Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0MKAIK
ADC Name
wO2025019776A2ADC 52-2
Synonyms
WO2025019776A2ADC 52-2
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Organization
EXELIXIS, INC.
Drug Status
Investigative
Drug-to-Antibody Ratio
2
Structure
Antibody Name
A52
  Antibody Info 
Antigen Name
Interleukin-13 receptor subunit alpha-2 (IL13RA2)
  Antigen Info 
Payload Name
Monomethyl auristatin E
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
WO2025019776A2, ADC 22-2, Linker
  Linker Info 
Conjugate Type
Random conjugation through nuckeophilic lysines
Combination Type
Vb-82a
General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
Click To Hide/Show 1 Absorption Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) ≈2200000 hr&#42ng/mL
Male JVC/FVC cannulated Sprague-Dawley rats (5 per group)were dosed intravenously with a single dose of 5mg/kg of the tested ADC on Day 1 after 16 hours of fasting.100uL K2EDTA plasma was collected at 30 min,4h,24h (on Day 2),168h (on Day 8),240h (on Day 11),336h (on Day 15),and 504h (on Day 22)post-dose,saved in bullet tubes and stored at -24°C until end of the study.

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 [1]
Distribution
Click To Hide/Show 1 Distribution Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) ≈2200000 hr&#42ng/mL
Male JVC/FVC cannulated Sprague-Dawley rats (5 per group)were dosed intravenously with a single dose of 5mg/kg of the tested ADC on Day 1 after 16 hours of fasting.100uL K2EDTA plasma was collected at 30 min,4h,24h (on Day 2),168h (on Day 8),240h (on Day 11),336h (on Day 15),and 504h (on Day 22)post-dose,saved in bullet tubes and stored at -24°C until end of the study.

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 [1]
Metabolism
Click To Hide/Show 1 Metabolism Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) ≈2200000 hr&#42ng/mL
Male JVC/FVC cannulated Sprague-Dawley rats (5 per group)were dosed intravenously with a single dose of 5mg/kg of the tested ADC on Day 1 after 16 hours of fasting.100uL K2EDTA plasma was collected at 30 min,4h,24h (on Day 2),168h (on Day 8),240h (on Day 11),336h (on Day 15),and 504h (on Day 22)post-dose,saved in bullet tubes and stored at -24°C until end of the study.

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 [1]
Excretion
Click To Hide/Show 3 Excretion Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) ≈2200000 hr&#42ng/mL
Male JVC/FVC cannulated Sprague-Dawley rats (5 per group)were dosed intravenously with a single dose of 5mg/kg of the tested ADC on Day 1 after 16 hours of fasting.100uL K2EDTA plasma was collected at 30 min,4h,24h (on Day 2),168h (on Day 8),240h (on Day 11),336h (on Day 15),and 504h (on Day 22)post-dose,saved in bullet tubes and stored at -24°C until end of the study.

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 [1]
Clearance (CL) ≈2.3 mL/hr/kg
Male JVC/FVC cannulated Sprague-Dawley rats (5 per group)were dosed intravenously with a single dose of 5mg/kg of the tested ADC on Day 1 after 16 hours of fasting.100uL K2EDTA plasma was collected at 30 min,4h,24h (on Day 2),168h (on Day 8),240h (on Day 11),336h (on Day 15),and 504h (on Day 22)post-dose,saved in bullet tubes and stored at -25°C until end of the study.

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 [1]
Elimination Half-Life (t1/2) ≈80 hr
Male JVC/FVC cannulated Sprague-Dawley rats (5 per group)were dosed intravenously with a single dose of 5mg/kg of the tested ADC on Day 1 after 16 hours of fasting.100uL K2EDTA plasma was collected at 30 min,4h,24h (on Day 2),168h (on Day 8),240h (on Day 11),336h (on Day 15),and 504h (on Day 22)post-dose,saved in bullet tubes and stored at -25°C until end of the study.

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 [1]
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
0.01
nM
CVCL_0132
Amelanotic melanoma
Half Maximal inhibitory Concentration (lC50) 
0.02-0.03
nM
CVCL_1495
Lung adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.04-0.08
nM
CVCL_1543
Lung adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
3-63
nM
CVCL_0630
Lung squamous cell carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.01 nM High hIL13Ra2 expression (hIL13Ra2 +++)
Method Description
The cytotoxic activity of ADC 52-2 was determined against cancer cell lines A375.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model Amelanotic melanoma A375 cells CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.02-0.03 nM Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description
The cytotoxic activity of ADC 52-2 was determined against cancer cell lines H1792.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model Lung adenocarcinoma H1792 cells CVCL_1495
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.04-0.08 nM Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description
The cytotoxic activity of ADC 52-2 was determined against cancer cell lines H2228.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model Lung adenocarcinoma H2228 cells CVCL_1543
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 3-63 nM Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description
The cytotoxic activity of ADC 52-2 was determined against cancer cell lines SK-MES-1.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model Lung squamous cell carcinoma SK-MES-1 cells CVCL_0630
References
Ref 1 Interleukin-13 receptor subunit alpha-2 antibody-drug conjugates and uses thereof