Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0IOYUA
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| ADC Name |
38850783 ADC 2
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| Synonyms |
ADC 2
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| Organization |
Yonsei University.
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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 |
Trastuzumab
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Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
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Antigen Info | ||||
| Payload Name |
Mertansine DM1
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Dimaleimide linker 2
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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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) | 8.15 | day*ug/mL |
PK values of T-Dxd, ADC 2-4 on 6-week-old ICR mice model (n = 6), AUCinf.
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Distribution
| Standard Type | Value | Units | Description | Reference |
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| Area Under the Concentration-Time Curve (AUC) | 8.15 | day*ug/mL |
PK values of T-Dxd, ADC 2-4 on 6-week-old ICR mice model (n = 6), AUCinf.
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| Volume of Distribution (Vd) | 279 | mL/kg |
PK values of T-Dxd, ADC 2-4 on 6-week-old ICR mice model (n = 6).
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Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 8.15 | day*ug/mL |
PK values of T-Dxd, ADC 2-4 on 6-week-old ICR mice model (n = 6), AUCinf.
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Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 8.15 | day*ug/mL |
PK values of T-Dxd, ADC 2-4 on 6-week-old ICR mice model (n = 6), AUCinf.
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| Clearance (CL) | 123 | mL/day/kg |
PK values of T-Dxd, ADC 2-4 on 6-week-old ICR mice model (n = 6).
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| Elimination Half-Life (t1/2) | 1.7 | mL/kg |
PK values of T-Dxd, ADC 2-4 on 6-week-old ICR mice model (n = 6), half-life (beta).
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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 | Ninety Percent Inhibitory Concentration (IC90) | 0.17- 0.55 ng/mL | Negative HER2 expression (HER2-) | ||
| Method Description |
We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).
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| In Vitro Model | Breast ductal carcinoma | HCC1937 cells | CVCL_0290 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Ninety Percent Inhibitory Concentration (IC90) | 0.19- 0.31 ng/mL | High HER2 expression (HER2 +++) | ||
| Method Description |
We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 0.24 ng/mL | High HER2 expression (HER2 +++) | ||
| Method Description |
We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 0.31 ng/mL | Negative HER2 expression (HER2-) | ||
| Method Description |
We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).
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| In Vitro Model | Breast ductal carcinoma | HCC1937 cells | CVCL_0290 | ||
References