Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0UDFEK
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| ADC Name |
dS-1062
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| Synonyms |
datopotamab deruxtecan (DS-1062)
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| Organization |
ASTRAZENECA UK LIMITED | DAIICHI SANKYO COMPANY
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
3.5-4.5
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| Structure |
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| Antibody Name |
anti-TROP2 antibody
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Antibody Info | ||||
| Antigen Name |
Tumor-associated calcium signal transducer 2 (TACSTD2)
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Antigen Info | ||||
| Payload Name |
DX-8951 derivative (DXd)
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Payload Info | ||||
| Therapeutic Target |
DNA topoisomerase 1 (TOP1)
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Target Info | ||||
| Linker Name |
Mc-Gly-Gly-Phe-Gly
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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| Combination Type |
Deruxtecan
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General Information of The Activity Data Related to This ADC
Discovered Using Patient-derived Xenograft Model
Discovered Using Cell Line-derived Xenograft Model
| Standard Type | Value | Units | Cell Line | Disease Model |
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| Tumor Growth lnhibition value (TGl) |
82
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%
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Undisclosed | Undisclosed |
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Patient-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) | 72% | Positive TROP2 expression (TROP2+++/++) | ||
| Method Description |
This PDX was obtained in accordance with appropriate consent procedures. This ovarian PDX model was subcutaneously passaged in vivo as fragments from animal to animal in nude mice. When tumors reached approximately 250 mm 3 similar-sized tumors were randomly assigned to treatment groups, DS-1062 was administered as a single dose at 10 mg/kg on day 1. Duration of dosing was 21 days. TGI responses (Day 28 TGI%) was measurede.
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| In Vivo Model | CTG-3718 human patient-derived xenograft (PDX) model | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) | 88% | Positive TROP2 expression (TROP2+++/++) | ||
| Method Description |
Female Nude mice (Charles River) aged 5-8 weeks were used, following 7 days acclimatisation before entry into the study. The human patient-derived xenograft (PDX) model, CTG-3303, was established from fragments of freshly resected tumor of a triple negative breast cancer (TNBC) patient whom relapsed on treatment with PARP inhibitor talazoparib. This PDX was obtained in accordance with appropriate consent procedures. This TNBC PDX model was subcutaneously passaged in vivo as fragments from animal to animal in nude mice. When tumors reached approximately 250 mm 3 , similar-sized tumors were randomly assigned to treatment groups. DS-1062 was administered as a single dose at 10 mg/kg on day 1. Duration of dosing schedule was 21 days. TGI responses (Day 46 TGI%) was measurede.
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| In Vivo Model | CTG-3303 human patient-derived xenograft (PDX) model | ||||
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) | 82% | Positive TROP2 expression (TROP2+++/++) | ||
| Method Description |
Nude mice (Charles River) aged 5-8 weeks wereused,following 7 days acclimatisation before entry intothe study.5x106 NCI-N87 tumor cells (gastric cancercell line) (1:1 in Matrigel)were implantedsubcutaneously onto the flank of the female Nude mice.When tumors reached approximately 250 mm,similar-sizedtumors were randomly assigned to treatment groups, DS-1062 was administered as a single dose at 10 mg/kg on day 1. Duration of dosing schedule was 21 days.
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| In Vivo Model | NCI-N87 Xenograft model | ||||
