EphA2 Overview
Molecule Name
Ephrin type-A receptor 2
Synonyms
EphA2
Drug Development Progress
Drugs in Clinical Trials9
Approved Drugs2
Highest Development StageApproved
Target Synonym
EC:2.7.10.1，Epithelial Cell Receptor Protein Tyrosine Kinase，Ephrin type-A receptor 2，Epithelial cell kinase，EPHA2，EPH Receptor A2，Tyrosine-Protein Kinase Receptor ECK，ECK，Soluble EPHA2 Variant 1，EC 2.7.10.1，CTRCT6，ARCC2，CTPP1，CTPA，Receptor， EphA2，EC 2.7.10
Background
Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Activated by the ligand ephrin-A1/EFNA1 regulates migration, integrin-mediated adhesion, proliferation and differentiation of cells. Regulates cell adhesion and differentiation through DSG1/desmoglein-1 and inhibition of the ERK1/ERK2 (MAPK3/MAPK1, respectively) signaling pathway. Engaged by the ligand ephrin-A5/EFNA5 may regulate lens fiber cells shape and interactions and be important for lens transparency development and maintenance. With ephrin-A2/EFNA2 may play a role in bone remodeling through regulation of osteoclastogenesis and osteoblastogenesis.
EphA2 Product List
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Clinical Drug Information
| English Name | Research Code | Highest Development Stage | Company | Indication | Clinical Trial |
|---|---|---|---|---|---|
| BT-5528 | BT-5528; BT5528 | Phase 2 Clinical | Bicycle Therapeutics | Carcinoma; Carcinoma, Non-Small-Cell Lung; Carcinoma, Pancreatic Ductal; Head and Neck Neoplasms; Ovarian Neoplasms; Triple Negative Breast Neoplasms | Details |
| siRNA-EphA2-DOPC | Phase 1 Clinical | The University Of Texas MD Anderson Cancer Center | Ovarian Neoplasms; Pancreatic Neoplasms; Solid tumours | Details | |
| 18F-Dasatinib | 18F-SKI-249380; [18F]-Fluoro-BMS-354825; [18F]Dasatinib; [18F]SKI-249380; [18F]Fluoro-BMS-354825 | Phase 1 Clinical | Memorial Sloan Kettering Cancer Center | Bone Marrow Neoplasms; Carcinoma; Diagnostic agents; Lymphoma; Melanoma; Neoplasms; Sarcoma | Details |
| E-Sync T Cell Therapy (University of California/National Cancer Institute/California Institute for Regenerative Medicine) | Phase 1 Clinical | University Of California San Francisco | Glioblastoma | Details | |
| SC-102 | SC-102 | Phase 1 Clinical | Tianjin Conjustar Biotechnology Co Ltd | Neoplasms; Solid tumours | Details |
| EphA2-targeted CAR-DCs therapy (Second Affiliated Hospital School Of Zhejiang University School Of Medicine) | Phase 1 Clinical | Second Affiliated Hospital School Of Zhejiang University School Of Medicine | Carcinoma, Non-Small-Cell Lung | Details | |
| EphA2-targeted CAR-T Cells therapy (Second Affiliated Hospital School Of Zhejiang University School Of Medicine) | Phase 1 Clinical | Second Affiliated Hospital School Of Zhejiang University School Of Medicine | Carcinoma, Non-Small-Cell Lung | Details | |
| Autologous Anti-EGFRvIII synNotch Receptor Induced Anti-EphA2/IL-13R alpha2 CAR (E-SYNC) T Cells therapy(California Institute For Regenerative Medicine) | Phase 1 Clinical | California Institute For Regenerative Medicine, National Cancer Institute | Glioblastoma | Details | |
| [18F]AlF-ETN | [18F]AlF-ETN | Phase 1 Clinical | Capital Medical University, Yunnan Baiyao Group Co Ltd | Prostatic Neoplasms; Solid tumours | Details |
Marketed Drug Information
| English Name | Research Code | Highest Development Stage | Company | First Brand Name | First Approved Country | First Indication | First Approved Company | First Approved Date | Indication | Clinical Trial |
|---|---|---|---|---|---|---|---|---|---|---|
| Regorafenib | DAST; BAY-73-4506 | Approved | Bayer AG | Stivarga, Resihance | United States | Colorectal Neoplasms | Bayer Healthcare Pharmaceuticals Inc | 2012-09-27 | Adenocarcinoma; Adenoma; Bile Duct Neoplasms; Carcinoma, Adenoid Cystic; Carcinoma, Hepatocellular; Carcinoma, Islet Cell; Carcinoma, Non-Small-Cell Lung; Carcinoma, Ovarian Epithelial; Carcinoma, Renal Cell; Carcinoma, Transitional Cell; Colonic Neoplasms; Colorectal Neoplasms; Esophageal adenocarcinoma; Esophageal Neoplasms; Fallopian Tube Neoplasms; Gastrinoma; Gastrointestinal Neoplasms; Gastrointestinal Stromal Tumors; Glucagonoma; Hemangiosarcoma; Insulinoma; Leukemia, Myeloid, Acute; Liver Neoplasms; Lung Neoplasms; Melanoma; Meningioma; Neoplasm Metastasis; Neoplasms; Osteosarcoma; Ovarian Neoplasms; Pancreatic Neoplasms; Peritoneal Neoplasms; Rectal Neoplasms; Sarcoma; Sarcoma, Ewing; Solid tumours; Somatostatinoma; Stomach Neoplasms; Thymoma; Thyroid Neoplasms | Details |
| Dasatinib Hydrate | NSC-732517; BMS-354825 | Approved | Bristol-Myers Squibb Company | Spraysel, 施达赛, Spricel, Sprycel | United States | Precursor Cell Lymphoblastic Leukemia-Lymphoma; Leukemia, Myelogenous, Chronic | Bristol-Myers Squibb Company | 2006-06-28 | Adenocarcinoma, Clear Cell; Angioimmunoblastic T-cell Lymphoma; Astrocytoma; Blast Crisis; Bone metastases; Brain Neoplasms; Breast Neoplasms; Burkitt Lymphoma; Carcinoma, Basosquamous; Carcinoma, Hepatocellular; Carcinoma, Non-Small-Cell Lung; Carcinoma, Squamous Cell; Carcinoma, Verrucous; Cholangiocarcinoma; Chondrosarcoma; Chordoma; Colonic Neoplasms; Coronavirus Disease 2019 (COVID-19); Cystadenocarcinoma; Endometrial Neoplasms; Fallopian Tube Neoplasms; Gastrointestinal Stromal Tumors; Giant Cell Tumor of Bone; Glioblastoma; Glioma; Gliosarcoma; Heart Arrest; Hemangiopericytoma; Hematologic Neoplasms; HIV Infections; Hodgkin Disease; Hormone-Resistant Prostate Neoplasms; Hypereosinophilic Syndrome; Hypopharyngeal Neoplasms; Idiopathic Pulmonary Fibrosis; Immunoproliferative Small Intestinal Disease; Intraocular Lymphoma; Laryngeal Diseases; Laryngeal Neoplasms; Leukemia; Leukemia, Hairy Cell; Leukemia, Large Granular Lymphocytic; Leukemia, Lymphocytic, Chronic, B-Cell; Leukemia, Lymphoid; Leukemia, Myel | Details |