Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0PBYAQ
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| ADC Name |
CN116916962A-ADC-B17
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| Synonyms |
ADC-B17
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| Organization |
TAKEDA PHARMACEUTICAL COMPANY LIMITED
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
3.8
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| Structure |
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| Antibody Name |
hIgG1
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Antibody Info | Antigen Name |
Undisclosed
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| Payload Name |
Compound No.14
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Payload Info | ||||
| Linker Name |
CN116916962A-C-38-linker
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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| Combination Type |
C-38
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General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 20400 | h*nM |
For in vivo evaluation of the ADCs in naive Balb/C mouse, female Balb/C mice at 6-8weeks of age were used.Pharmacokinetics of the ADCs (0.05mg/kg) were studied following injection of ADCs into Balb/C mice.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 14470 | h*nM |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 3mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
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|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 4092 | h*nM |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 1mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
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|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 885 | h*nM |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 0.3mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
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[1] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 20400 | h*nM |
For in vivo evaluation of the ADCs in naive Balb/C mouse, female Balb/C mice at 6-8weeks of age were used.Pharmacokinetics of the ADCs (0.05mg/kg) were studied following injection of ADCs into Balb/C mice.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 14470 | h*nM |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 3mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 4092 | h*nM |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 1mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 885 | h*nM |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 0.3mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
Click to Show/Hide
|
[1] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 20400 | h*nM |
For in vivo evaluation of the ADCs in naive Balb/C mouse, female Balb/C mice at 6-8weeks of age were used.Pharmacokinetics of the ADCs (0.05mg/kg) were studied following injection of ADCs into Balb/C mice.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 14470 | h*nM |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 3mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 4092 | h*nM |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 1mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 885 | h*nM |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 0.3mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
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|
[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Elimination Half-Life (t1/2) | 59 | h |
For in vivo evaluation of the ADCs in naive Balb/C mouse, female Balb/C mice at 6-8weeks of age were used.Pharmacokinetics of the ADCs (0.05mg/kg) were studied following injection of ADCs into Balb/C mice.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 20400 | h*nM |
For in vivo evaluation of the ADCs in naive Balb/C mouse, female Balb/C mice at 6-8weeks of age were used.Pharmacokinetics of the ADCs (0.05mg/kg) were studied following injection of ADCs into Balb/C mice.
Click to Show/Hide
|
[1] |
| Elimination Half-Life (t1/2) | 40 | h |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 3mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
Click to Show/Hide
|
[1] |
| Elimination Half-Life (t1/2) | 52 | h |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 1mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
Click to Show/Hide
|
[1] |
| Elimination Half-Life (t1/2) | 18 | h |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 0.3mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 14470 | h*nM |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 3mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 4092 | h*nM |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 1mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 885 | h*nM |
Pharmacokine ues evaluationin non-Human Prima (hecynomolgus monkey). A single dose study was performed with intravenous administration of ADC at 0.3mg/kg (2monkeys/sex/group) (proteindose). Serum samples were taken at various time points and stored frozen for analysis.
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|
[1] |
General Information of The Activity Data Related to This ADC
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 Effective Concentration (EC50) | 1.14 nM | High hCCR2 expression (hCCR2+++) | ||
| Method Description |
THP 1, 15,000cells/254uL per welld were plated at set in 384 well flat plate, in the appropriate growth media. The cell plates were dosed with 5uL of the hCCR2 targeting-ADC samples and then incubated at 37°C for 20 hours. At the end of the incubation 10uL/well of the QUANTJ-LucTM (InvivoGenftrep-qlc1) were added and luminescence was measured immediately using the LeadSeeker.
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| In Vitro Model | Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia | THP1 cells | CVCL_0006 | ||