Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0WUSYP
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| ADC Name |
T-DM1-IR700
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| Synonyms |
T-DM1-IRDye700DX
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| Drug Status |
Investigative
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| Indication |
In total 1 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
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| Drug-to-Antibody Ratio |
2+2
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| Antibody Name |
Trastuzumab
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Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
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Antigen Info | ||||
| Payload Name |
Mertansine DM1 plus IRDye700DX
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Succinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
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Linker Info | ||||
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) | ≈ 10.10% (Day 7) | Negative HER2 expression (HER2 -) | ||
| Method Description |
Tra-IR700 (3.6 ug/g) or T-DM1-IR700 (3.6 ug/g) was administered intravenously to mice on Day 1 (without NIR light, 6 days after tumor cell transplantation). The dose similar to that of T-DM1 administered to humans (3.6 mg/kg). The NIR-light was irradiated at 1 and 2 days after the drug administration.
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| In Vivo Model | MDA-MB-468GFP CDX model | ||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-468GFP cells | CVCL_DH83 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 36.40% (Day 7) | Negative HER2 expression (HER2 -) | ||
| Method Description |
Tra-IR700 (3.6 ug/g) or T-DM1-IR700 (3.6 ug/g) was administered intravenously to mice on Day 1 (without NIR light, 6 days after tumor cell transplantation). The dose similar to that of T-DM1 administered to humans (3.6 mg/kg). The NIR-light was irradiated at 1 and 2 days after the drug administration.
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| In Vivo Model | MDA-MB-468GFP CDX model | ||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-468GFP cells | CVCL_DH83 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.10 nM - 10 nM | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
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| In Vitro Model | Lung squamous cell carcinoma | NCI-H2170 cells | CVCL_1535 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.10 nM - 10 nM | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
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| In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.10 nM - 10 nM | Low HER2 expression (HER2+) | ||
| Method Description |
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.10 nM - 10 nM | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
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| In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 2.50 nM | Positive HER2 expression (HER2 +++/++) | ||
| Method Description |
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
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| In Vitro Model | Breast adenocarcinoma | 3T3/HER2-luc-GFP cells | Mus musculus | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 100 nM | Negative HER2 expression (HER2 -) | ||
| Method Description |
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468GFP cells | CVCL_DH83 | ||
References
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