Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0MICVG
|
|||||
|---|---|---|---|---|---|---|
| ADC Name |
wO2024222841A1 ADC38-4
|
|||||
| Synonyms |
ADC38-4
Click to Show/Hide
|
|||||
| Organization |
CSPC MEGALITH BIOPHARMACEUTICAL CO.,LTD.
|
|||||
| Drug Status |
Investigative
|
|||||
| Drug-to-Antibody Ratio |
4
|
|||||
| Structure |
|
|||||
| Antibody Name |
Trastuzumab
|
Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
|
Antigen Info | ||||
| Payload Name |
(S)B19
|
Payload Info | ||||
| Therapeutic Target |
Eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1)
|
Target Info | ||||
| Linker Name |
OXDc-VA-PAB (PEG)
|
Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
|
|||||
| Combination Type |
LD38
|
|||||
ADC-specific functional property(2027 Update)
Payload Release Efficiency
| Incubation Time | 7days | Release | 0.005% | Reference |
[1]
|
|---|---|---|---|---|---|
| Description |
The pharmacokinetic behaviors of the investigational compounds ADC38-4, ADC38, T-ADC-2, and Enhertu were studied in rats after a single intravenous injection of 6 mg/kg. The ADC compounds were administered via tail vein injection at a dose of 6 mg/kg. Blood samples were collected from the retro-orbital sinus before dosing and at 0.5 h, 18 h, 24 h, 48 h, 96 h, and 168 h post-dose. The blood was drawn into citrate tubes and processed to plasma. The content of the antibody-drug conjugates (ADC) in the blood samples was determined by enzyme-linked immunosorbent assay (ELISA), and pharmacokinetic parameters were calculated using a non-compartmental model. The content of free small molecules in the blood samples was determined using LC-MS/MS, and pharmacokinetic parameters were also calculated.
Click to Show/Hide
|
||||
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) | 61.48 | h*nmol/mL |
The pharmacokinetic behaviors of the investigational compounds ADC38-4, ADC38, T-ADC-2, and Enhertu were studied in rats after a single intravenous injection of 6 mg/kg. The ADC compounds were administered via tail vein injection at a dose of 6 mg/kg. Blood samples were collected from the retro-orbital sinus before dosing and at 0.5 h, 18 h, 24 h, 48 h, 96 h, and 168 h post-dose. The blood was drawn into citrate tubes and processed to plasma. The content of the antibody-drug conjugates (ADC) in the blood samples was determined by enzyme-linked immunosorbent assay (ELISA), and pharmacokinetic parameters were calculated using a non-compartmental model. The content of free small molecules in the blood samples was determined using LC-MS/MS, and pharmacokinetic parameters were also calculated.
Click to Show/Hide
|
[1] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 61.48 | h*nmol/mL |
The pharmacokinetic behaviors of the investigational compounds ADC38-4, ADC38, T-ADC-2, and Enhertu were studied in rats after a single intravenous injection of 6 mg/kg. The ADC compounds were administered via tail vein injection at a dose of 6 mg/kg. Blood samples were collected from the retro-orbital sinus before dosing and at 0.5 h, 18 h, 24 h, 48 h, 96 h, and 168 h post-dose. The blood was drawn into citrate tubes and processed to plasma. The content of the antibody-drug conjugates (ADC) in the blood samples was determined by enzyme-linked immunosorbent assay (ELISA), and pharmacokinetic parameters were calculated using a non-compartmental model. The content of free small molecules in the blood samples was determined using LC-MS/MS, and pharmacokinetic parameters were also calculated.
Click to Show/Hide
|
[1] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 61.48 | h*nmol/mL |
The pharmacokinetic behaviors of the investigational compounds ADC38-4, ADC38, T-ADC-2, and Enhertu were studied in rats after a single intravenous injection of 6 mg/kg. The ADC compounds were administered via tail vein injection at a dose of 6 mg/kg. Blood samples were collected from the retro-orbital sinus before dosing and at 0.5 h, 18 h, 24 h, 48 h, 96 h, and 168 h post-dose. The blood was drawn into citrate tubes and processed to plasma. The content of the antibody-drug conjugates (ADC) in the blood samples was determined by enzyme-linked immunosorbent assay (ELISA), and pharmacokinetic parameters were calculated using a non-compartmental model. The content of free small molecules in the blood samples was determined using LC-MS/MS, and pharmacokinetic parameters were also calculated.
Click to Show/Hide
|
[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 61.48 | h*nmol/mL |
The pharmacokinetic behaviors of the investigational compounds ADC38-4, ADC38, T-ADC-2, and Enhertu were studied in rats after a single intravenous injection of 6 mg/kg. The ADC compounds were administered via tail vein injection at a dose of 6 mg/kg. Blood samples were collected from the retro-orbital sinus before dosing and at 0.5 h, 18 h, 24 h, 48 h, 96 h, and 168 h post-dose. The blood was drawn into citrate tubes and processed to plasma. The content of the antibody-drug conjugates (ADC) in the blood samples was determined by enzyme-linked immunosorbent assay (ELISA), and pharmacokinetic parameters were calculated using a non-compartmental model. The content of free small molecules in the blood samples was determined using LC-MS/MS, and pharmacokinetic parameters were also calculated.
Click to Show/Hide
|
[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 inhibitory Concentration (lC50) | > 25 pM | High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of ADC to SK-BR-3 cells
|
||||
| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||