Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0KJDBA
ADC Name
HzMUC1-MMAE
Synonyms
HzMUC1 MMAE; HzMUC1-ADC; HzMUC1 ADC
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Drug Status
Investigative
Indication
In total 1 Indication(s)
Pancreatic cancer [ICD11:2C10]
Investigative
Drug-to-Antibody Ratio
4
Structure
Antibody Name
HzMUC1
  Antibody Info 
Antigen Name
Mucin-1 (MUC1)
  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 Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 33.5
%
HCC1954 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 83.1
%
Pancreatic cancer cells
Pancreatic cancer
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) 
26
nM
Capan-2 cells
Pancreatic ductal adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
50
nM
CFPAC-1 cells
Pancreatic ductal adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
59
nM
PANC-1 cells
Pancreatic ductal adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 10
uM
SW1990 cells
Pancreatic adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 33.50% (Day 21) High MUC1 expression (MUC1+++)
Method Description
To examine the efficacy of the HzMUC1-MMAE in decreasing pancreatic tumor growth in vivo,pancreatic tumor xenograft mouse model was established. BALB/c nu/nu mice were subcutaneously injected with CFPAC-1 cells. When the CFPAC-1 tumors reached the sizes of 150 mm3,mice were randomized into two groups and treated with PBS and HzMUC1-MMAE (5 mg/kg,every 6 days,for 2 doses).

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In Vivo Model Pancreatic cancer CDX model
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 83.10% (Day 28) High MUC1 expression (MUC1+++)
Method Description
To examine the efficacy of the HzMUC1-MMAE in decreasing pancreatic tumor growth in vivo,pancreatic tumor xenograft mouse model was established. BALB/c nu/nu mice were subcutaneously injected with Capan-2 cells. When the Capan-2 tumors reached the sizes of 120 mm3,mice were randomized into two groups and treated with PBS and HzMUC1-MMAE (5 mg/kg,every 6 days,for 2 doses).

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In Vivo Model Pancreatic cancer CDX model
In Vitro Model Pancreatic cancer Pancreatic cancer cells Homo sapiens
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) 26.00 nM High MUC1 expression (MUC1+++)
Method Description
The inhibitory activity of HzMUC1-ADC against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model Pancreatic ductal adenocarcinoma Capan-2 cells CVCL_0026
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 50.00 nM High MUC1 expression (MUC1+++)
Method Description
The inhibitory activity of HzMUC1-ADC against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model Pancreatic ductal adenocarcinoma CFPAC-1 cells CVCL_1119
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 59.00 nM Moderate MUC1 expression (MUC1++)
Method Description
The inhibitory activity of HzMUC1-ADC against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 uM Negative MUC1 expression (MUC1-)
Method Description
The inhibitory activity of HzMUC1-ADC against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model Pancreatic adenocarcinoma SW1990 cells CVCL_1723
References
Ref 1 Therapeutic effect of a MUC1-specific monoclonal antibody-drug conjugates against pancreatic cancer model. Cancer Cell Int. 2022 Dec 27;22(1):417.

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