General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0TQSIC
ADC Name
WBP301088-X2
Synonyms
WBP301088-X2
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Organization
DUALITY BIOLOGICS (SUZHOU) CO., LTD
Drug Status
Investigative
Drug-to-Antibody Ratio
5.68
Structure
Antibody Name
Anti-b7h3
 Antibody Info 
Antigen Name
CD276 antigen (CD276)
 Antigen Info 
Payload Name
Topo1 inhibitor F
 Payload Info 
Therapeutic Target
DNA topoisomerase I (TOP1)
 Target Info 
Linker Name
Mc-Gly-Gly-Phe-Gly
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
X2
General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
Click To Hide/Show 2 Absorption Data Related to This Level
Standard Type Value Units Description Reference
Maximum Observed Concentration (Cmax) 71.9 ug/mL
Blood was collected from the forelimb veins of cynomolgus monkeys in each group, and treated samples of the blood collected at 0 h before and 0.5 h, 1 h, 4 h, 8 h, 24 h, 48 h, 72 h, 96 h, 168 h, 240 h, 336 h, 504 h, and 672 h after the administration were used as PK samples.

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[1]
Area Under the Concentration-Time Curve (AUC) 2070 h*ug/mL
Blood was collected from the forelimb veins of cynomolgus monkeys in each group, and treated samples of the blood collected at 0 h before and 0.5 h, 1 h, 4 h, 8 h, 24 h, 48 h, 72 h, 96 h, 168 h, 240 h, 336 h, 504 h, and 672 h after the administration were used as PK samples.

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[1]
Distribution
Click To Hide/Show 1 Distribution Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 2070 h*ug/mL
Blood was collected from the forelimb veins of cynomolgus monkeys in each group, and treated samples of the blood collected at 0 h before and 0.5 h, 1 h, 4 h, 8 h, 24 h, 48 h, 72 h, 96 h, 168 h, 240 h, 336 h, 504 h, and 672 h after the administration were used as PK samples.

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[1]
Metabolism
Click To Hide/Show 1 Metabolism Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 2070 h*ug/mL
Blood was collected from the forelimb veins of cynomolgus monkeys in each group, and treated samples of the blood collected at 0 h before and 0.5 h, 1 h, 4 h, 8 h, 24 h, 48 h, 72 h, 96 h, 168 h, 240 h, 336 h, 504 h, and 672 h after the administration were used as PK samples.

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[1]
Excretion
Click To Hide/Show 1 Excretion Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 2070 h*ug/mL
Blood was collected from the forelimb veins of cynomolgus monkeys in each group, and treated samples of the blood collected at 0 h before and 0.5 h, 1 h, 4 h, 8 h, 24 h, 48 h, 72 h, 96 h, 168 h, 240 h, 336 h, 504 h, and 672 h after the administration were used as PK samples.

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[1]
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 10 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
4.8
nM
CVCL_1476
Lung adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
11.4
nM
CVCL_1559
Minimally invasive lung adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
52.3
nM
CVCL_0236
Lung adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
55.5
nM
CVCL_0031
Invasive breast carcinoma
Half Maximal inhibitory Concentration (lC50) 
86.5
nM
CVCL_0022
Glioblastoma
Half Maximal inhibitory Concentration (lC50) 
164.7
nM
CVCL_0132
Amelanotic melanoma
Half Maximal inhibitory Concentration (lC50) 
180.8
nM
CVCL_0035
Prostate carcinoma
Half Maximal inhibitory Concentration (lC50) 
268.8
nM
CVCL_1104
Breast carcinoma
Half Maximal inhibitory Concentration (lC50) 
369.3
nM
CVCL_0023
Lung adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
446
nM
CVCL_0320
Colon adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 10 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 4.8 nM Positive b7h3 expression (b7h3+++/++)
Method Description
Anti-B7H3 ADC WBP301088-X2 was incubated with human tumor cells that positively expressed B7H3 for 7 days, and the inhibitory effect thereof on cell proliferation was assessed through a CellTiter-Glo@ chemiluminescence cell viability assay
In Vitro Model Lung adenocarcinoma NCI-H1568 cells CVCL_1476
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 11.4 nM Positive b7h3 expression (b7h3+++/++)
Method Description
Anti-B7H3 ADC WBP301088-X2 was incubated with human tumor cells that positively expressed B7H3 for 7 days, and the inhibitory effect thereof on cell proliferation was assessed through a CellTiter-Glo@ chemiluminescence cell viability assay
In Vitro Model Minimally invasive lung adenocarcinoma NCI-H358 cells CVCL_1559
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 52.3 nM Positive b7h3 expression (b7h3+++/++)
Method Description
Anti-B7H3 ADC WBP301088-X2 was incubated with human tumor cells that positively expressed B7H3 for 7 days, and the inhibitory effect thereof on cell proliferation was assessed through a CellTiter-Glo@ chemiluminescence cell viability assay
In Vitro Model Lung adenocarcinoma Calu-6 cells CVCL_0236
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 55.5 nM Positive b7h3 expression (b7h3+++/++)
Method Description
Anti-B7H3 ADC WBP301088-X2 was incubated with human tumor cells that positively expressed B7H3 for 7 days, and the inhibitory effect thereof on cell proliferation was assessed through a CellTiter-Glo@ chemiluminescence cell viability assay
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 86.5 nM Positive b7h3 expression (b7h3+++/++)
Method Description
Anti-B7H3 ADC WBP301088-X2 was incubated with human tumor cells that positively expressed B7H3 for 7 days, and the inhibitory effect thereof on cell proliferation was assessed through a CellTiter-Glo@ chemiluminescence cell viability assay
In Vitro Model Glioblastoma U87 MG cells CVCL_0022
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 164.7 nM Positive b7h3 expression (b7h3+++/++)
Method Description
Anti-B7H3 ADC WBP301088-X2 was incubated with human tumor cells that positively expressed B7H3 for 7 days, and the inhibitory effect thereof on cell proliferation was assessed through a CellTiter-Glo@ chemiluminescence cell viability assay
In Vitro Model Amelanotic melanoma A375 cells CVCL_0132
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 180.8 nM Positive b7h3 expression (b7h3+++/++)
Method Description
Anti-B7H3 ADC WBP301088-X2 was incubated with human tumor cells that positively expressed B7H3 for 7 days, and the inhibitory effect thereof on cell proliferation was assessed through a CellTiter-Glo@ chemiluminescence cell viability assay
In Vitro Model Prostate carcinoma PC-3 cells CVCL_0035
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 268.8 nM Positive b7h3 expression (b7h3+++/++)
Method Description
Anti-B7H3 ADC WBP301088-X2 was incubated with human tumor cells that positively expressed B7H3 for 7 days, and the inhibitory effect thereof on cell proliferation was assessed through a CellTiter-Glo@ chemiluminescence cell viability assay
In Vitro Model Breast carcinoma CAL-120 cells CVCL_1104
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 369.3 nM Positive b7h3 expression (b7h3+++/++)
Method Description
Anti-B7H3 ADC WBP301088-X2 was incubated with human tumor cells that positively expressed B7H3 for 7 days, and the inhibitory effect thereof on cell proliferation was assessed through a CellTiter-Glo@ chemiluminescence cell viability assay
In Vitro Model Lung adenocarcinoma A549 cells CVCL_0023
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 446 nM Positive b7h3 expression (b7h3+++/++)
Method Description
Anti-B7H3 ADC WBP301088-X2 was incubated with human tumor cells that positively expressed B7H3 for 7 days, and the inhibitory effect thereof on cell proliferation was assessed through a CellTiter-Glo@ chemiluminescence cell viability assay
In Vitro Model Colon adenocarcinoma HT-29 cells CVCL_0320
References
Ref 1 Anti-b7h3 antibody-drug conjugate and use thereof