ADC ID	DRG0DAKKB
ADC Name	Patritumab deruxtecan
Synonyms	patritumab deruxtecan; U3-1402; HER3-DXd; MK-1022    Click to Show/Hide
Organization	Daiichi Sankyo (Originator);Merck & Co. (Top20 MNC)
Drug Status	New Drug Application
Drug-to-Antibody Ratio	8
Structure
				2D MOL
Antibody Name	Patritumab					Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-3 (ERBB3); Tumor-associated calcium signal transducer 2 (TACSTD2)					Antigen Info
Payload Name	DXd					Payload Info
Therapeutic Target	DNA topoisomerase 1 (TOP1)					Target Info
Linker Name	Mc-Gly-Gly-Phe-Gly					Linker Info
Conjugate Type	Random Cysteines
Combination Type	deruxtecan
Special Approval(s)	Breakthrough therapy (FDA)

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	881	day*ug/mL	Simulated Exposure Metrics of DXd-Conjugated Antibody for Patritumab Deruxtecan at 5.6 mg/kg Q3W,steady state	[1]
Maximum Observed Concentration (Cmax)	132	ug/mL	Simulated Exposure Metrics of DXd-Conjugated Antibody for Patritumab Deruxtecan at 5.6 mg/kg Q3W,steady state	[1]
Maximum Observed Concentration (Cmax)	40.7	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 1.6 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	113	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 1.6 mg/kg, Cycle 1.	[2]
Maximum Observed Concentration (Cmax)	33.4	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 1.6 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	106	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 1.6 mg/kg, Cycle 3.	[2]
Maximum Observed Concentration (Cmax)	60.9	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	207	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2 mg/kg, Cycle 1.	[2]
Maximum Observed Concentration (Cmax)	80	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	315	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2 mg/kg, Cycle 3.	[2]
Maximum Observed Concentration (Cmax)	98.5	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.8 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	408	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.8 mg/kg, Cycle 1.	[2]
Maximum Observed Concentration (Cmax)	120	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.8 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	645	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.8 mg/kg, Cycle 3.	[2]
Maximum Observed Concentration (Cmax)	146	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	630	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 6.4 mg/kg, Cycle 1.	[2]
Maximum Observed Concentration (Cmax)	158	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	978	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 6.4 mg/kg, Cycle 3.	[2]
Maximum Observed Concentration (Cmax)	171	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 8.0 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	795	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 8.0 mg/kg, Cycle 1.	[2]
Maximum Observed Concentration (Cmax)	169	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 8.0 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1190	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 8.0 mg/kg, Cycle 3.	[2]
Maximum Observed Concentration (Cmax)	73.2	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2/4.8/6/4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	270	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2/4.8/6/4 mg/kg, Cycle 1.	[2]
Maximum Observed Concentration (Cmax)	155	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2/4.8/6/4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	883	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2/4.8/6/4 mg/kg, Cycle 3.	[2]
Maximum Observed Concentration (Cmax)	84.2	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.2/6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	333	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.2/6.4 mg/kg, Cycle 1.	[2]
Maximum Observed Concentration (Cmax)	168	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.2/6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1080	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.2/6.4 mg/kg, Cycle 3.	[2]
Maximum Observed Concentration (Cmax)	117	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	499	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 1, AUCtau.	[2]
Maximum Observed Concentration (Cmax)	132	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	880	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 3, AUCtau.	[2]
Maximum Observed Concentration (Cmax)	138	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	562	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1, AUCtau.	[2]
Maximum Observed Concentration (Cmax)	165	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1080	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3, AUCtau.	[2]
Maximum Observed Concentration (Cmax)	134	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	533	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1, AUCtau.	[2]
Maximum Observed Concentration (Cmax)	158	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	988	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3, AUCtau.	[2]
Maximum Observed Concentration (Cmax)	151	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	569	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 1, AUCtau.	[2]
Maximum Observed Concentration (Cmax)	185	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1110	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 3, AUCtau.	[2]
Maximum Observed Concentration (Cmax)	72.6	ug/mL	Dose escalation PK properties of ADC, 3.2 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	227	day*ug/mL	Dose escalation PK properties of ADC, 3.2 mg/kg, AUClast.	[3]
Time to Maximum Concentration (Tmax)	2.67	h	Dose escalation PK properties of ADC, 3.2 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	232	day*ug/mL	Dose escalation PK properties of ADC, 3.2 mg/kg, AUCinf.	[3]
Maximum Observed Concentration (Cmax)	105	ug/mL	Dose escalation PK properties of ADC, 4.8 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	424	day*ug/mL	Dose escalation PK properties of ADC, 4.8 mg/kg, AUClast.	[3]
Time to Maximum Concentration (Tmax)	2.49	h	Dose escalation PK properties of ADC, 4.8 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	450	day*ug/mL	Dose escalation PK properties of ADC, 4.8 mg/kg, AUCinf.	[3]
Maximum Observed Concentration (Cmax)	130	ug/mL	Dose escalation PK properties of ADC, 5.6 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	597	day*ug/mL	Dose escalation PK properties of ADC, 5.6 mg/kg, AUClast.	[3]
Time to Maximum Concentration (Tmax)	1.57	h	Dose escalation PK properties of ADC, 5.6 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	666	day*ug/mL	Dose escalation PK properties of ADC, 5.6 mg/kg, AUCinf.	[3]
Maximum Observed Concentration (Cmax)	141	ug/mL	Dose escalation PK properties of ADC, 6.4 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	572	day*ug/mL	Dose escalation PK properties of ADC, 6.4 mg/kg, AUClast.	[3]
Time to Maximum Concentration (Tmax)	1.57	h	Dose escalation PK properties of ADC, 6.4 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	649	day*ug/mL	Dose escalation PK properties of ADC, 6.4 mg/kg, AUCinf.	[3]
Maximum Observed Concentration (Cmax)	121	ug/mL	Dose expansion PK properties of ADC, 5.6 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	515	day*ug/mL	Dose expansion PK properties of ADC, 5.6 mg/kg, AUClast.	[3]
Time to Maximum Concentration (Tmax)	2.71	h	Dose expansion PK properties of ADC, 5.6 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	556	day*ug/mL	Dose expansion PK properties of ADC, 5.6 mg/kg, AUCinf.	[3]
Maximum Observed Concentration (Cmax)	122.62	ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, Lyo-DP geometric means.    Click to Show/Hide	[3]
Area Under the Concentration-Time Curve (AUC)	534.54	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, Lyo-DP geometric means, AUClast.    Click to Show/Hide	[3]
Area Under the Concentration-Time Curve (AUC)	535.06	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, Lyo-DP geometric means, AUC0-21.    Click to Show/Hide	[3]
Maximum Observed Concentration (Cmax)	127.22	ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, FL-DP geometric means.    Click to Show/Hide	[3]
Area Under the Concentration-Time Curve (AUC)	571.61	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, FL-DP geometric means, AUClast.    Click to Show/Hide	[3]
Area Under the Concentration-Time Curve (AUC)	572.98	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, FL-DP geometric means, AUC0-21d.    Click to Show/Hide	[3]

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	881	day*ug/mL	Simulated Exposure Metrics of DXd-Conjugated Antibody for Patritumab Deruxtecan at 5.6 mg/kg Q3W,steady state	[1]
Volume of Distribution (Vd)	2.943	L	Parameter Estimates of the Final Population PK Model for DXd-Conjugated Antibody.	[1]
Trough Concentration (Cthrough)	0.21	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 1.6 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	113	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 1.6 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	0.21	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 1.6 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	106	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 1.6 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	0.93	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	207	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	2.3	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	315	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	3.57	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.8 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	408	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.8 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	8.12	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.8 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	645	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.8 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	8.14	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	630	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 6.4 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	18.3	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	978	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 6.4 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	11	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 8.0 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	795	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 8.0 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	21	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 8.0 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1190	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 8.0 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	0.81	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2/4.8/6/4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	270	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2/4.8/6/4 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	9.92	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2/4.8/6/4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	883	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2/4.8/6/4 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	6.34	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.2/6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	333	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.2/6.4 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	18.6	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.2/6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1080	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.2/6.4 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	5.24	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	499	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 1, AUCtau.	[2]
Trough Concentration (Cthrough)	13.1	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	880	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 3, AUCtau.	[2]
Trough Concentration (Cthrough)	5.61	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	562	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1, AUCtau.	[2]
Trough Concentration (Cthrough)	28	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1080	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3, AUCtau.	[2]
Trough Concentration (Cthrough)	5.32	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	533	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1, AUCtau.	[2]
Trough Concentration (Cthrough)	15.1	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	988	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3, AUCtau.	[2]
Trough Concentration (Cthrough)	5.29	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	569	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 1, AUCtau.	[2]
Trough Concentration (Cthrough)	17	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1110	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 3, AUCtau.	[2]
Area Under the Concentration-Time Curve (AUC)	227	day*ug/mL	Dose escalation PK properties of ADC, 3.2 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	232	day*ug/mL	Dose escalation PK properties of ADC, 3.2 mg/kg, AUCinf.	[3]
Volume of Distribution (Vd)	62.2	mL/kg	Dose escalation PK properties of ADC, 3.2 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	424	day*ug/mL	Dose escalation PK properties of ADC, 4.8 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	450	day*ug/mL	Dose escalation PK properties of ADC, 4.8 mg/kg, AUCinf.	[3]
Volume of Distribution (Vd)	69.4	mL/kg	Dose escalation PK properties of ADC, 4.8 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	597	day*ug/mL	Dose escalation PK properties of ADC, 5.6 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	666	day*ug/mL	Dose escalation PK properties of ADC, 5.6 mg/kg, AUCinf.	[3]
Volume of Distribution (Vd)	71.9	mL/kg	Dose escalation PK properties of ADC, 5.6 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	572	day*ug/mL	Dose escalation PK properties of ADC, 6.4 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	649	day*ug/mL	Dose escalation PK properties of ADC, 6.4 mg/kg, AUCinf.	[3]
Volume of Distribution (Vd)	90.9	mL/kg	Dose escalation PK properties of ADC, 6.4 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	515	day*ug/mL	Dose expansion PK properties of ADC, 5.6 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	556	day*ug/mL	Dose expansion PK properties of ADC, 5.6 mg/kg, AUCinf.	[3]
Volume of Distribution (Vd)	72.9	mL/kg	Dose expansion PK properties of ADC, 5.6 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	534.54	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, Lyo-DP geometric means, AUClast.    Click to Show/Hide	[3]
Area Under the Concentration-Time Curve (AUC)	535.06	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, Lyo-DP geometric means, AUC0-21.    Click to Show/Hide	[3]
Area Under the Concentration-Time Curve (AUC)	571.61	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, FL-DP geometric means, AUClast.    Click to Show/Hide	[3]
Area Under the Concentration-Time Curve (AUC)	572.98	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, FL-DP geometric means, AUC0-21d.    Click to Show/Hide	[3]

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	881	day*ug/mL	Simulated Exposure Metrics of DXd-Conjugated Antibody for Patritumab Deruxtecan at 5.6 mg/kg Q3W,steady state	[1]
Trough Concentration (Cthrough)	0.21	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 1.6 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	113	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 1.6 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	0.21	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 1.6 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	106	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 1.6 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	0.93	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	207	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	2.3	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	315	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	3.57	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.8 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	408	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.8 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	8.12	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.8 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	645	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.8 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	8.14	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	630	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 6.4 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	18.3	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	978	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 6.4 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	11	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 8.0 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	795	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 8.0 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	21	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 8.0 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1190	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 8.0 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	0.81	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2/4.8/6/4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	270	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2/4.8/6/4 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	9.92	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2/4.8/6/4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	883	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2/4.8/6/4 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	6.34	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.2/6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	333	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.2/6.4 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	18.6	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.2/6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1080	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.2/6.4 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	5.24	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	499	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 1, AUCtau.	[2]
Trough Concentration (Cthrough)	13.1	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	880	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 3, AUCtau.	[2]
Trough Concentration (Cthrough)	5.61	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	562	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1, AUCtau.	[2]
Trough Concentration (Cthrough)	28	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1080	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3, AUCtau.	[2]
Trough Concentration (Cthrough)	5.32	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	533	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1, AUCtau.	[2]
Trough Concentration (Cthrough)	15.1	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	988	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3, AUCtau.	[2]
Trough Concentration (Cthrough)	5.29	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	569	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 1, AUCtau.	[2]
Trough Concentration (Cthrough)	17	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1110	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 3, AUCtau.	[2]
Area Under the Concentration-Time Curve (AUC)	227	day*ug/mL	Dose escalation PK properties of ADC, 3.2 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	232	day*ug/mL	Dose escalation PK properties of ADC, 3.2 mg/kg, AUCinf.	[3]
Area Under the Concentration-Time Curve (AUC)	424	day*ug/mL	Dose escalation PK properties of ADC, 4.8 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	450	day*ug/mL	Dose escalation PK properties of ADC, 4.8 mg/kg, AUCinf.	[3]
Area Under the Concentration-Time Curve (AUC)	597	day*ug/mL	Dose escalation PK properties of ADC, 5.6 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	666	day*ug/mL	Dose escalation PK properties of ADC, 5.6 mg/kg, AUCinf.	[3]
Area Under the Concentration-Time Curve (AUC)	572	day*ug/mL	Dose escalation PK properties of ADC, 6.4 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	649	day*ug/mL	Dose escalation PK properties of ADC, 6.4 mg/kg, AUCinf.	[3]
Area Under the Concentration-Time Curve (AUC)	515	day*ug/mL	Dose expansion PK properties of ADC, 5.6 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	556	day*ug/mL	Dose expansion PK properties of ADC, 5.6 mg/kg, AUCinf.	[3]
Area Under the Concentration-Time Curve (AUC)	534.54	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, Lyo-DP geometric means, AUClast.    Click to Show/Hide	[3]
Area Under the Concentration-Time Curve (AUC)	535.06	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, Lyo-DP geometric means, AUC0-21.    Click to Show/Hide	[3]
Area Under the Concentration-Time Curve (AUC)	571.61	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, FL-DP geometric means, AUClast.    Click to Show/Hide	[3]
Area Under the Concentration-Time Curve (AUC)	572.98	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, FL-DP geometric means, AUC0-21d.    Click to Show/Hide	[3]

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	881	day*ug/mL	Simulated Exposure Metrics of DXd-Conjugated Antibody for Patritumab Deruxtecan at 5.6 mg/kg Q3W,steady state	[1]
Clearance (CL)	0.342	L/day	Parameter Estimates of the Final Population PK Model for DXd-Conjugated Antibody.	[1]
Trough Concentration (Cthrough)	0.21	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 1.6 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	113	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 1.6 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	0.21	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 1.6 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	106	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 1.6 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	0.93	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	207	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	2.3	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	315	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	3.57	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.8 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	408	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.8 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	8.12	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.8 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	645	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.8 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	8.14	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	630	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 6.4 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	18.3	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	978	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 6.4 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	11	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 8.0 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	795	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 8.0 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	21	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 8.0 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1190	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 8.0 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	0.81	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2/4.8/6/4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	270	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2/4.8/6/4 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	9.92	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 3.2/4.8/6/4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	883	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 3.2/4.8/6/4 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	6.34	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.2/6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	333	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.2/6.4 mg/kg, Cycle 1.	[2]
Trough Concentration (Cthrough)	18.6	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, 4.2/6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1080	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd onjugated antibody) in the dose-escalation and dose-finding cohorts, AUCtau, 4.2/6.4 mg/kg, Cycle 3.	[2]
Trough Concentration (Cthrough)	5.24	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	499	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 1, AUCtau.	[2]
Trough Concentration (Cthrough)	13.1	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	880	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 4.8 mg/kg, Cycle 3, AUCtau.	[2]
Trough Concentration (Cthrough)	5.61	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	562	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1, AUCtau.	[2]
Trough Concentration (Cthrough)	28	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1080	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3, AUCtau.	[2]
Trough Concentration (Cthrough)	5.32	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	533	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 1, AUCtau.	[2]
Trough Concentration (Cthrough)	15.1	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	988	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-low, HR+/HER2- MBC, 6.4 mg/kg, Cycle 3, AUCtau.	[2]
Trough Concentration (Cthrough)	5.29	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 1.	[2]
Area Under the Concentration-Time Curve (AUC)	569	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 1, AUCtau.	[2]
Trough Concentration (Cthrough)	17	ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 3.	[2]
Area Under the Concentration-Time Curve (AUC)	1110	day*ug/mL	Pharmacokinetic parameters for HER3-DXd (DXd-conjugated antibody) in the dose-expansion cohorts,HER3-high, TNBC, 6.4 mg/kg, Cycle 3, AUCtau.	[2]
Area Under the Concentration-Time Curve (AUC)	227	day*ug/mL	Dose escalation PK properties of ADC, 3.2 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	232	day*ug/mL	Dose escalation PK properties of ADC, 3.2 mg/kg, AUCinf.	[3]
Elimination Half-Life (t1/2)	3.64	day	Dose escalation PK properties of ADC, 3.2 mg/kg.	[3]
Clearance (CL)	15.3	mL/day/kg	Dose escalation PK properties of ADC, 3.2 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	424	day*ug/mL	Dose escalation PK properties of ADC, 4.8 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	450	day*ug/mL	Dose escalation PK properties of ADC, 4.8 mg/kg, AUCinf.	[3]
Elimination Half-Life (t1/2)	4.9	day	Dose escalation PK properties of ADC, 4.8 mg/kg.	[3]
Clearance (CL)	12.2	mL/day/kg	Dose escalation PK properties of ADC, 4.8 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	597	day*ug/mL	Dose escalation PK properties of ADC, 5.6 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	666	day*ug/mL	Dose escalation PK properties of ADC, 5.6 mg/kg, AUCinf.	[3]
Elimination Half-Life (t1/2)	6.73	day	Dose escalation PK properties of ADC, 5.6 mg/kg.	[3]
Clearance (CL)	9.47	mL/day/kg	Dose escalation PK properties of ADC, 5.6 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	572	day*ug/mL	Dose escalation PK properties of ADC, 6.4 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	649	day*ug/mL	Dose escalation PK properties of ADC, 6.4 mg/kg, AUCinf.	[3]
Elimination Half-Life (t1/2)	6.95	day	Dose escalation PK properties of ADC, 6.4 mg/kg.	[3]
Clearance (CL)	10.3	mL/day/kg	Dose escalation PK properties of ADC, 6.4 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	515	day*ug/mL	Dose expansion PK properties of ADC, 5.6 mg/kg, AUClast.	[3]
Area Under the Concentration-Time Curve (AUC)	556	day*ug/mL	Dose expansion PK properties of ADC, 5.6 mg/kg, AUCinf.	[3]
Elimination Half-Life (t1/2)	5.6	day	Dose expansion PK properties of ADC, 5.6 mg/kg.	[3]
Clearance (CL)	10.9	mL/day/kg	Dose expansion PK properties of ADC, 5.6 mg/kg.	[3]
Area Under the Concentration-Time Curve (AUC)	534.54	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, Lyo-DP geometric means, AUClast.    Click to Show/Hide	[3]
Area Under the Concentration-Time Curve (AUC)	535.06	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, Lyo-DP geometric means, AUC0-21.    Click to Show/Hide	[3]
Area Under the Concentration-Time Curve (AUC)	571.61	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, FL-DP geometric means, AUClast.    Click to Show/Hide	[3]
Area Under the Concentration-Time Curve (AUC)	572.98	day*ug/mL	Geometric Mean Ratios of Cycle 1 PK Parameters for Lyophilized Powder Drug Product (Dose-Expansion Cohort 1) and Frozen Liquid Drug Product (Dose Escalation) of HER3-DXd at 5.6 mg/kg Q3W, FL-DP geometric means, AUC0-21d.    Click to Show/Hide	[3]

Standard Type	NCT Number	Clinical Status	Clinical Trial Description
Objective Response Rate (ORR)	NCT03260491	PHASE1	A Multicenter, Open-Label Phase 1 Study of U3-1402 in Subjects With Metastatic or Unresectable Non-small Cell Lung Cancer
Objective Response Rate (ORR)	NCT04619004	PHASE2	HERTHENA-Lung01: A Phase 2 Randomized Open-Label Study of Patritumab Deruxtecan (U3-1402) in Subjects With Previously Treated Metastatic or Locally Advanced EGFR-mutated Non-Small Cell Lung Cancer (NSCLC)    Click to Show/Hide
Undisclosed	NCT02980341	PHASE1|||PHASE2	Phase 1/2, Multicenter, Open-label, Multiple-Dose First-in-human Study of U3-1402, in Subjects With HER3 Positive Metastatic Breast Cancer
Undisclosed	NCT05569811	PHASE2	A Phase 2 Trial of neoadjuVAnt muLti-agENT Chemotherapy or Patritumab Deruxtecan (HER3-DXd; U3-1402) With or Without endocrINE Therapy for High-risk HR+/HER2- Breast Cancer - VALENTINE Trial
Undisclosed	NCT06298084	PHASE1|||PHASE2	Phase 1b/2, Multicenter, Open-label, Dose-Expansion Modular Study To Explore the Safety, Tolerability, and Anti-tumor Activity of HER3- DXd Monotherapy and Combinations in Patients With Inoperable Advanced Breast Cancer (ABC) After Progression on T-DXd    Click to Show/Hide
Undisclosed	NCT06686394	PHASE1|||PHASE2	HERTHENA-Breast-01: A Phase 1b/2, Multicenter, Open-label, Dose-Finding Study to Evaluate the Safety and Antitumor Activity of Patritumab Deruxtecan in Participants With HER2 Positive Unresectable Locally Advanced Breast Cancer or Metastatic Breast Cancer    Click to Show/Hide
Undisclosed	NCT06797635	PHASE2	An Open-label Randomized Phase 2 Study to Evaluate Safety and Efficacy of Patritumab Deruxtecan Plus Pembrolizumab Administered Either Before or After Carboplatin/Paclitaxel Plus Pembrolizumab Compared With Pembrolizumab in Combination With Chemotherapy Followed by Surgery and Adjuvant Pembrolizumab for High-Risk Early-Stage Triple-Negative or Hormone Receptor-Low Positive/Human Epidermal Growth Factor Receptor-2 Negative Breast Cancer (HERTHENA-Breast03)    Click to Show/Hide
Undisclosed	NCT04610528	EARLY_PHASE1	A Window-of-opportunity Study of U3-1402, a HER3-targeting Antibody-drug Conjugate in Operable Breast Cancer According to ERBB3 Expression
Undisclosed	NCT04699630	PHASE2	A Phase II Study of U3-1402 (Patritumab Deruxtecan) in Patients with Metastatic Breast Cancer
Undisclosed	NCT04965766	PHASE2	Phase 2, Open Label Study of Patritumab Deruxtecan (U3-1402), an Anti-HER3-Antibody Drug Conjugate (ADC), in Patients With Advanced Breast Cancer, With Biomarker Analyses to Characterize Response to Therapy    Click to Show/Hide
Undisclosed	NCT06172478	PHASE2	HERTHENA-PanTumor01 (U31402-277): A Phase 2, Multicenter, Multicohort, Open-Label, Proof of Concept Study of Patritumab Deruxtecan (HER3-DXd; U3-1402) in Subjects With Locally Advanced or Metastatic Solid Tumors    Click to Show/Hide
Undisclosed	NCT04479436	PHASE2	A Multi-Center, Open-Label, Phase 2 Study to Evaluate Safety and Efficacy of U3-1402 in Subjects With Advanced or Metastatic Colorectal Cancer (CRC)
Undisclosed	NCT06596694	PHASE1|||PHASE2	A Phase 1/2 Study to Evaluate the Safety and Efficacy of Patritumab Deruxtecan in Gastrointestinal Cancers
Undisclosed	NCT04165070	PHASE1|||PHASE2	KEYMAKER-U01 Substudy 01A: A Phase 1/2, Umbrella Study With Rolling Arms of Investigational Agents With Pembrolizumab With or Without Chemotherapy in Treatment-Naive Participants With Stage IV Non-small Cell Lung Cancer (NSCLC)    Click to Show/Hide
Undisclosed	NCT04676477	PHASE1	A Phase 1 Open-Label Study of HER3-DXd (Patritumab Deruxtecan; U3-1402) in Combination With Osimertinib in Subjects With Locally Advanced or Metastatic EGFR-mutated Non-Small Cell Lung Cancer (NSCLC)
Undisclosed	NCT06099639	N.A.	Medical Access Program for Patritumab Deruxtecan (HER3 DXd, U3-1402)
Undisclosed	NCT06731907	PHASE2	KEYMAKER-U01 Substudy 01G: A Phase 2, Umbrella Study With Rolling Arms of Investigational Agents in Combination With Pembrolizumab With or Without Platinum-based Chemotherapy in Treatment-Naïve Participants With Stage IV Non-small Cell Lung Cancer (NSCLC)    Click to Show/Hide
Undisclosed	NCT05338970	PHASE3	A Phase 3, Randomized, Open-label Study of Patritumab Deruxtecan Versus Platinum-based Chemotherapy in Metastatic or Locally Advanced Epidermal Growth Factor Receptor-mutated (EGFRm) Non-small Cell Lung Cancer (NSCLC) After Failure of Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor (TKI) Therapy (HERTHENA-Lung02)    Click to Show/Hide
Undisclosed	NCT06383884	PHASE2	An Open Label, Phase 2 Basket Study of Patritumab Deruxtecan in Patients with Solid Tumor Harboring an NRG1 Fusion
Objective Response Rate (ORR)	NCT03260491	Phase 1	A multicenter, open-label phase 1 study of U3-1402 in subjects with metastatic or unresectable non-small cell lung cancer.

Standard Type	Value	Units	Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI)	≈ 40.3	%	Non-small cell lung cancer PDX model (PDX: DFCI-306)
Tumor Growth Inhibition value (TGI)	≈ 78.3	%	Non-small cell lung cancer PDX model (PDX: DFCI-259)
Tumor Growth Inhibition value (TGI)	≈ 82.2	%	Non-small cell lung cancer PDX model (PDX: DFCI-161)
Tumor Growth Inhibition value (TGI)	≈ 86.2	%	Non-small cell lung cancer PDX model (PDX: DFCI-284)

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 78.5	%	B16-F10 cells	Mouse melanoma
Tumor Growth Inhibition value (TGI)	≈ 95.1	%	MDA-MB-453 cells	Breast adenocarcinoma

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Objective Response Rate (ORR)	28%
Patients Enrolled	Eligibility requires locally advanced/metastatic NSCLC (RECIST v1.1 measurable lesions, ECOG 0-1). Dose escalation mandates EGFR TKI resistance (Jackman criteria), while expansion cohorts specify prior therapies (e.g., platinum-based regimens, KRAS-G12C inhibitors in Cohort 5). Exclusions include ILD, uncontrolled CVD, active infections, recent cytotoxic therapy, or contraindications like QT prolongation. Cohort-specific exclusions apply (e.g., EGFR mutations in Cohort 2, leptomeningeal disease in Cohort 4).    Click to Show/Hide
Administration Dosage	Participants in the Dose Escalation Cohort 1 will receive HER3-DXd intravenously (IV) once every three weeks at 3.2, 4.8, 5.6, 6.4 mg/kg.
Related Clinical Trial
NCT Number	NCT03260491	Clinical Status	PHASE1
Clinical Description	A Multicenter, Open-Label Phase 1 Study of U3-1402 in Subjects With Metastatic or Unresectable Non-small Cell Lung Cancer
Primary Endpoint	The study evaluates dose-limiting toxicities (DLTs) over 21 days in the dose-escalation phase and adverse event summaries over approximately 36 months. Efficacy measures include ORR (using RECIST v1.1 via BICR) during dose expansion. Pharmacokinetic endpoints-Cmax, AUCinf, and AUC (last)-for HER3-DXd, total anti-HER3, and MAAA-1181a are assessed across cycles with intensive blood sampling (pre-dose to Day 15).    Click to Show/Hide
Other Endpoint	Secondary outcomes include pharmacokinetics (Cmax, Tmax, AUC[0-21]) during dose escalation and efficacy metrics (ORR, DCR, DOR, TTR, PFS, OS) monitored over ~36 months. Dose expansion tracks similar endpoints over ~60 months, including NSCLC-SAQ symptom severity scores and PRO-CTCAE analyses to assess symptom progression. ADA status and PK parameters are also evaluated in specific cohorts.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Objective Response Rate (ORR)	29.80%
Patients Enrolled	Exclusion criteria include small cell or mixed histology NSCLC, active interstitial lung disease, uncontrolled respiratory conditions, symptomatic brain/spinal cord metastases, or inadequate washout periods (e.g., <14 days for chemo, <28 days for major surgery). Prior HER3 antibodies, topoisomerase I inhibitors, or ADCs containing such inhibitors are prohibited. Unresolved toxicities (>Grade 1), active secondary malignancies (except certain cured cancers), uncontrolled cardiovascular disease, or active HBV/HCV/HIV infections also exclude participation. Chronic systemic corticosteroids >10 mg prednisone/day or leptomeningeal disease are additional exclusions.    Click to Show/Hide
Administration Dosage	Patritumab deruxtecan will be dosed at 5.6 mg/kg as an intravenous (IV) infusion administered on Day 1 of each 21-day cycle; Patritumab deruxtecan will be dosed as an intravenous (IV) infusion administered at Cycle 1, 3.2 mg/kg; Cycle 2, 4.8 mg/kg; Cycle 3 and subsequent cycles, 6.4 mg/kg administered on Day 1 of each 21-day cycle.
Related Clinical Trial
NCT Number	NCT04619004	Clinical Status	PHASE2
Clinical Description	HERTHENA-Lung01: A Phase 2 Randomized Open-Label Study of Patritumab Deruxtecan (U3-1402) in Subjects With Previously Treated Metastatic or Locally Advanced EGFR-mutated Non-Small Cell Lung Cancer (NSCLC)
Primary Endpoint	The primary objective is to assess Objective Response Rate (ORR) by BICR per RECIST v1.1, defined as the proportion of participants achieving confirmed CR (disappearance of all target lesions) or PR (≥30% decrease in sum of diameters) from screening until progression, death, or study discontinuation (up to ~21 months). Secondary endpoints include Duration of Response (time from first confirmed response to progression/death), Progression-Free Survival (time from treatment start to PD/death), ORR by investigator, Disease Control Rate (CR+PR+SD), Time to Tumor Response, and Best Percentage Change in Sum of Diameters of measurable tumors. Overall Survival will track from treatment start to death (up to ~45 months). Safety will be evaluated through Treatment-Emergent AEs, SAEs, and AESIs from baseline to Day 47 post-last dose.    Click to Show/Hide
Other Endpoint	Eligible participants must be ≥18 years with histologically confirmed advanced/metastatic NSCLC progressing after osimertinib and platinum-based chemotherapy, harboring EGFR exon 19 or L858R mutations, and having ≥1 measurable lesion per RECIST v1.1. Required tumor tissue includes fresh biopsy or archival specimen obtained within 3 months post-progression. ECOG 0-1 and adequate organ function (platelets ≥100K/mm 3, hemoglobin ≥9 g/dL, ANC ≥1500/mm 3, creatinine clearance ≥30 mL/min, and liver function within specified limits) are mandatory.    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[6]
Patients Enrolled	Eligible patients must have HER3-positive advanced/metastatic breast cancer, ECOG 0-1, LVEF &ge;50%, and measurable disease (RECIST 1.1). Dose expansion requires prior taxane therapy (except TNBC cohort), while TNBC patients need HR-/HER2- status and 1-2 prior lines. Exclusions include prior HER3/ADC treatment (e.g., exatecan-based), severe cardiac/pulmonary disease, or corrected QT prolongation (>450ms males, >470ms females).    Click to Show/Hide
Administration Dosage	In DE/DF, U3-1402 was administered intravenously (IV) Q2W or Q3W at doses ranging from 1.6 to 8.0 mg/kg. Patients had HER3-expressing advanced/unresectable disease refractory/intolerant to standard treatment or for which no standard treatment was available. In the expansion part, U3-1402 was administered IV Q3W to patients with HER3-high (4.8 or 6.4 mg/kg) or HER3-low (6.4 mg/kg) HR+/HER2- MBC or with HER3-high triple-negative breast cancer (TNBC; 6.4 mg/kg).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02980341	Clinical Status	PHASE1|||PHASE2
Clinical Description	Phase 1/2, Multicenter, Open-label, Multiple-Dose First-in-human Study of U3-1402, in Subjects With HER3 Positive Metastatic Breast Cancer
Primary Endpoint	The primary safety and efficacy endpoints include the incidence of Treatment-emergent Adverse Events (TEAEs) up to 28 days post-last dose and Best Overall Response (CR, PR, or SD per RECIST 1.1) assessed via blinded independent review. ORR is defined as confirmed CR/PR, while SD indicates neither sufficient shrinkage nor progression (≥20% increase).    Click to Show/Hide
Other Endpoint	Pharmacokinetic parameters (AUC, Cmax, Tmax) for anti-HER3-ac-DXd and total anti-HER3 antibody were evaluated using IC-LC/MS across study phases (Dose Escalation, Finding, Expansion) over multiple cycles (21-day intervals). Data includes serum concentration-time profiles for both ADC and total antibody components.
Experiment 4 Reporting the Activity Date of This ADC					[7]
Patients Enrolled	Clinical assessments span from baseline through treatment and follow-up, evaluating pathological, molecular (CelTIL/HER3/Ki67), and QoL outcomes. Safety monitoring includes AEs, lab abnormalities, and protocol compliance until 30 days post-surgery. The study emphasizes strict eligibility around treatment history and comorbidities to ensure patient suitability for neoadjuvant therapy and surgery.    Click to Show/Hide
Administration Dosage	HER3-DXd will be administered as Lyo-DP, a sterile lyophilized powder in a dose of 5.6 mg/kg
Related Clinical Trial
NCT Number	NCT05569811	Clinical Status	PHASE2
Clinical Description	A Phase 2 Trial of neoadjuVAnt muLti-agENT Chemotherapy or Patritumab Deruxtecan (HER3-DXd; U3-1402) With or Without endocrINE Therapy for High-risk HR+/HER2- Breast Cancer - VALENTINE Trial
Primary Endpoint	The primary endpoint is pCRBL rate (ypT0/is ypN0) at surgery, indicating complete absence of invasive carcinoma in the breast and lymph nodes. Secondary endpoints include Residual Cancer Burden (RCB) categories, pCRB (breast-only response), tumor ORR per RECIST v1.1, iDFS at 3/5 years (covering recurrence types), CelTIL score changes, HER3/ERBB3 expression, Ki67 changes, Quality of Life via EORTC-BR45/QLQ-C30, and safety with AE monitoring per NCI CTCAE v5.0.    Click to Show/Hide
Other Endpoint	Inclusion criteria: Untreated, non-metastatic ER+/PgR+/HER2- breast adenocarcinoma with Ki67≥20% or high genomic risk, ECOG 0-1, chemotherapy/surgery eligibility, tumor sample availability, adequate organ function, and LVEF≥50%. Exclusion criteria: Metastatic/bilateral cancer, prior treatments (chemo/radiation/anti-HER3/topoisomerase inhibitors), excisional biopsy, cardiac/pulmonary diseases, other malignancies (exceptions apply), uncontrolled systemic conditions, infections (HIV/hepatitis), hypersensitivity to drug components, high anthracycline exposure, ILD history, unresolved toxicities (>grade 1), neuropathy, chronic steroids (>10mg prednisone), corneal disease, pregnancy, or hydroxychloroquine use within 14 days.    Click to Show/Hide
Experiment 5 Reporting the Activity Date of This ADC					[8]
Patients Enrolled	Eligible patients must have prior T-DXd progression, HER2+/HER2-low breast cancer, measurable lesions, and adequate organ function. Exclusions include ILD, uncontrolled systemic diseases, active brain metastases, unresolved toxicities, significant cardiovascular disorders, active HBV/HCV, pregnancy, or prior anti-HER3 therapy. Contraception and washout periods per protocol are mandatory.    Click to Show/Hide
Administration Dosage	.
Related Clinical Trial
NCT Number	NCT06298084	Clinical Status	PHASE1|||PHASE2
Clinical Description	Phase 1b/2, Multicenter, Open-label, Dose-Expansion Modular Study To Explore the Safety, Tolerability, and Anti-tumor Activity of HER3- DXd Monotherapy and Combinations in Patients With Inoperable Advanced Breast Cancer (ABC) After Progression on T-DXd
Primary Endpoint	The study evaluates DLTs, safety event frequency/severity, treatment modifications, lab abnormalities (graded by NCI-CTCAE v5.0), and radiographic changes for ILD/pneumonitis in parts 1a/1b over 21 months. For part 2 (51 months), endpoints include ORR, DOR, PFS, and CBR assessed via RECIST v1.1.
Other Endpoint	For part 1 (45 months), outcomes include ORR, DOR, PFS, CBR, PK/ADA analysis for HER3-DXd and olaparib. For part 2 (39 months), safety metrics (AEs, lab abnormalities, treatment modifications), PK/ADA analysis, and ILD assessments via CT/pulmonologist review are evaluated.
Experiment 6 Reporting the Activity Date of This ADC					[9]
Patients Enrolled	Eligible participants must have HER2+ locally advanced or metastatic breast cancer, meet specific HIV/HBV/HCV and ECOG criteria, and have prior anti-HER2 therapy history (varying by study arm). Exclusion criteria include uncontrolled cardiovascular/pulmonary disease, active infections, prior HER2-targeted TKIs (Arm 3), and certain malignancies or neurological conditions.    Click to Show/Hide
Administration Dosage	.
Related Clinical Trial
NCT Number	NCT06686394	Clinical Status	PHASE1|||PHASE2
Clinical Description	HERTHENA-Breast-01: A Phase 1b/2, Multicenter, Open-label, Dose-Finding Study to Evaluate the Safety and Antitumor Activity of Patritumab Deruxtecan in Participants With HER2 Positive Unresectable Locally Advanced Breast Cancer or Metastatic Breast Cancer
Primary Endpoint	This study evaluates dose-limiting toxicities (DLTs) and adverse events (AEs) associated with the investigational treatment, including the number of participants experiencing DLTs within 21 days, AEs within approximately 13 months, and discontinuations due to AEs within approximately 12 months.
Other Endpoint	Pharmacokinetic parameters including Cmax, Ctrough, and AUC for patritumab deruxtecan ADC, total patritumab deruxtecan antidrug antibody (ADA), and free payload will be assessed through blood samples collected at designated time points over a period of up to ~24 months.
Experiment 7 Reporting the Activity Date of This ADC					[10]
Patients Enrolled	Eligible participants have locally advanced TNBC/HR-low+/HER2- breast cancer (AJCC stages cT1c-T4/N0-N2), controlled HBV/HCV, ECOG 0-1, and LVEF &ge;50%/LLN. Exclusions include prior anti-PD-1/L1/HER3 therapy, active malignancies, CNS metastases, ILD, uncontrolled infections, or cardiovascular/corneal disease. Metastatic (M1) or cN3 disease is excluded.    Click to Show/Hide
Administration Dosage	.
Related Clinical Trial
NCT Number	NCT06797635	Clinical Status	PHASE2
Clinical Description	An Open-label Randomized Phase 2 Study to Evaluate Safety and Efficacy of Patritumab Deruxtecan Plus Pembrolizumab Administered Either Before or After Carboplatin/Paclitaxel Plus Pembrolizumab Compared With Pembrolizumab in Combination With Chemotherapy Followed by Surgery and Adjuvant Pembrolizumab for High-Risk Early-Stage Triple-Negative or Hormone Receptor-Low Positive/Human Epidermal Growth Factor Receptor-2 Negative Breast Cancer (HERTHENA-Breast03)
Primary Endpoint	Part 1 evaluates safety outcomes including AEs (up to ~43 weeks), DLTs (NCI CTCAE v5.0-defined toxicities within 21 days), and treatment discontinuations due to AEs (up to ~30 weeks). Part 2 assesses pCR (ypT0/Tis ypN0) as primary endpoint (~30 weeks), along with AEs (~103 weeks) and treatment discontinuations (~90 weeks).
Other Endpoint	Secondary efficacy endpoints in Part 2 include pCR-no DCIS (ypT0 ypN0), EFS (time to progression/recurrence/death, ~100 months), OS (time to death, ~100 months), DPDRFS (time to distant progression/death), and RCB classification (RCB-0 to RCB-3) at surgery (~30 weeks).
Experiment 8 Reporting the Activity Date of This ADC					[11]
Patients Enrolled	Eligible patients are adults (&ge;18y) with untreated, non-metastatic HR+/HER2- or TNBC (ASCO-CAP criteria), measurable lesions (&ge;1cm), Ki67&ge;10%, LVEF&ge;50%, and adequate organ function. Exclusions include prior HER3/topoisomerase I inhibitor therapy, cardiac/pulmonary disorders, unresolved grade&ge;2 toxicity, QT prolongation, active infections, or concurrent malignancies (exceptions: cured cancers in past 3 years).    Click to Show/Hide
Administration Dosage	.
Related Clinical Trial
NCT Number	NCT04610528	Clinical Status	EARLY_PHASE1
Clinical Description	A Window-of-opportunity Study of U3-1402, a HER3-targeting Antibody-drug Conjugate in Operable Breast Cancer According to ERBB3 Expression
Primary Endpoint	The study assesses mean CelTIL score changes (scaled 0-100 based on tumor cellularity and TILs) from baseline to Cycle 1 Day 21 post-U3-1402, capturing treatment-induced tumor microenvironment shifts.
Other Endpoint	Secondary evaluations include CelTIL changes by ERBB3 cohort/HER3 IHC/PAM50 subtype, CCCA (Ki67<2.7%), ERBB3-HER3 biomarker correlation, safety (NCI CTCAE v5.0-graded AEs), and longitudinal HER3 expression changes (baseline to Cycle 1 Day 21 with optional Day 3-7 sampling).
Experiment 9 Reporting the Activity Date of This ADC					[12]
Patients Enrolled	Eligible adults (&ge;18y) with HER2- (Parts A/B: 1-5 prior chemo lines, endocrine/CDK4/6i-refractory HR+) or HER2+ MBC (Part Z: &ge;2 anti-HER2 therapies including trastuzumab deruxtecan) must have measurable disease, ECOG 0-1, and adequate organ function. Key exclusions: prior HER3-targeted therapy, unresolved Grade>1 toxicity (except alopecia), active brain metastases/ILD, LVEF<50%, or severe cardiovascular/pulmonary conditions. HER2+ cohorts prohibit other exatecan ADCs (non-trastuzumab deruxtecan).    Click to Show/Hide
Administration Dosage	Participants will receive 5.6 mg/kg U3-1402 (Patritumab Deruxtecan) intravenously on day 1 every 3 weeks.
Related Clinical Trial
NCT Number	NCT04699630	Clinical Status	PHASE2
Clinical Description	A Phase II Study of U3-1402 (Patritumab Deruxtecan) in Patients with Metastatic Breast Cancer
Primary Endpoint	The study evaluates U3-1402 efficacy in HER2-/HER2+ MBC patients through ORR (confirmed CR/PR per RECIST v1.1), PFS-6 (proportion without progression at 6 months), and CBR (CR/PR/SD≥6 months), with tumor assessments every 6-9 weeks up to 33 months. PD is defined as ≥20% target lesion growth, new lesions, or non-target progression.
Other Endpoint	Safety endpoints include AE incidence (up to 40 days post-treatment), median DOR (time from response to PD/death), median PFS (time to PD/death), and HER2+ subgroup ORR/PFS-6 post-trastuzumab deruxtecan failure, all assessed per RECIST v1.1. Disease progression criteria mirror primary endpoints.
Experiment 10 Reporting the Activity Date of This ADC					[13]
Patients Enrolled	Exclusion criteria include curative-intent resectable disease, interstitial lung disease, uncontrolled systemic illnesses, active brain metastases, inadequate washout periods for prior therapies, cardiovascular risks (QT prolongation, LVEF <50%, recent MI), active HBV/HCV/HIV infections, pregnancy/breastfeeding, hypersensitivity to study drugs, and concurrent experimental treatments. Participants must not have unresolved grade &ge;2 toxicities (except alopecia) or other primary malignancies within 3 years (exceptions: cured non-melanoma skin cancer or in-situ lesions). Legal or psychological barriers to protocol compliance also disqualify.    Click to Show/Hide
Administration Dosage	All participants enrolled in the study will receive U3-1402 at a dose of 5.6 mg/kg every 3 weeks until progression or until unacceptable toxicity
Related Clinical Trial
NCT Number	NCT04965766	Clinical Status	PHASE2
Clinical Description	Phase 2, Open Label Study of Patritumab Deruxtecan (U3-1402), an Anti-HER3-Antibody Drug Conjugate (ADC), in Patients With Advanced Breast Cancer, With Biomarker Analyses to Characterize Response to Therapy
Primary Endpoint	The primary outcome is the investigator-assessed objective response rate (ORR), defined as the proportion of participants achieving complete response (CR) or partial response (PR), measured over an average of 8 months during treatment. Secondary outcomes include duration of response (DOR), progression-free survival (PFS), and clinical benefit ratio (CBR), all assessed by investigators and central review over up to 42 months. Safety endpoints cover adverse events, lab abnormalities, ECG changes, and quality of life measures via EORTC QLQ-C30 and ECOG performance status. Additional efficacy metrics include overall survival (OS) and central-review ORR.    Click to Show/Hide
Other Endpoint	Eligible participants are adults with histologically confirmed HER2-negative, hormone receptor-positive (HR+), unresectable locally advanced or metastatic breast cancer who progressed after CDK4/6 inhibitor therapy with endocrine treatment. Key requirements include accessible tumor biopsy sites, measurable lesions, ECOG PS 0-1, life expectancy ≥12 weeks, adequate organ function, and compliance with contraception protocols. Prior treatments may include anthracyclines, taxanes, PI3K/mTOR/AKT inhibitors, or PARP inhibitors, but only one line of chemotherapy for advanced disease is permitted.    Click to Show/Hide
Experiment 11 Reporting the Activity Date of This ADC					[14]
Patients Enrolled	Eligibility requires &ge;18y/o patients with advanced/metastatic disease progression after prior therapies (1-3 lines depending on tumor type), ECOG 0-1. Exclusions include HER2+ gastric cancer, active ILD, recent malignancies (except cured carcinomas), prior HER3/TOP1-ADC treatment, and metastatic irinotecan exposure. Tumor tissue confirmation and biomarker status (e.g., HPV, HER2) are mandated per protocol-specific thresholds.    Click to Show/Hide
Administration Dosage	Participants with locally advanced or metastatic cancer (melanoma, head and neck, gastric cancer, ovarian carcinoma, cervical cancer, endometrial cancer, bladder cancer, esophageal carcinoma, pancreatic carcinoma, and prostate cancer) will receive an intravenous infusion of HER3-DXd monotherapy 5.6 mg/kg every 3 weeks (Q3W).
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NCT Number	NCT06172478	Clinical Status	PHASE2
Clinical Description	HERTHENA-PanTumor01 (U31402-277): A Phase 2, Multicenter, Multicohort, Open-Label, Proof of Concept Study of Patritumab Deruxtecan (HER3-DXd; U3-1402) in Subjects With Locally Advanced or Metastatic Solid Tumors
Primary Endpoint	This study evaluates HER3-DXd monotherapy efficacy in various cancer cohorts (excluding prostate cancer) with primary endpoints including confirmed objective response rate (ORR) per RECIST v1.1 and PSA reduction ≥50% (prostate cohort only), assessed over 27 months. ORR combines complete (CR) and partial response (PR) rates, while prostate-specific outcomes focus on biochemical markers.    Click to Show/Hide
Other Endpoint	Safety and efficacy assessments cover all cohorts, tracking treatment-emergent adverse events (graded via NCI-CTCAE v5.0), duration of response (DoR), clinical benefit rate (CR+PR+SD≥183d), and pharmacokinetics (Cmax, Tmax, AUC). The prostate cohort adds PCWG3-based radiographic PFS, time to first skeletal event, and subsequent therapy metrics over 27 months, with intensive PK sampling during cycles 1-8.    Click to Show/Hide
Experiment 12 Reporting the Activity Date of This ADC					[15]
Patients Enrolled	Eligible participants (&ge;18y/o, ECOG 0-1) must have progressed on &ge;2 prior lines including fluoropyrimidine/irinotecan/anti-EGFR/VEGF therapies, with measurable lesions and adequate organ function. Key exclusions: active ILD, uncontrolled cardiovascular disease, untreated CNS metastases, unresolved CTCAE Grade &ge;2 toxicities, prior HER3/exatecan-ADC exposure, or HIV/HBV/HCV viremia outside protocol-permitted thresholds. Tumor tissue requirements mandate pretreatment biopsy unless recent archival samples exist.    Click to Show/Hide
Administration Dosage	U3-1402 will be dosed at 5.6 mg/kg as an intravenous (IV) infusion administered on Day 1 of each 21-day cycle.
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NCT Number	NCT04479436	Clinical Status	PHASE2
Clinical Description	A Multi-Center, Open-Label, Phase 2 Study to Evaluate Safety and Efficacy of U3-1402 in Subjects With Advanced or Metastatic Colorectal Cancer (CRC)
Primary Endpoint	The study evaluates U3-1402 in advanced/metastatic colorectal cancer, assessing primary endpoints including blinded independent central review (BICR)-confirmed ORR (CR+PR per RECIST v1.1) and investigator-assessed efficacy outcomes (ORR, DoR, DCR) over 27 months, with tumor response metrics capturing both radiographic and clinical progression events.    Click to Show/Hide
Other Endpoint	Secondary objectives include safety profiling (TEAEs, lab abnormalities), pharmacokinetics (Cmax, Tmax, AUClast), and immunogenicity (ADA incidence), with intensive PK sampling during cycles 1-8. Disease control parameters (PFS by BICR/investigator, OS) and biomarker analyses (HER3 expression) are tracked alongside protocol-defined washout periods for prior therapies.    Click to Show/Hide
Experiment 13 Reporting the Activity Date of This ADC					[16]
Patients Enrolled	Key inclusion criteria involve unresectable/metastatic colorectal cancer, biliary tract cancer (BTC), or hepatocellular carcinoma (HCC), with prior therapy and recovery from treatment side effects. Exclusion criteria cover interstitial lung disease (ILD), severe respiratory compromise, leptomeningeal disease, corneal disease, uncontrolled cardiovascular/cerebrovascular conditions, or active systemic infections, ensuring patient safety in the study.    Click to Show/Hide
Administration Dosage	Participants receive patritumab deruxtecan intravenous (IV) infusion on Day 1 of each 21-day cycle (every 3 weeks) until disease progression, intolerable toxicity, or investigator decision.
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NCT Number	NCT06596694	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Phase 1/2 Study to Evaluate the Safety and Efficacy of Patritumab Deruxtecan in Gastrointestinal Cancers
Primary Endpoint	The primary endpoints include Dose-Limiting Toxicity (DLT) evaluated over 21 days in the dose-escalation phase, Adverse Events (AEs) monitored over approximately 45 months, and participants discontinuing treatment due to AEs. Additionally, Objective Response Rate (ORR) per RECIST 1.1 via Blinded Independent Central Review (BICR) will assess Complete Response (CR) or Partial Response (PR) rates. All endpoints aim to evaluate safety and efficacy.    Click to Show/Hide
Other Endpoint	Secondary endpoints include Duration of Response (DOR) and Progression-Free Survival (PFS) using RECIST 1.1 criteria (assessed by BICR), measuring time to progressive disease (PD) or death. Overall Survival (OS) tracks time from treatment initiation until death. Pharmacokinetic endpoints include maximum plasma concentration (Cmax) and trough concentration (Ctrough) of patritumab deruxtecan, measured at designated time points over ~45 months. These metrics evaluate treatment efficacy and drug exposure.    Click to Show/Hide
Experiment 14 Reporting the Activity Date of This ADC					[17]
Patients Enrolled	Eligibility requires untreated Stage IV NSCLC (squamous/nonsquamous) with archived tumor tissue. Exclusions include prior systemic therapy for metastatic disease, uncontrolled CNS metastases, active autoimmune/immunodeficiency conditions, recent major surgery/radiotherapy (>30Gy to lungs), live vaccines (excluding licensed COVID-19 vaccines), or severe irAEs from prior immunotherapy. GI/liver dysfunction affecting drug absorption and unresolved prior treatment toxicities (>CTCAE Grade 1) also preclude enrollment.    Click to Show/Hide
Administration Dosage	.
Related Clinical Trial
NCT Number	NCT04165070	Clinical Status	PHASE1|||PHASE2
Clinical Description	KEYMAKER-U01 Substudy 01A: A Phase 1/2, Umbrella Study With Rolling Arms of Investigational Agents With Pembrolizumab With or Without Chemotherapy in Treatment-Naive Participants With Stage IV Non-small Cell Lung Cancer (NSCLC)
Primary Endpoint	Part A evaluates ORR (CR or PR per RECIST 1.1) over ~24 months. Part B tracks safety endpoints: AEs (~27 months), discontinuations due to AEs (~24 months), and DLTs (3 weeks). PK metrics (Cmax/Ctrough) for I-DXd, HER3-DXd, and pembrolizumab are measured via plasma/serum sampling up to ~2 years.
Other Endpoint	Part A assesses PFS (time to PD/death per RECIST 1.1) over ~24 months, alongside AE reporting. Part B measures ORR/DOR via BICR (~24 months) and PK parameters (Cmax/Ctrough) for I-DXd, HER3-DXd, and pembrolizumab through multi-point blood sampling up to ~2 years. Safety and efficacy data are captured across both parts.
Experiment 15 Reporting the Activity Date of This ADC					[18]
Patients Enrolled	Exclusion criteria include small-cell histology, active ILD/pneumonitis, untreated brain metastases, unresolved Grade &ge;2 toxicities, uncontrolled cardiovascular disease (QTcF >450 ms, LVEF &le;45%, recent MI), strong CYP3A4 inducers, recent radiation/immunotherapy, prior malignancies (exceptions: non-melanoma skin cancer, curatively treated early-stage tumors), and poorly controlled HIV. Concomitant conditions jeopardizing protocol compliance also exclude participation.    Click to Show/Hide
Administration Dosage	Pts receive HER3-DXd 1.6, 3.2, 4.8, or 5.6 mg/kg intravenously (IV) every 3 weeks (Q3W) in combination with osimertinib 40 or 80 mg orally (PO) once daily (QD).
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NCT Number	NCT04676477	Clinical Status	PHASE1
Clinical Description	A Phase 1 Open-Label Study of HER3-DXd (Patritumab Deruxtecan; U3-1402) in Combination With Osimertinib in Subjects With Locally Advanced or Metastatic EGFR-mutated Non-Small Cell Lung Cancer (NSCLC)
Primary Endpoint	The study evaluates dose-limiting toxicities (DLTs), treatment-emergent adverse events (TEAEs), serious adverse events (SAEs), and adverse events of special interest (AESIs) during dose escalation, classified per NCI-CTCAE v5.0. Objective response rate (ORR) is assessed in dose expansion phases, defined as confirmed CR or PR by RECIST v1.1 via blinded independent central review (BICR). Additional endpoints include duration of response (DoR), clinical benefit rate (CBR), disease control rate (DCR), time to response (TTR), progression-free survival (PFS), overall survival (OS), immunogenicity (ADA assessment), and pharmacokinetic parameters (Cmax, Tmax, AUC).    Click to Show/Hide
Other Endpoint	Key inclusion criteria for dose escalation and second-line expansion include confirmed EGFR exon 19del/L858R mutations, prior osimertinib treatment (≥6 weeks) with progression. First-line expansion requires untreated EGFR-mutant NSCLC eligible for osimertinib. All participants must have measurable disease per RECIST v1.1, adequate organ function, and provide tumor tissue (pre-/on-treatment biopsies for certain cohorts).    Click to Show/Hide
Experiment 16 Reporting the Activity Date of This ADC					[19]
Patients Enrolled	Inclusion criteria require signed consent, age &ge;18, confirmed EGFRm NSCLC with progression post EGFR TKI (including osimertinib) and platinum-based chemotherapy, ECOG PS 0-1, adequate organ function, and contraception compliance. For resupply, continued treatment benefit and safety reporting are mandatory. Exclusion criteria include participation in Daiichi Sankyo ADC trials, small cell histology, active/past ILD, severe respiratory compromise, unresolved toxicities (Grade >1), uncontrolled cardiovascular disease, active HBV/HCV/HIV, HER3-DXd hypersensitivity, pregnancy, clinically significant infections, or corneal disease.    Click to Show/Hide
Administration Dosage	.
Related Clinical Trial
NCT Number	NCT06099639	Clinical Status	N.A.
Clinical Description	Medical Access Program for Patritumab Deruxtecan (HER3 DXd, U3-1402)
Experiment 17 Reporting the Activity Date of This ADC					[20]
Patients Enrolled	Eligible patients must have stage IV NSCLC (squamous/non-squamous), ECOG 0-1, available tumor tissue, and controlled HIV/HBV if applicable. Key exclusions include small cell histology, EGFR/ALK/ROS1 alterations (squamous), active CNS metastases, uncontrolled cardiovascular disease (recent MI, NYHA 3-4 CHF), prior topoisomerase I inhibitors/anti-HER3 ADCs, recent radiotherapy/vaccines, concurrent HBV/HCV, immunosuppressive therapy, or active autoimmune disease/infections requiring treatment. Washout periods for prior therapies and adequate recovery from major surgery are required.    Click to Show/Hide
Administration Dosage	HER3-Dxd 5.6mg/kg IV infusion.
Related Clinical Trial
NCT Number	NCT06731907	Clinical Status	PHASE2
Clinical Description	KEYMAKER-U01 Substudy 01G: A Phase 2, Umbrella Study With Rolling Arms of Investigational Agents in Combination With Pembrolizumab With or Without Platinum-based Chemotherapy in Treatment-Naïve Participants With Stage IV Non-small Cell Lung Cancer (NSCLC)
Primary Endpoint	The primary efficacy endpoint is overall response rate (ORR) defined as confirmed complete or partial response per RECIST 1.1 assessed by blinded independent central review (BICR). Safety assessments include monitoring of adverse events (AEs) and treatment discontinuations due to AEs over approximately 2-5 years.
Other Endpoint	Secondary efficacy endpoints include duration of response (DOR) for responders, progression-free survival (PFS) from randomization to progression/death, and overall survival (OS) from randomization to death, all assessed per RECIST 1.1 by BICR over ~5 years.
Experiment 18 Reporting the Activity Date of This ADC					[21]
Patients Enrolled	Key exclusions include small cell/mixed histology, active ILD, uncontrolled respiratory conditions, symptomatic brain/spinal metastases, prior HER3 antibodies/topoisomerase I ADCs, other systemic therapies beyond EGFR TKIs in metastatic setting, active HBV/HCV/HIV, or secondary malignancies (excluding cured non-melanoma skin/cervical cancers). Chronic steroids >10 mg prednisone/day or leptomeningeal disease are excluded. Cardiovascular instability and clinically significant corneal disease also preclude participation.    Click to Show/Hide
Administration Dosage	Participants who will be randomized to receive patritumab deruxtecan (HER3-DXd) 5.6 mg/kg q3W.
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NCT Number	NCT05338970	Clinical Status	PHASE3
Clinical Description	A Phase 3, Randomized, Open-label Study of Patritumab Deruxtecan Versus Platinum-based Chemotherapy in Metastatic or Locally Advanced Epidermal Growth Factor Receptor-mutated (EGFRm) Non-small Cell Lung Cancer (NSCLC) After Failure of Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor (TKI) Therapy (HERTHENA-Lung02)
Primary Endpoint	The primary endpoint is Progression-Free Survival (PFS) per BICR, measured from randomization to first documented disease progression or death (up to ~49 months). Secondary efficacy outcomes include Overall Survival (OS), PFS by investigator/local practice, Objective Response Rate (CR+PR), Duration of Response (time from first response to progression/death), and Clinical/Disease Control Rates (CR+PR±SD). Intracranial PFS will be assessed by BICR per CNS-RECIST in patients with baseline CNS lesions. Patient-reported outcomes include NSCLC symptom burden (NSCLC-SAQ), QoL (EORTC-QLQ-C30, EQ-5D-5L), and treatment tolerability (PGI scales). Safety will evaluate TEAEs (CTCAE v5.0) and immunogenicity (ADA incidence).    Click to Show/Hide
Other Endpoint	Eligible patients must be ≥18 years with confirmed metastatic/locally advanced non-squamous EGFR-mutant NSCLC (exon 19del/L858R) progressing after 1-2 prior EGFR TKIs (including 3rd-gen TKI). Prior neoadjuvant/adjuvant therapy is allowed if recurrence occurred >12 months post-treatment. Patients must have ≥1 measurable lesion per RECIST v1.1, ECOG 0-1, and adequate organ function (platelets ≥100K/mm 3, ANC ≥1500/mm 3, Hb ≥9 g/dL, CrCl ≥45 mL/min, liver enzymes ≤3×ULN). Archival/fresh tumor tissue is required.    Click to Show/Hide
Experiment 19 Reporting the Activity Date of This ADC					[22]
Patients Enrolled	Eligible participants include adults (&ge;18) with locally advanced/metastatic NRG1 fusion-positive solid tumors, measurable lesions per RECIST v1.1, ECOG PS 0-1, and adequate organ function. Key exclusions involve interstitial lung disease, uncontrolled cardiovascular conditions, active hepatitis B/C, unresolved prior toxicities, certain recent treatments, and other active malignancies.    Click to Show/Hide
Administration Dosage	Patritumab deruxtecan will be administered as an IV infusion Q3W on Day 1 of each 21-day cycle as a fixed dose regimen of 5.6 mg/kg Q3W.
Related Clinical Trial
NCT Number	NCT06383884	Clinical Status	PHASE2
Clinical Description	An Open Label, Phase 2 Basket Study of Patritumab Deruxtecan in Patients with Solid Tumor Harboring an NRG1 Fusion
Primary Endpoint	The primary endpoint is objective response rate (ORR) assessed per RECIST v1.1 at 12 months post-enrollment.
Other Endpoint	Secondary endpoints evaluate efficacy and safety up to 30 months, including duration of response (DoR), progression-free survival (PFS), disease-control rate (DCR), tumor size changes (SoD), and overall survival (OS) as per RECIST v1.1 criteria.
Experiment 20 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Objective Response Rate (ORR)	39%
Patients Enrolled	In dose escalation phase, pts with metastatic or unresectable non-small cell lung cancer (NSCLC) with EGFR activating mutation after disease progression during/after EGFR TKI therapy; In Dose Expansion phase, pts with metastatic or unresectable NSCLC with EGFR activating mutation or squamous or non-squamous NSCLC with disease progression during/after systemic treatment for locally advanced or metastatic disease.    Click to Show/Hide
Administration Dosage	Dose of 3.20, 4.80, 5.60, 6.40, iv Q3W in Dose Escalation phase; EGFR mutant pts at 5.60 mg/kg IV, Q3W, and EGFR wild-type pts at RDE IV, Q3W, in Dose Expansion phase.
Related Clinical Trial
NCT Number	NCT03260491	Clinical Status	Phase 1
Clinical Description	A multicenter, open-label phase 1 study of U3-1402 in subjects with metastatic or unresectable non-small cell lung cancer.
Primary Endpoint	The confirmed ORR by blinded independent central review (BICR) was 39.00% [95% confidence interval (CI), 26.00-52.40] in patients who received HER3-DXd at a dose of 5.60 mg/kg i.v. once every 3 weeks. There was 1 complete response (CR) and 21 partial responses (PR); 19 patients had stable disease (SD) as a best response.
Other Endpoint	At a median follow-up of 10.20 months, median PFS was 8.20 (95% CI, 4.40-8.30) months (16 of 57 patients were ongoing without events), and the median OS was not reached at the time of data cutoff (95% CI, 9.40-NE months; 35 of 57 patients were ongoing without events).

Experiment 1 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 40.30%	Negative HER3 expression (HER3-; IHC H score=1)
Method Description	Single-agent efficacy of HER3DXd in EGFR inhibitorresistant models of NSCLC. The dose was ten mg/kg HER3DXd or IgG control, weekly.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: DFCI-306)
Experiment 2 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.30%	High HER3 expression (HER3+++; IHC H score=202)
Method Description	Single-agent efficacy of HER3DXd in EGFR inhibitorresistant models of NSCLC. The dose was ten mg/kg HER3DXd or IgG control, weekly.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: DFCI-259)
Experiment 3 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.20%	Moderate HER3 expression (HER3++; IHC H score=181)
Method Description	Single-agent efficacy of HER3DXd in EGFR inhibitorresistant models of NSCLC. The dose was ten mg/kg HER3DXd or IgG control, weekly.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: DFCI-161)
Experiment 4 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.20%	High HER3 expression (HER3+++; IHC H score=248)
Method Description	Single-agent efficacy of HER3DXd in EGFR inhibitorresistant models of NSCLC. The dose was ten mg/kg HER3DXd or IgG control, weekly.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: DFCI-284)

Experiment 1 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.50%	Positive HER3 expression (HER3 +++/++)
Method Description	U3-1402 (30 mg/kg body weight in 200 uL ABS, weekly), ABS (200 L, weekly; vehicle), anti-PD-1 antibody (10 mg/kg body weight in 200 L PBS, twice a week), or a combination of U3-1402 and anti-PD-1 were received intraperitoneal injections.
In Vivo Model	B16-F10 CDX model
In Vitro Model	Mouse melanoma	B16-F10 cells		CVCL_0159
Experiment 2 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.10%	Positive HER3 expression (HER3+++/++)
Method Description	U3-1402 (6 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of breast cancer cell line MDA-MB-453 with HER2 expression with high expression.
In Vivo Model	MDA-MB-453 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Ref 1	Population Pharmacokinetics of Patritumab Deruxtecan in Patients With Solid Tumors
Ref 2	Patritumab Deruxtecan (HER3-DXd), a Human Epidermal Growth Factor Receptor 3-Directed Antibody-Drug Conjugate, in Patients With Previously Treated Human Epidermal Growth Factor Receptor 3-Expressing Metastatic Breast Cancer: A Multicenter, Phase I/II Trial
Ref 3	Efficacy and Safety of Patritumab Deruxtecan (HER3-DXd) in EGFR Inhibitor-Resistant, EGFR-Mutated Non-Small Cell Lung Cancer
Ref 4	U3-1402 in Metastatic or Unresectable Non-Small Cell Lung Cancer
Ref 5	HERTHENA-Lung01: Patritumab Deruxtecan in Subjects With Metastatic or Locally Advanced EGFR-mutated Non-Small Cell Lung Cancer
Ref 6	Phase I/II Study of U3-1402 in Subjects With Human Epidermal Growth Factor Receptor 3 (HER3) Positive Metastatic Breast Cancer
Ref 7	NeoadjuVAnt muLti-agENT Chemotherapy or Patritumab Deruxtecan With or Without endocrINE Therapy for High-risk HR+/HER2- Breast Cancer - VALENTINE Trial
Ref 8	Dose-Expansion Modular Study To Explore the Safety, Tolerability, and Anti-tumor Activity of HER3- DXd Monotherapy and Combinations in Patients With Inoperable Advanced Breast Cancer (ABC) After Progression on T-DXd
Ref 9	Study of Patritumab Deruxtecan With Other Anticancer Agents in Participants With HER2 Positive Breast Cancer That Has Spread and Cannot Be Surgically Removed (MK-1022-009)
Ref 10	Study of Patritumab Deruxtecan Plus Pembrolizumab With Other Anticancer Agents in Participants With High-Risk Early-Stage Triple-Negative or Hormone Receptor-Low Positive/HER-2 Negative Breast Cancer (MK-1022-010, HERTHENA-Breast-03)
Ref 11	A Window-of-opportunity Study of U3-1402, a HER3-targeting Antibody-drug Conjugate in Operable Breast Cancer According to ERBB3 Expression
Ref 12	A Study of U3-1402 (Patritumab Deruxtecan) in Subjects with Metastatic Breast Cancer
Ref 13	Patritumab Deruxtecan (U3-1402) in Unresectable Locally Advanced or Metastatic Breast Cancer
Ref 14	A Study of HER3-DXd in Subjects With Locally Advanced or Metastatic Solid Tumors
Ref 15	A Study to Evaluate U3-1402 in Subjects With Advanced or Metastatic Colorectal Cancer
Ref 16	Study of Patritumab Deruxtecan in Participants With Gastrointestinal Cancers (MK-1022-011)
Ref 17	KEYMAKER-U01 Substudy 01A: Efficacy and Safety Study of Pembrolizumab (MK-3475) With or Without Chemotherapy When Used With Investigational Agents in Treatment-naïve Participants With Stage IV Non-small Cell Lung Cancer (NSCLC) (MK-3475-01A/KEYMAKER-U01A)
Ref 18	HER3-DXd (Patritumab Deruxtecan; U3-1402) in Combination With Osimertinib in Subjects With Locally Advanced or Metastatic EGFR-mutated Non-Small Cell Lung Cancer
Ref 19	Medical Access Program for Patritumab Deruxtecan
Ref 20	A Study of Pembrolizumab With or Without Chemotherapy in Combination With Additional Treatments for Advanced Non-Small Cell Lung Cancer (NSCLC) (MK-3475-01G/KEYMAKER U01)
Ref 21	HERTHENA-Lung02: A Study of Patritumab Deruxtecan Versus Platinum-based Chemotherapy in Metastatic or Locally Advanced EGFRm NSCLC After Failure of EGFR TKI Therapy
Ref 22	Patritumab Deruxtecan in Patients with Solid Tumor Harboring an NRG1 Fusion
Ref 23	Efficacy and Safety of Patritumab Deruxtecan (HER3-DXd) in EGFR Inhibitor-Resistant, EGFR-Mutated Non-Small Cell Lung Cancer. Cancer Discov. 2022 Jan;12(1):74-89.
Ref 24	EGFR Inhibition Enhances the Cellular Uptake and Antitumor-Activity of the HER3 Antibody-Drug Conjugate HER3-DXd. Cancer Res. 2022 Jan 1;82(1):130-141.
Ref 25	Two drugs for advanced HER2-positive breast cancer (Enhertu and Tukysa). Med Lett Drugs Ther. 2020 Nov 16;62(1611):182-184.
Ref 26	A Novel HER3-Targeting Antibody-Drug Conjugate, U3-1402, Exhibits Potent Therapeutic Efficacy through the Delivery of Cytotoxic Payload by Efficient Internalization. Clin Cancer Res. 2019 Dec 1;25(23):7151-7161. doi: 10.1158/1078-0432.CCR-19-1745. Epub 2019 Aug 30.