Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0KSNKZ
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| ADC Name |
US11147852B2 5T4-V422C 1.37
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| Synonyms |
5T4-V422C
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| Organization |
PFIZER INC.
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
1.37
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| Structure |
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| Antibody Name |
undisclosed
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| Antigen Name |
Trophoblast glycoprotein (TPBG)
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Antigen Info | ||||
| Payload Name |
Undisclosed
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| Therapeutic Target |
Stimulator of interferon genes protein (STING1)
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Target Info | ||||
| Linker Name |
Undisclosed
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| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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| Combination Type |
McMMAD
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General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Maximum Observed Concentration (Cmax) | 70.2 | ug/mL |
A study was conducted to determine the pharmacokinetic parameters of human anti-5T4 antibody comprising a wild type IgG1 Fe region and human cys mutant anti-5T4 antibody site specifically conjugated to a payload (ADC) in female nu/nu mice (non tumor bearing) given a single 3 mg/kg IV dose of either 5T4 antibody alone, 5T4-mcM
MAD ADC (conventional cys-conjugation) or various 5T4 cys-mutant mcMMAD ADCs.
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|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6740 | ug*h/mL |
A study was conducted to determine the pharmacokinetic parameters of human anti-5T4 antibody comprising a wild type IgG1 Fe region and human cys mutant anti-5T4 antibody site specifically conjugated to a payload (ADC) in female nu/nu mice (non tumor bearing) given a single 3 mg/kg IV dose of either 5T4 antibody alone, 5T4-mcM
MAD ADC (conventional cys-conjugation) or various 5T4 cys-mutant mcMMAD ADCs.
Click to Show/Hide
|
[1] |
| Maximum Observed Concentration (Cmax) | 78.5 | ug/mL |
A study was conducted to determine the pharmacokinetic parameters of human anti-5T4 antibody comprising a wild type IgG1 Fe region and human cys mutant anti-5T4 antibody site specifically conjugated to a payload (ADC) in female nu/nu mice (non tumor bearing) given a single 3 mg/kg IV dose of either 5T4 antibody alone, 5T4-mcM
MAD ADC (conventional cys-conjugation) or various 5T4 cys-mutant mcMMAD ADCs.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 5440 | ug*h/mL |
A study was conducted to determine the pharmacokinetic parameters of human anti-5T4 antibody comprising a wild type IgG1 Fe region and human cys mutant anti-5T4 antibody site specifically conjugated to a payload (ADC) in female nu/nu mice (non tumor bearing) given a single 3 mg/kg IV dose of either 5T4 antibody alone, 5T4-mcM
MAD ADC (conventional cys-conjugation) or various 5T4 cys-mutant mcMMAD ADCs.
Click to Show/Hide
|
[1] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 6740 | ug*h/mL |
A study was conducted to determine the pharmacokinetic parameters of human anti-5T4 antibody comprising a wild type IgG1 Fe region and human cys mutant anti-5T4 antibody site specifically conjugated to a payload (ADC) in female nu/nu mice (non tumor bearing) given a single 3 mg/kg IV dose of either 5T4 antibody alone, 5T4-mcM
MAD ADC (conventional cys-conjugation) or various 5T4 cys-mutant mcMMAD ADCs.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 5440 | ug*h/mL |
A study was conducted to determine the pharmacokinetic parameters of human anti-5T4 antibody comprising a wild type IgG1 Fe region and human cys mutant anti-5T4 antibody site specifically conjugated to a payload (ADC) in female nu/nu mice (non tumor bearing) given a single 3 mg/kg IV dose of either 5T4 antibody alone, 5T4-mcM
MAD ADC (conventional cys-conjugation) or various 5T4 cys-mutant mcMMAD ADCs.
Click to Show/Hide
|
[1] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 6740 | ug*h/mL |
A study was conducted to determine the pharmacokinetic parameters of human anti-5T4 antibody comprising a wild type IgG1 Fe region and human cys mutant anti-5T4 antibody site specifically conjugated to a payload (ADC) in female nu/nu mice (non tumor bearing) given a single 3 mg/kg IV dose of either 5T4 antibody alone, 5T4-mcM
MAD ADC (conventional cys-conjugation) or various 5T4 cys-mutant mcMMAD ADCs.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 5440 | ug*h/mL |
A study was conducted to determine the pharmacokinetic parameters of human anti-5T4 antibody comprising a wild type IgG1 Fe region and human cys mutant anti-5T4 antibody site specifically conjugated to a payload (ADC) in female nu/nu mice (non tumor bearing) given a single 3 mg/kg IV dose of either 5T4 antibody alone, 5T4-mcM
MAD ADC (conventional cys-conjugation) or various 5T4 cys-mutant mcMMAD ADCs.
Click to Show/Hide
|
[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 6740 | ug*h/mL |
A study was conducted to determine the pharmacokinetic parameters of human anti-5T4 antibody comprising a wild type IgG1 Fe region and human cys mutant anti-5T4 antibody site specifically conjugated to a payload (ADC) in female nu/nu mice (non tumor bearing) given a single 3 mg/kg IV dose of either 5T4 antibody alone, 5T4-mcM
MAD ADC (conventional cys-conjugation) or various 5T4 cys-mutant mcMMAD ADCs.
Click to Show/Hide
|
[1] |
| Clearance (CL) | 0.46 | mL/h/kg |
A study was conducted to determine the pharmacokinetic parameters of human anti-5T4 antibody comprising a wild type IgG1 Fe region and human cys mutant anti-5T4 antibody site specifically conjugated to a payload (ADC) in female nu/nu mice (non tumor bearing) given a single 3 mg/kg IV dose of either 5T4 antibody alone, 5T4-mcM
MAD ADC (conventional cys-conjugation) or various 5T4 cys-mutant mcMMAD ADCs.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 5440 | ug*h/mL |
A study was conducted to determine the pharmacokinetic parameters of human anti-5T4 antibody comprising a wild type IgG1 Fe region and human cys mutant anti-5T4 antibody site specifically conjugated to a payload (ADC) in female nu/nu mice (non tumor bearing) given a single 3 mg/kg IV dose of either 5T4 antibody alone, 5T4-mcM
MAD ADC (conventional cys-conjugation) or various 5T4 cys-mutant mcMMAD ADCs.
Click to Show/Hide
|
[1] |
| Clearance (CL) | 0.56 | mL/h/kg |
A study was conducted to determine the pharmacokinetic parameters of human anti-5T4 antibody comprising a wild type IgG1 Fe region and human cys mutant anti-5T4 antibody site specifically conjugated to a payload (ADC) in female nu/nu mice (non tumor bearing) given a single 3 mg/kg IV dose of either 5T4 antibody alone, 5T4-mcM
MAD ADC (conventional cys-conjugation) or various 5T4 cys-mutant mcMMAD ADCs.
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|
[1] |
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC56) | 84000 ng/ml | Negative 5T4 expression (5T4-) | ||
| Method Description |
The 5T4 Cys-mutated mcMMAD and vcMMAD ADCs were each able to inhibit the growth of the 5T4 expressing cell lines
MDAMB435/57T4 (a high 514 expressor) and MDAMB-468 (a HER2 resistant cell line with moderate 5T4 expression).
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| In Vitro Model | EBV-related Burkitt lymphoma | Raji cells | CVCL_0511 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 15 ng/ml | Positive 5T4 expression (5T4+++/++) | ||
| Method Description |
The 5T4 Cys-mutated mcMMAD and vcMMAD ADCs were each able to inhibit the growth of the 5T4 expressing cell lines
MDAMB435/57T4 (a high 514 expressor) and MDAMB-468 (a HER2 resistant cell line with moderate 5T4 expression).
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| In Vitro Model | Amelanotic melanoma | MDA?MB?435 cells (5t4+) | CVCL_0417 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 270 ng/ml | Positive 5T4 expression (5T4+++/++) | ||
| Method Description |
The 5T4 Cys-mutated mcMMAD and vcMMAD ADCs were each able to inhibit the growth of the 5T4 expressing cell lines
MDAMB435/57T4 (a high 514 expressor) and MDAMB-468 (a HER2 resistant cell line with moderate 5T4 expression).
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| In Vitro Model | Amelanotic melanoma | MDA?MB?435 cells (5t4+) | CVCL_0417 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 36000 ng/ml | Positive 5T4 expression (5T4+++/++) | ||
| Method Description |
The 5T4 Cys-mutated mcMMAD and vcMMAD ADCs were each able to inhibit the growth of the 5T4 expressing cell lines
MDAMB435/57T4 (a high 514 expressor) and MDAMB-468 (a HER2 resistant cell line with moderate 5T4 expression).
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
References