FLT3

Synonyms

EC 2.7.10, EC:2.7.10.1, Receptor-type tyrosine-protein kinase FLT3, FLT3, FLT-3, FLK2, STK-1, FL cytokine receptor, Fms Related Tyrosine Kinase 3, Stem Cell Tyrosine Kinase 1, CD135 Antigen, CD135, STK1, Growth Factor Receptor Tyrosine Kinase Type III, Fms-Related Tyrosine Kinase 3, Fetal Liver Kinase 2, Fetal Liver Kinase-2, EC 2.7.10.1, fms-Like Tyrosine Kinase 3, Fms Related Receptor Tyrosine Kinase 3, FLK-2,

Description

Tyrosine-protein kinase receptor FLT3 is a protein that in humans is encoded by the FLT3 gene. FLT3 is a cytokine receptor which belongs to the receptor tyrosine kinase class III. CD135 is the receptor for the cytokine Flt3 ligand (FLT3L).Promotes phosphorylation of SHC1 and AKT1, and activation of the downstream effector MTOR. Promotes activation of RAS signaling and phosphorylation of downstream kinases, including MAPK1/ERK2 and/or MAPK3/ERK1. Promotes phosphorylation of FES, FER, PTPN6/SHP, PTPN11/SHP-2, PLCG1, and STAT5A and/or STAT5B. Activation of wild-type FLT3 causes only marginal activation of STAT5A or STAT5B. Mutations that cause constitutive kinase activity promote cell proliferation and resistance to apoptosis via the activation of multiple signaling pathways.

KO Status

F1 (+/-)

Drug Information

Launched drugs: 30
Drugs in clinical trials: 10
Latest Research Phase:Approved

Drug Name

Code

Phase

Company

Indications

Clinical Trials

Midostaurin

PKC-412, PKC-412A, CGP-41231, CGP-41251

Approved

Novartis Pharma Ag

Hematologic Neoplasms, Leukemia, Mastocytosis, Systemic, Leukemia, Mast-Cell, Precursor Cell Lymphoblastic Leukemia-Lymphoma, Hepatic Insufficiency, Leukemia, Myeloid, Acute, Mastocytosis

CTx-0294886

CTx-294886, AMP-886

Preclinical

Cancer Therapeutics, Amplia Therapeutics Ltd

Pulmonary Fibrosis

Sunitinib Malate

SU-11248, SU-010398, PHA-290940, PNU-290940, PHA-290940AD, PNU-290940AD, SU-011248-L-malate salt, GB-102

Approved

Pfizer Pharmaceuticals Ltd (China)

Kidney Neoplasms, Liver Neoplasms, Solid tumours, Carcinoma, Renal Cell, Carcinoma, Islet Cell, Stomach Neoplasms, Pancreatic neuroendocrine tumors (pNET), Pancreatic Neoplasms, Neoplasms by Histologic Type, Kidney Diseases, Neuroendocrine Tumors, Urologic Diseases, Prostatic Neoplasms, Diabetic macular oedema, Breast Neoplasms, Gastrointestinal Stromal Tumors, Colorectal Neoplasms, Urologic Neoplasms, Urogenital Neoplasms, Carcinoma, Hepatocellular, Carcinoma, Non-Small-Cell Lung, Macular Degeneration, Retinal Vein Occlusion

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, Colorectal Neoplasms, Hepatic Insufficiency, Genital Neoplasms, Female, Carcinoma, Hepatocellular, Carcinoma, Non-Small-Cell Lung

Ponatinib Hydrochloride

AP-24534, INCB-84344, AP24534 HCl, AP24534-HCL, AP24534 hydrochloride

Approved

Ariad

Leukemia, Leukemia, Myeloid, Accelerated Phase, Leukemia, Myelogenous, Chronic, BCR-ABL Positive, Solid tumours, Hematologic Neoplasms, Blast Crisis, Precursor Cell Lymphoblastic Leukemia-Lymphoma, Leukemia, Myeloid, Chronic-Phase, Philadelphia Chromosome, Gastrointestinal Stromal Tumors, Leukemia, Myeloid, Acute, Lymphoma, Leukemia, Biphenotypic, Acute

Pexidartinib

PLX-3397

Approved

Daiichi Sankyo Co Ltd

Giant Cell Tumor of Tendon Sheath, Solid tumours, Synovitis, Pigmented Villonodular, Hodgkin Disease, Arthritis, Rheumatoid, Glioblastoma, Giant Cell Tumors, Prostatic Neoplasms, Gastrointestinal Stromal Tumors, Leukemia, Myeloid, Acute

Gilteritinib fumarate

ASP-2215 hemifumarate, ASP-2215, 66D-92MGC8M (UNII code)

Approved

Astellas

Hepatic Insufficiency, Leukemia, Myeloid, Acute

Fedratinib

TG-101348, SAR-302503

Approved

Sanofi

Hematologic Neoplasms, Polycythemia Vera, Kidney Diseases, Primary Myelofibrosis, Hepatic Insufficiency, Thrombocythemia, Essential

Quizartinib

AC-220, ASP-2689, AC-010220

Approved

Ambit Biosciences

Leukemia, Myelodysplastic Syndromes, Myeloproliferative Disorders, Hepatic Insufficiency, Leukemia, Myeloid, Acute

Brigatinib

AP-26113

Approved

Ariad, Takeda Pharmaceutical Co Ltd

Carcinoma, Lung Neoplasms, Lymphoma, Large-Cell, Anaplastic, Carcinoma, Non-Small-Cell Lung

Sorafenib Tosylate

NSC-724772, BAY-43-0006, BAY-43-9006, BAY-54-9085

Approved

Onyx Pharmaceuticals Inc

Liver Neoplasms, Solid tumours, Kidney Neoplasms, Ovarian Neoplasms, Leukemia, Myelogenous, Chronic, BCR-ABL Positive, Carcinoma, Renal Cell, Carcinoma, Pancreatic Neoplasms, Kidney Diseases, Neoplasms, Liver Diseases, Hepatitis B, Breast Neoplasms, Hepatitis C, Thyroid Neoplasms, Lung Neoplasms, Carcinoma, Hepatocellular, Carcinoma, Non-Small-Cell Lung, Fasting, Neoplasm Metastasis, Melanoma

HH-30134

Preclinical

Neoplasms

HY-008

HY-008

Preclinical

Heyuan Biotechnology (Tianjin) Co Ltd

Leukemia, Myeloid, Acute

Lestaurtinib

SP-924, CEP-701, KT-5555, SPM-924, A-154475.0

Phase 3 Clinical

Kyowa Hakko Kirin

Bone Marrow Neoplasms, Leukemia, Myeloid, Polycythemia Vera, Precursor Cell Lymphoblastic Leukemia-Lymphoma, Prostatic Neoplasms, Psoriasis, Leukemia, Myeloid, Acute, Thrombocythemia, Essential

Pacritinib

SB-1518, ONX-0803

Phase 3 Clinical

S*Bio, Concert

Lymphoma, B-Cell, Leukemia, Myelogenous, Chronic, BCR-ABL Positive, Polycythemia Vera, Hodgkin Disease, Myelodysplastic Syndromes, Myeloproliferative Disorders, Leukemia, Myelomonocytic, Chronic, Coronavirus Infections, Lymphoma, Mantle-Cell, Primary Myelofibrosis, Lymphoma, Non-Hodgkin, Leukemia, Myeloid, Acute, Lymphoma, Thrombocythemia, Essential

SKLB-1028

SKLB-1028

Phase 3 Clinical

Sichuan University, China Shijiazhuang Pharmaceutical Group/Cspc

Leukemia, Leukemia, Myeloid, Acute

Crenolanib Besylate

ARO-002, CP-868596, ARO-002-26, IND-112201, CP-868596-26

Phase 3 Clinical

Pfizer Pharmaceuticals Ltd (China)

Recurrence, Esophageal Neoplasms, Glioblastoma, Neoplasms, Gastrointestinal Stromal Tumors, Leukemia, Myeloid, Acute, Glioma, Carcinoma, Non-Small-Cell Lung

SEL-24

SEL-24, MEN-1703, SEL-24-1, SEL-24-B489, SEL-24 program

Phase 2 Clinical

Selvita

Leukemia, Myeloid, Acute

HM-43239

Phase 2 Clinical

Hanmi Pharmaceutical Co Ltd

Leukemia, Myeloid, Acute

RIVAL-01

TBio-6517

Phase 2 Clinical

Turnstone Biologics

Triple Negative Breast Neoplasms, Colorectal Neoplasms