Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
ADC ID |
DRG0LJDDS
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ADC Name |
Pertuzumab-Compound(la)
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Synonyms |
Pertuzumab Compound(la)
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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 | ||||||
Antibody Name |
Pertuzumab
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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 |
Pertuzumab-Compound(la) 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
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 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 | ||
Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 67.00% (Day 22) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Mice were orthotopically implanted with 1x107 HCC1569 human breast cancer cells suspended in amixture of Matrigel and culture media in the inguinal fat pad. Following group allocation, mice were treated with a single 10 ml/kg lateral tail vein injection of a Pertuzumab-Compound (la) conjugate at 3 mg/kg.
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In Vivo Model | HCC1569 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | HCC1569 cells | CVCL_1255 | ||
Experiment 3 Reporting the Activity Date of This ADC | [2] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 95.00% (Day 22) | Positive HER2 expression (HER2 +++/++) | ||
Method Description |
Mice were orthotopically implanted with 1x107 HCC1569 human breast cancer cells suspended in amixture of Matrigel and culture media in the inguinal fat pad. Following group allocation, mice were treated with a single 10 ml/kg lateral tail vein injection of a Pertuzumab-Compound (la) conjugate at 10 mg/kg.
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In Vivo Model | HCC1569 CDX model | ||||
In Vitro Model | Breast ductal carcinoma | HCC1569 cells | CVCL_1255 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 4.19 pM | High HER2 expression (HER2+++) | ||
Method Description |
The cells, at a predetermined concentration, were plated into 96 well plates, and, after overnight incubation at 37°C/5% CO2, serial dilutions of each test article (TA) were added to the cells. Cells were incubated with test articles for 72 hours. and viability was detected with CellTiter-Gloreagent.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.11 nM
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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 | Adult hepatocellular carcinoma | SNU-182 cells | CVCL_0090 | ||
Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 14.00 nM | 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 |
References
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