Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0UUFIR
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| ADC Name |
SYD998
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| Synonyms |
WO2015177360A1_ADC-wt; SYD 998; SYD-998
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| Organization |
Byodes Private Ltd.
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| Drug Status |
Investigative
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| Indication |
In total 1 Indication(s)
Prostate cancer [ICD11:2C82]
Investigative
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| Drug-to-Antibody Ratio |
1.8
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| Antibody Name |
Anti-PSMA mAb wt
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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) | ≈ 35.67% (Day 69) | Positive PSMA expression (PSMA+++/++) | ||
| Method Description |
Tumours were induced subcutaneously by injecting of 10,000,000 LnCap C4.2 cells in 200 uL of RPMI 1640 containing matrigel into the right flank of male CB17.SCID mice. Treatments were started when the tumors reached a mean volume of 100-200 mm3. Mice were randomized according to their individual tumor volume into groups and received a single i.v, 2 mg/kg inection of anti-PSMA ADC.
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| In Vivo Model | LNCaP C4-2 CDX model | ||||
| In Vitro Model | Lymph node metastasis of prostate carcinoma | LNCaP C4-2 cells | CVCL_4782 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.68% (Day 69) | Positive PSMA expression (PSMA+++/++) | ||
| Method Description |
Tumours were induced subcutaneously by injecting of 10,000,000 LnCap C4.2 cells in 200 uL of RPMI 1640 containing matrigel into the right flank of male CB17.SCID mice. Treatments were started when the tumors reached a mean volume of 100-200 mm3. Mice were randomized according to their individual tumor volume into groups and received a single i.v, 10 mg/kg inection of anti-PSMA ADC.
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| In Vivo Model | LNCaP C4-2 CDX model | ||||
| In Vitro Model | Lymph node metastasis of prostate carcinoma | LNCaP C4-2 cells | CVCL_4782 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Max inhibition rate (MIR) | 82.00% | 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 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Max inhibition rate (MIR) | 97.00% | 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 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.23 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 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.70 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 5 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 | ||
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