General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0OVEOI
ADC Name
LRG1-ADC 5
Synonyms
LRG1 ADC 5; Magacizumab PD-MMAE ADC 5
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Drug Status
Investigative
Indication
In total 1 Indication(s)
Melanoma [ICD11:2C30]
Investigative
Drug-to-Antibody Ratio
4
Structure
Antibody Name
Magacizumab
 Antibody Info 
Antigen Name
Leucine-rich alpha-2-glycoprotein (LRG1)
 Antigen Info 
Payload Name
Monomethyl auristatin E
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Dipeptide-diBrPD (dibromopyridazinedione )
 Linker Info 
Conjugate Type
Rebridge conjugation through reduced inter-chain cysteines.
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) 
≈ 52.4
%
Melanoma cells
Melanoma
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
0.9
nM
B16-F0 cells
Mouse melanoma
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) ≈ 52.40% (Day 16) Positive LRG1 expression (LRG1+++/++)
Method Description
Single-cell suspensions of 1 x106 B16F0 cells were injected subcutaneously into the lower back of Lrg1+/+ C57BL/6 mice in 100 mL PBS. Tumours were measured and therapy was initiated when tumour volumes reached 0.1 cm3. ADC was administered at a dose of 20 mg/kg treatments were administered by a single intraperitoneal injection every 7 days for 3 weeks.

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In Vivo Model Melanoma CDX model
In Vitro Model Melanoma Melanoma cells Homo sapiens
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.90 nM Positive LRG1 expression (LRG1+++/++)
Method Description
5 x104 cells were seeded in 96-well plates and incubated at 37 overnight. Cells were thenexposed to a range of concentrations of the test compounds diluted in growth medium at pH 6.5 and at 37 as ADC 5 (0100 nM, 72 h). MTT reagent (12 mM) was then added to each well and cells were incubated for 4 h at 37 , followed by the addition of DMSO and further incubation at 37 1C for 1 h.

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In Vitro Model Mouse melanoma B16-F0 cells CVCL_0604
References
Ref 1 Leucine-rich alpha-2-glycoprotein 1 (LRG1) as a novel ADC target. RSC Chem Biol. 2021 May 31;2(4):1206-1220.

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