Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0JMIOG
ADC Name
LSR-ADC
Synonyms
LSR ADC
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Drug Status
Investigative
Indication
In total 1 Indication(s)
Epithelial ovarian cancer [ICD11:2B5D]
Investigative
Drug-to-Antibody Ratio
2.8
Structure
Antibody Name
Anti-LSR mAb
  Antibody Info 
Antigen Name
Lipolysis-stimulated lipoprotein receptor (LSR)
  Antigen Info 
Payload Name
Monomethyl auristatin E
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
Mc-Val-Cit-PABC
  Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
Vedotin
General Information of The Activity Data Related to This ADC
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI) 
≈ 44.53
%
Ovarian cancer PDX model (PDX: Ovx6)
Tumor Growth Inhibition value (TGI) 
≈ 55.47
%
Ovarian cancer PDX model (PDX: Ovx6)
Tumor Growth Inhibition value (TGI) 
≈ 67.5
%
Ovarian high-grade serous carcinoma PDX model (PDX: OVCAR3-LUC)
Tumor Growth Inhibition value (TGI) 
≈ 97.24
%
Ovarian cancer PDX model (PDX: Ovx6)
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) 
≈ 21.41
%
OVCAR-3 cells
Ovarian serous adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 46.43
%
OVCAR-3 cells
Ovarian serous adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 99.01
%
OVCAR-3 cells
Ovarian serous adenocarcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
449
pM
OVCAR-3 cells
Ovarian serous adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.19
nM
OVCAR-3 Luc cells
Ovarian serous adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
1.74
nM
NOVC-7C cells
Ovarian cancer ascites
Half Maximal Inhibitory Concentration (IC50) 
> 10
uM
ES2 cells
Ewing sarcoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 44.53% (Day 70) High LSR expression (LSR+++; 89,382.9 LSR expression (ABC/cell))
Method Description
The model was Ovx6 PDX,which was generated by implanting human tumor tissues expressing LSR at high levels. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (1 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model Ovarian cancer PDX model (PDX: Ovx6)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 55.47% (Day 70) High LSR expression (LSR+++; 89,382.9 LSR expression (ABC/cell))
Method Description
The model was Ovx6 PDX,which was generated by implanting human tumor tissues expressing LSR at high levels. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (3 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model Ovarian cancer PDX model (PDX: Ovx6)
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 67.50% (Day 21) High LSR expression (LSR+++; 89,382.9 LSR expression (ABC/cell))
Method Description
To assess the efficacy of LSR-ADC against omental/bowel metastasis,OVCAR3-Luc xenograft models were used. The OVCAR3-Luc xenograft models was established by implanting OVCAR3-Luc cells intraperitoneally,into the subscapular areas. Six or seven weeks after the inoculation,the treatment was initiated. PBS and 10 mg/kg of LSR-ADC were intravenously injected twice a week,for a total of four times.

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In Vivo Model Ovarian high-grade serous carcinoma PDX model (PDX: OVCAR3-LUC)
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.24% (Day 70) High LSR expression (LSR+++; 86,697.7 LSR expression (ABC/cell))
Method Description
The model was Ovx6 PDX,which was generated by implanting human tumor tissues expressing LSR at high levels. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (10 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model Ovarian cancer PDX model (PDX: Ovx6)
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) ≈ 21.41% (Day 28) High LSR expression (LSR+++)
Method Description
The model was established by subcutaneously implanting OVCAR3 cells into CB17/SCID mice. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (1 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model Ovarian high-grade serous carcinoma CDX model
In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 46.43% (Day 28) High LSR expression (LSR+++)
Method Description
The model was established by subcutaneously implanting OVCAR3 cells into CB17/SCID mice. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (3 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model Ovarian high-grade serous carcinoma CDX model
In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.01% (Day 28) High LSR expression (LSR+++)
Method Description
The model was established by subcutaneously implanting OVCAR3 cells into CB17/SCID mice. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (10 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model Ovarian high-grade serous carcinoma CDX model
In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 449.00 pM High LSR expression (LSR+++; 89,382.9 LSR expression (ABC/cell))
Method Description
Cytotoxicity assays were performed in the presence of the anti-LSR mAb (#16-6),the mouse IgG2a isotype control antibody,the LSR-ADC or the control-ADC. After 24 h,the cells were incubated with serial dilutions of the agents in triplicate wells for 144 h,at 37°C,in a humidified 5% CO2 atmosphere. Cell viability was determined with the CellTiter-Glo Luminescent Cell Viability Assay Kit.

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In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.19 nM High LSR expression (LSR+++; 86,697.7 LSR expression (ABC/cell))
Method Description
Cytotoxicity assays were performed in the presence of the anti-LSR mAb (#16-6),the mouse IgG2a isotype control antibody,the LSR-ADC or the control-ADC. After 24 h,the cells were incubated with serial dilutions of the agents in triplicate wells for 144 h,at 37°C,in a humidified 5% CO2 atmosphere. Cell viability was determined with the CellTiter-Glo Luminescent Cell Viability Assay Kit.

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In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 Luc cells CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1.74 nM High LSR expression (LSR+++; 84,008.8 LSR expression (ABC/cell))
Method Description
Cytotoxicity assays were performed in the presence of the anti-LSR mAb (#16-6),the mouse IgG2a isotype control antibody,the LSR-ADC or the control-ADC. After 24 h,the cells were incubated with serial dilutions of the agents in triplicate wells for 144 h,at 37°C,in a humidified 5% CO2 atmosphere. Cell viability was determined with the CellTiter-Glo Luminescent Cell Viability Assay Kit.

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In Vitro Model Ovarian cancer ascites NOVC-7C cells Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 uM Moderate LSR expression (LSR++; 2,631.9 LSR expression (ABC/cell))
Method Description
Cytotoxicity assays were performed in the presence of the anti-LSR mAb (#16-6),the mouse IgG2a isotype control antibody,the LSR-ADC or the control-ADC. After 24 h,the cells were incubated with serial dilutions of the agents in triplicate wells for 144 h,at 37°C,in a humidified 5% CO2 atmosphere. Cell viability was determined with the CellTiter-Glo Luminescent Cell Viability Assay Kit.

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In Vitro Model Ewing sarcoma ES2 cells CVCL_AX39
References
Ref 1 Lipolysis-stimulated lipoprotein receptor-targeted antibody-drug conjugate demonstrates potent antitumor activity against epithelial ovarian cancer. Neoplasia. 2023 Jan;35:100853.

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