Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0QJUWT
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| ADC Name |
AGS-62P1
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| Synonyms |
AGS62P1; ASP-1235; AGS 62P1; ASP1235
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| Organization |
Astellas Pharma, Inc.
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| Drug Status |
Terminated in phase 1
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| Indication |
In total 1 Indication(s)
Terminated in phase 1
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| Drug-to-Antibody Ratio |
2
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| Antibody Name |
AGS62P Anti-ody with pAF residues
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Antibody Info | ||||
| Antigen Name |
Receptor-type tyrosine-protein kinase FLT3 (FLT3)
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Antigen Info | ||||
| Payload Name |
AGD-0182
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
AGS-62P1 linker
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Linker Info | ||||
| Conjugate Type |
Site-specific conjugation through the para-acetyl phenylalanine unit at the unnatural amino acid.
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| Combination Type |
AGL-0182-30
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| Puchem SID | ||||||
| ChEBI ID | ||||||
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line Data
| Standard Type | Value | Units | Cell Line | Disease Model |
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| Half Maximal Inhibitory Concentration (IC50) |
0.20-12.00
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nM
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Acute myeloid leukemia cells
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Acute myeloid leukemia
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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) | 27.00% | Positive FLT3 Expression (FLT3+++/++) | ||
| Method Description |
The in vivo antitumor activity of ASP1235 was evaluated in a FLT3 positive THP-1 xenograft model. THP-1 cells were subcutaneously inoculated in the right frank of mice at 5 x106 cells/head. The vehicle of each drug is shown as follows: ASP1235 (20 mM Histidine/L-Histidine-HCl, 5.5% trehalose dihydrate, 0.01% Polysorbate 20, pH6.0), venetoclax (60% phosal 50PG, 30% PEG400, 10% ethanol), azacitidine (PBS). ASP1235 was intravenously administrated to each mouse once per week. One day before ASP1235 treatment, each mouse received intraperitoneal injection of 20 mg/kg of nonspecific human IgG1 antibody. Venetoclax was orally administered daily at 100 mg/kg. Azacitidine was intravenously injected at 3 mg/kg for five consecutive days in the first week of treatment.
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| In Vivo Model | FLT3-expressing THP-1 xenograft model | ||||
| In Vitro Model | Childhood acute monocytic leukemia | THP-1 cells | CVCL_0006 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 35.10% | Positive FLT3 Expression (FLT3+++/++) | ||
| Method Description |
The in vivo antitumor activity of ASP1235 was evaluated in a FLT3 positive THP-1 xenograft model. THP-1 cells were subcutaneously inoculated in the right frank of mice at 5 x106 cells/head. The vehicle of each drug is shown as follows: ASP1235 (20 mM Histidine/L-Histidine-HCl, 5.5% trehalose dihydrate, 0.01% Polysorbate 20, pH6.0), venetoclax (60% phosal 50PG, 30% PEG400, 10% ethanol), azacitidine (PBS). ASP1235 was intravenously administrated to each mouse once per week. One day before ASP1235 treatment, each mouse received intraperitoneal injection of 20 mg/kg of nonspecific human IgG1 antibody. Venetoclax was orally administered daily at 100 mg/kg. Azacitidine was intravenously injected at 3 mg/kg for five consecutive days in the first week of treatment.
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| In Vivo Model | FLT3-expressing THP-1 xenograft model | ||||
| In Vitro Model | Childhood acute monocytic leukemia | THP-1 cells | CVCL_0006 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 38.00% | Positive FLT3 Expression (FLT3+++/++) | ||
| Method Description |
The in vivo antitumor activity of ASP1235 was evaluated in a FLT3 positive THP-1 xenograft model. THP-1 cells were subcutaneously inoculated in the right frank of mice at 5 x106 cells/head. The vehicle of each drug is shown as follows: ASP1235 (20 mM Histidine/L-Histidine-HCl, 5.5% trehalose dihydrate, 0.01% Polysorbate 20, pH6.0), venetoclax (60% phosal 50PG, 30% PEG400, 10% ethanol), azacitidine (PBS). ASP1235 was intravenously administrated to each mouse once per week. One day before ASP1235 treatment, each mouse received intraperitoneal injection of 20 mg/kg of nonspecific human IgG1 antibody. Venetoclax was orally administered daily at 100 mg/kg. Azacitidine was intravenously injected at 3 mg/kg for five consecutive days in the first week of treatment.
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| In Vivo Model | FLT3-expressing THP-1 xenograft model | ||||
| In Vitro Model | Childhood acute monocytic leukemia | THP-1 cells | CVCL_0006 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 84.00% | Positive FLT3 Expression (FLT3+++/++) | ||
| Method Description |
The in vivo antitumor activity of ASP1235 was evaluated in a FLT3 positive THP-1 xenograft model. THP-1 cells were subcutaneously inoculated in the right frank of mice at 5 x106 cells/head. The vehicle of each drug is shown as follows: ASP1235 (20 mM Histidine/L-Histidine-HCl, 5.5% trehalose dihydrate, 0.01% Polysorbate 20, pH6.0), venetoclax (60% phosal 50PG, 30% PEG400, 10% ethanol), azacitidine (PBS). ASP1235 was intravenously administrated to each mouse once per week. One day before ASP1235 treatment, each mouse received intraperitoneal injection of 20 mg/kg of nonspecific human IgG1 antibody. Venetoclax was orally administered daily at 100 mg/kg. Azacitidine was intravenously injected at 3 mg/kg for five consecutive days in the first week of treatment.
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| In Vivo Model | FLT3-expressing THP-1 xenograft model | ||||
| In Vitro Model | Childhood acute monocytic leukemia | THP-1 cells | CVCL_0006 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.20-12.00 nM | Positive FLT3 Expression (FLT3+++/++) | ||
| Method Description |
The cytotoxic activity of AGS-62P1 was evaluated against a panel of AmL cell lines in vitro.
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| In Vitro Model | Acute myeloid leukemia | Acute myeloid leukemia cells | Homo sapiens | ||
References
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