Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0OVEOI
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| ADC Name |
LRG1-ADC 5
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| Synonyms |
LRG1 ADC 5; Magacizumab PD-MMAE ADC 5
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| Drug Status |
Investigative
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| Indication |
In total 1 Indication(s)
Investigative
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| Drug-to-Antibody Ratio |
4
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| Structure |
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| Antibody Name |
Magacizumab
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Antibody Info | ||||
| Antigen Name |
Leucine-rich alpha-2-glycoprotein (LRG1)
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Antigen Info | ||||
| Payload Name |
Monomethyl auristatin E
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Dipeptide-diBrPD (dibromopyridazinedione )
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Linker Info | ||||
| Conjugate Type |
Rebridge conjugation through reduced inter-chain cysteines.
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General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
| Standard Type | Value | Units | Cell Line | Disease Model |
|---|---|---|---|---|
| Tumor Growth Inhibition value (TGI) |
≈ 52.4
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%
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Melanoma cells
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Melanoma
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Revealed Based on the Cell Line Data
| Standard Type | Value | Units | Cell Line | Disease Model |
|---|---|---|---|---|
| Half Maximal Inhibitory Concentration (IC50) |
0.9
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nM
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B16-F0 cells
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Mouse melanoma
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Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
| 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
| 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
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