxtecan-dlnk are 154 μg/mL and 671 μgday/mL, respectively. The mean Cmax and AUC of released DXd are 2.8 ng/mL and 18 ngday/mL, respectively.
Distribution	At steady-state, the mean volume of distribution of datopotamab deruxtecan-dlnk 3.5 liters.
Metabolism	Following internalization into the target cell, datopotamab deruxtecan is cleaved by lysosomal enzymes to release DXd, which itself is further metabolized by CYP3A4.1 As with endogenous IgG, the antibody component (datopotamab) is likely degraded by catabolic processes to smaller peptides and amino acids.

Standard Type	Value	Units	Description	Reference
Maximum Observed Concentration (Cmax)	166	ug/mL	Cycle 1, in Triple-Negative Breast Cancer patients	[1]
Area Under the Concentration-Time Curve (AUC)	774	day*ug/mL	Cycle 1, in Triple-Negative Breast Cancer patients	[1]
Maximum Observed Concentration (Cmax)	172	ug/mL	Cycle 1, in Advanced or Metastatic HR+/HER2- patients	[1]
Area Under the Concentration-Time Curve (AUC)	822	day*ug/mL	Cycle 1, in Advanced or Metastatic HR+/HER2- patients	[1]
Maximum Observed Concentration (Cmax)	166	ug/mL	Dato-DXd pharmacokinetic profiles for the 6mg/kg dose in patients with TNBC (N=42).	[1]
Area Under the Concentration-Time Curve (AUC)	774	day*ug/mL	Dato-DXd pharmacokinetic profiles for the 6mg/kg dose in patients with TNBC (N=42).	[1]
Maximum Observed Concentration (Cmax)	172	ug/mL	Dato-DXd pharmacokinetic profiles for the 6mg/kg dose in patients with HR+/HER2- breast cancer (N=41).	[1]
Area Under the Concentration-Time Curve (AUC)	796	day*ug/mL	Dato-DXd pharmacokinetic profiles for the 6mg/kg dose in patients with HR+/HER2- breast cancer (N=41).	[1]
Area Under the Concentration-Time Curve (AUC)	1.96	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in Capan-1 NOD-SCID plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	2.75	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in JIMT-1 Nude plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	2.48	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in MDA-MB-468 NOD-SCID plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	0.2	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in NCI-N87 Nude plasma, 1 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	2.4	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in NCI-N87 Nude plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	237.6	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, Capan-1 NOD-SCID.	[3]
Area Under the Concentration-Time Curve (AUC)	168.4	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, JIMT-1 Nude.	[3]
Area Under the Concentration-Time Curve (AUC)	156.5	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, MDA-MB-468 NOD-SCID.	[3]
Area Under the Concentration-Time Curve (AUC)	493.6	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, NCI-N87 Nude.	[3]
Maximum Observed Concentration (Cmax)	39.3	nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, Capan-1 NOD-SCID.	[3]
Maximum Observed Concentration (Cmax)	19.4	nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, JIMT-1 Nude.	[3]
Maximum Observed Concentration (Cmax)	31.8	nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, MDA-MB-468 NOD-SCID.	[3]
Maximum Observed Concentration (Cmax)	74.2	nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, NCI-N87 Nude.	[3]

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	774	day*ug/mL	Cycle 1, in Triple-Negative Breast Cancer patients	[1]
Area Under the Concentration-Time Curve (AUC)	822	day*ug/mL	Cycle 1, in Advanced or Metastatic HR+/HER2- patients	[1]
Volume of Distribution (Vd)	2.983	L	Parameter estimates of the final PopPK model for Dato-DXd, central volume	[2]
Volume of Distribution (Vd)	2.373	L	Parameter estimates of the final PopPK model for Dato-DXd, peripheral volume	[2]
Area Under the Concentration-Time Curve (AUC)	774	day*ug/mL	Dato-DXd pharmacokinetic profiles for the 6mg/kg dose in patients with TNBC (N=42).	[1]
Area Under the Concentration-Time Curve (AUC)	796	day*ug/mL	Dato-DXd pharmacokinetic profiles for the 6mg/kg dose in patients with HR+/HER2- breast cancer (N=41).	[1]
Volume of Distribution (Vd)	2.983	L	Parameter estimates of the final PopPK model for Dato-DXd, central volume.	[2]
Volume of Distribution (Vd)	2.373	L	Parameter estimates of the final PopPK model for Dato-DXd, peripheral volume.	[2]
Area Under the Concentration-Time Curve (AUC)	1.96	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in Capan-1 NOD-SCID plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	2.75	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in JIMT-1 Nude plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	2.48	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in MDA-MB-468 NOD-SCID plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	0.2	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in NCI-N87 Nude plasma, 1 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	2.4	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in NCI-N87 Nude plasma, 10 mg/kg.	[3]
Volume of Distribution (Vd)	79.5	mL/kg	Pharmacokinetic parameters of total antibody and T-DXd in Capan-1 NOD-SCID plasma, 10 mg/kg.	[3]
Volume of Distribution (Vd)	105.5	mL/kg	Pharmacokinetic parameters of total antibody and T-DXd in JIMT-1 Nude plasma, 10 mg/kg.	[3]
Volume of Distribution (Vd)	99.6	mL/kg	Pharmacokinetic parameters of total antibody and T-DXd in MDA-MB-468 NOD-SCID plasma, 10 mg/kg.	[3]
Volume of Distribution (Vd)	123.7	mL/kg	Pharmacokinetic parameters of total antibody and T-DXd in NCI-N87 Nude plasma, 1 mg/kg.	[3]
Volume of Distribution (Vd)	146.3	mL/kg	Pharmacokinetic parameters of total antibody and T-DXd in NCI-N87 Nude plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	237.6	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, Capan-1 NOD-SCID.	[3]
Area Under the Concentration-Time Curve (AUC)	168.4	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, JIMT-1 Nude.	[3]
Area Under the Concentration-Time Curve (AUC)	156.5	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, MDA-MB-468 NOD-SCID.	[3]
Area Under the Concentration-Time Curve (AUC)	493.6	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, NCI-N87 Nude.	[3]

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	774	day*ug/mL	Cycle 1, in Triple-Negative Breast Cancer patients	[1]
Area Under the Concentration-Time Curve (AUC)	822	day*ug/mL	Cycle 1, in Advanced or Metastatic HR+/HER2- patients	[1]
Area Under the Concentration-Time Curve (AUC)	774	day*ug/mL	Dato-DXd pharmacokinetic profiles for the 6mg/kg dose in patients with TNBC (N=42).	[1]
Area Under the Concentration-Time Curve (AUC)	796	day*ug/mL	Dato-DXd pharmacokinetic profiles for the 6mg/kg dose in patients with HR+/HER2- breast cancer (N=41).	[1]
Area Under the Concentration-Time Curve (AUC)	1.96	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in Capan-1 NOD-SCID plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	2.75	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in JIMT-1 Nude plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	2.48	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in MDA-MB-468 NOD-SCID plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	0.2	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in NCI-N87 Nude plasma, 1 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	2.4	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in NCI-N87 Nude plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	237.6	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, Capan-1 NOD-SCID.	[3]
Area Under the Concentration-Time Curve (AUC)	168.4	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, JIMT-1 Nude.	[3]
Area Under the Concentration-Time Curve (AUC)	156.5	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, MDA-MB-468 NOD-SCID.	[3]
Area Under the Concentration-Time Curve (AUC)	493.6	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, NCI-N87 Nude.	[3]

Standard Type	Value	Units	Description	Reference
Elimination Half-Life (t1/2)	4.8	days	The mean half-life of Dato-DXd at cycle 1 was 4.8 days for 6 mg/kg Dato-DXd, supporting once every 3 weeks dosing	[1]
Area Under the Concentration-Time Curve (AUC)	774	day*ug/mL	Cycle 1, in Triple-Negative Breast Cancer patients	[1]
Elimination Half-Life (t1/2)	5.04	day	Cycle 1, in Triple-Negative Breast Cancer patients	[1]
Area Under the Concentration-Time Curve (AUC)	822	day*ug/mL	Cycle 1, in Advanced or Metastatic HR+/HER2- patients	[1]
Elimination Half-Life (t1/2)	5.26	day	Cycle 1, in Advanced or Metastatic HR+/HER2- patients	[1]
Clearance (CL)	0.429	L/day	Parameter estimates of the final PopPK, linear clearance model for Dato-DXd, linear clearance	[2]
Clearance (CL)	0.342	L/day	Parameter estimates of the final PopPK model for Dato-DXd, intercompartmental clearance	[2]
Area Under the Concentration-Time Curve (AUC)	774	day*ug/mL	Dato-DXd pharmacokinetic profiles for the 6mg/kg dose in patients with TNBC (N=42).	[1]
Elimination Half-Life (t1/2)	5.04	day	Dato-DXd pharmacokinetic profiles for the 6mg/kg dose in patients with TNBC (N=42).	[1]
Area Under the Concentration-Time Curve (AUC)	796	day*ug/mL	Dato-DXd pharmacokinetic profiles for the 6mg/kg dose in patients with HR+/HER2- breast cancer (N=41).	[1]
Elimination Half-Life (t1/2)	4.93	day	Dato-DXd pharmacokinetic profiles for the 6mg/kg dose in patients with HR+/HER2- breast cancer (N=41).	[1]
Clearance (CL)	0.429	L/d	Parameter estimates of the final PopPK model for Dato-DXd, linear clearance.	[2]
Clearance (CL)	0.342	L/d	Parameter estimates of the final PopPK model for Dato-DXd, intercompartmental clearance.	[2]
Area Under the Concentration-Time Curve (AUC)	1.96	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in Capan-1 NOD-SCID plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	2.75	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in JIMT-1 Nude plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	2.48	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in MDA-MB-468 NOD-SCID plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	0.2	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in NCI-N87 Nude plasma, 1 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	2.4	uM*day	Pharmacokinetic parameters of total antibody and T-DXd in NCI-N87 Nude plasma, 10 mg/kg.	[3]
Elimination Half-Life (t1/2)	1.5	day	Pharmacokinetic parameters of total antibody and T-DXd in Capan-1 NOD-SCID plasma, 10 mg/kg.	[3]
Elimination Half-Life (t1/2)	3.4	day	Pharmacokinetic parameters of total antibody and T-DXd in JIMT-1 Nude plasma, 10 mg/kg.	[3]
Elimination Half-Life (t1/2)	3.2	day	Pharmacokinetic parameters of total antibody and T-DXd in MDA-MB-468 NOD-SCID plasma, 10 mg/kg.	[3]
Elimination Half-Life (t1/2)	2.9	day	Pharmacokinetic parameters of total antibody and T-DXd in NCI-N87 Nude plasma, 1 mg/kg.	[3]
Elimination Half-Life (t1/2)	4.5	day	Pharmacokinetic parameters of total antibody and T-DXd in NCI-N87 Nude plasma, 10 mg/kg.	[3]
Clearance (CL)	33.2	mL/kg/day	Pharmacokinetic parameters of total antibody and T-DXd in Capan-1 NOD-SCID plasma, 10 mg/kg.	[3]
Clearance (CL)	23.7	mL/kg/day	Pharmacokinetic parameters of total antibody and T-DXd in JIMT-1 Nude plasma, 10 mg/kg.	[3]
Clearance (CL)	26.2	mL/kg/day	Pharmacokinetic parameters of total antibody and T-DXd in MDA-MB-468 NOD-SCID plasma, 10 mg/kg.	[3]
Clearance (CL)	32.5	mL/kg/day	Pharmacokinetic parameters of total antibody and T-DXd in NCI-N87 Nude plasma, 1 mg/kg.	[3]
Clearance (CL)	26.6	mL/kg/day	Pharmacokinetic parameters of total antibody and T-DXd in NCI-N87 Nude plasma, 10 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	237.6	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, Capan-1 NOD-SCID.	[3]
Area Under the Concentration-Time Curve (AUC)	168.4	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, JIMT-1 Nude.	[3]
Area Under the Concentration-Time Curve (AUC)	156.5	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, MDA-MB-468 NOD-SCID.	[3]
Area Under the Concentration-Time Curve (AUC)	493.6	day*nmol/L	AUC and Cmax of released DXd in tumors at 10 mg/kg, NCI-N87 Nude.	[3]

Standard Type	NCT Number	Clinical Status	Clinical Trial Description
Undisclosed	NCT05104866	PHASE3	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)    Click to Show/Hide
Undisclosed	NCT05374512	PHASE3	A Phase 3, Open-label, Randomised Study of Datopotamab Deruxtecan (Dato-DXd) Versus Investigator's Choice of Chemotherapy in Patients Who Are Not Candidates for PD-1/PD-L1 Inhibitor Therapy in First-line Locally Recurrent Inoperable or Metastatic Triple-negative Breast Cancer (TROPION Breast02)    Click to Show/Hide
Undisclosed	NCT05629585	PHASE3	A Phase 3 Open-label, Randomised Study of Datopotamab Deruxtecan (DatoDXd) With or Without Durvalumab Versus Investigator's Choice of Therapy in Patients With Stage I-III Triple-negative Breast Cancer Who Have Residual Invasive Disease in the Breast and/or Axillary Lymph Nodes at Surgical Resection Following Neoadjuvant Systemic Therapy (TROPION-Breast03)    Click to Show/Hide
Undisclosed	NCT06103864	PHASE3	A Phase III, Open-label, Randomised Study of Datopotamab Deruxtecan (Dato-DXd) With or Without Durvalumab Compared With Investigator's Choice of Chemotherapy (Paclitaxel, Nab-paclitaxel or Gemcitabine + Carboplatin) in Combination With Pembrolizumab in Patients With PD-L1 Positive Locally Recurrent Inoperable or Metastatic Triple-negative Breast Cancer (TROPION-Breast05)    Click to Show/Hide
Undisclosed	NCT06112379	PHASE3	A Phase III, Open-label, Randomised Study of Neoadjuvant Datopotamab Deruxtecan (Dato-DXd) Plus Durvalumab Followed by Adjuvant Durvalumab With or Without Chemotherapy Versus Neoadjuvant Pembrolizumab Plus Chemotherapy Followed by Adjuvant Pembrolizumab With or Without Chemotherapy for the Treatment of Adult Patients With Previously Untreated Triple-Negative or Hormone Receptor-low/HER2-negative Breast Cancer (D926QC00001; TROPION-Breast04)    Click to Show/Hide
Undisclosed	NCT06176261	PHASE2	DATO-BASE: a Phase 2 Trial of DATOpotamab-deruxtecan for Breast Cancer Brain MetAstaSEs
Undisclosed	NCT05866432	PHASE2	Phase II Study of Datopotamab-Deruxtecan (Dato-DXd; DS-1026a) in Triple-negative Breast Cancer Patients With Newly Diagnosed or Progressing Brain Metastases
Undisclosed	NCT03401385	PHASE1	Phase 1, Two-part, Multicenter, Open-label, Multiple Dose, First-in-human Study of DS-1062a in Subjects With Advanced Solid Tumors (TROPION-PanTumor01)
Undisclosed	NCT05460273	PHASE1|||PHASE2	Phase 1/2, Multicentre, Open-label, Multiple-cohort Study of Dato-DXd in Chinese Patients With Advanced Non-small-cell Lung Cancer, Triple-negative Breast Cancer, Gastric/Gastroesophageal Junction Cancer, Urothelial Cancer, and Other Solid Tumours (TROPION-PanTumor02)    Click to Show/Hide
Undisclosed	NCT05489211	PHASE2	A Phase II, Multicentre, Open-label, Master Protocol to Evaluate the Efficacy and Safety of Datopotamab Deruxtecan (Dato-DXd) as Monotherapy and in Combination With Anticancer Agents in Patients With Advanced/Metastatic Solid Tumours    Click to Show/Hide
Undisclosed	NCT06417814	PHASE3	A Phase III, Open-label, Sponsor-blind, Randomized Study of Dato-DXd With or Without Osimertinib Versus Platinum-based Doublet Chemotherapy for Participants With EGFR-mutated Locally Advanced or Metastatic Non-small Cell Lung Cancer Whose Disease Has Progressed on Prior Osimertinib Treatment (TROPION-Lung15)    Click to Show/Hide
Undisclosed	NCT06564844	PHASE3	A Phase III, Randomised, Open-label, Global Study of Adjuvant Datopotamab Deruxtecan (Dato-DXd) in Combination With Rilvegostomig or Rilvegostomig Monotherapy Versus Standard of Care, Following Complete Tumour Resection, in Participants With Stage I Adenocarcinoma Non-small Cell Lung Cancer Who Are ctDNA-positive or Have High-risk Pathological Features (TROPION-Lung12)    Click to Show/Hide
Undisclosed	NCT03944772	PHASE2	A Biomarker-directed Phase 2 Platform Study in Patients With Advanced Non-Small Lung Cancer Whose Disease Has Progressed on First-Line Osimertinib Therapy.
Undisclosed	NCT04526691	PHASE1	Phase 1b, Multicenter, Open-label Study of 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)    Click to Show/Hide
Undisclosed	NCT04612751	PHASE1	A Phase 1b, Multicenter, 2-Part, Open-Label Study of Datopotamab Deruxtecan (Dato-DXd) in Combination With Immunotherapy With or Without Carboplatin in Participants With Advanced or Metastatic Non-Small Cell Lung Cancer (Tropion-Lung04)    Click to Show/Hide
Undisclosed	NCT06279728	N.A.	Medical Access Program for Datopotamab Deruxtecan (Dato-DXd, DS-1062a)
Undisclosed	NCT06676917	PHASE2	A Multicenter, Open-label, Non-comparative, Single-arm, Phase II Trial of Datopotamab Deruxtecan for Non-small Cell Lung Cancer Patients with Active Brain Metastases (The TUXEDO-5 Study)
Undisclosed	NCT04484142	PHASE2	Phase 2, Single-arm, Open-label Study of DS-1062a in Advanced or Metastatic Non-small Cell Lung Cancer With Actionable Genomic Alterations and Progressed On or After Applicable Targeted Therapy and Platinum Based Chemotherapy (TROPION-Lung05)    Click to Show/Hide
Undisclosed	NCT04656652	PHASE3	Phase 3 Randomized Study of DS-1062a Versus Docetaxel in Previously Treated Advanced or Metastatic Non-Small Cell Lung Cancer (TROPION-LUNG01)
Undisclosed	NCT04940325	PHASE2	Phase 2, Open Label Study of DS-1062a, an Anti-TROP-2-Antibody-Drug Conjugate (ADC), in Patients With Advanced and/or Unresectable Non-Small Cell Lung Cancer (NSCLC), With Biomarker Analysis to Characterize Response to Therapy    Click to Show/Hide
Undisclosed	NCT06244485	PHASE1	A Phase 1b, Multicenter, Open-Label Study of Valemetostat Tosylate in Combination With DXd ADCs in Subjects With Solid Tumors
Objective Response Rate (ORR)	NCT03401385	Phase 1/2	Phase 1, two-part, multicenter, open-label, multiple dose, first-in-human study of DS-1062a in subjects with advanced solid tumors (TROPION-PanTumor01).
Objective Response Rate (ORR)	NCT03742102	Phase 1/2	A phase 1b/2, 2-stage, open-label, multicenter study to determine the efficacy and safety of durvalumab (MEDI4736) + paclitaxel and durvalumab (MEDI4736) in combination with novel oncology therapies with or without paclitaxel for first-line metastatic triple negative breast cancer.    Click to Show/Hide
Objective Response Rate (ORR)	NCT03401385	Phase 1	Phase 1, two-part, multicenter, open-label, multiple dose, first-in-human study of DS-1062a in subjects with advanced solid tumors (TROPION-PanTumor01).
Objective Response Rate (ORR)	NCT03401385	Phase 1	Phase 1, two-part, multicenter, open-label, multiple dose, first-in-human study of DS-1062a in subjects with advanced solid tumors (TROPION-PanTumor01).
Objective Response Rate (ORR)	NCT03401385	Phase 1	Phase 1, two-part, multicenter, open-label, multiple dose, first-in-human study of DS-1062a in subjects with advanced solid tumors (TROPION-PanTumor01).
Objective Response Rate (ORR)	NCT04526691	Phase 1	Phase 1b, multicenter, open-label study of 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).    Click to Show/Hide
Undisclosed	NCT04656652	Phase 3	Phase 3 randomized study of DS-1062a versus docetaxel in previously treated advanced or metastatic non-small cell lung cancer (TROPION-LUNG01).
Undisclosed	NCT05629585	Phase 3	A phase 3 open-label, randomised study of datopotamab deruxtecan (DatoDXd) with or without durvalumab versus investigator's choice of therapy in patients with stage i-2i triple-negative breast cancer who have residual invasive disease in the breast and/or axillary lymph nodes at surgical resection following neoadjuvant systemic therapy (TROPION-Breast03).    Click to Show/Hide
Undisclosed	NCT05104866	Phase 3	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).    Click to Show/Hide
Undisclosed	NCT05374512	Phase 3	A phase 3, open-label, randomised study of datopotamab deruxtecan (Dato-DXd) versus investigator's choice of chemotherapy in patients who are not candidates for PD-1/PD-L1 inhibitor therapy in first-line locally recurrent inoperable or metastatic triple-negative breast cancer (TROPION Breast02).    Click to Show/Hide
Undisclosed	NCT05215340	Phase 3	A randomized, open-label, phase 3 trial of Dato-DXd plus pembrolizumab vs pembrolizumab alone in treatment-nave subjects with advanced or metastatic PD-L1 high (TPS 50%) non-small cell lung cancer without actionable genomic alterations (TROPION-Lung08).    Click to Show/Hide
Undisclosed	NCT05687266	Phase 3	A phase 3, randomised, open-label, multicentre, global study of datopotamab deruxtecan (Dato-DXd) in combination with durvalumab and carboplatin versus pembrolizumab in combination with platinum-based chemotherapy for the first-line treatment of patients with locally advanced or metastatic NSCLC without actionable genomic alterations (D926NC00001; AVANZAR).    Click to Show/Hide
Undisclosed	NCT05555732	Phase 3	A randomized phase 3 study of datopotamab deruxtecan (Dato-DXd) and pembrolizumab with or without platinum chemotherapy in subjects with no prior therapy for advanced or metastatic PD-L1 TPS <50% non-squamous non-small cell lung cancer without actionable genomic alterations (TROPION-Lung07).    Click to Show/Hide
Undisclosed	NCT04940325	Phase 2	Phase 2, open label study of DS-1062a, an anti-TROP-2-antibody-drug conjugate (ADC), in patients with advanced and/or unresectable non-small cell lung cancer (NSCLC), with biomarker analysis to characterize response to therapy.    Click to Show/Hide
Undisclosed	NCT01042379	Phase 2	I-SPY trial (investigation of serial studies to predict your therapeutic response with imaging and molecular analysis 2).
Undisclosed	NCT03944772	Phase 2	A biomarker-directed phase 2 platform study in patients with advanced non-small lung cancer whose disease has progressed on first-line osimertinib therapy.
Undisclosed	NCT05061550	Phase 2	A phase 2, open-label, multicentre, randomised study of neoadjuvant and adjuvant treatment in patients with resectable, early-stage (2 to 2IB) non-small cell lung cancer (NeoCOAST-2).
Undisclosed	NCT04484142	Phase 2	Phase 2, single-arm, open-label study of DS-1062A in advanced or metastatic non-small cell lung cancer with actionable genomic alterations and progressed on or after applicable targeted therapy and platinum based chemotherapy (TROPION-Lung05).    Click to Show/Hide
Undisclosed	NCT05489211	Phase 2	A phase 2, multicentre, open-label, master protocol to evaluate the efficacy and safety of datopotamab deruxtecan (Dato-DXd) as monotherapy and in combination with anticancer agents in patients with advanced/metastatic solid tumours (TROPION-PanTumor03).    Click to Show/Hide
Undisclosed	NCT05460273	Phase 1/2	Phase 1/2, multicentre, open-label, multiple-cohort study of Dato-DXd in Chinese patients with advanced non-small-cell lung cancer, triple-negative breast cancer, gastric/gastroesophageal junction cancer, urothelial cancer, and other solid tumours (TROPION-PanTumor02).    Click to Show/Hide
Undisclosed	NCT04644068	Phase 1	A modular phase 1/2a, open-label, multicentre study to assess the safety, tolerability, pharmacokinetics, pharmacodynamics and preliminary efficacy of ascending doses of AZD5305 as monotherapy and in combination with anti-cancer agents in patients with advanced solid malignancies.    Click to Show/Hide
Undisclosed	NCT04612751	Phase 1	A phase 1b, multicenter, 2-part, open-label study of datopotamab deruxtecan (Dato-DXd) in combination with immunotherapy with or without carboplatin in participants with advanced or metastatic non-small cell lung cancer (Tropion-Lung04).    Click to Show/Hide

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 96	%	NCI-N87 cells	Gastric tubular adenocarcinoma

Experiment 1 Reporting the Activity Date of This ADC					[4]
Patients Enrolled	Eligible participants are ≥18 years with inoperable/metastatic HR+/HER2-negative breast cancer, progressed on 1-2 prior chemotherapy lines, and eligible for ICC options. Key criteria: ECOG PS 0-1, ≥1 measurable lesion (RECIST 1.1), stable brain metastases (if applicable), adequate organ function (hematologic, hepatic, renal, LVEF ≥50%), and washout periods (3 weeks for prior therapies, 4 weeks for radiotherapy). FFPE tumor samples and 12-week life expectancy are required.    Click to Show/Hide
Administration Dosage	Experimental drug. Provided in 100mg vials. IV infusion.
Related Clinical Trial
NCT Number	NCT05104866	Clinical Status	PHASE3
Clinical Description	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)
Primary Endpoint	The primary endpoints include Progression-Free Survival (PFS) assessed by BICR per RECIST 1.1 from randomization until progression or death (21-month timeframe), analyzed via hazard ratio for all randomized participants regardless of treatment discontinuation or additional therapies. Overall Survival (OS) is measured from randomization to death (44-month timeframe), with hazard ratio analysis similarly inclusive of all randomized participants.    Click to Show/Hide
Other Endpoint	Secondary endpoints encompass Objective Response Rate (ORR; confirmed CR/PR per RECIST 1.1), Duration of Response (DoR; time from first response to progression/death), Investigator-assessed PFS, Disease Control Rate (DCR; CR/PR/SD at 12 weeks), Time to First/Second Subsequent Therapy (TFST/TSST), PFS2 (time to second progression/death), and PROs (TTD in pain, physical functioning, GHS/QoL via EORTC QLQ-C30). Pharmacokinetics (Dato-DXd plasma concentrations) and immunogenicity (ADA testing) are also evaluated.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[5]
Patients Enrolled	Eligible participants are ≥18 years with locally recurrent/metastatic TNBC (ER/PR/HER2-negative), no prior metastatic chemotherapy, and ineligible for PD-1/PD-L1 inhibitors. Key criteria: ECOG PS 0-1, ≥1 measurable lesion (RECIST 1.1), stable brain metastases (if applicable), adequate organ function (hematologic, hepatic, renal), and washout periods (3-6 weeks for prior therapies). Required: FFPE tumor sample (≤3 months old), 12-week life expectancy, and contraception compliance. Exclusion: active HBV, recent transfusions/G-CSF, or pregnancy. Informed consent and optional genetic research consent are mandatory.    Click to Show/Hide
Administration Dosage	Experimental drug. Provided in 100mg vials. IV infusion.
Related Clinical Trial
NCT Number	NCT05374512	Clinical Status	PHASE3
Clinical Description	A Phase 3, Open-label, Randomised Study of Datopotamab Deruxtecan (Dato-DXd) Versus Investigator's Choice of Chemotherapy in Patients Who Are Not Candidates for PD-1/PD-L1 Inhibitor Therapy in First-line Locally Recurrent Inoperable or Metastatic Triple-negative Breast Cancer (TROPION Breast02)
Primary Endpoint	The primary endpoints include Progression-Free Survival (PFS), defined as time from randomization to BICR-assessed progression per RECIST 1.1 or death (26-month timeframe), analyzed via hazard ratio (HR) for all randomized participants, with censoring for missed visits. Overall Survival (OS) measures time from randomization to death (42-month timeframe), analyzed by HR. Both endpoints include all randomized participants regardless of treatment discontinuation or additional therapies.    Click to Show/Hide
Other Endpoint	Secondary endpoints include Objective Response Rate (ORR; confirmed CR/PR per RECIST 1.1), Duration of Response (DoR; time from first response to progression/death), Investigator-assessed PFS, Disease Control Rate (DCR; CR/PR/SD at 12 weeks), and Time to Deterioration (TTD) in pain, physical functioning, breast/arm symptoms, and GHS/QoL (EORTC scales). Additional endpoints: Time to First/Second Subsequent Therapy (TFST/TSST), PFS2 (second progression/death), pharmacokinetics (Dato-DXd plasma concentrations), immunogenicity (ADA testing), and safety (AEs per CTCAE v5.0). All analyses use HR or odds ratios and include all randomized participants.    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[6]
Patients Enrolled	Eligible participants are ≥18 years with residual invasive TNBC post-neoadjuvant therapy (anthracycline/taxane ± platinum/pembrolizumab), ECOG PS 0-1, and no relapse. Key requirements: FFPE tumor sample from residual disease, LVEF ≥50%, no adjuvant therapy, and adequate organ function. Exclusion: germline BRCA mutations. Radiotherapy must be completed ≤6 weeks pre-randomization (or surgery ≤16 weeks if no radiotherapy).    Click to Show/Hide
Administration Dosage	Experimental drug. Provided in 100mg vials. IV infusion.
Related Clinical Trial
NCT Number	NCT05629585	Clinical Status	PHASE3
Clinical Description	A Phase 3 Open-label, Randomised Study of Datopotamab Deruxtecan (DatoDXd) With or Without Durvalumab Versus Investigator's Choice of Therapy in Patients With Stage I-III Triple-negative Breast Cancer Who Have Residual Invasive Disease in the Breast and/or Axillary Lymph Nodes at Surgical Resection Following Neoadjuvant Systemic Therapy (TROPION-Breast03)
Primary Endpoint	The primary endpoints include Progression-Free Survival (PFS), defined as time from randomization to BICR-assessed progression per RECIST 1.1 or death (26-month timeframe), analyzed via hazard ratio (HR) for all randomized participants, with censoring for missed visits. Overall Survival (OS) measures time from randomization to death (42-month timeframe), analyzed by HR. Both endpoints include all randomized participants regardless of treatment discontinuation or additional therapies.    Click to Show/Hide
Other Endpoint	Patient-reported outcomes assess time to deterioration (TTD) in physical function (PROMIS SF-8c), GHS/QoL (EORTC IL172), and fatigue (PROMIS SF-7a) over 24-36 months, analyzed via HR and mean score differences. Pharmacokinetics (Dato-DXd plasma concentrations) and immunogenicity (ADA titres) are evaluated at specific cycle timepoints. Safety/tolerability (AEs per CTCAE v5.0) is monitored until 90 days post-treatment. All analyses maintain intent-to-treat principles.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[7]
Patients Enrolled	Eligible participants have PD-L1+ (CPS ≥10) locally recurrent/metastatic TNBC per ASCO-CAP guidelines, ECOG PS 0-1, and measurable disease (RECIST 1.1). Key requirements: FFPE tumor sample (≤3 months old), no prior metastatic therapy (except completed curative treatment ≥6 months prior for recurrent cases), and eligibility for ICC (paclitaxel/nab-paclitaxel/gemcitabine-carboplatin). Adequate organ function and contraception use are mandatory.    Click to Show/Hide
Administration Dosage	Provided in 100mg vials. IV infusion. Experimental drug.
Related Clinical Trial
NCT Number	NCT06103864	Clinical Status	PHASE3
Clinical Description	A Phase III, Open-label, Randomised Study of Datopotamab Deruxtecan (Dato-DXd) With or Without Durvalumab Compared With Investigator's Choice of Chemotherapy (Paclitaxel, Nab-paclitaxel or Gemcitabine + Carboplatin) in Combination With Pembrolizumab in Patients With PD-L1 Positive Locally Recurrent Inoperable or Metastatic Triple-negative Breast Cancer (TROPION-Breast05)
Primary Endpoint	The primary endpoint is Progression-Free Survival (PFS), defined as time from randomization to BICR-assessed progression per RECIST 1.1 or death (33-month timeframe), analyzed via hazard ratio (HR) for all randomized participants. Censoring applies if progression/death follows ≥2 missed visits. Secondary efficacy measures include Overall Survival (OS; 64-month follow-up), Objective Response Rate (ORR), Duration of Response (DoR), and Clinical Benefit Rate at 24 weeks (CBR-24), all assessed per RECIST 1.1 by BICR/investigator.    Click to Show/Hide
Other Endpoint	Patient-reported outcomes evaluate Time to Deterioration (TTD) in breast/arm symptoms (EORTC IL116), pain (EORTC IL199), physical function (PROMIS SF8c), and GHS/QoL (EORTC IL172). Additional endpoints include Time to First/Second Subsequent Therapy (TFST/TSST), PFS2 (second progression/death), pharmacokinetics (Dato-DXd plasma concentrations), immunogenicity (ADA testing), and safety (AEs). All time-to-event endpoints use HR analysis with follow-up to 64 months.    Click to Show/Hide
Experiment 5 Reporting the Activity Date of This ADC					[8]
Patients Enrolled	Eligible participants are adults (≥18 years) with stage II-III TNBC or HR-low/HER2-negative breast cancer, ECOG PS 0-1, adequate organ function.
Administration Dosage	Participants receive durvalumab every 3 weeks (Q3W) + Dato-DXd Q3W as neoadjuvant therapy prior to surgery.
Related Clinical Trial
NCT Number	NCT06112379	Clinical Status	PHASE3
Clinical Description	A Phase III, Open-label, Randomised Study of Neoadjuvant Datopotamab Deruxtecan (Dato-DXd) Plus Durvalumab Followed by Adjuvant Durvalumab With or Without Chemotherapy Versus Neoadjuvant Pembrolizumab Plus Chemotherapy Followed by Adjuvant Pembrolizumab With or Without Chemotherapy for the Treatment of Adult Patients With Previously Untreated Triple-Negative or Hormone Receptor-low/HER2-negative Breast Cancer (D926QC00001; TROPION-Breast04)
Primary Endpoint	The primary endpoints include pathologic complete response (pCR) rate assessed at definitive surgery (ypT0/Tis ypN0) and event-free survival (EFS) measuring time from randomization to disease progression/recurrence/second primary cancer/death (68-month follow-up), both analyzed via between-arm difference (pCR) or hazard ratio (EFS) for all randomized participants regardless of treatment discontinuation.    Click to Show/Hide
Other Endpoint	Key secondary endpoints comprise overall survival (OS; 82-month follow-up), distant disease-free survival (DDFS; 68-month follow-up), patient-reported outcomes (breast/arm symptoms, physical function, fatigue, QoL via EORTC/PROMIS scales), pharmacokinetics (Dato-DXd plasma concentrations), immunogenicity (ADA), and safety (AEs per CTCAE v5.0), analyzed through hazard ratios or mean score differences.    Click to Show/Hide
Experiment 6 Reporting the Activity Date of This ADC					[9]
Patients Enrolled	Eligible patients are adults (≥18) with HER2-negative metastatic breast cancer and CNS involvement: Cohorts A/B require measurable brain metastases (≥1cm, RANO-BM) with/without prior therapy; Cohort C requires leptomeningeal disease.
Administration Dosage	A HER2-directed ADC, 100mg/vial, via intravenous (into the vein) infusion per protocol.
Related Clinical Trial
NCT Number	NCT06176261	Clinical Status	PHASE2
Clinical Description	DATO-BASE: a Phase 2 Trial of DATOpotamab-deruxtecan for Breast Cancer Brain MetAstaSEs
Primary Endpoint	The primary endpoint is objective response rate (ORR) based on RANO-BM criteria (intracranial lesions) and RECIST v1.1 (systemic lesions), measuring complete/partial response rates over 3 years.
Other Endpoint	Secondary endpoints include clinical benefit rates at 18/24 weeks (CBR18/CBR24 requiring stable/better extracranial disease with intracranial response), median progression-free/overall survival (PFS/OS per Kaplan-Meier), site of first progression (RANO-BM), and grade 3-5 treatment-related toxicity rates (CTCAE v5).
Experiment 7 Reporting the Activity Date of This ADC					[10]
Patients Enrolled	Eligible patients are adults (&ge;18) with triple-negative breast cancer (ER/PR <10%, HER2-negative), measurable brain metastases (RANO-BM) not requiring immediate local therapy, KPS &ge;70%, and adequate organ function. Prior PD-1/PD-L1 or TROP-2 inhibitors are allowed. Required washout periods: &ge;3 weeks for chemotherapy/surgery, &ge;4 weeks for chest radiation/antibody therapies.    Click to Show/Hide
Administration Dosage	Datopotamab-deruxtecan (DS-1062a) 6.0 mg/kg body weight i.v. on day 1 once every three weeks.
Related Clinical Trial
NCT Number	NCT05866432	Clinical Status	PHASE2
Clinical Description	Phase II Study of Datopotamab-Deruxtecan (Dato-DXd; DS-1026a) in Triple-negative Breast Cancer Patients With Newly Diagnosed or Progressing Brain Metastases
Primary Endpoint	The primary endpoint is intracranial response rate to datopotamab-deruxtecan assessed by RANO-BM criteria over 36 months, measuring tumor response in the central nervous system from treatment initiation until progression, death, or discontinuation.
Other Endpoint	Secondary endpoints include extracranial response rate (RECIST 1.1), progression-free survival (time to progression/death), overall survival (time to death), and safety profile (hematologic/non-hematologic adverse events and lab parameters), all evaluated over 36 months.
Experiment 8 Reporting the Activity Date of This ADC					[11]
Patients Enrolled	Eligibility requires relapsed/progressed advanced solid tumors with mandatory TROP2 biomarker testing (no minimum threshold), age &ge;18, ECOG 0-1, LVEF &ge;50%, adequate organ function, and no prior TROP2/deruxtecan ADC therapy. Disease-specific criteria apply for NSCLC, TNBC, HR+/HER2-low breast cancer (prior T-DXd required), SCLC, ovarian, prostate, and other cancers, with contraception mandates and &ge;3-month life expectancy. The sub-study assesses oral mucositis/stomatitis via daily patient-reported outcomes.    Click to Show/Hide
Administration Dosage	.
Related Clinical Trial
NCT Number	NCT03401385	Clinical Status	PHASE1
Clinical Description	Phase 1, Two-part, Multicenter, Open-label, Multiple Dose, First-in-human Study of DS-1062a in Subjects With Advanced Solid Tumors (TROPION-PanTumor01)
Primary Endpoint	The primary endpoints include dose-limiting toxicities (DLTs) assessed within the first 8 cycles (21-day cycles), adverse events (AEs) monitored up to 4 years, and Grade ≥2 oral mucositis/stomatitis evaluated at 8 weeks in the sub-study.
Other Endpoint	Key secondary endpoints focus on pharmacokinetics (PK) parameters such as Cmax, Tmax, AUClast, AUCtau, and Ctrough for DS-1062a, total anti-TROP2 antibody, and MAAA-1181a, measured during the initial 8 treatment cycles.
Experiment 9 Reporting the Activity Date of This ADC					[12]
Patients Enrolled	Eligible participants must be &ge;18 years with ECOG 0-1 and measurable disease per RECIST 1.1. Cohort-specific criteria: NSCLC (Stage IIIB-IV, with/without actionable genomic alterations requiring prior targeted therapy) and TNBC (hormone receptor-negative, HER2-negative, &ge;2 prior chemotherapy regimens including taxane).
Administration Dosage	.
Related Clinical Trial
NCT Number	NCT05460273	Clinical Status	PHASE1|||PHASE2
Clinical Description	Phase 1/2, Multicentre, Open-label, Multiple-cohort Study of Dato-DXd in Chinese Patients With Advanced Non-small-cell Lung Cancer, Triple-negative Breast Cancer, Gastric/Gastroesophageal Junction Cancer, Urothelial Cancer, and Other Solid Tumours (TROPION-PanTumor02)
Primary Endpoint	The primary endpoint is confirmed objective response rate (ORR) assessed by independent central review (ICR) per RECIST 1.1, measuring the proportion of participants achieving complete or partial response over 36 months.
Other Endpoint	Secondary endpoints include investigator-assessed ORR, duration of response (DoR), disease control rate (DCR), best overall response (BoR), time to response (TTR), progression-free survival (PFS), overall survival (OS), treatment-emergent adverse events (TEAEs), pharmacokinetics (Tmax, AUC, Cmax), and immunogenicity (ADA detection) over 36 months.
Experiment 10 Reporting the Activity Date of This ADC					[13]
Patients Enrolled	Eligible participants must be &ge;18 years with advanced/metastatic malignancy, ECOG 0-1, measurable disease (except prostate cancer bone metastases), adequate organ function, and compliance with contraceptive requirements. Tumor tissue submission and informed consent for genetic research are mandatory.
Administration Dosage	Intravenous (IV) Antibody drug conjugate
Related Clinical Trial
NCT Number	NCT05489211	Clinical Status	PHASE2
Clinical Description	A Phase II, Multicentre, Open-label, Master Protocol to Evaluate the Efficacy and Safety of Datopotamab Deruxtecan (Dato-DXd) as Monotherapy and in Combination With Anticancer Agents in Patients With Advanced/Metastatic Solid Tumours
Primary Endpoint	Primary endpoints include objective response rate (ORR) per RECIST 1.1 by investigator assessment, safety profile (adverse events/serious adverse events), and PSA50 response (≥50% PSA reduction) in prostate cancer substudies, all evaluated over approximately 1 year.
Other Endpoint	Secondary endpoints comprise progression-free survival (PFS), duration of response (DoR), disease control rate (DCR), tumor size changes, pharmacokinetics (Cmax, Tmax, AUC), immunogenicity (ADA), and biomarker analysis (TROP2/MAAA-1181a), with substudy-specific assessments like radiographic PFS and CA-125 response.
Experiment 11 Reporting the Activity Date of This ADC					[14]
Patients Enrolled	Eligible participants must have histologically confirmed non-squamous NSCLC with EGFR mutations (Ex19del/L858R/G719X/S768I/L861Q), progression on prior osimertinib (&le;2 prior EGFR TKIs), &ge;1 measurable lesion per RECIST v1.1, ECOG 0-1, and adequate organ function.
Administration Dosage	Dato-DXd will be administered as IV infusion.
Related Clinical Trial
NCT Number	NCT06417814	Clinical Status	PHASE3
Clinical Description	A Phase III, Open-label, Sponsor-blind, Randomized Study of Dato-DXd With or Without Osimertinib Versus Platinum-based Doublet Chemotherapy for Participants With EGFR-mutated Locally Advanced or Metastatic Non-small Cell Lung Cancer Whose Disease Has Progressed on Prior Osimertinib Treatment (TROPION-Lung15)
Primary Endpoint	The primary endpoint is progression-free survival (PFS) assessed by blinded independent central review (BICR) per RECIST v1.1, measuring time from randomization to disease progression or death over 2.5 years.
Other Endpoint	Secondary endpoints include overall survival (OS), CNS PFS, objective response rate (ORR), duration of response (DoR), PFS-2, patient-reported outcomes (pulmonary symptoms, physical functioning, QoL), pharmacokinetics (Dato-DXd concentration), and immunogenicity (ADA detection), all evaluated up to 3.5 years.
Experiment 12 Reporting the Activity Date of This ADC					[15]
Patients Enrolled	Eligible participants must have completely resected (R0) Stage I NSCLC (T <4cm, AJCC 8th ed), ctDNA-positive status or high-risk features (VPI, LVI, high-grade histology), ECOG 0-1, and adequate organ function, with no evidence of disease post-surgery.
Administration Dosage	Participants in the Dato-DXd in combination with rilvegostomig group will receive Dato-DXd and rilvegostomig as intravenous (IV) infusion every 3 weeks (Q3W).
Related Clinical Trial
NCT Number	NCT06564844	Clinical Status	PHASE3
Clinical Description	A Phase III, Randomised, Open-label, Global Study of Adjuvant Datopotamab Deruxtecan (Dato-DXd) in Combination With Rilvegostomig or Rilvegostomig Monotherapy Versus Standard of Care, Following Complete Tumour Resection, in Participants With Stage I Adenocarcinoma Non-small Cell Lung Cancer Who Are ctDNA-positive or Have High-risk Pathological Features (TROPION-Lung12)
Primary Endpoint	The primary endpoint is disease-free survival (DFS) assessed by BICR in Stage I adenocarcinoma NSCLC patients (ctDNA-positive or high-risk pathological features) comparing adjuvant Dato-DXd + rilvegostomig versus standard of care (SoC), with hazard ratio (HR) analysis over 10 years.
Other Endpoint	Secondary endpoints include overall survival (OS), patient-reported outcomes (physical function and GHS/QoL via PROMIS SF PF 8c and EORTC IL172), pharmacokinetics (Dato-DXd, rilvegostomig, and MAAA-1181a concentrations), and immunogenicity (ADA detection), all evaluated up to 90 days post-treatment.
Experiment 13 Reporting the Activity Date of This ADC					[16]
Patients Enrolled	Key inclusion criteria cover histologically confirmed EGFR-mutant adenocarcinoma NSCLC (locally advanced/metastatic), progression on first-line osimertinib, measurable disease per RECIST 1.1, mandatory biopsy feasibility, adequate coagulation parameters (INR/aPTT <1.5&times;ULN), and ECOG 0-1 status, while permitting prior adjuvant/neoadjuvant therapy if completed >6 months pre-recurrence.    Click to Show/Hide
Administration Dosage	The patients in this group will receive osimertinib taken in combination with datopotamab deruxtecan.Datopotamab deruxtecan given IV at 4 or 6 mg/kg on Day 1 of every 3-week cycle.
Related Clinical Trial
NCT Number	NCT03944772	Clinical Status	PHASE2
Clinical Description	A Biomarker-directed Phase 2 Platform Study in Patients With Advanced Non-Small Lung Cancer Whose Disease Has Progressed on First-Line Osimertinib Therapy.
Primary Endpoint	The primary endpoint is objective response rate (ORR) per RECIST 1.1 by investigator assessment, measuring confirmed complete/partial responses with follow-up every 6 weeks (first 24 weeks) then every 9 weeks until progression/treatment cessation (average 3-month timeframe).
Other Endpoint	Secondary endpoints include ORR assessment using the same methodology and timeframe as the primary endpoint, with identical response criteria and follow-up schedule for disease progression monitoring.
Experiment 14 Reporting the Activity Date of This ADC					[17]
Patients Enrolled	Eligible participants must have histologically confirmed advanced/metastatic NSCLC with documented negative/unknown status for actionable EGFR/ALK alterations (non-squamous) or meeting specific testing criteria (squamous), allowing KRAS mutations or non-actionable genomic variants, with prior therapy limits (&le;2 lines for dose escalation; immunotherapy-naive status for expansion cohorts), mandatory biopsy compliance, available archival tissue for biomarker analysis, adequate baseline organ function, and ineligibility for curative resection/chemoradiation.    Click to Show/Hide
Administration Dosage	Intravenous infusion every 3 weeks (Q3W) on Day 1 of each 21-day cycle (starting datopotamab deruxtecan dose of 4.0 mg/kg)
Related Clinical Trial
NCT Number	NCT04526691	Clinical Status	PHASE1
Clinical Description	Phase 1b, Multicenter, Open-label Study of 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)
Primary Endpoint	The primary endpoint evaluates dose-limiting toxicities (DLTs) during Cycle 1 (Days 1-21) and treatment-emergent adverse events (TEAEs) up to 28 days post-last dose, with monitoring extending approximately 30 months post-treatment initiation.
Other Endpoint	Secondary endpoints include objective response rate (ORR), duration of response (DoR), progression-free survival (PFS), and overall survival (OS) assessed over ~30 months, alongside pharmacokinetic parameters (Cmax, Tmax, AUC) of Dato-DXd components measured through serial plasma sampling during 21-day treatment cycles, with immunogenicity monitoring for anti-drug antibodies against Dato-DXd and pembrolizumab.    Click to Show/Hide
Experiment 15 Reporting the Activity Date of This ADC					[18]
Patients Enrolled	Eligible participants (&ge;18 years) must have advanced/metastatic NSCLC without EGFR/ALK alterations (KRAS mutations permitted), with cohort-specific prior therapy requirements (treatment-na&iuml;ve to &le;2 prior lines), measurable disease per RECIST 1.1, ECOG 0-1, adequate organ function, mandatory biopsy compliance, and PD-L1 testing for Cohorts 5-14 using validated assays.    Click to Show/Hide
Administration Dosage	Intravenous infusion every 3 weeks (Q3W) on Day 1 of each 21-day cycle (starting datopotamab deruxtecan dose of 4.0 mg/kg)
Related Clinical Trial
NCT Number	NCT04612751	Clinical Status	PHASE1
Clinical Description	A Phase 1b, Multicenter, 2-Part, Open-Label Study of Datopotamab Deruxtecan (Dato-DXd) in Combination With Immunotherapy With or Without Carboplatin in Participants With Advanced or Metastatic Non-Small Cell Lung Cancer (Tropion-Lung04)
Primary Endpoint	The primary safety endpoints include DLTs assessed during the first 21-day cycle and TEAEs monitored throughout the study period (approximately 60 months), covering comprehensive safety parameters such as SAEs, AESIs, ECOG PS, vital signs, lab tests, ECG/ECHO findings, and ophthalmologic evaluations.
Other Endpoint	Key efficacy endpoints (ORR, DoR, DCR, PFS, TTR, OS) and PK parameters (Cmax, Tmax, AUC) will be evaluated per RECIST 1.1 at final analysis (~60 months), alongside immunogenicity assessments measuring ADA prevalence/incidence for Dato-DXd, durvalumab, and other investigational agents.
Experiment 16 Reporting the Activity Date of This ADC					[19]
Patients Enrolled	Eligibility requires age &ge;18 years, confirmed NSCLC histology, proper documentation of treatment history, compliance with reproductive restrictions (sperm/ova preservation advisories), and signed informed consent, while excluding patients who don't meet these criteria from the Medical Access Program.
Administration Dosage	6 mg/kg intravenous infusion Q3W (on Day 1 of each 21-day cycle)
Related Clinical Trial
NCT Number	NCT06279728	Clinical Status	N.A.
Clinical Description	Medical Access Program for Datopotamab Deruxtecan (Dato-DXd, DS-1062a)
Experiment 17 Reporting the Activity Date of This ADC					[20]
Patients Enrolled	Eligibility requires &ge;18 years with histologically confirmed non-squamous NSCLC (symptomatic BM allowed), measurable intracranial disease (&ge;10mm), ECOG PS&le;2, and biomarker-defined subgroups (AGA/non-AGA). Prior therapy mandates include platinum/immunotherapy for non-AGA patients and targeted therapy sequences for AGA patients, with stringent organ function requirements (LVEF&ge;50%, hematologic/hepatic parameters) and reproductive safeguards (contraception for 4-7 months post-treatment). Archival/metastatic tumor tissue and washout periods for prior treatments are mandatory.    Click to Show/Hide
Administration Dosage	Dato-DXd, administered as 6 mg/kg intravenous (IV) infusion on day 1 (D1) of each 21-day cycle until unacceptable toxicity, disease progression, patient's consensus withdrawal, death, or discontinuation from the study treatment for any other reason, whichever occurs first.
Related Clinical Trial
NCT Number	NCT06676917	Clinical Status	PHASE2
Clinical Description	A Multicenter, Open-label, Non-comparative, Single-arm, Phase II Trial of Datopotamab Deruxtecan for Non-small Cell Lung Cancer Patients with Active Brain Metastases (The TUXEDO-5 Study)
Primary Endpoint	The study evaluates intracranial efficacy (ORR-IC per RANO-BM criteria) and extracranial/systemic response (ORR-EC/bicompartmental ORR per RECIST v1.1) over an average 8-month period, alongside comprehensive assessments including PFS, CBR, DCR, TTR, DoR, tumor burden changes, OS, safety (CTCAE v5.0), and patient-reported outcomes (QoL via QLQ-C30/BN20, neurofunction via NANO scale).    Click to Show/Hide
Other Endpoint	Key secondary endpoints measure treatment impact across disease compartments, with standardized response criteria (RANO-BM for brain lesions, RECIST v1.1 for systemic disease), while capturing longitudinal quality-of-life metrics and neurocognitive function in NSCLC patients with active brain metastases receiving Dato-DXd therapy.
Experiment 18 Reporting the Activity Date of This ADC					[21]
Patients Enrolled	Eligibility requires adults (&ge;18) with stage IIIB-IV NSCLC harboring actionable mutations (EGFR/ALK/ROS1/NTRK/BRAF/MET/RET), prior platinum/CPI/targeted therapy exposure, measurable disease (RECIST v1.1), ECOG PS 0-1, and mandatory tumor biopsy, excluding KRAS-mutant/EGFR-overexpressed cases without qualifying alterations.
Administration Dosage	DS-1062a will be administered as an intravenous (IV) infusion once every 3 weeks
Related Clinical Trial
NCT Number	NCT04484142	Clinical Status	PHASE2
Clinical Description	Phase 2, Single-arm, Open-label Study of DS-1062a in Advanced or Metastatic Non-small Cell Lung Cancer With Actionable Genomic Alterations and Progressed On or After Applicable Targeted Therapy and Platinum Based Chemotherapy (TROPION-Lung05)
Primary Endpoint	The primary endpoint assesses ORR (confirmed CR/PR per RECIST v1.1) via BICR evaluation from baseline until progression/death (up to ~24 months), providing objective tumor response measurement.
Other Endpoint	Secondary endpoints include efficacy outcomes (DOR, PFS, OS over 24 months), pharmacokinetics (Cmax, Tmax, AUC), and safety monitoring (TEAE incidence), offering comprehensive treatment benefit-risk profiling.
Experiment 19 Reporting the Activity Date of This ADC					[22]
Patients Enrolled	Eligibility requires adults (&ge;18) with stage IIIB-IV NSCLC (with/without actionable mutations), life expectancy &ge;3 months, prior therapy per genomic status (platinum/immunotherapy for non-AGA; targeted therapy sequences for AGA including osimertinib for EGFR+), measurable disease (RECIST v1.1), ECOG PS 0-1, adequate organ function, and reproductive safeguards (contraception for 4-7 months post-treatment), with mandatory tumor tissue submission (fresh or archival within 2 years) for biomarker analysis.    Click to Show/Hide
Administration Dosage	DS-1062a will be administered as an intravenous (IV) infusion on Day 1 of each 3-week cycle
Related Clinical Trial
NCT Number	NCT04656652	Clinical Status	PHASE3
Clinical Description	Phase 3 Randomized Study of DS-1062a Versus Docetaxel in Previously Treated Advanced or Metastatic Non-Small Cell Lung Cancer (TROPION-LUNG01)
Primary Endpoint	The primary endpoints evaluate PFS (time to progression/death) and OS (time to death) assessed by BICR per RECIST v1.1 comparing DS-1062a versus docetaxel over ~43 months, providing key efficacy measures for this phase 3 trial.
Other Endpoint	Secondary endpoints include investigator-assessed PFS, ORR (CR/PR rate), DOR (response duration), DCR (disease control), TTR (response timing), TTD (symptom worsening), safety profiles (TEAEs), pharmacokinetics (Cmax/Tmax/AUC of DS-1062a/anti-TROP2/MAAA-1181a), and immunogenicity (ADA incidence), offering comprehensive therapeutic evaluation across efficacy, safety, and drug exposure parameters.    Click to Show/Hide
Experiment 20 Reporting the Activity Date of This ADC					[23]
Patients Enrolled	Eligible participants must have advanced NSCLC refractory to 1-3 prior lines (including platinum/immunotherapy for non-mutated cases or targeted therapy+platinum for mutated cases), measurable disease (RECIST v1.1), ECOG &le;1, life expectancy &ge;3 months, stable treated brain metastases, and adequate organ function, with reproductive safeguards (contraception for 7 months post-treatment).    Click to Show/Hide
Administration Dosage	All patients included in the study will receive DS-1062a at a dose of 6 mg/kg every 3 weeks until progression or until unacceptable toxicity
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NCT Number	NCT04940325	Clinical Status	PHASE2
Clinical Description	Phase 2, Open Label Study of DS-1062a, an Anti-TROP-2-Antibody-Drug Conjugate (ADC), in Patients With Advanced and/or Unresectable Non-Small Cell Lung Cancer (NSCLC), With Biomarker Analysis to Characterize Response to Therapy
Primary Endpoint	The primary endpoint measures ORR (confirmed CR/PR) by investigator assessment during treatment (average 4 months), evaluating initial treatment efficacy in advanced NSCLC patients.
Other Endpoint	Secondary endpoints include DoR/PFS/CBR (assessed over ~39 months), safety monitoring (AEs/TEAEs/SAEs/AESIs), treatment modifications, lab/ECG abnormalities, LVEF changes, and ECOG PS deterioration, providing comprehensive efficacy and safety profiling throughout treatment and follow-up periods.
Experiment 21 Reporting the Activity Date of This ADC					[24]
Patients Enrolled	Eligibility requires adults (&ge;18) with measurable disease (RECIST v1.1), ECOG PS 0-1, and tumor sample availability, with protocol-specific criteria: Sub-Protocol A for HER2-low metastatic breast cancer (1-2 prior chemotherapy lines), Sub-Protocol B for trastuzumab-refractory gastric/GEJ adenocarcinoma, and Sub-Protocol C for NSCLC (platinum/immunotherapy for non-AGA; targeted therapy sequences for AGA). Key exclusions include prior EZH2 inhibitor use, uncontrolled CNS metastases, active infections, CYP3A inducer use, and prior topoisomerase I/TROP2-targeted therapy exposure.    Click to Show/Hide
Administration Dosage	One IV infusion Q3W on Day 1 of each 21-day cycle.
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NCT Number	NCT06244485	Clinical Status	PHASE1
Clinical Description	A Phase 1b, Multicenter, Open-Label Study of Valemetostat Tosylate in Combination With DXd ADCs in Subjects With Solid Tumors
Primary Endpoint	The study evaluates dose-limiting toxicities and treatment-emergent adverse events in Part 1 (dose escalation), while Part 2 (dose expansion) assesses investigator-evaluated ORR (confirmed CR/PR per RECIST v1.1) with tumor assessments every 6-12 weeks for up to 5 years.
Other Endpoint	Key secondary endpoints include OS (time to death), PFS (time to progression/death), DoR (response duration), safety monitoring, and pharmacokinetics (plasma concentrations of valemetostat and DXd ADCs) across multiple cycles (21-day duration), providing comprehensive efficacy and safety data for up to 5 years.
Experiment 22 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Objective Response Rate (ORR)	24.00 26.00 24.00 39.00 %
Patients Enrolled	Patients were unselected for TROP2 expression and had measurable disease per RECIST version 1.1; patients with stable/treated brain metastases were permitted.
Administration Dosage	Dato-DXd 4 mg/kg (n=50), 6 mg/kg (n=50), or 8 mg/kg (n=80) intravenously every 3 weeks.
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NCT Number	NCT03401385	Clinical Status	Phase 1/2
Clinical Description	Phase 1, two-part, multicenter, open-label, multiple dose, first-in-human study of DS-1062a in subjects with advanced solid tumors (TROPION-PanTumor01).
Experiment 23 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Objective Response Rate (ORR)	34.00 52.00 %
Patients Enrolled	Unresectable a/mTNBC pts eligible for 1L treatment, regardless of PD-L1/TROP2 status.
Administration Dosage	Intravenous Dato-DXd 6 mg/kg + durvalumab 1120 mg every 3 weeks.
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NCT Number	NCT03742102	Clinical Status	Phase 1/2
Clinical Description	A phase 1b/2, 2-stage, open-label, multicenter study to determine the efficacy and safety of durvalumab (MEDI4736) + paclitaxel and durvalumab (MEDI4736) in combination with novel oncology therapies with or without paclitaxel for first-line metastatic triple negative breast cancer.
Experiment 24 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Objective Response Rate (ORR)	22%	High TROP2 expression (TROP2 +++)
Patients Enrolled	Two hundred ten adults with locally advanced/metastatic non-small cell lung cancer (NSCLC).
Administration Dosage	0.27-10 mg/kg Dato-DXd once every 3 weeks during escalation or 4 mg/kg Dato-DXd once every 3 weeks during expansion.
Related Clinical Trial
NCT Number	NCT03401385	Clinical Status	Phase 1
Clinical Description	Phase 1, two-part, multicenter, open-label, multiple dose, first-in-human study of DS-1062a in subjects with advanced solid tumors (TROPION-PanTumor01).
Experiment 25 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Objective Response Rate (ORR)	23.80%	High TROP2 expression (TROP2 +++)
Patients Enrolled	Two hundred ten adults with locally advanced/metastatic non-small cell lung cancer (NSCLC).
Administration Dosage	0.27-10 mg/kg Dato-DXd once every 3 weeks during escalation or 8 mg/kg Dato-DXd once every 3 weeks during expansion.
Related Clinical Trial
NCT Number	NCT03401385	Clinical Status	Phase 1
Clinical Description	Phase 1, two-part, multicenter, open-label, multiple dose, first-in-human study of DS-1062a in subjects with advanced solid tumors (TROPION-PanTumor01).
Experiment 26 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Objective Response Rate (ORR)	26%	High TROP2 expression (TROP2 +++)
Patients Enrolled	Two hundred ten adults with locally advanced/metastatic non-small cell lung cancer (NSCLC).
Administration Dosage	0.27-10 mg/kg Dato-DXd once every 3 weeks during escalation or 6 mg/kg Dato-DXd once every 3 weeks during expansion.
Related Clinical Trial
NCT Number	NCT03401385	Clinical Status	Phase 1
Clinical Description	Phase 1, two-part, multicenter, open-label, multiple dose, first-in-human study of DS-1062a in subjects with advanced solid tumors (TROPION-PanTumor01).
Primary Endpoint	Patients receiving 6 mg/kg (n = 50), median duration on study, including follow-up, and median exposure were 13.30 and 3.50 months, respectively. The most frequent any-grade treatment-emergent adverse events (TEAEs) were nausea (64.00%), stomatitis (60.00%), and alopecia (42.00%).
Experiment 27 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Objective Response Rate (ORR)	50.00 57.00 %
Patients Enrolled	Pts in escalation may have received 2 prior lines of therapy for a non-small cell lung cancer (NSCLC). Pts in expansion were primarily treatment (tx) naive (pts receiving Dato-DXd + pembro may have 1 prior Pt-based tx).
Administration Dosage	Dato-DXd (4 or 6 mg/kg) + pembro 200 mg Pt-CT (cisplatin 75 mg/m2 or carboplatin AUC 5) every 21 days across 6 cohorts.
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NCT Number	NCT04526691	Clinical Status	Phase 1
Clinical Description	Phase 1b, multicenter, open-label study of 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).
Experiment 28 Reporting the Activity Date of This ADC					[29]
Related Clinical Trial
NCT Number	NCT04656652	Clinical Status	Phase 3
Clinical Description	Phase 3 randomized study of DS-1062a versus docetaxel in previously treated advanced or metastatic non-small cell lung cancer (TROPION-LUNG01).
Experiment 29 Reporting the Activity Date of This ADC					[30]
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NCT Number	NCT05629585	Clinical Status	Phase 3
Clinical Description	A phase 3 open-label, randomised study of datopotamab deruxtecan (DatoDXd) with or without durvalumab versus investigator's choice of therapy in patients with stage i-2i triple-negative breast cancer who have residual invasive disease in the breast and/or axillary lymph nodes at surgical resection following neoadjuvant systemic therapy (TROPION-Breast03).
Experiment 30 Reporting the Activity Date of This ADC					[31]
Patients Enrolled	Patients with inoperable or metastatic HR+/HER2 breast cancer.
Administration Dosage	Dato-DXd 6 mg/kg IV Q3W or ICC (eribulin, capecitabine, vinorelbine, or gemcitabine).
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NCT Number	NCT05104866	Clinical Status	Phase 3
Clinical Description	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).
Experiment 31 Reporting the Activity Date of This ADC					[32]
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NCT Number	NCT05374512	Clinical Status	Phase 3
Clinical Description	A phase 3, open-label, randomised study of datopotamab deruxtecan (Dato-DXd) versus investigator's choice of chemotherapy in patients who are not candidates for PD-1/PD-L1 inhibitor therapy in first-line locally recurrent inoperable or metastatic triple-negative breast cancer (TROPION Breast02).
Experiment 32 Reporting the Activity Date of This ADC					[33]
Patients Enrolled	Advanced non-small cell lung cancer (NSCLC).
Administration Dosage	Dato-DXd 6 mg/kg plus pembrolizumab 200 mg every 3 weeks (arm 1) and pembrolizumab 200 mg every 3 weeks (arm 2).
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NCT Number	NCT05215340	Clinical Status	Phase 3
Clinical Description	A randomized, open-label, phase 3 trial of Dato-DXd plus pembrolizumab vs pembrolizumab alone in treatment-nave subjects with advanced or metastatic PD-L1 high (TPS 50%) non-small cell lung cancer without actionable genomic alterations (TROPION-Lung08).
Experiment 33 Reporting the Activity Date of This ADC					[34]
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NCT Number	NCT05687266	Clinical Status	Phase 3
Clinical Description	A phase 3, randomised, open-label, multicentre, global study of datopotamab deruxtecan (Dato-DXd) in combination with durvalumab and carboplatin versus pembrolizumab in combination with platinum-based chemotherapy for the first-line treatment of patients with locally advanced or metastatic NSCLC without actionable genomic alterations (D926NC00001; AVANZAR).
Experiment 34 Reporting the Activity Date of This ADC					[35]
Patients Enrolled	Patients with previously untreated, advanced or metastatic non-squamous NSCLC with less than 50% programmed death-ligand (PD-L1) expression (tumor proportion score [TPS] < 50%) and without actionable genomic alterations.
Administration Dosage	Arm A (datopotamab deruxtecan [6 mg/kg] plus pembrolizumab 200 mg IV plus platinum chemotherapy every three weeks), Arm B (datopotamab deruxtecan [6 mg/kg] plus pembrolizumab 200 mg IV every three weeks), and Arm C (pembrolizumab 200 mg IV plus pemetrexed [500 mg/m2] plus platinum chemotherapy every three weeks).
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NCT Number	NCT05555732	Clinical Status	Phase 3
Clinical Description	A randomized phase 3 study of datopotamab deruxtecan (Dato-DXd) and pembrolizumab with or without platinum chemotherapy in subjects with no prior therapy for advanced or metastatic PD-L1 TPS <50% non-squamous non-small cell lung cancer without actionable genomic alterations (TROPION-Lung07).
Experiment 35 Reporting the Activity Date of This ADC					[36]
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NCT Number	NCT04940325	Clinical Status	Phase 2
Clinical Description	Phase 2, open label study of DS-1062a, an anti-TROP-2-antibody-drug conjugate (ADC), in patients with advanced and/or unresectable non-small cell lung cancer (NSCLC), with biomarker analysis to characterize response to therapy.
Experiment 36 Reporting the Activity Date of This ADC					[37]
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NCT Number	NCT01042379	Clinical Status	Phase 2
Clinical Description	I-SPY trial (investigation of serial studies to predict your therapeutic response with imaging and molecular analysis 2).
Experiment 37 Reporting the Activity Date of This ADC					[38]
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NCT Number	NCT03944772	Clinical Status	Phase 2
Clinical Description	A biomarker-directed phase 2 platform study in patients with advanced non-small lung cancer whose disease has progressed on first-line osimertinib therapy.
Experiment 38 Reporting the Activity Date of This ADC					[39]
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NCT Number	NCT05061550	Clinical Status	Phase 2
Clinical Description	A phase 2, open-label, multicentre, randomised study of neoadjuvant and adjuvant treatment in patients with resectable, early-stage (2 to 2IB) non-small cell lung cancer (NeoCOAST-2).
Experiment 39 Reporting the Activity Date of This ADC					[40]
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NCT Number	NCT04484142	Clinical Status	Phase 2
Clinical Description	Phase 2, single-arm, open-label study of DS-1062A in advanced or metastatic non-small cell lung cancer with actionable genomic alterations and progressed on or after applicable targeted therapy and platinum based chemotherapy (TROPION-Lung05).
Experiment 40 Reporting the Activity Date of This ADC					[41]
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NCT Number	NCT05489211	Clinical Status	Phase 2
Clinical Description	A phase 2, multicentre, open-label, master protocol to evaluate the efficacy and safety of datopotamab deruxtecan (Dato-DXd) as monotherapy and in combination with anticancer agents in patients with advanced/metastatic solid tumours (TROPION-PanTumor03).
Experiment 41 Reporting the Activity Date of This ADC					[42]
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NCT Number	NCT05460273	Clinical Status	Phase 1/2
Clinical Description	Phase 1/2, multicentre, open-label, multiple-cohort study of Dato-DXd in Chinese patients with advanced non-small-cell lung cancer, triple-negative breast cancer, gastric/gastroesophageal junction cancer, urothelial cancer, and other solid tumours (TROPION-PanTumor02).
Experiment 42 Reporting the Activity Date of This ADC					[43]
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NCT Number	NCT04644068	Clinical Status	Phase 1
Clinical Description	A modular phase 1/2a, open-label, multicentre study to assess the safety, tolerability, pharmacokinetics, pharmacodynamics and preliminary efficacy of ascending doses of AZD5305 as monotherapy and in combination with anti-cancer agents in patients with advanced solid malignancies.
Experiment 43 Reporting the Activity Date of This ADC					[44]
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NCT Number	NCT04612751	Clinical Status	Phase 1
Clinical Description	A phase 1b, multicenter, 2-part, open-label study of datopotamab deruxtecan (Dato-DXd) in combination with immunotherapy with or without carboplatin in participants with advanced or metastatic non-small cell lung cancer (Tropion-Lung04).

Experiment 1 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96%	High TROP2 expression (TROP2+++)
Method Description	Dato-DXd was intravenously administered at 10 mg/kg to NCI-N87 xenograft model mice. When the tumor volume reached approximately 150-300 mm3,the tumor-bearing mice were assigned to the vehicle control group,the treatment groups and the satellite sampling groups,and Dato-DXd or other test substances were administered intravenously once on day 0.    Click to Show/Hide
In Vivo Model	NCI-N87 cell line xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Ref 1	Datopotamab Deruxtecan in Advanced or Metastatic HR+/HER2- and Triple-Negative Breast Cancer: Results From the Phase I TROPION-PanTumor01 Study
Ref 2	Application of the model-informed drug development paradigm to datopotamab deruxtecan dose selection for late-stage development
Ref 3	Quantitative evaluation of trastuzumab deruxtecan pharmacokinetics and pharmacodynamics in mouse models of varying degrees of HER2 expression
Ref 4	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)
Ref 5	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)
Ref 6	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)
Ref 7	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
Ref 8	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
Ref 9	DATO-BASE: DATOpotamab-deruxtecan for Breast Cancer Brain MetAstaSEs
Ref 10	Phase II Study of Dato-DXd in Triple-negative Breast Cancer Patients With Newly Diagnosed or Progressing Brain Metastases
Ref 11	First-in-human Study of DS-1062a for Advanced Solid Tumors (TROPION-PanTumor01)
Ref 12	A Study of Dato-DXd in Chinese Patients With Advanced Non-Small Cell Lung Cancer, Triple-negative Breast Cancer and Other Solid Tumors (TROPION-PanTumor02)
Ref 13	Study of Dato-Dxd as Monotherapy and in Combination With Anti-cancer Agents in Patients With Advanced Solid Tumours (TROPION-PanTumor03)
Ref 14	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
Ref 15	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
Ref 16	Phase 2 Platform Study in Patients With Advanced Non-Small Lung Cancer Who Progressed on First-Line Osimertinib Therapy (ORCHARD)
Ref 17	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)
Ref 18	Phase 1b Study of Dato-DXd in Combination With Immunotherapy With or Without Carboplatin in Advanced or Metastatic Non-Small Cell Lung Cancer
Ref 19	Medical Access Program for Datopotamab Deruxtecan in EGFRm NSCLC Patients
Ref 20	Datopotamab Deruxtecan (Dato-DXd) for Non-Small Cell Lung Cancer (NSCLC) Patients with Active Brain Metastases
Ref 21	Study of DS-1062a in Advanced or Metastatic Non-small Cell Lung Cancer With Actionable Genomic Alterations (TROPION-Lung05)
Ref 22	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)
Ref 23	Datopotamab Deruxtecan (Dato-DXd, DS-1062a) in Advanced and/or Unresectable Non-Small Cell Lung Cancer
Ref 24	A Study of Valemetostat Tosylate in Combination With DXd ADCs in Subjects With Solid Tumors
Ref 25	Datopotamab deruxtecan in advanced/metastatic HER2- breast cancer: Results from the phase 1 TROPION-PanTumor01 study. Cancer Res (2022) 82 (4_Supplement): GS1-05.
Ref 26	Datopotamab deruxtecan (Dato-DXd) + durvalumab (D) as first-line (1L) treatment for unresectable locally advanced/metastatic triple-negative breast cancer (a/mTNBC): Initial results from BEGONIA, a phase Ib/II study. J Thorac Oncol. 2022 May; 33(3):Supplement S199.
Ref 27	First-in-Human, Phase I Dose-Escalation and Dose-Expansion Study of Trophoblast Cell-Surface Antigen 2-Directed Antibody-Drug Conjugate Datopotamab Deruxtecan in Non-Small-Cell Lung Cancer: TROPION-PanTumor01. J Clin Oncol. 2023 Jun 16:JCO2300059. doi: 10.1200/JCO.23.00059. Online ahead of print.
Ref 28	TROPION-Lung08: Phase III study of datopotamab deruxtecan plus pembrolizumab as first-line therapy for advanced NSCLC. Future Oncol. 2023 May 30. doi: 10.2217/fon-2023-0230.
Ref 29	Phase 3 Randomized Study of DS-1062a Versus Docetaxel in Previously Treated Advanced or Metastatic Non-Small Cell Lung Cancer (TROPION-LUNG01), NCT04656652
Ref 30	A Phase 3 Open-label, Randomised Study of Datopotamab Deruxtecan (DatoDXd) With or Without Durvalumab Versus Investigator's Choice of Therapy in Patients With Stage I-III Triple-negative Breast Cancer Who Have Residual Invasive Disease in the Breast and/or Axillary Lymph Nodes at Surgical Resection Following Neoadjuvant Systemic Therapy (TROPION-Breast03), NCT05629585
Ref 31	MA03.02 TROPION-PanTumor01: Updated Results From the NSCLC Cohort of the Phase 1 Study of Datopotamab Deruxtecan in Solid Tumors. J Thorac Oncol. 2021 Sept; 16(10):Supplement S892-S893.
Ref 32	A Phase 3, Open-label, Randomised Study of Datopotamab Deruxtecan (Dato-DXd) Versus Investigator's Choice of Chemotherapy in Patients Who Are Not Candidates for PD-1/PD-L1 Inhibitor Therapy in First-line Locally Recurrent Inoperable or Metastatic Triple-negative Breast Cancer (TROPION Breast02), NCT05374512
Ref 33	Datopotamab deruxtecan (Dato-DXd), a TROP2 antibody-drug conjugate, vs investigators choice of chemotherapy in previously-treated, inoperable or metastatic HR+/HER2 breast cancer: TROPION-Breast01. Cancer Res (2023) 83 (5_Supplement): OT1-03-04.
Ref 34	A Phase III, Randomised, Open-label, Multicentre, Global Study of Datopotamab Deruxtecan (Dato-DXd) in Combination With Durvalumab and Carboplatin Versus Pembrolizumab in Combination With Platinum-based Chemotherapy for the First-line Treatment of Patients With Locally Advanced or Metastatic NSCLC Without Actionable Genomic Alterations (D926NC00001; AVANZAR), NCT05687266
Ref 35	A Randomized Phase 3 Study of Datopotamab Deruxtecan (Dato-DXd) and Pembrolizumab With or Without Platinum Chemotherapy in Subjects With No Prior Therapy for Advanced or Metastatic PD-L1 TPS <50% Non-squamous Non-small Cell Lung Cancer Without Actionable Genomic Alterations (TROPION-Lung07), NCT05555732
Ref 36	Phase 2, Open Label Study of DS-1062a, an Anti-TROP-2-Antibody-Drug Conjugate (ADC), in Patients With Advanced and/or Unresectable Non-Small Cell Lung Cancer (NSCLC), With Biomarker Analysis to Characterize Response to Therapy, NCT04940325
Ref 37	I-SPY Trial (Investigation of Serial Studies to Predict Your Therapeutic Response With Imaging And moLecular Analysis 2), NCT01042379
Ref 38	A Biomarker-directed Phase 2 Platform Study in Patients With Advanced Non-Small Lung Cancer Whose Disease Has Progressed on First-Line Osimertinib Therapy. NCT03944772
Ref 39	A Phase II, Open-label, Multicentre, Randomised Study of Neoadjuvant and Adjuvant Treatment in Patients With Resectable, Early-stage (II to IIIB) Non-small Cell Lung Cancer (NeoCOAST-2), NCT05061550
Ref 40	Phase 2, Single-arm, Open-label Study of DS-1062a in Advanced or Metastatic Non-small Cell Lung Cancer With Actionable Genomic Alterations and Progressed On or After Applicable Targeted Therapy and Platinum Based Chemotherapy (TROPION-Lung05), NCT04484142
Ref 41	A Phase II, Multicentre, Open-label, Master Protocol to Evaluate the Efficacy and Safety of Datopotamab Deruxtecan (Dato-DXd) as Monotherapy and in Combination With Anticancer Agents in Patients With Advanced/Metastatic Solid Tumours (TROPION-PanTumor03), NCT05489211
Ref 42	Phase 1/2, Multicentre, Open-label, Multiple-cohort Study of Dato-DXd in Chinese Patients With Advanced Non-small-cell Lung Cancer, Triple-negative Breast Cancer, Gastric/Gastroesophageal Junction Cancer, Urothelial Cancer, and Other Solid Tumours (TROPION-PanTumor02), NCT05460273
Ref 43	A Modular Phase I/IIa, Open-label, Multicentre Study to Assess the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics and Preliminary Efficacy of Ascending Doses of AZD5305 as Monotherapy and in Combination With Anti-cancer Agents in Patients With Advanced Solid Malignancies, NCT04644068
Ref 44	A Phase 1b, Multicenter, 2-Part, Open-Label Study of Datopotamab Deruxtecan (Dato-DXd) in Combination With Immunotherapy With or Without Carboplatin in Participants With Advanced or Metastatic Non-Small Cell Lung Cancer (Tropion-Lung04), NCT04612751
Ref 45	Datopotamab Deruxtecan, a Novel TROP2-directed Antibody-drug Conjugate, Demonstrates Potent Antitumor Activity by Efficient Drug Delivery to Tumor Cells. Mol Cancer Ther. 2021 Dec;20(12):2329-2340.