Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0GAFBL
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| ADC Name |
WO2015177360A1 ADC-LC41
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| Synonyms |
WO2015177360A1_ADC LC41
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| Organization |
Byodes Private Ltd.
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| Drug Status |
Investigative
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| Indication |
In total 2 Indication(s)
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| Drug-to-Antibody Ratio |
1.8
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| Antibody Name |
Anti-PSMA mAb wt LC G41C
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Antibody Info | ||||
| Antigen Name |
Glutamate carboxypeptidase 2 (FOLH1)
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Antigen Info | ||||
| Payload Name |
seco-DUBA
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Payload Info | ||||
| Therapeutic Target |
Human Deoxyribonucleic acid (hDNA)
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Target Info | ||||
| Linker Name |
Mal-PEG2-Val-Cit-PABA-Cyclization Spacer
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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| Combination Type |
Duocarmazine
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General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 43.85% (Day 47) | Positive 5T4 expression (5T4+++/++) | ||
| Method Description |
Tumours were induced subcutaneously by injecting of 10,000,000 PA-1 cells in 100 uL of RPMI 1640 containing matrigel into the right flank of male Balb/c nude mice. Treatments were started when the tumors reached a mean volume of 200-300 mm3. Mice were randomized according to their individual tumor volume into groups and received a single i.v, 3 mg/kg inection of anti-5T4 ADC.
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| In Vivo Model | PA-1 CDX model | ||||
| In Vitro Model | Ovarian mixed germ cell tumor | PA-1 cells | CVCL_0479 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 85.04% (Day 47) | Positive 5T4 expression (5T4+++/++) | ||
| Method Description |
Tumours were induced subcutaneously by injecting of 10,000,000 PA-1 cells in 100 uL of RPMI 1640 containing matrigel into the right flank of male Balb/c nude mice. Treatments were started when the tumors reached a mean volume of 200-300 mm3. Mice were randomized according to their individual tumor volume into groups and received a single i.v, 10 mg/kg inection of anti-5T4 ADC.
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| In Vivo Model | PA-1 CDX model | ||||
| In Vitro Model | Ovarian mixed germ cell tumor | PA-1 cells | CVCL_0479 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Max inhibition rate (MIR) | 50.00% | Negative PSMA expression (PSMA-) | ||
| Method Description |
To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.
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| In Vitro Model | Prostate carcinoma | DU145 cells | CVCL_0105 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Max inhibition rate (MIR) | 80.00% | Positive PSMA expression (PSMA+++/++) | ||
| Method Description |
LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
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| In Vitro Model | Lymph node metastasis of prostate carcinoma | LNCaP C4-2 cells | CVCL_4782 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Max inhibition rate (MIR) | 91.00% | Positive 5T4 expression (5T4+++/++) | ||
| Method Description |
MDA-MB-468 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Max inhibition rate (MIR) | 98.00% | Negative 5T4 expression (5T4-) | ||
| Method Description |
To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, 5T4-negative SK-MEL-30 cells (2,000 cells/well) was cultured with the ADCs for 6 days, and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.
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| In Vitro Model | Cutaneous melanoma | SK-MEL-30 cells | CVCL_0039 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.09 nM | Positive 5T4 expression (5T4+++/++) | ||
| Method Description |
MDA-MB-468 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.31 nM | Positive PSMA expression (PSMA+++/++) | ||
| Method Description |
LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
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| In Vitro Model | Lymph node metastasis of prostate carcinoma | LNCaP C4-2 cells | CVCL_4782 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.35 nM | Negative 5T4 expression (5T4-) | ||
| Method Description |
To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, 5T4-negative SK-MEL-30 cells (2,000 cells/well) was cultured with the ADCs for 6 days, and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.
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| In Vitro Model | Cutaneous melanoma | SK-MEL-30 cells | CVCL_0039 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 nM | Negative PSMA expression (PSMA-) | ||
| Method Description |
To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.
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| In Vitro Model | Prostate carcinoma | DU145 cells | CVCL_0105 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 70.00 nM | Negative PSMA expression (PSMA-) | ||
| Method Description |
DU-145 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
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| In Vitro Model | Prostate carcinoma | DU145 cells | CVCL_0105 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 90.00 nM | Negative 5T4 expression (5T4-) | ||
| Method Description |
SK-MEL-30 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
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| In Vitro Model | Cutaneous melanoma | SK-MEL-30 cells | CVCL_0039 | ||