Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0KRMTA
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| ADC Name |
AB1380049-SG3932 (DAR8)
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| Synonyms |
AB1380049-SG3932
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| Organization |
ASTRAZENECA AB
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
8
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| Structure |
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| Antibody Name |
AB1380049
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Antibody Info | ||||
| Antigen Name |
Folate receptor alpha (FOLR1)
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Antigen Info | ||||
| Payload Name |
(4-NH2)-Exatecan
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Payload Info | ||||
| Therapeutic Target |
DNA topoisomerase I (TOP1)
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Target Info | ||||
| Linker Name |
SG3932 Linker
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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| Combination Type |
SG3932
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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) | 127.48 | ug/mL |
Wild-type SCID mice (n=3 per group) were dosed intravenously (bolus) with the exemplary anti-FRa ADCs (5 mg/kg).
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 696.25 | ug*day/mL |
Wild-type SCID mice (n=3 per group) were dosed intravenously (bolus) with the exemplary anti-FRa ADCs (6 mg/kg).
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[1] |
| Maximum Observed Concentration (Cmax) | 110 | ug/mL |
Human FcRn Tg32 mice (n=3 per group) were dosed intravenously (bolus) with the DAR4 or DAR8 ADCs formed from AB1370049 and SG3932 (5 mg/kg).
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 405 | ug*day/mL |
Human FcRn Tg32 mice (n=3 per group) were dosed intravenously (bolus) with the DAR4 or DAR8 ADCs formed from AB1370049 and SG3932 (5 mg/kg).
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| Maximum Observed Concentration (Cmax) | 396 | ug/mL |
Male cynomolgus monkeys (N=3) were intravenously administered with 2 single (each 3 weeks apart i.e. Day 1 and 22) doses of AB1370049-SG3932 DAR8 at 15 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 1620 | ug*day/mL |
Male cynomolgus monkeys (N=3) were intravenously administered with 2 single (each 3 weeks apart i.e. Day 1 and 22) doses of AB1370049-SG3932 DAR8 at 15 mg/kg.
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| Maximum Observed Concentration (Cmax) | 773 | ug/mL |
Male cynomolgus monkeys (N=3) were intravenously administered with 2 single (each 3 weeks apart i.e. Day 1 and 22) doses of AB1370049-SG3932 DAR8 at 25 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 3990 | ug*day/mL |
Male cynomolgus monkeys (N=3) were intravenously administered with 2 single (each 3 weeks apart i.e. Day 1 and 22) doses of AB1370049-SG3932 DAR8 at 25 mg/kg.
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[1] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 696.25 | ug*day/mL |
Wild-type SCID mice (n=3 per group) were dosed intravenously (bolus) with the exemplary anti-FRa ADCs (6 mg/kg).
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[1] |
| Volume of Distribution (Vd) | 97.63 | ml/kg |
Wild-type SCID mice (n=3 per group) were dosed intravenously (bolus) with the exemplary anti-FRa ADCs (9 mg/kg).
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 405 | ug*day/mL |
Human FcRn Tg32 mice (n=3 per group) were dosed intravenously (bolus) with the DAR4 or DAR8 ADCs formed from AB1370049 and SG3932 (5 mg/kg).
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[1] |
| Volume of Distribution (Vd) | 120 | ml/kg |
Human FcRn Tg32 mice (n=3 per group) were dosed intravenously (bolus) with the DAR4 or DAR8 ADCs formed from AB1370049 and SG3932 (5 mg/kg).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1620 | ug*day/mL |
Male cynomolgus monkeys (N=3) were intravenously administered with 2 single (each 3 weeks apart i.e. Day 1 and 22) doses of AB1370049-SG3932 DAR8 at 15 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3990 | ug*day/mL |
Male cynomolgus monkeys (N=3) were intravenously administered with 2 single (each 3 weeks apart i.e. Day 1 and 22) doses of AB1370049-SG3932 DAR8 at 25 mg/kg.
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[1] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 696.25 | ug*day/mL |
Wild-type SCID mice (n=3 per group) were dosed intravenously (bolus) with the exemplary anti-FRa ADCs (6 mg/kg).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 405 | ug*day/mL |
Human FcRn Tg32 mice (n=3 per group) were dosed intravenously (bolus) with the DAR4 or DAR8 ADCs formed from AB1370049 and SG3932 (5 mg/kg).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1620 | ug*day/mL |
Male cynomolgus monkeys (N=3) were intravenously administered with 2 single (each 3 weeks apart i.e. Day 1 and 22) doses of AB1370049-SG3932 DAR8 at 15 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3990 | ug*day/mL |
Male cynomolgus monkeys (N=3) were intravenously administered with 2 single (each 3 weeks apart i.e. Day 1 and 22) doses of AB1370049-SG3932 DAR8 at 25 mg/kg.
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[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 696.25 | ug*day/mL |
Wild-type SCID mice (n=3 per group) were dosed intravenously (bolus) with the exemplary anti-FRa ADCs (6 mg/kg).
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| Clearance (CL) | 4.56 | ml/kg/days |
Wild-type SCID mice (n=3 per group) were dosed intravenously (bolus) with the exemplary anti-FRa ADCs (7 mg/kg).
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[1] |
| Elimination Half-Life (t1/2) | 15.94 | days |
Wild-type SCID mice (n=3 per group) were dosed intravenously (bolus) with the exemplary anti-FRa ADCs (8 mg/kg).
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 405 | ug*day/mL |
Human FcRn Tg32 mice (n=3 per group) were dosed intravenously (bolus) with the DAR4 or DAR8 ADCs formed from AB1370049 and SG3932 (5 mg/kg).
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[1] |
| Clearance (CL) | 10.4 | ml/kg/days |
Human FcRn Tg32 mice (n=3 per group) were dosed intravenously (bolus) with the DAR4 or DAR8 ADCs formed from AB1370049 and SG3932 (5 mg/kg).
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[1] |
| Elimination Half-Life (t1/2) | 8 | days |
Human FcRn Tg32 mice (n=3 per group) were dosed intravenously (bolus) with the DAR4 or DAR8 ADCs formed from AB1370049 and SG3932 (5 mg/kg).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1620 | ug*day/mL |
Male cynomolgus monkeys (N=3) were intravenously administered with 2 single (each 3 weeks apart i.e. Day 1 and 22) doses of AB1370049-SG3932 DAR8 at 15 mg/kg.
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[1] |
| Clearance (CL) | 8.4 | ml/kg/days |
Male cynomolgus monkeys (N=3) were intravenously administered with 2 single (each 3 weeks apart i.e. Day 1 and 22) doses of AB1370049-SG3932 DAR8 at 15 mg/kg.
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[1] |
| Elimination Half-Life (t1/2) | 6.6 | days |
Male cynomolgus monkeys (N=3) were intravenously administered with 2 single (each 3 weeks apart i.e. Day 1 and 22) doses of AB1370049-SG3932 DAR8 at 15 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3990 | ug*day/mL |
Male cynomolgus monkeys (N=3) were intravenously administered with 2 single (each 3 weeks apart i.e. Day 1 and 22) doses of AB1370049-SG3932 DAR8 at 25 mg/kg.
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[1] |
| Clearance (CL) | 5.8 | ml/kg/days |
Male cynomolgus monkeys (N=3) were intravenously administered with 2 single (each 3 weeks apart i.e. Day 1 and 22) doses of AB1370049-SG3932 DAR8 at 25 mg/kg.
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[1] |
| Elimination Half-Life (t1/2) | 6.2 | days |
Male cynomolgus monkeys (N=3) were intravenously administered with 2 single (each 3 weeks apart i.e. Day 1 and 22) doses of AB1370049-SG3932 DAR8 at 25 mg/kg.
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[1] |