General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0FTEON
ADC Name
Anti-PIEZO1-MMAE
Synonyms
AntiPIEZO1 MMAE
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Drug Status
Investigative
Indication
In total 1 Indication(s)
Esophageal squamous cell carcinoma [ICD11:2B71]
Investigative
Drug-to-Antibody Ratio
4
Structure
Antibody Name
Anti-PIEZO1 mAb
 Antibody Info 
Antigen Name
Piezo-type mechanosensitive ion channel component 1 (PIEZO1)
 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 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 80
%
Esophageal squamous cell carcinoma 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 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.00% (Day 27) High PIEZO1 expression (PIEZO1+++)
Method Description
1 x107 TE1 cells were suspended in Matrigel and injected subcutaneously in the right armpit. The treatment of AntiPIEZO1MMAE or control reagents started when the tumor volume reached 300mm3. Treatments for each group were given every 3 days in total four times.
In Vivo Model Esophageal squamous cell carcinoma CDX model
In Vitro Model Esophageal squamous cell carcinoma Esophageal squamous cell carcinoma cells Homo sapiens
References
Ref 1 High-throughput membrane-anchored proteome screening reveals PIEZO1 as a promising antibody-drug target for human esophageal squamous cell carcinoma. Cancer Med. 2022 Oct;11(19):3700-3713.

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