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VEGF R1

Brief Information

Name:Vascular endothelial growth factor receptor 1
Target Synonym:EC 2.7.10,Fms Related Receptor Tyrosine Kinase 1,EC:2.7.10.1,VEGFR1,Tyrosine-protein kinase receptor FLT,FRT,Fms-like tyrosine kinase 1,FLT1,Vascular Permeability Factor Receptor,Vascular Endothelial Growth Factor Receptor 1,Tyrosine-Protein Kinase FRT,FL
Number of Launched Drugs:12
Number of Drugs in Clinical Trials:12
Lastest Research Phase:Approved

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Part of Bioactivity data

VE1-H82E3-BLI
Human_FcRn_Heterodimer_Protein_Bli

Loaded Biotinylated Human VEGF R1, His,Avitag (Cat. No. VE1-H82E3) on SA Biosensor, can bind Human VEGF165, His Tag (Cat. No. VE5-H5248) with an affinity constant of 0.236 nM as determined in BLI assay (ForteBio Octet Red96e) (Routinely tested).

VE1-H5220-BLI
Human_FcRn_Heterodimer_Protein_Bli

Loaded Human VEGF R1, His Tag (Cat. No. VE1-H5220) on HIS1K Biosensor, can bind ActiveMax® Human VEGF165, Tag Free (Cat. No. VE5-H4210) with an affinity constant of 43.4 pM as determined in BLI assay (ForteBio Octet Red96e) (Routinely tested).

Synonym Name

FLT,VEGFR1,FLT1

Background

Vascular endothelial growth factor receptor 1 (VEGFR1) is also known as Fms-like tyrosine kinase 1 (FLT-1), Tyrosine-protein kinase receptor FLT, is a single-pass type I membrane protein and secreted protein which belongs to the protein kinase superfamily, Tyr protein kinase family and CSF-1/PDGF receptor subfamily. VEGFR1 is detected in normal lung, but also in placenta, liver, kidney, heart and brain tissues and specifically expressed in most of the vascular endothelial cells, and also expressed in peripheral blood monocytes. VEGFR1 acts as a cell-surface receptor for VEGFA, VEGFB and PGF, and plays an essential role in the development of embryonic vasculature, the regulation of angiogenesis, cell survival, cell migration, macrophage function, chemotaxis, and cancer cell invasion. VEGFR1 may play an essential role as a negative regulator of embryonic angiogenesis by inhibiting excessive proliferation of endothelial cells. VEGFR1 can promote endothelial cell proliferation, survival and angiogenesis in adulthood.

Clinical and Translational Updates

Public Drug Information

Name Research Code Research Phase Company First Brand Name First Approved Country First Indication First Approved Company First Approved Date Indications Clinical Trials
Tivozanib AV-951; KRN-951; ASP-4130; Kil-8951 Approved Kyowa Hakko Kirin Co Ltd Fotivda United States Carcinoma, Renal Cell Aveo Pharmaceuticals Inc 2017-08-24 Solid tumours; Carcinoma, Renal Cell; Hepatic Insufficiency; Carcinoma, Non-Small-Cell Lung Details
Plitidepsin APLD Approved Pharma Mar Sa Aplidin Australia Multiple Myeloma null 2018-12-11 Leukemia; Coronavirus Disease 2019 (COVID-19); Multiple Myeloma; Prostatic Neoplasms; Primary Myelofibrosis; Lymphoma Details
Sorafenib Tosylate NSC-724772; BAY-43-0006; BAY-43-9006; BAY-54-9085 Approved Onyx Pharmaceuticals Inc 多吉美, Nexavar EU Thyroid Neoplasms Bayer Ag 2005-12-01 Liver Diseases; Neoplasm Metastasis; Fasting; Melanoma; Carcinoma, Hepatocellular; Carcinoma, Non-Small-Cell Lung; Lung Neoplasms; Thyroid Neoplasms; Hepatitis C; Hepatitis B; Breast Neoplasms; Liver Neoplasms; Neoplasms; Pancreatic Neoplasms; Kidney Diseases; Carcinoma; Carcinoma, Renal Cell; Kidney Neoplasms; Solid tumours; Ovarian Neoplasms; Leukemia, Myelogenous, Chronic, BCR-ABL Positive Details
Pazopanib Hydrochloride GW-786034; SB-786034; GSK-786034; GW-786034B Approved Glaxosmithkline Plc, Novartis Pharma Ag 维全特, Armala, Patorma, Votrient Mainland China Carcinoma, Renal Cell Novartis Pharma Schweiz Ag 2009-10-19 Osteosarcoma; Macular Degeneration; Carcinoma, Non-Small-Cell Lung; Melanoma; Carcinoma, Hepatocellular; Fallopian Tube Neoplasms; Glioma; Peritoneal Neoplasms; Colorectal Neoplasms; Prostatic Neoplasms; Ovarian Neoplasms; Breast Neoplasms; Sarcoma; Pancreatic Neoplasms; Small Cell Lung Carcinoma; Hemangiosarcoma; Carcinoma, Renal Cell; Solid tumours; Chondrosarcoma; Telangiectasia, Hereditary Hemorrhagic Details
Fruquintinib HMPL-013 Approved Hutchison Medipharma Ltd 爱优特, Elunate Mainland China Colorectal Neoplasms Hutchison Huangpu Medicine (Shanghai) Co Ltd 2018-09-04 Solid tumours; Rectal Neoplasms; Esophageal Neoplasms; Colonic Neoplasms; Triple Negative Breast Neoplasms; Breast Neoplasms; Colorectal Neoplasms; Lung Neoplasms; Carcinoma, Non-Small-Cell Lung Details
Regorafenib Monohydrate BAY-73-4506; DAST Approved Bayer Ag Stivarga, Resihance Mainland China Gastrointestinal Stromal Tumors Bayer Pharma Ag 2012-09-27 Solid tumours; Rectal Neoplasms; Carcinoma, Renal Cell; Colonic Neoplasms; Colorectal Neoplasms; Gastrointestinal Stromal Tumors; Carcinoma, Hepatocellular; Gastrointestinal Neoplasms Details
Axitinib AG-013736; PF-01367866; AG-13736 Approved Pfizer Pharmaceuticals Ltd (China) 英立达, Inlyta Mainland China Carcinoma, Renal Cell Pfizer Europe Ma Eeig 2012-01-27 Kidney Neoplasms; Solid tumours; Carcinoma, Renal Cell; Carcinoma; Skin Neoplasms; Myelodysplastic Syndromes; Endometriosis; Hepatic Insufficiency; Thyroid Neoplasms; Lung Neoplasms; Leukemia, Myeloid, Acute; Adenocarcinoma; Carcinoma, Hepatocellular; Carcinoma, Non-Small-Cell Lung; Melanoma; Macular Degeneration Details
Anlotinib Dihydrochloride AL-3818 Approved Advenchen Laboratories, Jiangsu Chia Tai-Tianqing Pharmaceutical Co Ltd 福可维 Mainland China Small Cell Lung Carcinoma Jiangsu Chia Tai-Tianqing Pharmaceutical Co Ltd 2018-05-08 Esophageal Squamous Cell Carcinoma; Nasopharyngeal Carcinoma; Gastrointestinal Stromal Tumors; Bone Neoplasms; Peritoneal Neoplasms; Colorectal Neoplasms; Endometrial Neoplasms; Thyroid Neoplasms; Sarcoma, Alveolar Soft Part; Cholangiocarcinoma; Lung Neoplasms; Fallopian Tube Neoplasms; Uterine Cervical Neoplasms; Carcinoma, Non-Small-Cell Lung; Carcinoma, Hepatocellular; Melanoma; Adenocarcinoma; Osteoma; Triple Negative Breast Neoplasms; Solid tumours; Ovarian Neoplasms; Leiomyosarcoma; Liver Neoplasms; Genital Diseases, Female; Carcinoma, Renal Cell; Stomach Neoplasms; Esophageal Neoplasms; Biliary Tract Neoplasms; Small Cell Lung Carcinoma; Lymphoma, Large B-Cell, Diffuse; Carcinoma, Ovarian Epithelial; Sarcoma, Synovial; Neuroendocrine Tumors; Medullary thyroid cancer (MTC); Sarcoma Details
Nintedanib Esylate BIBF-1120 Approved C.H. Boehringer Sohn Ag & Co. Kg Ofev, Vargatef Mainland China Idiopathic Pulmonary Fibrosis Boehringer Ingelheim International Gmbh 2014-10-15 Ovarian Neoplasms; Solid tumours; Carcinoma, Renal Cell; Scleroderma, Systemic; Idiopathic Pulmonary Fibrosis; Pulmonary Fibrosis; Lung Diseases, Interstitial; Multiple Myeloma; Prostatic Neoplasms; Peritoneal Neoplasms; Hepatic Insufficiency; Genital Neoplasms, Female; Colorectal Neoplasms; Carcinoma, Hepatocellular; Carcinoma, Non-Small-Cell Lung Details
Lenvatinib Mesylate ER-203492-00; E-7080 Approved Eisai Co Ltd Kisplyx, Lenvima, Lenvima/Kisplyx, 乐卫玛 United States Endometrial Neoplasms Eisai Inc 2015-02-13 Urinary Bladder Neoplasms; Uterine Cervical Neoplasms; Melanoma; Carcinoma, Non-Small-Cell Lung; Carcinoma, Hepatocellular; Gallbladder Neoplasms; Lymphoma; Endometrial Neoplasms; Thyroid Neoplasms; Hepatic Insufficiency; Cholangiocarcinoma; Sarcoma; Liver Diseases; Liver Neoplasms; Triple Negative Breast Neoplasms; Kidney Diseases; Small Cell Lung Carcinoma; Thyroid Carcinoma, Anaplastic; Adenocarcinoma of Lung; Esophageal Neoplasms; Renal Insufficiency; Squamous Cell Carcinoma of Head and Neck; Carcinoma, Renal Cell; Biliary Tract Neoplasms; Solid tumours Details
Cabozantinib S-malate BMS-907351; XL-184 Approved Exelixis Inc Cometriq, Cabometyx Japan Carcinoma, Renal Cell Takeda 2012-11-29 Solid tumours; Pain; Stomach Neoplasms; Carcinoma, Renal Cell; Esophageal Neoplasms; Glioblastoma; Kidney Diseases; Prostatic Neoplasms; Colorectal Neoplasms; Astrocytoma; Hepatic Insufficiency; Thyroid Neoplasms; Carcinoma, Neuroendocrine; Lymphoma; Carcinoma, Non-Small-Cell Lung; Carcinoma, Hepatocellular Details
Sunitinib Malate PHA-290940; SU-010398; SU-11248; GB-102; PNU-290940; SU-011248-L-malate salt; PNU-290940AD; PHA-290940AD Approved Pfizer Pharmaceuticals Ltd (China) Sutent, 索坦 Japan Pancreatic neuroendocrine tumors (pNET) Pfizer Inc 2006-01-26 Diabetic macular oedema; Macular Degeneration; Carcinoma, Non-Small-Cell Lung; Retinal Vein Occlusion; Carcinoma, Hepatocellular; Urogenital Neoplasms; Urologic Neoplasms; Colorectal Neoplasms; Gastrointestinal Stromal Tumors; Prostatic Neoplasms; Breast Neoplasms; Kidney Neoplasms; Neuroendocrine Tumors; Urologic Diseases; Kidney Diseases; Pancreatic neuroendocrine tumors (pNET); Pancreatic Neoplasms; Carcinoma, Islet Cell; Stomach Neoplasms; Carcinoma, Renal Cell; Solid tumours; Liver Neoplasms Details

Clinical Drug Information

Name Research Code Research Phase Company Indications Clinical Trials
OCV-101 OCV-101; OTS-11101 Phase 2 Clinical Oncotherapy Science Pancreatic Neoplasms Details
VEGFR-1/2 peptide vaccine (Keio University) Phase 2 Clinical Keio University Neurofibromatoses; Brain Neoplasms; Glioma Details
Glesatinib MG-90265; MGCD-265; MG-90265X; 7Q29OXD98N; MG-90265H9; MG-90265gly Phase 2 Clinical Mirati Therapeutics Carcinoma, Non-Small-Cell Lung Details
Icrucumab 18-F-1; IMC-18-F-1; LY-3012212 Phase 2 Clinical Imclone Systems, Eli Lilly And Company Rectal Neoplasms; Colonic Neoplasms; Breast Neoplasms; Urethral Neoplasms; Colorectal Neoplasms; Urologic Neoplasms; Ureteral Neoplasms; Urogenital Neoplasms Details
Hydroxychloroquine/Sorafenib Phase 1 Clinical Vg Life Sciences Ovarian Neoplasms Details
Sorafenib/MG-005 MGD-1509 Phase 1 Clinical Metagone Biotech, Tri-Service General Hospital Solid tumours Details
Dovitinib TKI-258; CHIR-258; GFKI-258; CHIR-258LC; NVP-TKI258 Phase 2 Clinical Novartis Pharma Ag Carcinoma, Adenoid Cystic; Carcinoma, Endometrioid; Carcinoma, Non-Small-Cell Lung; Carcinoma, Hepatocellular; Melanoma; Leukemia, Myeloid, Acute; Thyroid Neoplasms; Endometrial Neoplasms; Colorectal Neoplasms; Gastrointestinal Stromal Tumors; Hepatic Insufficiency; Prostatic Neoplasms; Breast Neoplasms; Solid tumours; Adrenocortical Carcinoma; Multiple Myeloma; Pancreatic Neoplasms; Glioblastoma; Adenocarcinoma, Scirrhous; Carcinoma; Carcinoma, Renal Cell; Stomach Neoplasms; Liver Neoplasms; Linitis Plastica; Stomach Diseases Details
Cediranib AZD2171; AZD-2171; NSC-732208 Phase 2 Clinical Astrazeneca Plc Glioblastoma; Carcinoma, Non-Small-Cell Lung; Lung Neoplasms; Hepatic Insufficiency; Gastrointestinal Stromal Tumors; Colorectal Neoplasms; Brain Neoplasms; Prostatic Neoplasms; Breast Neoplasms; Sarcoma; Biliary Tract Neoplasms; Carcinoma; Carcinoma, Renal Cell; Stomach Neoplasms; Liver Neoplasms; Leukemia; Head and Neck Neoplasms; Solid tumours; Ovarian Neoplasms Details
Lucitanib AL-3810; CO-3810; S-80881 Phase 3 Clinical Advenchen Laboratories Nanjing Ltd Ovarian Neoplasms; Solid tumours; Stomach Neoplasms; Carcinoma, Transitional Cell; Triple Negative Breast Neoplasms; Small Cell Lung Carcinoma; Breast Neoplasms; Nasopharyngeal Carcinoma; Colorectal Neoplasms; Thymus Neoplasms; Genital Neoplasms, Female; Carcinoma, Small Cell; Lung Neoplasms; Carcinoma, Non-Small-Cell Lung; Carcinoma, Hepatocellular Details
Sitravatinib MG-516; MG-91516; MGCD-516; IND-155305 Phase 3 Clinical Mirati Therapeutics Solid tumours; Carcinoma; Carcinoma, Renal Cell; Carcinoma, Transitional Cell; Neoplasms; Hepatic Insufficiency; Ureteral Neoplasms; Carcinoma, Non-Small-Cell Lung; Gastrointestinal Neoplasms; Carcinoma, Hepatocellular Details
Chiauranib CS-2164 Phase 3 Clinical Shenzhen Chipscreen Biosciences Co Ltd Ovarian Neoplasms; Solid tumours; Small Cell Lung Carcinoma; Lymphoma, Non-Hodgkin; Carcinoma, Hepatocellular Details

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