Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0NANHM
ADC Name
Trastuzumab-T1000-exatecan
Synonyms
MTX-1000
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 2 Indication(s)
Colon cancer [ICD11:2B90]
Investigative
Lung cancer [ICD11:2C25]
Investigative
Antibody Name
Trastuzumab
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
Exatecan
  Payload Info 
Therapeutic Target
DNA topoisomerase 1 (TOP1)
  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 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 59
%
MDA-MB-468 cells
Breast adenocarcinoma
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) ≈ 59.00% (Day 27) Negative HER2 expression (HER2 -)
Method Description
T moiety (We conducted a four-week (day 1, 8, 15, 22, and 29) intermittent intravenous dose toxicity study of exatecan mesylate in rats (six animals/group) with a four-week recovery period (three of the six animals).
In Vivo Model MDA-MB-468 CDX model
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
References
Ref 1 Antibody-Exatecan Conjugates with a Novel Self-immolative Moiety Overcome Resistance in Colon and Lung Cancer. Cancer Discov. 2023 Apr 3;13(4):950-973. doi: 10.1158/2159-8290.CD-22-1368.

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