General Information of This Antibody
Antibody ID
ANTI0GRATU
Antibody Name
A anti-EPHA2 (1C1) mAb
Antigen Name
EphA2
 Antigen Info 
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Heavy Chain Varible Domain
EVQLLESGGGLVQPGGSLRLSCAASGFTFSHYMMAWVRQAPGKGLEWVSRIGPSGGPTHY
ADSVKGRFTISRDNSKNTLYLQMNSLRAEDTAVYYCAGYDSGYDYVAVAGPAEYFQHWGQ
GTLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHT
FPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSC
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Light Chain Varible Domain
DIQMTQSPSSLSASVGDRVTITCRASQSISTWLAWYQQKPGKAPKLLIYKASNLHTGVPS
RFSGSGSGTEFSLTISGLQPDDFATYYCQQYNSYSRTFGQGTKVEIKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
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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
MEDI-547 [Phase 1 (discontinued)]
Identified from the Human Clinical Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data stable disease (SD)
16.70%
Patients Enrolled
Eligible patients must have relapsed/refractory solid tumors (ovarian, prostate, NSCLC, etc.) with prior histologic confirmation, ECOG 0-2, adequate organ function, and measurable disease (for dose expansion). Exclusions include uncontrolled CNS metastases, active infections, significant cardiac history, recent stroke/TIA, uncontrolled hypertension, anticoagulant use, and pregnancy/lactation. Prior therapies must be completed ≥30 days before enrollment.

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Administration Dosage
All 6 patients were exposed to MEDI-547 at a dose of 0.08 mg/kg once every 3 weeks.
Related Clinical Trial
NCT Number NCT00796055  Clinical Status PHASE1
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
Primary Endpoint
The safety and tolerability of MEDI-547 will be evaluated through monitoring adverse events (AEs), serious AEs (SAEs), lab abnormalities, physical exam changes, treatment discontinuations due to toxicity, and drug-related deaths during treatment and up to 30 days post-treatment.
Other Endpoint
Antitumor activity will be assessed via objective response rate (ORR), time to response (TTR), duration of response (DR), time to progression (TTP), progression-free survival (PFS), and overall survival (OS), with measurements continuing until 30 days after the last MEDI-547 dose.
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data progressive disease (PD)
83.30%
Patients Enrolled
Eligible patients must have relapsed/refractory solid tumors (ovarian, prostate, NSCLC, etc.) with prior histologic confirmation, ECOG 0-2, adequate organ function, and measurable disease (for dose expansion). Exclusions include uncontrolled CNS metastases, active infections, significant cardiac history, recent stroke/TIA, uncontrolled hypertension, anticoagulant use, and pregnancy/lactation. Prior therapies must be completed ≥30 days before enrollment.

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Administration Dosage
All 6 patients were exposed to MEDI-547 at a dose of 0.08 mg/kg once every 3 weeks.
Related Clinical Trial
NCT Number NCT00796055  Clinical Status PHASE1
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
Primary Endpoint
The safety and tolerability of MEDI-547 will be evaluated through monitoring adverse events (AEs), serious AEs (SAEs), lab abnormalities, physical exam changes, treatment discontinuations due to toxicity, and drug-related deaths during treatment and up to 30 days post-treatment.
Other Endpoint
Antitumor activity will be assessed via objective response rate (ORR), time to response (TTR), duration of response (DR), time to progression (TTP), progression-free survival (PFS), and overall survival (OS), with measurements continuing until 30 days after the last MEDI-547 dose.
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Objective Response Rate (ORR)
0%
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.
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.
Primary Endpoint
Best response included progressive disease (n=5, 83.33%) and stable disease (n=1, 16.67%), No complete or partial tumor responses.
Other Endpoint
MTD could not be selected.
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 48% 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.
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.
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% 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.
In Vivo Model Endometrial cancer CDX model
In Vitro Model Endometrial adenocarcinoma Ishikawa cells CVCL_2529
References
Ref 1 Study of MEDI-547 to Evaluate the Safety, Tolerability, and Biologic Activity of IV Administration in Subjects With Relapsed or Refractory Solid Tumors
Ref 2 Phase 1, open-label study of MEDI-547 in patients with relapsed or refractory solid tumors. Invest New Drugs. 2013 Feb;31(1):77-84.
Ref 3 EphA2 targeted chemotherapy using an antibody drug conjugate in endometrial carcinoma. Clin Cancer Res. 2010 May 1;16(9):2562-70.