Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0YFLRB
ADC Name
AXL02
Synonyms
AXL02-vc-MMAE
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Drug Status
Investigative
Indication
In total 2 Indication(s)
Non-small cell lung cancer [ICD11:2C25]
Investigative
Triple negative breast cancer [ICD11:2C60-2C65]
Investigative
Drug-to-Antibody Ratio
4
Structure
Antibody Name
AXL Anti-ody YW327.6S2
  Antibody Info 
Antigen Name
Tyrosine-protein kinase receptor UFO (AXL)
  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
The free sulfhydryl group obtained by the reduction of interchain cysteine is site-specific conjugated with maleimide, michael addition reaction.
Combination Type
BL20-MMAE
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 Inhibition value (TGI) 
≈ 96.1
%
PC-9 cells
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 96.7
%
NCI-H1299 cells
Lung large cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 98.7
%
LCLC-103H cells
Lung large cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 99.5
%
U-87MG cells
Glioblastoma
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 Inhibition value (TGI) ≈ 96.10% (Day 35) High AXL expression (AXL+++)
Method Description
Cells were suspended in PBS then injected subcutaneously to the flank of Balb/c female nude mice (46 weeks old). Tumors were measured by caliper every 23 days. Before therapeutic treatment,tumor-bearing mice were staged at initial tumor volume of 100 to 300 mm3 (growth) or 1800 mm3 (regression) and randomized into treatment groups(n = 8). The ADCs were dosed i.v. once weekly,or total twice during entire study.

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In Vivo Model Lung cancer CDX model
In Vitro Model Lung adenocarcinoma PC-9 cells CVCL_B260
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.70% (Day 35) High AXL expression (AXL+++)
Method Description
Cells were suspended in PBS then injected subcutaneously to the flank of Balb/c female nude mice (46 weeks old). Tumors were measured by caliper every 23 days. Before therapeutic treatment,tumor-bearing mice were staged at initial tumor volume of 100 to 300 mm3 (growth) or 1800 mm3 (regression) and randomized into treatment groups(n = 8). The ADCs were dosed i.v. once weekly,or total twice during entire study.

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In Vivo Model Non-small cell lung cancer CDX model
In Vitro Model Lung large cell carcinoma NCI-H1299 cells CVCL_0060
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.70% (Day 35) High AXL expression (AXL+++)
Method Description
Cells were suspended in PBS then injected subcutaneously to the flank of Balb/c female nude mice (46 weeks old). Tumors were measured by caliper every 23 days. Before therapeutic treatment,tumor-bearing mice were staged at initial tumor volume of 100 to 300 mm3 (growth) or 1800 mm3 (regression) and randomized into treatment groups(n = 8). The ADCs were dosed i.v. once weekly,or total twice during entire study.

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In Vivo Model Lung cancer CDX model
In Vitro Model Lung large cell carcinoma LCLC-103H cells CVCL_1375
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.50% (Day 32) High AXL expression (AXL+++)
Method Description
Cells were suspended in PBS then injected subcutaneously to the flank of Balb/c female nude mice (46 weeks old). Tumors were measured by caliper every 23 days. Before therapeutic treatment,tumor-bearing mice were staged at initial tumor volume of 100 to 300 mm3 (growth) or 1800 mm3 (regression) and randomized into treatment groups(n = 8). The ADCs were dosed i.v. once weekly,or total twice during entire study.

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In Vivo Model Astrocytic glioblastoma CDX model
In Vitro Model Glioblastoma U-87MG cells CVCL_0022
References
Ref 1 AXL antibody and AXL-ADC mediate antitumor efficacy via targeting AXL in tumor-intrinsic epithelial-mesenchymal transition and tumor-associated M2-like macrophage. Acta Pharmacol Sin. 2023 Jun;44(6):1290-1303.

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