FGFR3

Synonyms

EC 2.7.10, EC:2.7.10.1, Fibroblast Growth Factor Receptor 3-S, JTK4, CD333, FGFR3, Fibroblast Growth Factor Receptor 3, FGFR-3, Fibroblast Growth Factor Receptor 3 Variant 4, Achondroplasia, Thanatophoric Dwarfism, Hydroxyaryl-Protein Kinase, Tyrosine Kinase JTK4, CD333 Antigen, EC 2.7.10.1, HSFGFR3EX, CEK2, ACH, Receptor, Fibroblast Growth Factor, Type 3

KO Status

RenMab: F0

Drug Information

Launched drugs: 7
Drugs in clinical trials: 16
Latest Research Phase: Approved

Drug Name

Code

Phase

Company

Indications

Clinical Trials

Erdafitinib

G-024, JNJ-493, 890E37NHMV, JNJ-42756493

Approved

Astex Pharmaceuticals Inc

Solid tumours, Carcinoma, Esophageal Neoplasms, Stomach Neoplasms, Carcinoma, Transitional Cell, Urinary Bladder Neoplasms, Bile Duct Neoplasms, Urologic Neoplasms, Hepatic Insufficiency, Lymphoma, Carcinoma, Hepatocellular, Adenocarcinoma, Carcinoma, Non-Small-Cell Lung

Pemigatinib

IBI-375, INCB-054828, INCB-54828, BH-009

Approved

Incyte Corp

Solid tumours, Biliary Tract Neoplasms, Carcinoma, Renal Cell, Carcinoma, Transitional Cell, Cholangiocarcinoma, Translocation, Genetic, Bile Duct Neoplasms, Endometrial Neoplasms

Infigratinib

BGJ-398, NVP-BGJ398

Approved

Novartis Pharma Ag

Solid tumours, Biliary Tract Neoplasms, Hematologic Neoplasms, Esophageal Neoplasms, Stomach Neoplasms, Carcinoma, Transitional Cell, Achondroplasia, Urinary Bladder Neoplasms, Cholangiocarcinoma, Carcinoma, Squamous Cell, Melanoma, Adenocarcinoma

Pazopanib Hydrochloride

GW-786034, SB-786034, GSK-786034, GW-786034B

Approved

Glaxosmithkline Plc, Novartis Pharma Ag

Ovarian Neoplasms, Telangiectasia, Hereditary Hemorrhagic, Chondrosarcoma, Solid tumours, Carcinoma, Renal Cell, Hemangiosarcoma, Small Cell Lung Carcinoma, Pancreatic Neoplasms, Sarcoma, Breast Neoplasms, Osteosarcoma, Prostatic Neoplasms, Colorectal Neoplasms, Peritoneal Neoplasms, Glioma, Fallopian Tube Neoplasms, Carcinoma, Hepatocellular, Melanoma, Carcinoma, Non-Small-Cell Lung, Macular Degeneration

Lenvatinib Mesylate

ER-203492-00, E-7080

Approved

Eisai Co Ltd

Liver Neoplasms, Solid tumours, Biliary Tract Neoplasms, Carcinoma, Renal Cell, Squamous Cell Carcinoma of Head and Neck, Renal Insufficiency, Small Cell Lung Carcinoma, Adenocarcinoma of Lung, Thyroid Carcinoma, Anaplastic, Kidney Diseases, Urinary Bladder Neoplasms, Liver Diseases, Sarcoma, Hepatic Insufficiency, Endometrial Neoplasms, Thyroid Neoplasms, Lymphoma, Carcinoma, Hepatocellular, Carcinoma, Non-Small-Cell Lung, Melanoma

Anlotinib Dihydrochloride

AL-3818

Approved

Advenchen Laboratories, Jiangsu Chia Tai-Tianqing Pharmaceutical Co Ltd

Leiomyosarcoma, Head and Neck Neoplasms, Solid tumours, Biliary Tract Neoplasms, Ovarian Neoplasms, Thoracic Neoplasms, Esophageal Neoplasms, Stomach Neoplasms, Genital Diseases, Female, Carcinoma, Renal Cell, Triple Negative Breast Neoplasms, Small Cell Lung Carcinoma, Lymphoma, Large B-Cell, Diffuse, Sarcoma, Synovial, Neuroendocrine Tumors, Sarcoma, Bile Duct Diseases, Medullary thyroid cancer (MTC), Cholangiocarcinoma, Nasopharyngeal Carcinoma, Urologic Neoplasms, Colorectal Neoplasms, Gastrointestinal Stromal Tumors, Bone Neoplasms, Sarcoma, Alveolar Soft Part, Gallbladder Neoplasms, Endometrial Neoplasms, Thyroid Neoplasms, Esophageal Squamous Cell Carcinoma, Lung Neoplasms, Uterine Cervical Neoplasms, Carcinoma, Hepatocellular, Carcinoma, Non-Small-Cell Lung, Melanoma, Osteoma

Nintedanib Esylate

BIBF-1120

Approved

C.H. Boehringer Sohn Ag & Co. Kg

Ovarian Neoplasms, Solid tumours, Carcinoma, Renal Cell, Scleroderma, Systemic, Idiopathic Pulmonary Fibrosis, Lung Diseases, Interstitial, Pulmonary Fibrosis, Multiple Myeloma, Prostatic Neoplasms, Peritoneal Neoplasms, Hepatic Insufficiency, Genital Neoplasms, Female, Colorectal Neoplasms, Carcinoma, Hepatocellular, Carcinoma, Non-Small-Cell Lung

Masitinib mesylate

AB-1010, AB19001

NDA/BLA

Ab Science

Ovarian Neoplasms, Pancreatic Neoplasms, Coronavirus Disease 2019 (COVID-19), Mastocytosis, Systemic, Arthritis, Rheumatoid, Multiple Sclerosis, Multiple Myeloma, Multiple Sclerosis, Chronic Progressive, Prostatic Neoplasms, Psoriasis, Alzheimer Disease, Asthma, Gastrointestinal Stromal Tumors, Colorectal Neoplasms, Amyotrophic Lateral Sclerosis, Melanoma, Mastocytosis

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

Futibatinib

TAS-120

Phase 3 Clinical

Otsuka Pharmaceutical Co Ltd, Taiho Pharmaceutical Co Ltd

Bone Marrow Neoplasms, Solid tumours, Stomach Neoplasms, Carcinoma, Esophageal Neoplasms, Carcinoma, Transitional Cell, Central Nervous System Neoplasms, Cholangiocarcinoma, Breast Neoplasms, Lymphoma, Carcinoma, Non-Small-Cell Lung

References


Title

Authors

Source

Asn540Thr substitution in the fibroblast growth factor receptor 3 tyrosine kinase domain causing hypochondroplasia

Deutz-Terlouw P.P., Losekoot M., Aalfs C.M., Hennekam R.C.M., Bakker E.,

Hum. Mutat. Suppl. 1:S62-S65(1998)

Lys650Met substitution in the tyrosine kinase domain of the fibroblast growth factor receptor gene causes thanatophoric dysplasia type I

Kitoh H., Brodie S.G., Kupke K.G., Lachman R.S., Wilcox W.R.,

Hum. Mutat. 12:362-363(1998)

Deafness due to Pro250Arg mutation of FGFR3

Hollway G.E., Suthers G.K., Battese K.M., Turner A.M., David D.J., Mulley J.C.,

Lancet 351:877-878(1998)

Platyspondylic lethal skeletal dysplasia, San Diego type, is caused by FGFR3 mutations

Brodie S.G., Kitoh H., Lachman R.S., Nolasco L.M., Mekikian P.B., Wilcox W.R.,

Am. J. Med. Genet. 84:476-480(1999)

Sex related expressivity of the phenotype in coronal craniosynostosis caused by the recurrent P250R FGFR3 mutation

Lajeunie E., El Ghouzzi V., Le Merrer M., Munnich A., Bonaventure J., Renier D.,

J. Med. Genet. 36:9-13(1999)

Frequent activating mutations of FGFR3 in human bladder and cervix carcinomas

Cappellen D., De Oliveira C., Ricol D., Gil Diez de Medina S., Bourdin J., Sastre-Garau X., Chopin D., Thiery J.P., Radvanyi F.,

Nat. Genet. 23:18-20(1999)

Distinct missense mutations of the FGFR3 Lys650 codon modulate receptor kinase activation and the severity of the skeletal dysplasia phenotype

Bellus G.A., Spector E.B., Speiser P.W., Weaver C.A., Garber A.T., Bryke C.R., Israel J., Rosengren S.S., Webster M.K., Donoghue D.J., Francomano C.A.,

Am. J. Hum. Genet. 67:1411-1421(2000)

Clinical and radiographic features of a family with hypochondroplasia owing to a novel asn540ser mutation in the fibroblast growth factor receptor 3 gene

Mortier G., Nuytinck L., Craen M., Renard J.-P., Leroy J.G., De Paepe A.,

J. Med. Genet. 37:220-224(2000)

Syndrome of coronal craniosynostosis, Klippel-Feil anomaly, and sprengel shoulder with and without Pro250Arg mutation in the FGFR3 gene

Lowry R.B., Jabs E.W., Graham G.E., Gerritsen J., Fleming J.,

Am. J. Med. Genet. 104:112-119(2001)

Analysis of FGFR3 gene mutations in multiple myeloma patients with t(4;14)

Intini D., Baldini L., Fabris S., Lombardi L., Ciceri G., Maiolo A.T., Neri A.,

Br. J. Haematol. 114:362-364(2001)