Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0DWZNW
|
|||||
|---|---|---|---|---|---|---|
| ADC Name |
hL49-HALC-MDpr-PEG (12)-gluc-MMAE
|
|||||
| Synonyms |
hL49-HALC-MDpr-PEG (12)-gluc-MMAE
Click to Show/Hide
|
|||||
| Organization |
SEAGEN INC.
|
|||||
| Drug Status |
Investigative
|
|||||
| Drug-to-Antibody Ratio |
8
|
|||||
| Structure |
|
|||||
| Antibody Name |
hL49-HALC
|
Antibody Info | ||||
| Antigen Name |
Melanotransferrin (MELTF)
|
Antigen Info | ||||
| Payload Name |
Monomethyl auristatin E
|
Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
|
Target Info | ||||
| Linker Name |
MDpr-PEG (12)gluc
|
Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
|
|||||
| Combination Type |
MDpr-PEG (12)-gluc-MMAE
|
|||||
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) | 41 | day*kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=41.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 50 | day*kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=50.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 63 | day*kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=63.
Click to Show/Hide
|
[1] |
| Maximum Observed Concentration (Cmax) | 8.8 | kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=41.Csub>max/Dose (kg*ug/mL/mg)=8.8
Click to Show/Hide
|
[1] |
| Maximum Observed Concentration (Cmax) | 8.1 | kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=50.Csub>max/Dose (kg*ug/mL/mg)=8.1
Click to Show/Hide
|
[1] |
| Maximum Observed Concentration (Cmax) | 13.3 | kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=63.Csub>max/Dose (kg*ug/mL/mg)=13.3
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 41 | day*kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=41.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 50 | day*kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=50.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 63 | day*kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=63.
Click to Show/Hide
|
[1] |
| Maximum Observed Concentration (Cmax) | 8.8 | kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=41.Csub>max/Dose (kg*ug/mL/mg)=8.8
Click to Show/Hide
|
[1] |
| Maximum Observed Concentration (Cmax) | 8.1 | kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=50.Csub>max/Dose (kg*ug/mL/mg)=8.1
Click to Show/Hide
|
[1] |
| Maximum Observed Concentration (Cmax) | 13.3 | kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=63.Csub>max/Dose (kg*ug/mL/mg)=13.3
Click to Show/Hide
|
[1] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 41 | day*kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=41.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 50 | day*kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=50.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 63 | day*kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=63.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 41 | day*kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=41.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 50 | day*kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=50.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 63 | day*kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=63.
Click to Show/Hide
|
[1] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 41 | day*kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=41.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 50 | day*kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=50.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 63 | day*kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=63.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 41 | day*kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=41.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 50 | day*kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=50.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 63 | day*kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=63.
Click to Show/Hide
|
[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 41 | day*kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=41.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 50 | day*kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=50.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 63 | day*kg*ug/mL/mg |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=63.
Click to Show/Hide
|
[1] |
| Elimination Half-Life (t1/2) | 4.7 | day |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=41.Halflife (day)=4.7
Click to Show/Hide
|
[1] |
| Elimination Half-Life (t1/2) | 4.4 | day |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=50.Halflife (day)=4.4
Click to Show/Hide
|
[1] |
| Elimination Half-Life (t1/2) | 5.1 | day |
Nude mice were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=63.Halflife (day)=5.1
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 41 | day*kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=41.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 50 | day*kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=50.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 63 | day*kg*ug/mL/mg |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=63.
Click to Show/Hide
|
[1] |
| Elimination Half-Life (t1/2) | 4.7 | day |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=41.Halflife (day)=4.7
Click to Show/Hide
|
[1] |
| Elimination Half-Life (t1/2) | 4.4 | day |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=50.Halflife (day)=4.4
Click to Show/Hide
|
[1] |
| Elimination Half-Life (t1/2) | 5.1 | day |
Sprague-Dawley rats were intravenously administered hL49-MDpr-PEG (12)-gluc-MMAE. Plasmaconcentrations of the ADC were measured over time usingTab ELISA with an anti-human antibody as the captureantibody. AUCinf/Dose (day*kg*ug/mL/mg)=63.Halflife (day)=5.1
Click to Show/Hide
|
[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 (lC65) |
14.9 nM
|
|||
| Method Description |
Tumor cells (A375) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
|
||||
| In Vitro Model | Amelanotic melanoma | A375 cells | CVCL_0132 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC64) | 7.3 nM | Moderate MELTF expression (MELTF++) | ||
| Method Description |
Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
|
||||
| In Vitro Model | Melanoma | A2058 cells | CVCL_1059 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC64) |
13.7 nM
|
|||
| Method Description |
Tumor cells (IGR37) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
|
||||
| In Vitro Model | Melanoma | IGR37 cells | CVCL_2075 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC58) |
3.7 nM
|
|||
| Method Description |
Tumor cells (Colo853) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
|
||||
| In Vitro Model | Cutaneous melanoma | Colo853 cells | CVCL_2003 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC51) |
2.5 nM
|
|||
| Method Description |
Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
|
||||
| In Vitro Model | Cutaneous melanoma | SK-MEL-5 cells | CVCL_0527 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
2.8 nM
|
|||
| Method Description |
Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
|
||||
| In Vitro Model | Cutaneous melanoma | SK-MEL-5 cells | CVCL_0527 | ||