Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0ULZKE
ADC Name
Fv-LDP-D3-AE
Synonyms
Fv-LDP-D3 AE
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Drug Status
Investigative
Indication
In total 2 Indication(s)
Esophageal cancer [ICD11:2B70]
Investigative
Esophageal squamous cell carcinoma [ICD11:2B71]
Investigative
Antibody Name
Fv-LDP-D3
  Antibody Info 
Antigen Name
Epidermal growth factor receptor (EGFR)
  Antigen Info 
Payload Name
Lidamycin
  Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
  Target Info 
Linker Name
Undisclosed
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) 
≈ 64
%
KYSE-150 cells
Esophageal squamous cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 73
%
KYSE-150 cells
Esophageal squamous cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 81
%
KYSE-150 cells
Esophageal squamous cell 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) 
33
ng/mL
KYSE-150 cells
Esophageal squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
44
ng/mL
KYSE-520 cells
Esophageal squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
75
ng/mL
Eca-109 cells
Esophageal squamous cell 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) ≈ 64.00% (Day 28) High EGFR expression (EGFR+++)
Method Description
KYSE150 cells (5 10 6 cells/200 L) suspended in PBS were inoculated subcutaneously into the right armpit of athymic mice. When the tumor volume reached about 80mm3, nude mice were randomized into two groups (n=6, per group), a control group and a Fv-LDP-D3-AE (0.2 mg/kg) group. The drug treatment group was given by tail vein injection once a week for two consecutive weeks.

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In Vivo Model Esophageal squamous cell carcinoma CDX model
In Vitro Model Esophageal squamous cell carcinoma KYSE-150 cells CVCL_1348
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 73.00% (Day 28) High EGFR expression (EGFR+++)
Method Description
KYSE150 cells (5 10 6 cells/200 L) suspended in PBS were inoculated subcutaneously into the right armpit of athymic mice. When the tumor volume reached about 80mm3, nude mice were randomized into two groups (n=6, per group), a control group and a Fv-LDP-D3-AE (0.25 mg/kg) group. The drug treatment group was given by tail vein injection once a week for two consecutive weeks.

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In Vivo Model Esophageal squamous cell carcinoma CDX model
In Vitro Model Esophageal squamous cell carcinoma KYSE-150 cells CVCL_1348
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 81.00% (Day 28) High EGFR expression (EGFR+++)
Method Description
KYSE150 cells (5 10 6 cells/200 L) suspended in PBS were inoculated subcutaneously into the right armpit of athymic mice. When the tumor volume reached about 80mm3, nude mice were randomized into two groups (n=6, per group), a control group and a Fv-LDP-D3-AE (0.5 mg/kg) group. The drug treatment group was given by tail vein injection once a week for two consecutive weeks.

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In Vivo Model Esophageal squamous cell carcinoma CDX model
In Vitro Model Esophageal squamous cell carcinoma KYSE-150 cells CVCL_1348
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 [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 33.00 ng/mL High EGFR expression (EGFR+++)
Method Description
The CCK8 method was used to evaluate the cytotoxicity of Fv-LDP-D3 and Fv-LDP-D3-AE in KYSE150, KYSE520, and Eca109 cells.
In Vitro Model Esophageal squamous cell carcinoma KYSE-150 cells CVCL_1348
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 44.00 ng/mL High EGFR expression (EGFR+++)
Method Description
The CCK8 method was used to evaluate the cytotoxicity of Fv-LDP-D3 and Fv-LDP-D3-AE in KYSE150, KYSE520, and Eca109 cells.
In Vitro Model Esophageal squamous cell carcinoma KYSE-520 cells CVCL_1355
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 75.00 ng/mL Moderate EGFR expression (EGFR++)
Method Description
The CCK8 method was used to evaluate the cytotoxicity of Fv-LDP-D3 and Fv-LDP-D3-AE in KYSE150, KYSE520, and Eca109 cells.
In Vitro Model Esophageal squamous cell carcinoma Eca-109 cells CVCL_6898
References
Ref 1 A recombinant scFv antibody-based fusion protein that targets EGFR associated with IMPDH2 downregulation and its drug conjugate show therapeutic efficacy against esophageal cancer. Drug Deliv. 2022 Dec;29(1):1243-1256.

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