Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0VMSSD
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| ADC Name |
ASG-5ME
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| Synonyms |
ASG-5ME
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| Organization |
Seagen (Top20 MNC) (Originator);Agensys (Top20 MNC)
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| Drug Status |
Phase 1 (discontinued)
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| Drug-to-Antibody Ratio |
3.7
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| Structure |
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| Antibody Name |
Anti-SLC44A4 IgG2 mAb
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Antibody Info | ||||
| Antigen Name |
Choline transporter-like protein 4 (SLC44A4)
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Antigen Info | ||||
| Payload Name |
MMAE
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Mc-Val-Cit-PABC
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Linker Info | ||||
| Conjugate Type |
Random Cysteines
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| Combination Type |
vedotin
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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 | ||
|---|---|---|---|---|---|---|---|---|---|
| Gastric cancer |
1 Trials
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| Pancreatic cancer |
1 Trials
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| Prostate cancer |
1 Trials
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ADC-specific functional property(2027 Update)
Binding Affinity
| Dissocation Constant (Kd) | Binding Target | Description | Reference |
|---|---|---|---|
| 1.7 nM |
human SLC44A4
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Results from affinity binding studies with recombinant PC3 cells engineered to express human SLC44A4 demonstrated similar affinities (Kd) for the parental antibody, AGS5-M2 (1.6 nmol/L) and the ADC ASG-5ME (1.7 nmol/L
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[3]
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| 1.4 nM |
cynomolgus monkey SLC44A4
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Results from affinity binding studies with recombinant PC3 cells engineered to express human SLC44A4 demonstrated similar affinities (Kd) for the parental antibody, AGS5-M2 (1.6 nmol/L) and the ADC ASG-5ME (1.7 nmol/L)
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[3]
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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) | 15.25 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.3 mg/kg, AUC0-7d.
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[1] |
| Maximum Observed Concentration (Cmax) | 5.67 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.3 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 26.2 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.6 mg/kg, AUC0-7d.
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[1] |
| Maximum Observed Concentration (Cmax) | 13.42 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.6 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 37.88 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.9 mg/kg, AUC0-7d.
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[1] |
| Maximum Observed Concentration (Cmax) | 16.88 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.9 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 43.31 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.2 mg/kg, AUC0-7d.
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[1] |
| Maximum Observed Concentration (Cmax) | 17.69 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.2 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 54.32 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.5 mg/kg, AUC0-7d.
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[1] |
| Maximum Observed Concentration (Cmax) | 21.07 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.5 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 26.9±2.06 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.3 mg/kg, AUC0-21d.
|
[2] |
| Maximum Observed Concentration (Cmax) | 7.1±0.44 | mg/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.3 mg/kg.
|
[2] |
| Time to Maximum Concentration (Tmax) | 0.04±0.036 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.3 mg/kg.
|
[2] |
| Maximum Observed Concentration (Cmax) | 7.5±1.43 | mg/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week4, 0.3 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 55.3±12.54 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.6 mg/kg, AUC0-21d.
|
[2] |
| Maximum Observed Concentration (Cmax) | 13.1±3.38 | mg/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.6 mg/kg.
|
[2] |
| Time to Maximum Concentration (Tmax) | 0.02 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.6 mg/kg.
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[2] |
| Maximum Observed Concentration (Cmax) | 13.8±3.66 | mg/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week4, 0.6 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 122.3±4.93 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.2 mg/kg, AUC0-21d.
|
[2] |
| Maximum Observed Concentration (Cmax) | 28.1±1.78 | mg/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.2 mg/kg.
|
[2] |
| Time to Maximum Concentration (Tmax) | 0.09±0.073 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.2 mg/kg.
|
[2] |
| Maximum Observed Concentration (Cmax) | 26.6±3.32 | mg/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week4, 1.2 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 131.7±10.02 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.8 mg/kg, AUC0-21d.
|
[2] |
| Maximum Observed Concentration (Cmax) | 30.9±2.75 | mg/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.8 mg/kg.
|
[2] |
| Time to Maximum Concentration (Tmax) | 0.09±0.073 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.8 mg/kg.
|
[2] |
| Maximum Observed Concentration (Cmax) | 29.1±6.29 | mg/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week4, 1.8 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 239±28 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.4 mg/kg, AUC0-21d.
|
[2] |
| Maximum Observed Concentration (Cmax) | 52.3±9.63 | mg/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.4 mg/kg.
|
[2] |
| Time to Maximum Concentration (Tmax) | 0.05±0.075 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.4 mg/kg.
|
[2] |
| Maximum Observed Concentration (Cmax) | 79.8±48.42 | mg/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week4, 2.4 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 213.3±34.8 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.7 mg/kg, AUC0-21d.
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[2] |
| Maximum Observed Concentration (Cmax) | 48.9±21.6 | mg/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.7 mg/kg.
|
[2] |
| Time to Maximum Concentration (Tmax) | 0.35±0.678 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.7 mg/kg.
|
[2] |
| Maximum Observed Concentration (Cmax) | 63±47.68 | mg/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week4, 2.7 mg/kg.
|
[2] |
| Maximum Observed Concentration (Cmax) | 52.1±2.26 | mg/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 3.0 mg/kg.
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[2] |
| Time to Maximum Concentration (Tmax) | 0.02 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 3.0 mg/kg.
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[2] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 15.25 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.3 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 0.68 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.3 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 26.2 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.6 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 1.78 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.6 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 37.88 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.9 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 2.05 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.9 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 43.31 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.2 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 2.69 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.2 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 54.32 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.5 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 3.51 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.5 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 26.9±2.06 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.3 mg/kg, AUC0-21d.
|
[2] |
| Volume of Distribution (Vd) | 33.6±8.84 | mL/kg |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.3 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 55.3±12.54 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.6 mg/kg, AUC0-21d.
|
[2] |
| Volume of Distribution (Vd) | 51.9±24.25 | mL/kg |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.6 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 122.3±4.93 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.2 mg/kg, AUC0-21d.
|
[2] |
| Volume of Distribution (Vd) | 40.5±40.45 | mL/kg |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.2 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 131.7±10.02 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.8 mg/kg, AUC0-21d.
|
[2] |
| Volume of Distribution (Vd) | 60.2±38.15 | mL/kg |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.8 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 239±28 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.4 mg/kg, AUC0-21d.
|
[2] |
| Volume of Distribution (Vd) | 40.8±14.15 | mL/kg |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.4 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 213.3±34.8 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.7 mg/kg, AUC0-21d.
|
[2] |
| Volume of Distribution (Vd) | 140.1±122.61 | mL/kg |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.7 mg/kg.
|
[2] |
| Volume of Distribution (Vd) | 82.1±16.12 | mL/kg |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 3.0 mg/kg.
|
[2] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 15.25 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.3 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 0.68 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.3 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 26.2 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.6 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 1.78 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.6 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 37.88 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.9 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 2.05 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.9 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 43.31 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.2 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 2.69 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.2 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 54.32 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.5 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 3.51 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.5 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 26.9±2.06 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.3 mg/kg, AUC0-21d.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 55.3±12.54 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.6 mg/kg, AUC0-21d.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 122.3±4.93 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.2 mg/kg, AUC0-21d.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 131.7±10.02 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.8 mg/kg, AUC0-21d.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 239±28 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.4 mg/kg, AUC0-21d.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 213.3±34.8 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.7 mg/kg, AUC0-21d.
|
[2] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 15.25 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.3 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 0.68 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.3 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 26.2 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.6 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 1.78 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.6 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 37.88 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.9 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 2.05 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 0.9 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 43.31 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.2 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 2.69 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.2 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 54.32 | day*ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.5 mg/kg, AUC0-7d.
|
[1] |
| Trough Concentration (Cthrough) | 3.51 | ug/mL |
Pharmacokinetic Parameters for ASG-5ME ADC, 1.5 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 26.9±2.06 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.3 mg/kg, AUC0-21d.
|
[2] |
| Elimination Half-Life (t1/2) | 6.59±2.015 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.3 mg/kg.
|
[2] |
| Elimination Half-Life (t1/2) | 5.8±3.26 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week4, 0.3 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 55.3±12.54 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.6 mg/kg, AUC0-21d.
|
[2] |
| Elimination Half-Life (t1/2) | 11.21±4.643 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 0.6 mg/kg.
|
[2] |
| Elimination Half-Life (t1/2) | 8.1±1.85 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week4, 0.6 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 122.3±4.93 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.2 mg/kg, AUC0-21d.
|
[2] |
| Elimination Half-Life (t1/2) | 5.51±1.373 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.2 mg/kg.
|
[2] |
| Elimination Half-Life (t1/2) | 10±0.7 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week4, 1.2 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 131.7±10.02 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.8 mg/kg, AUC0-21d.
|
[2] |
| Elimination Half-Life (t1/2) | 6.75±0.718 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 1.8 mg/kg.
|
[2] |
| Elimination Half-Life (t1/2) | 8.3±3.68 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week4, 1.8 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 239±28 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.4 mg/kg, AUC0-21d.
|
[2] |
| Elimination Half-Life (t1/2) | 7.03±2.142 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.4 mg/kg.
|
[2] |
| Elimination Half-Life (t1/2) | 6.7±1.62 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week4, 2.4 mg/kg.
|
[2] |
| Area Under the Concentration-Time Curve (AUC) | 213.3±34.8 | mg*day/mL |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.7 mg/kg, AUC0-21d.
|
[2] |
| Elimination Half-Life (t1/2) | 37±98.515 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 2.7 mg/kg.
|
[2] |
| Elimination Half-Life (t1/2) | 7.4±1.74 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week4, 2.7 mg/kg.
|
[2] |
| Elimination Half-Life (t1/2) | 6.54±1.81 | day |
A phase I study of the antibody drug conjugate ASG-5ME, an SLC44A4-targeting antibody carrying auristatin E, in metastatic castration-resistant prostate cancer, Study week1, 3.0 mg/kg.
|
[2] |
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [4] | ||||
| Patients Enrolled |
Inclusion: Metastatic pancreatic adenocarcinoma or AGS-5+ gastric/GEJ adenocarcinoma (measurable disease ≥10-15 mm), ECOG 0-1; untreated or ≤1 prior systemic therapy (2/4-week washout). Exclusion: CNS metastases, active malignancy (<3y remission), recent cardiac/CV events (NYHA III-IV), or untreated major organ dysfunction.
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| Administration Dosage |
0.3-3.0 mg/kg IV on Days 1, 8, and 15 of 28-day cycles
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| Related Clinical Trial | |||||
| NCT Number | NCT01166490 | Clinical Status | PHASE1 | ||
| Clinical Description | A Phase 1, Open-Label, Dose Escalation Study of ASG-5ME in Patients With Pancreatic or Gastric Adenocarcinoma | ||||
| Primary Endpoint |
Safety analysis includes incidence of adverse events and lab abnormalities (assessed until 1 month post-treatment), ASG-5ME/metabolite blood concentrations, and antitherapeutic antibody development.
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| Other Endpoint |
Efficacy measures involve best clinical response (assessed every 2 months), overall survival, progression-free survival (monthly until death/study closure), and pharmacokinetic monitoring of ASG-5ME.
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| Experiment 2 Reporting the Activity Date of This ADC | [5] | ||||
| Patients Enrolled |
Inclusion: Castration-resistant prostate cancer (progression post-standard therapy, no effective therapy, or patient declines), testosterone ≤50 ng/dL, ECOG 0-1, life expectancy >6 months, adequate hematologic/renal/hepatic function, stable LHRH/GnRH therapy, prior docetaxel allowed only if refractory/intolerant. Exclusion: CNS metastases, active malignancy (<3-year remission), significant cardiac disease, recent chemo/radiation/anti-androgens, neuropathy ≥grade 2, major surgery/infection, HIV/HepB/HepC positivity, recent thromboembolic events.
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| Administration Dosage |
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| Related Clinical Trial | |||||
| NCT Number | NCT01228760 | Clinical Status | PHASE1 | ||
| Clinical Description | A Phase 1, Open-label, Multi-center, Dose Escalation Study of the Safety and Pharmacokinetics of ASG-5ME Monotherapy in Subjects With Castration-Resistant Prostate Cancer (CRPC) | ||||
| Primary Endpoint |
Safety is evaluated through adverse events, lab tests (hematology, biochemistry), and vital signs during the 12-week treatment and 4-week follow-up. Pharmacokinetics of ASG-5ME is analyzed via blood samples (Cycle 1 & 4, pre-dose Cycles 2 & 3, and periodically thereafter if treatment continues).
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| Other Endpoint |
Efficacy measures include anti-ASG-5ME antibody formation, tumor response (every 12 weeks), PSA levels, bone scans, circulating tumor cells, and cytokeratin-18 levels (assessed periodically during treatment).
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References