Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0HPUIL
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| ADC Name |
Farletuzumab ecteribulin
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| Synonyms |
MORAb 202; MORAb-202; Eribulin/farletuzumab antibody drug conjugate; Farletuzumab/eribulin ADC; ER-001159569; VCP-Eribulin
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| Organization |
Eisai Co., Ltd.; Bristol Myers Squibb Co.
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| Drug Status |
Phase 2
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| Indication |
In total 7 Indication(s)
Fallopian tube cancer [ICD11:2C74]
Phase 2
Metastatic breast cancer [ICD11:2C6Y]
Phase 2
Non-small cell lung cancer [ICD11:2C25]
Phase 2
Ovary endometrioid adenocarcinoma [ICD11:2C73]
Phase 2
Peritoneal cancer [ICD11:2C51]
Phase 2
Solid tumors [ICD11:2A00-2A0Z|2B50-2F9Z]
Phase 2
Breast cancer [ICD11:2C60-2C65]
Phase 1
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| Drug-to-Antibody Ratio |
4
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| Structure |
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| Antibody Name |
Farletuzumab
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Antibody Info | ||||
| Antigen Name |
Folate receptor alpha (FOLR1)
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Antigen Info | ||||
| Payload Name |
Eribulin
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Mal-PEG2Val-Cit-PAB-OH
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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| Puchem SID | ||||||
| ChEBI ID | ||||||
General Information of The Activity Data Related to This ADC
Discovered Using Patient-derived Xenograft Model
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Patient-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 2.10% (Day 60) | Moderate FOLR1 expression (FOLR1++) | ||
| Method Description |
The each group was randomized to be a similar mean volume of 100-250 mm3.The treatment schedule was as follows: a single IV injection of vehicle at day 0, and a single IV injection of MORAb-202 at 2.5 mg/kg at day 0 ((Q1Dx1) or every 11 days (Q11Dx2)).
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| In Vivo Model | Breast cancer PDX model (PDX: OD-BRE-0631) | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 65.70% (Day 60) | Moderate FOLR1 expression (FOLR1++) | ||
| Method Description |
The each group was randomized to be a similar mean volume of 100-250 mm3.The treatment schedule was as follows: a single IV injection of vehicle at day 0, and a single IV injection of MORAb-202 at 5 mg/kg at day 0 ((Q1Dx1) or every 11 days (Q11Dx2)).
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| In Vivo Model | Breast cancer PDX model (PDX: OD-BRE-0631) | ||||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.30% (Day 60) | High FOLR1 expression (FOLR1+++) | ||
| Method Description |
The each group was randomized to be a similar mean volume of 100-250 mm3.The treatment schedule was as follows: a single IV injection of vehicle at day 0, and a single IV injection of MORAb-202 at 5 mg/kg at day 0 ((Q1Dx1) or every 11 days (Q11Dx2)).
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| In Vivo Model | Breast cancer PDX model (PDX: IM-BRE-563) | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.01 pM | High FOLR1 expression (FOLR1+++) | ||
| Method Description |
Threefold serial dilutions of MORAb-202 (5.1x1012 - 1.0x107 mol/L) were added to the cell lines, and the cells were cultured for 5 days. Cells were stained with 0.2% crystal violet solution, a triarylmethane dye which accumulates in the nucleus of viable cells, washed with water, and solubilized with 1% sodium dodecyl sulfate. The viable cell number was determined by measuring the optical density (OD 570 nm) of the resulting lysate.
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| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.74 pM | High FOLR1 expression (FOLR1+++) | ||
| Method Description |
Threefold serial dilutions of MORAb-202 (5.1x1012 - 1.0x107 mol/L) were added to the cell lines, and the cells were cultured for 5 days. Cells were stained with 0.2% crystal violet solution, a triarylmethane dye which accumulates in the nucleus of viable cells, washed with water, and solubilized with 1% sodium dodecyl sulfate. The viable cell number was determined by measuring the optical density (OD 570 nm) of the resulting lysate.
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| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1.00 pM | Negative FOLR1 expression (FOLR1-) | ||
| Method Description |
Threefold serial dilutions of MORAb-202 (5.1x1012 - 1.0x107 mol/L) were added to the cell lines, and the cells were cultured for 5 days. Cells were stained with 0.2% crystal violet solution, a triarylmethane dye which accumulates in the nucleus of viable cells, washed with water, and solubilized with 1% sodium dodecyl sulfate. The viable cell number was determined by measuring the optical density (OD 570 nm) of the resulting lysate.
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| In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 23.00 pM | Moderate FOLR1 expression (FOLR1++) | ||
| Method Description |
Threefold serial dilutions of MORAb-202 (5.1x1012 - 1.0x107 mol/L) were added to the cell lines, and the cells were cultured for 5 days. Cells were stained with 0.2% crystal violet solution, a triarylmethane dye which accumulates in the nucleus of viable cells, washed with water, and solubilized with 1% sodium dodecyl sulfate. The viable cell number was determined by measuring the optical density (OD 570 nm) of the resulting lysate.
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| In Vitro Model | Skin squamous cell carcinoma | A431-A3 cells | CVCL_0037 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.02 nM | High FOLR1 expression(FOLR1+++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.42 nM | Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.43 nM | Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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| In Vitro Model | Ovarian serous adenocarcinoma | Caov-3 cells | CVCL_0201 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.75 nM | Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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| In Vitro Model | Ovarian serous adenocarcinoma | OVCAR-3 cells | CVCL_0465 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 1.03 nM | Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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| In Vitro Model | Endometrial adenocarcinoma | HEC-59 cells | CVCL_2930 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 1.42 nM | Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 11 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 1.76 nM | Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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| In Vitro Model | Gastric tubular adenocarcinoma | MKN74 cells | CVCL_2791 | ||
| Experiment 12 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 1.81 nM | Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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| In Vitro Model | Endometrial adenocarcinoma | HEC-1-A cells | CVCL_0293 | ||
| Experiment 13 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 2.17 nM | Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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| In Vitro Model | Gastric tubular adenocarcinoma | MKN7 cells | CVCL_1417 | ||
| Experiment 14 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 4.42 nM | Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 15 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 13.15 nM | Moderate FOLR1 expression(FOLR1++) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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| In Vitro Model | Endometrial carcinoma | HEC-251 cells | CVCL_2927 | ||
| Experiment 16 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 24.58 nM | Low FOLR1 expression(FOLR1+) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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| In Vitro Model | Gastric carcinoma | NUGC-3 cells | CVCL_1612 | ||
| Experiment 17 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Negative FOLR1 expression(FOLR1-) | ||
| Method Description |
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
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| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
References
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