Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0YJCVC
ADC Name
ASG-15MF
Synonyms
ASG-15MF; AGS-15MF; ASG 15MF; ASG15MF
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 2 Indication(s)
Bladder cancer [ICD11:2C94]
Investigative
Lung cancer [ICD11:2C25]
Investigative
Drug-to-Antibody Ratio
4
Structure
Antibody Name
Sirtratumab
  Antibody Info 
Antigen Name
SLIT and NTRK-like protein 6 (SLITRK6)
  Antigen Info 
Payload Name
Monomethyl auristatin F
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
Maleimido-caproyl
  Linker Info 
Conjugate Type
Inter-chain cysteine.
Combination Type
Mafodotin
General Information of The Activity Data Related to This ADC
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI) 
≈ 62.9
%
Bladder cancer PDX model (PDX: AG-B8)
Tumor Growth Inhibition value (TGI) 
≈ 63.4
%
Bladder cancer PDX model (PDX: AG-B7)
Tumor Growth Inhibition value (TGI) 
≈ 80
%
Bladder cancer PDX model (PDX: AG-B8)
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) 
≈ 35.2
%
NCI-322M cells
Lung cancer
Tumor Growth Inhibition value (TGI) 
≈ 81.3
%
Bladder cancer cells
Bladder cancer
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Patient-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) ≈ 62.90% (Day 17) High SLITRK6 expression (SLITRK6+++; IHC H-score=250)
Method Description
PDX models were established by subcutaneous implantation of xenograft fragments (AG-B7 or AG-B8) in the flanks of SCID mice. When the tumor volume reached approximately 200 mm3,ASG-15MF was dosed at 0.25 mg/kg,2x per week i.v in AG-B8 PDX model. The last dose was given on day 14.
In Vivo Model Bladder cancer PDX model (PDX: AG-B8)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 63.40% (Day 25) High SLITRK6 expression (SLITRK6+++; IHC H-score=230)
Method Description
PDX models were established by subcutaneous implantation of xenograft fragments (AG-B7 or AG-B8) in the flanks of SCID mice. When the tumor volume reached approximately 200 mm3,ASG-15MF was dosed at 0.5 mg/kg,2x per week i.v in AG-B7 PDX model. The last dose was given on day 21.
In Vivo Model Bladder cancer PDX model (PDX: AG-B7)
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.00% (Day 17) High SLITRK6 expression (SLITRK6+++; IHC H-score=250)
Method Description
PDX models were established by subcutaneous implantation of xenograft fragments (AG-B7 or AG-B8) in the flanks of SCID mice. When the tumor volume reached approximately 200 mm3,ASG-15MF was dosed at 0.5 mg/kg,2x per week i.v in AG-B8 PDX model. The last dose was given on day 14.
In Vivo Model Bladder cancer PDX model (PDX: AG-B8)
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) ≈ 35.20% (Day 21) Moderate SLITRK6 expression (SLITRK6++; IHC H-score=185)
Method Description
CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. ASG-15MF was administered twice weekly at 3 mg/kg (n = 6) starting when the tumor volume reached approximately 200 mm3.
In Vivo Model NCI-322M CDX model
In Vitro Model Lung cancer NCI-322M cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 81.30% (Day 30) High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
Method Description
CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. When the tumor volume reached approximately 230 mm3, a single dose of ASG-15MF, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model Bladder cancer CDX model
In Vitro Model Bladder cancer Bladder cancer cells Homo sapiens
References
Ref 1 Development of ASG-15ME, a Novel Antibody-Drug Conjugate Targeting SLITRK6, a New Urothelial Cancer Biomarker. Mol Cancer Ther. 2016 Jun;15(6):1301-10.

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