Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0UQTJG
ADC Name	Lifastuzumab vedotin
Synonyms	lifastuzumab vedotin; RG7599; DNIB0600A; RO5541081 Click to Show/Hide
Organization	Roche (Top20 MNC) (Originator)
Drug Status	Phase 2 (discontinued)
Drug-to-Antibody Ratio	3 to 4
Structure
		2D MOL
Antibody Name	Lifastuzumab		Antibody Info
Antigen Name
Payload Name	MMAE		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	Mc-Val-Cit-PABC		Linker Info
Conjugate Type	Random Cysteines
Combination Type	vedotin

The indication landscape of This ADC(2027 Update)

The clinical trial pipeline of This ADC(2027 Update)

Indication

Phase 1

Phase 1/2

Phase 2

Phase 2/3

Phase 3

New Drug Application

Approved

Lung cancer

1 Trials

Trial ID
NCT01363947; EudraCT2014-000527-25

Ovarian cancer

1 Trials

Trial ID
NCT01363947; EudraCT2014-000527-25

1 Trials

Trial ID
NCT01991210; EudraCT2012-005776-34

General Information of The ADMET Data Related to This ADC(2027 Update)

Absorption

Click To Hide/Show 32 Absorption Data Related to This Level

Standard Type	Value	Units	Description	Reference
Maximum Observed Concentration (C_max)	530	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma:LIFA 1.2 mg/kg + carboplatin (n=4) .	[1]
Maximum Observed Concentration (C_max)	687	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma:LIFA 1.8 mg/kg + carboplatin (n=5) .	[1]
Maximum Observed Concentration (C_max)	1130	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg + carboplatin (n=7) .	[1]
Maximum Observed Concentration (C_max)	945	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg, 1.8 mg/kg + carboplatin (n=11) .	[1]
Maximum Observed Concentration (C_max)	1050	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg + carboplatin + bevacizumab (n=12) .	[1]
Area Under the Concentration-Time Curve (AUC)	1650	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma:LIFA 1.2 mg/kg + carboplatin (n=4), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	2250	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma:LIFA 1.8 mg/kg + carboplatin (n=5), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	3530	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg + carboplatin (n=7), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	3230	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg, 1.8 mg/kg + carboplatin (n=11), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	3510	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg + carboplatin + bevacizumab (n=12), AUCinf.	[1]
Maximum Observed Concentration (C_max)	855	ng/mL	Exposure and Pharmacokinetics of Analytesof acMMAE.	[2]
Area Under the Concentration-Time Curve (AUC)	2685	ng*day/mL	Exposure and Pharmacokinetics of Analytesof acMMAE, AUCinf.	[2]
Maximum Observed Concentration (C_max)	70.6	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 1, 0.2 mg/kg. (n=3)	[3]
Maximum Observed Concentration (C_max)	136	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 2, 0.4 mg/kg. (n=3)	[3]
Maximum Observed Concentration (C_max)	291	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 3, 0.7 mg/kg. (n=3)	[3]
Maximum Observed Concentration (C_max)	469	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 4, 1.2 mg/kg. (n=3)	[3]
Maximum Observed Concentration (C_max)	691	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 5, 1.8 mg/kg. (n=3)	[3]
Maximum Observed Concentration (C_max)	831	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 6, 2.4 mg/kg. (n=3)	[3]
Maximum Observed Concentration (C_max)	1050	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 7, 2.8 mg/kg. (n=3)	[3]
Maximum Observed Concentration (C_max)	996	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 8, 2.4 mg/kg. (n=15)	[3]
Maximum Observed Concentration (C_max)	904	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 9, 2.4 mg/kg. (n=30)	[3]
Maximum Observed Concentration (C_max)	837	ng/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 10, 2.4 mg/kg. (n=4)	[3]
Area Under the Concentration-Time Curve (AUC)	145	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 1, 0.2 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	249	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 2, 0.4 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	590	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 3, 0.7 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	1120	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 4, 1.2 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	1610	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 5, 1.8 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	1990	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 6, 2.4 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	2790	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 7, 2.8 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	2560	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 8, 2.4 mg/kg, AUCinf. (n=15)	[3]
Area Under the Concentration-Time Curve (AUC)	2240	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 9, 2.4 mg/kg, AUCinf. (n=30)	[3]
Area Under the Concentration-Time Curve (AUC)	2580	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 10, 2.4 mg/kg, AUCinf. (n=4)	[3]

Distribution

Click To Hide/Show 32 Distribution Data Related to This Level

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	1650	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma:LIFA 1.2 mg/kg + carboplatin (n=4), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	2250	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma:LIFA 1.8 mg/kg + carboplatin (n=5), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	3530	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg + carboplatin (n=7), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	3230	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg, 1.8 mg/kg + carboplatin (n=11), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	3510	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg + carboplatin + bevacizumab (n=12), AUCinf.	[1]
Volume of Distribution (V_d)	56.27	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma:LIFA 1.2 mg/kg + carboplatin (n=4) .	[1]
Volume of Distribution (V_d)	56.79	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma:LIFA 1.8 mg/kg + carboplatin (n=5) .	[1]
Volume of Distribution (V_d)	48.53	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg + carboplatin (n=7) .	[1]
Volume of Distribution (V_d)	59.88	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg, 1.8 mg/kg + carboplatin (n=11) .	[1]
Volume of Distribution (V_d)	58.33	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg + carboplatin + bevacizumab (n=12) .	[1]
Area Under the Concentration-Time Curve (AUC)	2685	ng*day/mL	Exposure and Pharmacokinetics of Analytesof acMMAE, AUCinf.	[2]
Volume of Distribution (V_d)	70	mL/kg	Exposure and Pharmacokinetics of Analytesof acMMAE.	[2]
Area Under the Concentration-Time Curve (AUC)	145	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 1, 0.2 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	249	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 2, 0.4 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	590	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 3, 0.7 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	1120	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 4, 1.2 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	1610	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 5, 1.8 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	1990	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 6, 2.4 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	2790	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 7, 2.8 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	2560	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 8, 2.4 mg/kg, AUCinf. (n=15)	[3]
Area Under the Concentration-Time Curve (AUC)	2240	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 9, 2.4 mg/kg, AUCinf. (n=30)	[3]
Area Under the Concentration-Time Curve (AUC)	2580	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 10, 2.4 mg/kg, AUCinf. (n=4)	[3]
Volume of Distribution (V_d)	112.91	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 1, 0.2 mg/kg. (n=3)	[3]
Volume of Distribution (V_d)	96.07	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 2, 0.4 mg/kg. (n=3)	[3]
Volume of Distribution (V_d)	71.05	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 3, 0.7 mg/kg. (n=3)	[3]
Volume of Distribution (V_d)	77.18	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 4, 1.2 mg/kg. (n=3)	[3]
Volume of Distribution (V_d)	86.37	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 5, 1.8 mg/kg. (n=3)	[3]
Volume of Distribution (V_d)	115.85	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 6, 2.4 mg/kg. (n=3)	[3]
Volume of Distribution (V_d)	97.62	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 7, 2.8 mg/kg. (n=3)	[3]
Volume of Distribution (V_d)	79.91	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 8, 2.4 mg/kg. (n=15)	[3]
Volume of Distribution (V_d)	93.86	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 9, 2.4 mg/kg. (n=30)	[3]
Volume of Distribution (V_d)	85.25	mL/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 10, 2.4 mg/kg. (n=4)	[3]

Metabolism

Click To Hide/Show 16 Metabolism Data Related to This Level

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	1650	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma:LIFA 1.2 mg/kg + carboplatin (n=4), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	2250	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma:LIFA 1.8 mg/kg + carboplatin (n=5), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	3530	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg + carboplatin (n=7), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	3230	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg, 1.8 mg/kg + carboplatin (n=11), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	3510	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg + carboplatin + bevacizumab (n=12), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	2685	ng*day/mL	Exposure and Pharmacokinetics of Analytesof acMMAE, AUCinf.	[2]
Area Under the Concentration-Time Curve (AUC)	145	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 1, 0.2 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	249	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 2, 0.4 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	590	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 3, 0.7 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	1120	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 4, 1.2 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	1610	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 5, 1.8 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	1990	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 6, 2.4 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	2790	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 7, 2.8 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	2560	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 8, 2.4 mg/kg, AUCinf. (n=15)	[3]
Area Under the Concentration-Time Curve (AUC)	2240	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 9, 2.4 mg/kg, AUCinf. (n=30)	[3]
Area Under the Concentration-Time Curve (AUC)	2580	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 10, 2.4 mg/kg, AUCinf. (n=4)	[3]

Excretion

Click To Hide/Show 43 Excretion Data Related to This Level

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	1650	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma:LIFA 1.2 mg/kg + carboplatin (n=4), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	2250	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma:LIFA 1.8 mg/kg + carboplatin (n=5), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	3530	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg + carboplatin (n=7), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	3230	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg, 1.8 mg/kg + carboplatin (n=11), AUCinf.	[1]
Area Under the Concentration-Time Curve (AUC)	3510	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg + carboplatin + bevacizumab (n=12), AUCinf.	[1]
Elimination Half-Life (t_1/2)	5.61	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma:LIFA 1.2 mg/kg + carboplatin (n=4) .	[1]
Elimination Half-Life (t_1/2)	5.59	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma:LIFA 1.8 mg/kg + carboplatin (n=5) .	[1]
Elimination Half-Life (t_1/2)	4.71	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg + carboplatin (n=7) .	[1]
Elimination Half-Life (t_1/2)	5.04	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg, 1.8 mg/kg + carboplatin (n=11) .	[1]
Elimination Half-Life (t_1/2)	5	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma: LIFA 2.4 mg/kg + carboplatin + bevacizumab (n=12) .	[1]
Area Under the Concentration-Time Curve (AUC)	2685	ng*day/mL	Exposure and Pharmacokinetics of Analytesof acMMAE, AUCinf.	[2]
Elimination Half-Life (t_1/2)	5.1	day	Exposure and Pharmacokinetics of Analytesof acMMAE.	[2]
Clearance (CL)	16	mL/kg/day	Exposure and Pharmacokinetics of Analytesof acMMAE.	[2]
Area Under the Concentration-Time Curve (AUC)	145	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 1, 0.2 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	249	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 2, 0.4 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	590	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 3, 0.7 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	1120	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 4, 1.2 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	1610	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 5, 1.8 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	1990	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 6, 2.4 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	2790	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 7, 2.8 mg/kg, AUCinf. (n=3)	[3]
Area Under the Concentration-Time Curve (AUC)	2560	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 8, 2.4 mg/kg, AUCinf. (n=15)	[3]
Area Under the Concentration-Time Curve (AUC)	2240	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 9, 2.4 mg/kg, AUCinf. (n=30)	[3]
Area Under the Concentration-Time Curve (AUC)	2580	ng*day/mL	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 10, 2.4 mg/kg, AUCinf. (n=4)	[3]
Elimination Half-Life (t_1/2)	6.11	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 1, 0.2 mg/kg. (n=3)	[3]
Elimination Half-Life (t_1/2)	4.33	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 2, 0.4 mg/kg. (n=3)	[3]
Elimination Half-Life (t_1/2)	3.77	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 3, 0.7 mg/kg. (n=3)	[3]
Elimination Half-Life (t_1/2)	4.79	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 4, 1.2 mg/kg. (n=3)	[3]
Elimination Half-Life (t_1/2)	5.88	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 5, 1.8 mg/kg. (n=3)	[3]
Elimination Half-Life (t_1/2)	6.14	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 6, 2.4 mg/kg. (n=3)	[3]
Elimination Half-Life (t_1/2)	5.52	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 7, 2.8 mg/kg. (n=3)	[3]
Elimination Half-Life (t_1/2)	5.14	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 8, 2.4 mg/kg. (n=15)	[3]
Elimination Half-Life (t_1/2)	5.48	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 9, 2.4 mg/kg. (n=30)	[3]
Elimination Half-Life (t_1/2)	6.09	day	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 10, 2.4 mg/kg. (n=4)	[3]
Clearance (CL)	24.81	mL/day/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 1, 0.2 mg/kg. (n=3)	[3]
Clearance (CL)	29.3	mL/day/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 2, 0.4 mg/kg. (n=3)	[3]
Clearance (CL)	22.65	mL/day/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 3, 0.7 mg/kg. (n=3)	[3]
Clearance (CL)	18.91	mL/day/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 4, 1.2 mg/kg. (n=3)	[3]
Clearance (CL)	20.19	mL/day/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 5, 1.8 mg/kg. (n=3)	[3]
Clearance (CL)	22.71	mL/day/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 6, 2.4 mg/kg. (n=3)	[3]
Clearance (CL)	19.73	mL/day/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 7, 2.8 mg/kg. (n=3)	[3]
Clearance (CL)	17.08	mL/day/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 8, 2.4 mg/kg. (n=15)	[3]
Clearance (CL)	19.83	mL/day/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 9, 2.4 mg/kg. (n=30)	[3]
Clearance (CL)	16.45	mL/day/kg	Mean (standard deviation) of the pharmacokinetic parameters for antibody-conjugated MMAE in plasma, Cohort 10, 2.4 mg/kg. (n=4)	[3]

General Information of The Activity Data Related to This ADC

Identified from the Human Clinical Data

Click To Hide/Show 10 Activity Data Related to This Level

Standard Type	NCT Number	Clinical Status	Clinical Trial Description
Partial Response (PR)	NCT01911598	Phase 1a	A phase 1b open-label study of the safety and pharmacokinetics of MEHD7945A in combination with either cisplatin and 5-fu or paclitaxel and carboplatin in patients with recurrent/metastatic squamous cell carcinoma of the head and neck. Click to Show/Hide
Objective Response Rate (ORR)	NCT01991210	Phase 2	A randomized, open-label, multicenter, phase 2 trial evaluating the safety and activity of DNIB0600A compared to pegylated liposomal doxorubicin administered intravenously to patients with platinum-resistant ovarian cancer. Click to Show/Hide
Objective Response Rate (ORR)	NCT01991210	Phase 2	A randomized, open-label, multicenter, phase 2 trial evaluating the safety and activity of DNIB0600A compared to pegylated liposomal doxorubicin administered intravenously to patients with platinum-resistant ovarian cancer. Click to Show/Hide
Objective Response Rate (ORR)	NCT01363947	Phase 1	A phase 1, open-label study of the safety and pharmacokinetics of escalating doses of DNIB0600A in patients with non-small cell lung cancer and platinum-resistant ovarian cancer.
Complete Remission (CR)	NCT01995188	Phase 1b	A phase 1b, open-label, dose-escalation study of the safety and pharmacology of DNIB0600A in combination with carboplatin (with or without bevacizumab) in patients with platinum-sensitive ovarian cancer or non-squamous non-small cell lung cancer. Click to Show/Hide
Undisclosed	NCT01995188	Phase 1	A phase 1b, open-label, dose-escalation study of the safety and pharmacology of DNIB0600A in combination with carboplatin (with or without bevacizumab) in patients with platinum-sensitive ovarian cancer or non-squamous non-small cell lung cancer. Click to Show/Hide
Progression Free Survival	NCT01995188	PHASE1	A Phase Ib, Open-Label, Dose-Escalation Study of the Safety and Pharmacology of DNIB0600A in Combination With Carboplatin (With or Without Bevacizumab) in Patients With Platinum-Sensitive Ovarian Cancer or Non-Squamous Non-small Cell Lung Cancer Click to Show/Hide
Objective Response Rate (ORR)	NCT01991210	PHASE2	A Randomized, Open-Label, Multicenter, Phase II Trial Evaluating the Safety and Activity of DNIB0600A Compared to Pegylated Liposomal Doxorubicin Administered Intravenously to Patients With Platinum-Resistant Ovarian Cancer Click to Show/Hide
Objective Response Rate (ORR)	NCT01995188	PHASE1	A Phase Ib, Open-Label, Dose-Escalation Study of the Safety and Pharmacology of DNIB0600A in Combination With Carboplatin (With or Without Bevacizumab) in Patients With Platinum-Sensitive Ovarian Cancer or Non-Squamous Non-small Cell Lung Cancer Click to Show/Hide
Undisclosed	NCT01363947	PHASE1	A Phase I, Open-Label Study of the Safety and Pharmacokinetics of Escalating Doses of DNIB0600A in Patients With Non-Small Cell Lung Cancer and Platinum-Resistant Ovarian Cancer

Discovered Using Patient-derived Xenograft Model

Click To Hide/Show 6 Activity Data Related to This Level

Standard Type	Value	Units	Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI)	≈ 19.6	%	Non-small cell lung cancer PDX model (PDX: CTG-0860)
Tumor Growth Inhibition value (TGI)	≈ 25.4	%	Lung cancer PDX model (PDX: CTG-0178)
Tumor Growth Inhibition value (TGI)	≈ 27.6	%	Lung cancer PDX model (PDX: CTG-0178)
Tumor Growth Inhibition value (TGI)	≈ 59.3	%	Lung cancer PDX model (PDX: CTG-0852)
Tumor Growth Inhibition value (TGI)	≈ 62.7	%	Lung cancer PDX model (PDX: CTG-0852)
Tumor Growth Inhibition value (TGI)	≈ 62.8	%	Lung cancer PDX model (PDX: CTG-0852)

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 41.2	%	OVCAR-3 cells	Ovarian serous adenocarcinoma

Full List of Activity Data of This Antibody-drug Conjugate

Identified from the Human Clinical Data

Click To Hide/Show 10 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[4]
Efficacy Data	Partial Response (PR)	7.84 45.83 25.00 6.67 %
Patients Enrolled	Incurable, locally advanced, or metastatic disease (non-squamous NSCLC or non-mucinous PROC) that had progressed on or following prior chemotherapy and for which no standard therapy existed, Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1.
Administration Dosage	The starting dose for LIFA was 0.20 mg/kg administered by intravenous infusion (IV) every 3 weeks (Q3W), in this 3+3 dose-escalation design, followed by cohort expansion at the recommended phase II dose (RP2D).
*Related Clinical Trial*
NCT Number	NCT01911598	Clinical Status	Phase 1a
Clinical Description	A phase 1b open-label study of the safety and pharmacokinetics of MEHD7945A in combination with either cisplatin and 5-fu or paclitaxel and carboplatin in patients with recurrent/metastatic squamous cell carcinoma of the head and neck.
Primary Endpoint	The MTD was not reached on this study and the maximum administered dose (MAD) was 2.80 mg/kg. Upon evaluation of the safety data of the 6 patients treated at the MAD, the dose of 2.40 mg/kg was established as the RP2D.
Other Endpoint	At active doses 1.80 mg/kg, partial responses were observed in four of 51 (7.84%) patients with NSCLC and 11 of 24 (45.83%) patients. In the NSCLC cohorts, PRs were seen in 1 of 4 (25.00%) at 1.80 mg/kg and in 3 of 45 (6.67%) patients at 2.40 mg/kg, mDoR=161 days. In PROC, PRs were seen at 1.80 mg/kg in one of two (50.00%), at 2.40 mg/kg in seven of 18 (38.89%), and at 2.80 mg/kg in three of four (75.00%) patients; mDoR=342 days. Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC				[5]
Efficacy Data	Objective Response Rate (ORR)	34.00 36.00 %
Patients Enrolled	Platinum-resistant patients with histologically documented advanced epithelial ovarian, primary peritoneal, or fallopian tube cancer.
Administration Dosage	2.40 mg/kg, intravenously, every 3 weeks (Q3W).
*Related Clinical Trial*
NCT Number	NCT01991210	Clinical Status	Phase 2
Clinical Description	A randomized, open-label, multicenter, phase 2 trial evaluating the safety and activity of DNIB0600A compared to pegylated liposomal doxorubicin administered intravenously to patients with platinum-resistant ovarian cancer.
Experiment 3 Reporting the Activity Date of This ADC				[6]
Efficacy Data	Objective Response Rate (ORR)	34.00 36.00 %
Patients Enrolled	Advanced epithelial ovarian, primary peritoneal, or fallopian tube cancer that had progressed or relapsed within 6months of the most recent treatment with a platinum-containing chemotherapy regimen and for whom PLD was considered an appropriate therapy.
Administration Dosage	2.40 mg/kg, intravenously, every 3 weeks (Q3W).
*Related Clinical Trial*
NCT Number	NCT01991210	Clinical Status	Phase 2
Clinical Description	A randomized, open-label, multicenter, phase 2 trial evaluating the safety and activity of DNIB0600A compared to pegylated liposomal doxorubicin administered intravenously to patients with platinum-resistant ovarian cancer.
Primary Endpoint	The stratified PFS hazard ratio was 0.78 (95% CI,0.46-1.31; p=0.34) with a median PFS of 5.30 vs. 3.10 months (LIFA vs. PLD arm,respectively) in the ITT population, and 0.71 (95% CI,0.40-1.26; p=0.24) with a median PFS of 5.30 vs. 3.40 months (LIFA vs. PLD arm,respectively) in NaPi2bxhigh patients. The objective response rate (ORR) was 34.00% (95% CI,22.00-49.00%,LIFA) vs. 15.00% (95% CI, 7.00-28.00%,PLD) in the ITT population (p=0.03), and 36.00% (95% CI, 22.00-52.00%,LIFA) vs.14.00% (95% CI,6.00-27.00%,PLD) in NaPi2bxhigh patients (p=0.02). Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC				[7]
Efficacy Data	Objective Response Rate (ORR)	25.00 7.00 50.00 39.00 75.00 %
Patients Enrolled	Patients with nonsmall cell lung cancer (NSCLC) and platinum-resistant ovarian cancer (PROC).
Administration Dosage	Dose-escalation: 0.20-2.80 mg/kg once every 3 weeks, dose-expansion: 4 mg/kg once every 3 weeks.
*Related Clinical Trial*
NCT Number	NCT01363947	Clinical Status	Phase 1
Clinical Description	A phase 1, open-label study of the safety and pharmacokinetics of escalating doses of DNIB0600A in patients with non-small cell lung cancer and platinum-resistant ovarian cancer.
Experiment 5 Reporting the Activity Date of This ADC				[8]
Efficacy Data	Complete Remission (CR)	58.54%
Patients Enrolled	Polycystic ovary syndrome (PSOC) patients (epithelial ovarian cancer, primary peritoneal cancer, or fallopian tube cancer) with documented radiographic progression or relapse according to RECIST v1.1.
Administration Dosage	The starting dose of LIFA was 1.20 mg/kg, once every 3 weeks (Q3W) on the first day of 21-day cycles, traditional 3 + 3 study design.
*Related Clinical Trial*
NCT Number	NCT01995188	Clinical Status	Phase 1b
Clinical Description	A phase 1b, open-label, dose-escalation study of the safety and pharmacology of DNIB0600A in combination with carboplatin (with or without bevacizumab) in patients with platinum-sensitive ovarian cancer or non-squamous non-small cell lung cancer.
Primary Endpoint	The median duration of progression-free survival was 10.71 months (95% CI: 8.54,13.86) with confirmed complete/partial responses in 24 (58.54%) patients.
Other Endpoint	The maximum tolerated dose was not reached. The recommended phase 2 dose (RP2D) was LIFA 2.40 mg/kg + carboplatin AUC6 (cycles 16), with or without bevacizumab 15 mg/kg.
Experiment 6 Reporting the Activity Date of This ADC				[9]
*Related Clinical Trial*
NCT Number	NCT01995188	Clinical Status	Phase 1
Clinical Description	A phase 1b, open-label, dose-escalation study of the safety and pharmacology of DNIB0600A in combination with carboplatin (with or without bevacizumab) in patients with platinum-sensitive ovarian cancer or non-squamous non-small cell lung cancer.
Experiment 7 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Progression Free Survival	10.7 months
Patients Enrolled	Inclusion criteria: ECOG 0-1; histologically confirmed platinum-sensitive ovarian, peritoneal, or fallopian tube cancer or NSCLC with ≤2 prior regimens (additional targeted therapy permitted for EGFR/ALK mutations). NSCLC requires NaPi2b IHC 2+/3+. Exclusions: recent anti-tumor therapy/surgery, active infections, untreated CNS metastases, prior NaPi2b therapy, or specific contraindications for bevacizumab (e.g., uncontrolled hypertension, recent thrombosis). Click to Show/Hide
Administration Dosage	Patients received LIFA at 1.2, 1.8, and 2.4 mg (n = 4, 5, and 20, respectively) with carboplatin.
*Related Clinical Trial*
NCT Number	NCT01995188	Clinical Status	PHASE1
Clinical Description	A Phase Ib, Open-Label, Dose-Escalation Study of the Safety and Pharmacology of DNIB0600A in Combination With Carboplatin (With or Without Bevacizumab) in Patients With Platinum-Sensitive Ovarian Cancer or Non-Squamous Non-small Cell Lung Cancer
Primary Endpoint	The study evaluates dose-limiting toxicities (DLTs) in participants over 21 days, tracks adverse events (AEs) and serious adverse events (SAEs) from Day 1 until 30 days post-last infusion (up to ~3 years), and monitors anti-DNIB0600A antibodies at pre-infusion, specific cycles, and 30 days post-last infusion.
Other Endpoint	Pharmacokinetic parameters include AUC (0-inf), Cmax, Cmin, CL, Vss, and t1/2, measured at pre-infusion, post-infusion time points, and follow-up (up to ~3 years). Efficacy is assessed via RECIST v1.1, measuring objective response rate, duration of response, and progression-free survival (PFS) from screening until disease progression or death.
Experiment 8 Reporting the Activity Date of This ADC				[2]
Efficacy Data	Objective Response Rate (ORR)	34 15 36 14 %
Patients Enrolled	Eligible patients must have ECOG 0-1, histologically confirmed advanced ovarian, peritoneal, or fallopian tube cancer refractory to platinum therapy, ≤2 prior regimens, adequate organ function, and contraception compliance. Exclusions include prior anthracycline/NaPi2b therapy, major surgery within 4 weeks, uncontrolled comorbidities, active infections, hepatitis/HIV, CNS metastases, pregnancy, NaPi2b deficiency, or severe hypersensitivity to monoclonal antibodies. Click to Show/Hide
Administration Dosage	DNIB0600A will be administered at a dose of 2.4 mg/kg IV every 3 weeks.
*Related Clinical Trial*
NCT Number	NCT01991210	Clinical Status	PHASE2
Clinical Description	A Randomized, Open-Label, Multicenter, Phase II Trial Evaluating the Safety and Activity of DNIB0600A Compared to Pegylated Liposomal Doxorubicin Administered Intravenously to Patients With Platinum-Resistant Ovarian Cancer
Primary Endpoint	The primary endpoint is progression-free survival (PFS) based on RECIST v1.1, measured from baseline until disease progression or death within 30 days of last study drug administration, with an overall timeframe of approximately 2.5 years.
Other Endpoint	Secondary endpoints include objective response rate (ORR) and duration of response per RECIST v1.1, overall survival (OS), incidence of adverse events (AEs), and pharmacokinetic parameters such as AUC, Cmax, CL, t½, and Vss of DNIB0600A, along with anti-therapeutic antibody (ATA) formation. Assessments span from baseline up to 30 days post-treatment or longer, with detailed time points for PK analysis. Click to Show/Hide
Experiment 9 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Objective Response Rate (ORR)	59%
Patients Enrolled	Inclusion criteria: ECOG 0-1; histologically confirmed platinum-sensitive ovarian, peritoneal, or fallopian tube cancer or NSCLC with ≤2 prior regimens (additional targeted therapy permitted for EGFR/ALK mutations). NSCLC requires NaPi2b IHC 2+/3+. Exclusions: recent anti-tumor therapy/surgery, active infections, untreated CNS metastases, prior NaPi2b therapy, or specific contraindications for bevacizumab (e.g., uncontrolled hypertension, recent thrombosis). Click to Show/Hide
Administration Dosage	Patients received LIFA at 1.2, 1.8, and 2.4 mg (n = 4, 5, and 20, respectively) with carboplatin.
*Related Clinical Trial*
NCT Number	NCT01995188	Clinical Status	PHASE1
Clinical Description	A Phase Ib, Open-Label, Dose-Escalation Study of the Safety and Pharmacology of DNIB0600A in Combination With Carboplatin (With or Without Bevacizumab) in Patients With Platinum-Sensitive Ovarian Cancer or Non-Squamous Non-small Cell Lung Cancer
Primary Endpoint	The study evaluates dose-limiting toxicities (DLTs) in participants over 21 days, tracks adverse events (AEs) and serious adverse events (SAEs) from Day 1 until 30 days post-last infusion (up to ~3 years), and monitors anti-DNIB0600A antibodies at pre-infusion, specific cycles, and 30 days post-last infusion.
Other Endpoint	Pharmacokinetic parameters include AUC (0-inf), Cmax, Cmin, CL, Vss, and t1/2, measured at pre-infusion, post-infusion time points, and follow-up (up to ~3 years). Efficacy is assessed via RECIST v1.1, measuring objective response rate, duration of response, and progression-free survival (PFS) from screening until disease progression or death.
Experiment 10 Reporting the Activity Date of This ADC				[11]
Patients Enrolled	Outcomes included safety (AE incidence), pharmacokinetics (Cmax of DNIB0600A components), immunogenicity (ADA development), and efficacy (OR and DOR per RECIST v1.1). Key endpoints spanned up to 84 weeks, assessing tumor response dynamics-complete or partial shrinkage (≥30% reduction), stable disease, or progression (≥20% increase or new lesions)-while monitoring drug-related toxicities and immunologic reactions. Rigorous eligibility criteria balanced participant safety with disease relevance, excluding high-risk conditions or recent therapies to isolate investigational drug effects. Click to Show/Hide
Administration Dosage	Several dose levels will be evaluated for DNIB0600A administered via IV infusion on Day 1 of each 21-day cycle until disease progression.
*Related Clinical Trial*
NCT Number	NCT01363947	Clinical Status	PHASE1
Clinical Description	A Phase I, Open-Label Study of the Safety and Pharmacokinetics of Escalating Doses of DNIB0600A in Patients With Non-Small Cell Lung Cancer and Platinum-Resistant Ovarian Cancer
Primary Endpoint	The study assessed adverse events (AEs) over approximately 2 years, defined as any unfavorable or unintended sign, symptom, or disease temporally linked to investigational medicinal product (IMP) use, irrespective of causality. Peak concentrations (Cmax) of DNIB0600A components-acMMAE, total antibody, and unconjugated MMAE-were evaluated on Day 21, alongside the percentage of participants developing anti-drug antibodies (ADAs) over 84 weeks, measuring baseline prevalence and post-baseline incidence. Objective response (OR) per RECIST v1.1 criteria, including complete response (disappearance of target lesions) and partial response (≥30% decrease in lesion diameters), was tracked for 84 weeks, along with duration of response (DOR), stable disease, and progression criteria (≥20% increase in lesion diameters or new lesions). Click to Show/Hide
Other Endpoint	Inclusion criteria required an ECOG performance status of 0 or 1, histologic evidence of incurable locally advanced/metastatic disease (e.g., non-squamous NSCLC or platinum-resistant ovarian cancer), measurable disease, access to archival tumor samples, and contraception use for fertile participants. Exclusion criteria encompassed recent anti-tumor therapy, major surgery within 4 weeks, active infections, significant liver disease, untreated CNS metastases, oxygen dependency, uncontrolled comorbidities, and prior treatments (≤2 regimens for NSCLC expansion cohort). Pregnancy or breastfeeding also disqualified participation. Click to Show/Hide

Discovered Using Patient-derived Xenograft Model

Click To Hide/Show 6 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 19.60%	Moderate SLC34A2 expression (SLC34A2++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm³. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3. Click to Show/Hide
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0860)
Experiment 2 Reporting the Activity Date of This ADC				[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 25.40%	Moderate SLC34A2 expression (SLC34A2++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm³. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3. Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0178)
Experiment 3 Reporting the Activity Date of This ADC				[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 27.60%	Moderate SLC34A2 expression (SLC34A2++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm³. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3. Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0178)
Experiment 4 Reporting the Activity Date of This ADC				[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.30%	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm³. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3. Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0852)
Experiment 5 Reporting the Activity Date of This ADC				[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.70%	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm³. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3. Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0852)
Experiment 6 Reporting the Activity Date of This ADC				[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.80%	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm³. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3. Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0852)

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 41.20%	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm³. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg. Click to Show/Hide
In Vivo Model	Ovarian adenocarcinoma CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

References

Ref 1	Phase 1b study of anti-NaPi2b antibody-drug conjugate lifastuzumab vedotin (DNIB0600A) in patients with platinum-sensitive recurrent ovarian cancer
Ref 2	Anti-NaPi2b antibody-drug conjugate lifastuzumab vedotin (DNIB0600A) compared with pegylated liposomal doxorubicin in patients with platinum-resistant ovarian cancer in a randomized, open-label, phase II study
Ref 3	Phase Ia Study of Anti-NaPi2b Antibody-Drug Conjugate Lifastuzumab Vedotin DNIB0600A in Patients with Non-Small Cell Lung Cancer and Platinum-Resistant Ovarian Cancer
Ref 4	Phase Ia Study of Anti-NaPi2b Antibody-Drug Conjugate Lifastuzumab Vedotin DNIB0600A in Patients with Non-Small Cell Lung Cancer and Platinum-Resistant Ovarian Cancer. Clin Cancer Res. 2020 Jan 15;26(2):364-372.
Ref 5	Deka biosciences biotechnology company product pipeline.
Ref 6	Anti-NaPi2b antibody-drug conjugate lifastuzumab vedotin (DNIB0600A) compared with pegylated liposomal doxorubicin in patients with platinum-resistant ovarian cancer in a randomized, open-label, phase II study. Ann Oncol. 2018 Apr 1;29(4):917-923.
Ref 7	ADC review: basic information about LCB14-2NM.
Ref 8	Phase 1b study of anti-NaPi2b antibody-drug conjugate lifastuzumab vedotin (DNIB0600A) in patients with platinum-sensitive recurrent ovarian cancer. Gynecol Oncol. 2020 Sep;158(3):631-639.
Ref 9	A Phase Ib, Open-Label, Dose-Escalation Study of the Safety and Pharmacology of DNIB0600A in Combination With Carboplatin (With or Without Bevacizumab) in Patients With Platinum-Sensitive Ovarian Cancer or Non-Squamous Non-small Cell Lung Cancer, NCT01995188
Ref 10	The Dolaflexin-based Antibody-Drug Conjugate XMT-1536 Targets the Solid Tumor Lineage Antigen SLC34A2/NaPi2b. Mol Cancer Ther. 2021 May;20(5):896-905.
Ref 11	Safety and Pharmacokinetics of Escalating Doses of DNIB0600A in Participants With Non-Small Cell Lung Cancer (NSCLC) and Platinum Resistant Ovarian Cancer

Antibody-drug Conjugate Information

Citation

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Correspondence

Prof. Feng ZHU (zhufeng@zju.edu.cn)

Prof. Xiaowu DONG (dongxw@zju.edu.cn)

Prof. Luo FANG (fangluo@zjcc.org.cn)