Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0REALL
ADC Name
EDB-ADC
Synonyms
EDB ADC; EDBADC
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 5 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Head and neck cancer [ICD11:2B60-2B6E]
Investigative
Non-small cell lung cancer [ICD11:2C25]
Investigative
Ovarian cancer [ICD11:2C73]
Investigative
Pancreatic cancer [ICD11:2C10]
Investigative
Drug-to-Antibody Ratio
3.9
Structure
Antibody Name
Anti-EDB-FN L19
  Antibody Info 
Antigen Name
Fibronectin (FN1)
  Antigen Info 
Payload Name
Auristatin 0101
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
Mc-Val-Cit-PABC
  Linker Info 
Conjugate Type
Site-specific conjugated of maleimidocaproyl with cysteine free thiol via Michael addition.
Combination Type
Pelidotin
General Information of The Activity Data Related to This ADC
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 6 Activity Data Related to This Level
Standard Type Value Units Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Pancreatic cancer PDX model (PDX: PDX-PAX-13565)
Tumor Growth Inhibition value (TGI) 
≈ 26.2
%
Pancreatic cancer PDX model (PDX: PDX-PAX-13565)
Tumor Growth Inhibition value (TGI) 
≈ 43.2
%
Nonsmall cell lung cancer PDX model (PDX: PDX-NSX-11122)
Tumor Growth Inhibition value (TGI) 
≈ 79.3
%
Nonsmall cell lung cancer PDX model (PDX: PDX-NSX-11122)
Tumor Growth Inhibition value (TGI) 
≈ 87.8
%
Pancreatic cancer PDX model (PDX: PDX-PAX-13565)
Tumor Growth Inhibition value (TGI) 
≈ 97.2
%
Nonsmall cell lung cancer PDX model (PDX: PDX-NSX-11122)
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) 
≈ 67
%
NCI-H1975 cells
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 80.1
%
NCI-H1975 cells
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
NCI-H1975 cells
Lung adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 6 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 14) High FN1 expression (FN1+++)
Method Description
EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Mice were treated intravenously every 4 days with phosphate-buffered saline (PBS),Neg-vc0101 (Neg-ADC),EDC-vc0101 (EDB-ADC). This tumor model was injected intravenously with EDB-ADC 0.75 mg/kg q4dx4.
In Vivo Model Pancreatic cancer PDX model (PDX: PDX-PAX-13565)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 26.20% (Day 14) High FN1 expression (FN1+++)
Method Description
EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Mice were treated intravenously every 4 days with phosphate-buffered saline (PBS),Neg-vc0101 (Neg-ADC),EDC-vc0101 (EDB-ADC). This tumor model was injected intravenously with EDB-ADC 1.5 mg/kg q4dx4.
In Vivo Model Pancreatic cancer PDX model (PDX: PDX-PAX-13565)
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 43.20% (Day 28) High FN1 expression (FN1+++)
Method Description
EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Mice were treated intravenously every 4 days with phosphate-buffered saline (PBS),Neg-vc0101 (Neg-ADC),EDC-vc0101 (EDB-ADC). This tumor model was injected intravenously with EDB-ADC 0.3 mg/kg q4dx4.
In Vivo Model Nonsmall cell lung cancer PDX model (PDX: PDX-NSX-11122)
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 79.30% (Day 28) High FN1 expression (FN1+++)
Method Description
EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Mice were treated intravenously every 4 days with phosphate-buffered saline (PBS),Neg-vc0101 (Neg-ADC),EDC-vc0101 (EDB-ADC). This tumor model was injected intravenously with EDB-ADC 1 mg/kg q4dx4.
In Vivo Model Nonsmall cell lung cancer PDX model (PDX: PDX-NSX-11122)
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 87.80% (Day 14) High FN1 expression (FN1+++)
Method Description
EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Mice were treated intravenously every 4 days with phosphate-buffered saline (PBS),Neg-vc0101 (Neg-ADC),EDC-vc0101 (EDB-ADC). This tumor model was injected intravenously with EDB-ADC 3 mg/kg q4dx4.
In Vivo Model Pancreatic cancer PDX model (PDX: PDX-PAX-13565)
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.20% (Day 28) High FN1 expression (FN1+++)
Method Description
EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Mice were treated intravenously every 4 days with phosphate-buffered saline (PBS),Neg-vc0101 (Neg-ADC),EDC-vc0101 (EDB-ADC). This tumor model was injected intravenously with EDB-ADC 3 mg/kg q4dx4.
In Vivo Model Nonsmall cell lung cancer PDX model (PDX: PDX-NSX-11122)
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) ≈ 67.00% (Day 15) High FN1 expression (FN1+++)
Method Description
EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Athymic nu/nu nude mice were injected subcutaneously in the right flank with 8 10 6 cells suspended in 100% Matrigel. This tumor model was injected intravenously with EDB-ADC 1 mg/kg q4dx4.
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.10% (Day 15) High FN1 expression (FN1+++)
Method Description
EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Athymic nu/nu nude mice were injected subcutaneously in the right flank with 8 10 6 cells suspended in 100% Matrigel. This tumor model was injected intravenously with EDB-ADC 3 mg/kg q4dx4.
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 30) High FN1 expression (FN1+++)
Method Description
EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Athymic nu/nu nude mice were injected subcutaneously in the right flank with 8 10 6 cells suspended in 100% Matrigel. This tumor model was injected intravenously with EDB-ADC 3 mg/kg q4dx4.
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
References
Ref 1 Anti-Extra Domain B Splice Variant of Fibronectin Antibody-Drug Conjugate Eliminates Tumors with Enhanced Efficacy When Combined with Checkpoint Blockade. Mol Cancer Ther. 2022 Sep 6;21(9):1462-1472.

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