Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0XKVWL
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| ADC Name |
Trastuzumab-Compound (la) DAR 1.6
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| Synonyms |
Trastuzumab Compound (la) DAR 1.6
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| Organization |
Orum Therapeutics, Inc.
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| Drug Status |
Investigative
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| Indication |
In total 2 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
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| Drug-to-Antibody Ratio |
1.6
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| Structure |
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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 |
NeoDegrader P1
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Payload Info | ||||
| Therapeutic Target |
Protein cereblon (CRBN)
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Target Info | ||||
| Linker Name |
Trastuzumab-Compound (la) DAR 1.6 linker
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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
| Standard Type | Value | Units | Cell Line | Disease Model |
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| Half Maximal Inhibitory Concentration (IC50) |
25
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pM
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BT-474 cells
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Invasive breast carcinoma
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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) | ≈ 0.00% (Day 42) | Positive CD20 expression (CD20+++/++) | ||
| Method Description |
Daudi human NHL fragments were implanted subcutaneously in theright flank of the mice. Mice were divided into 4 treatment groups (N=8/group), as follows: trastuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (1 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (5 mg/kg, iv, qd x 1).
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| In Vivo Model | Daudi CDX model | ||||
| In Vitro Model | Burkitt lymphoma | Daudi cells | CVCL_0008 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 25.30% (Day 24) | Positive CD33 expression (CD33+++/++) | ||
| Method Description |
HL-60 human AML fragments were implanted subcutaneously in theright flank of the mice. Mice were divided into 4 treatment groups (N=8/group), as follows: trastuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (1 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (5 mg/kg, iv, qd x 1).
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| In Vivo Model | HL-60 CDX model | ||||
| In Vitro Model | Adult acute myeloid leukemia | HL-60 cells | CVCL_0002 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 82.76% (Day 30) | High HER2 expression (HER2+++) | ||
| Method Description |
BT474 human breast carcinomas fragments were implanted subcutaneously in theright flank of the mice. Mice were divided into 4 treatment groups (N=8/group), as follows: trastuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); pertuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1).
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| In Vivo Model | BT-474 CDX model | ||||
| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 25.00 pM | High HER2 expression (HER2+++) | ||
| Method Description |
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
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