General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0LJDDS
ADC Name
Pertuzumab-Compound(la)
Synonyms
Pertuzumab Compound(la)
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Organization
Orum Therapeutics, Inc.
Drug Status
Investigative
Indication
In total 2 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
Drug-to-Antibody Ratio
1.6
Structure
Antibody Name
Pertuzumab
 Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
 Antigen Info 
Payload Name
NeoDegrader P1
 Payload Info 
Therapeutic Target
Protein cereblon (CRBN)
 Target Info 
Linker Name
Pertuzumab-Compound(la) linker
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 0
%
BT-474 cells
Invasive breast carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 67
%
HCC1569 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 95
%
HCC1569 cells
Breast ductal carcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
4.19
pM
BT-474 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.11
nM
SNU-182 cells
Adult hepatocellular carcinoma
Half Maximal Inhibitory Concentration (IC50) 
14
nM
BT-474 cells
Invasive breast carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
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).
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.
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.
In Vivo Model HCC1569 CDX model
In Vitro Model Breast ductal carcinoma HCC1569 cells CVCL_1255
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
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.
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
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.
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.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
References
Ref 1 Neodegrader conjugates; 2021-10-07.
Ref 2 Linkers for use in antibody drug conjugates; 2023-03-16.

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