Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0UYCLU
ADC Name
AU2023308528A1 ADC2
Synonyms
AU2023308528A1 ADC2
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Organization
PHEON THERAPEUTICS LTD
Drug Status
Investigative
Drug-to-Antibody Ratio
4.2
Structure
Antibody Name
Trastuzumab
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
PBD-butanamide derivative
  Payload Info 
Therapeutic Target
DNA topoisomerase I (TOP1)
  Target Info 
Linker Name
6-Maleimidocaproic acid
  Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
N- (4- ((S)-2- ((S)-2- (6- (2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamido)-3 methylbutanamido)propanamido)phenyl)-4- (4- (( (S)-2-methoxy-12-oxo-6a,7,8,9,10,12 hexahydrobenzo[e]pyrido[1,2-a][1,4]diazepin-3-yl)oxy)butanamido)-1-methyl-1H pyrrole-2-carboxamide
General Information of The ADMET Data Related to This ADC(2027 Update)
Excretion
Click To Hide/Show 1 Excretion Data Related to This Level
Standard Type Value Units Description Reference
Clearance (CL) >50 %
The PK profile of unconjugated mAb and ADC2 was examined in male CD1 mouse plasma for 7 days.
 [1]
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth lnhibition value (TGl) 
> 50
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
> 75
%
Undisclosed Undisclosed
Complete Remission (CR)  . . Undisclosed Undisclosed
Complete Remission (CR)  . . Undisclosed Undisclosed
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 50%
Method Description
mean tumour volume versus time after multiple doses of ADC2 (either Days 1, 8 and 15 or Days 1, 22 and 43) against MDA-MB-231 at 5 mg/kg.
In Vivo Model MDA-MB-231 Xenograft Model
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 75%
Method Description
one dose of ADC2 (Day 1) against MDA-MB-231 at 5 mg/kg, single IV.
In Vivo Model MDA-MB-231 Xenograft Model
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Complete Remission (CR) . . .
Method Description
one dose of ADC2 (Day 1) against MDA-MB-231 at 10 mg/kg, single IV.
In Vivo Model MDA-MB-231 Xenograft Model
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Complete Remission (CR) . . .
Method Description
mean tumour volume versus time after multiple doses of ADC2 (either Days 1, 8 and 15 or Days 1, 22 and 43) against MDA-MB-231 at 10 mg/kg.
In Vivo Model MDA-MB-231 Xenograft Model
References
Ref 1 Antibody-drug conjugates