Antibody Information
General Information of This Antibody
| Antibody ID | ANI0LHHXZ |
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| Antibody Name | Anti-EPHA2 mAb 1C1 |
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| Antibody Type | Monoclonal antibody (mAb) |
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| Antibody Subtype | Humanized IgG1-kappa |
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| Antigen Name | Ephrin type-A receptor 2 (EPHA2) |
Antigen Info | ||||
| Click to Show/Hide the Sequence Information of This Antibody | ||||||
| Heavy Chain Sequence |
EVQLLESGGGLVQPGGSLRLSCAASGFTFSHYMMAWVRQAPGKGLEWVSRIGPSGGPTHY
ADSVKGRFTISRDNSKNTLYLQMNSLRAEDTAVYYCAGYDSGYDYVAVAGPAEYFQHWGQ GTLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHT FPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSC Click to Show/Hide
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| Light Chain Sequence |
DIQMTQSPSSLSASVGDRVTITCRASQSISTWLAWYQQKPGKAPKLLIYKASNLHTGVPS
RFSGSGSGTEFSLTISGLQPDDFATYYCQQYNSYSRTFGQGTKVEIKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC Click to Show/Hide
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Each Antibody-drug Conjugate Related to This Antibody
Full Information of The Activity Data of The ADC(s) Related to This Antibody
CN106459205B ADC-2 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
42.20 ng/mL
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Positive EPHA2 expression (EPHA2+++/++) | ||
| Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
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| In Vitro Model | Prostate carcinoma | DU145 cells | CVCL_0105 | ||
CN106459205B ADC-4 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
53.90 ng/mL
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Positive EPHA2 expression (EPHA2+++/++) | ||
| Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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| In Vitro Model | Prostate carcinoma | DU145 cells | CVCL_0105 | ||
CN106459205B ADC-1 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
75.60 ng/mL
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Positive EPHA2 expression (EPHA2+++/++) | ||
| Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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| In Vitro Model | Prostate carcinoma | DU145 cells | CVCL_0105 | ||
CN106459205B ADC-5 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
95.20 ng/mL
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Positive EPHA2 expression (EPHA2+++/++) | ||
| Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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| In Vitro Model | Prostate carcinoma | DU145 cells | CVCL_0105 | ||
CN106459205B ADC-3 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
199.30 ng/mL
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Positive EPHA2 expression (EPHA2+++/++) | ||
| Method Description |
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.
Click to Show/Hide
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| In Vitro Model | Prostate carcinoma | DU145 cells | CVCL_0105 | ||
MEDI-547 [Terminated in phase 1]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Objective Response Rate (ORR) |
0.00%
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| Patients Enrolled |
Malignant solid tumor thought to be associated with increased expression of EphA2 (endometrial, breast, ovarian, prostate, non-small cell lung, colon, esophageal, gastric, and bladder cancers, renal cell carcinoma, melanoma), relapsed or refractory to standard therapy, and an Eastern Cooperative Oncology Group (ECOG) performance status score of 0-2.
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| Administration Dosage |
0.08 mg/kg, 1-h intravenous (IV) infusion once q3wks or qwk for 3 consecutive weeks until unacceptable toxicity, progressive disease.
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| Related Clinical Trial | |||||
| NCT Number | NCT00796055 | Clinical Status | Phase 1 | ||
| Clinical Description |
A phase 1, open-label study of MEDI-547 to evaluate the safety, tolerability, pharmacokinetics, and biologic activity of intravenous administration in subjects with relapsed or refractory solid tumors associated with epha2 expression.
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| Primary Endpoint |
Best response included progressive disease (n=5, 83.33%) and stable disease (n=1, 16.67%), No complete or partial tumor responses.
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| Other Endpoint |
MTD could not be selected.
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Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 48.00% | Negative EPHA2 expression (EPHA2-) | ||
| Method Description |
Mice injected with EphA2-negative SPEC-2 cell was assigned to one of four groups (n = 10 mice per group),MEDI-547,3 mg/kg weekly.
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| In Vivo Model | Endometrial cancer CDX model | ||||
| In Vitro Model | Endometrial cancer | Endometrial cancer cells | Homo sapiens | ||
| Experiment 2 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 86.67% | Positive EPHA2 expression (EPHA2+++/++) | ||
| Method Description |
Mice injected with either Hec-1A or Ishikawa were assigned to one of four groups (n = 10 mice per group),MEDI-547,3 mg/kg weekly.
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| In Vivo Model | Endometrial cancer CDX model | ||||
| In Vitro Model | Endometrial adenocarcinoma | HEC-1-A cells | CVCL_0293 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 92.00% | Positive EPHA2 expression (EPHA2+++/++) | ||
| Method Description |
Mice injected with either Hec-1A or Ishikawa were assigned to one of four groups (n = 10 mice per group),MEDI-547,3 mg/kg weekly.
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| In Vivo Model | Endometrial cancer CDX model | ||||
| In Vitro Model | Endometrial adenocarcinoma | Ishikawa cells | CVCL_2529 | ||
References
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