Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0IVLAR
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| ADC Name |
US20250025567A1 ExL1A1
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| Synonyms |
US20250025567A1 ExL1A1
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| Organization |
ASTELLAS PHARMA INC.
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
3.44
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| Structure |
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| Antibody Name |
anti-hCLDN6 antibody Ab1
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Antibody Info | ||||
| Antigen Name |
Claudin-6 (CLDN6)
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Antigen Info | ||||
| Payload Name |
5-[ (4-{[ (2S)-2- (fluoromethyl)piperazin-1-yl]methyl}-2-methoxyphenyl)methyl|]-N4-pentyl-5H-pyrrolo[3,2-d]pyrimidine-2,4-diamine
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Payload Info | ||||
| Therapeutic Target |
Toll-like receptor 7 (TLR7); Toll-like receptor 8 (TLR8)
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Target Info | ||||
| Linker Name |
3-Maleimidopropionic acid linker
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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| Combination Type |
1-{3-[ (3S)-4-[ (4-{[2-amino-4- (pentylamino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl]methyl}-3-methoxyphenyl])methyl]-3- (fluo-romethyl)piperazin-1-yl]-3-oxopropy1}-1H-pyrrole-2,5-dione (trifluoroacetic acid) salt
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General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
| Standard Type | Value | Units | Cell Line | Disease Model |
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| Tumor Growth lnhibition value (TGl) |
> 50
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%
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Undisclosed | Undisclosed |
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 lnhibition value (TGl) | > 50% | Positive CLDN6 expression (CLDN6+++/++) | ||
| Method Description |
ExL1A1 was tested in SCID mice that subcutaneously transplanted NUGC33, 3 mg/kg was administeredthrough the tail vein of the tumor-bearing mice.
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| In Vivo Model | NUGC-3 cells SCID mice model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | The ADC concentration required to produce 10,000 pg/mL TNF-alpha was evaluated. | 100- 1000 nM | Positive CLDN6 expression (CLDN6+++/++) | ||
| Method Description |
ExL1A1 was tested in co-culture system consisting of Human peripheral blood mononuclear cells (PBMCs) and NUGC33 cells, with the concentration range of 5.5 uM to 0.97 uM,TNF-a and INF-y productions were measured.
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| In Vitro Model | Normal; Gastric adenocarcinoma | PBMC cells; NUGC3 cells | .;CVCL_1612 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | The ADC concentration required to produce 10,000 pg/mL INF-Gamma was evaluated. | 10- 100 nM | Positive CLDN6 expression (CLDN6+++/++) | ||
| Method Description |
ExL1A1 was tested in co-culture system consisting of Human peripheral blood mononuclear cells (PBMCs) and NUGC33 cells, with the concentration range of 5.5 uM to 0.97 uM,TNF-a and INF-y productions were measured.
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| In Vitro Model | Normal; Gastric adenocarcinoma | PBMC cells; NUGC3 cells | .;CVCL_1612 | ||