MERTK Overview
Molecule Name
Tyrosine-protein kinase Mer
Synonyms
MERTK,Mer
Drug Development Progress
Drugs in Clinical Trials8
Approved Drugs1
Highest Development StageApproved
Target Synonym
EC 2.7.10，MER，MERTK，C-Mer Proto-Oncogene Tyrosine Kinase，Receptor Tyrosine Kinase MerTK，Tyrosine-Protein Kinase Mer，EC 2.7.10.1，STK Kinase，EC:2.7.10.1，Proto-oncogene c-Mer，MER Proto-Oncogene， Tyrosine Kinase，MER Receptor Tyrosine Kinase，Tyro12，C-Eyk，C-Mer，RP38，c-Mer Tyrosine Kinase
Background
Tyrosine-protein kinase Mer(MERTK) is a member of the TYRO3/AXL/MER (TAM) receptor kinase family and encodes a transmembrane protein with two fibronectin type-III domains, two Ig-like C2-type (immunoglobulin-like) domains, and one tyrosine kinase domain. Following activation by ligand, interacts with GRB2 or PLCG2 and induces phosphorylation of MAPK1, MAPK2, FAK/PTK2 or RAC1. MERTK signaling plays a role in various processes such as macrophage clearance of apoptotic cells, platelet aggregation, cytoskeleton reorganization and engulfment. Functions in the retinal pigment epithelium (RPE) as a regulator of rod outer segments fragments phagocytosis. Plays also an important role in inhibition of Toll-like receptors (TLRs)-mediated innate immune response by activating STAT1, which selectively induces production of suppressors of cytokine signaling SOCS1 and SOCS3.
MERTK Product List
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Clinical Drug Information
| English Name | Research Code | Highest Development Stage | Company | Indication | Clinical Trial |
|---|---|---|---|---|---|
| Sitravatinib | MG-516; MG-91516; MGCD-516; IND-155305; MGCD-0516 | Phase 3 Clinical | Mirati Therapeutics Inc | Biliary Tract Neoplasms; Breast Neoplasms; Carcinoma; Carcinoma, Hepatocellular; Carcinoma, Non-Small-Cell Lung; Carcinoma, Renal Cell; Carcinoma, Transitional Cell; Endometrial Neoplasms; Esophageal Squamous Cell Carcinoma; Gastrointestinal Neoplasms; Hepatic Insufficiency; Kidney Neoplasms; Liposarcoma; Lung Diseases; Lung Neoplasms; Metastatic breast cancer; Neoplasms; Oral Squamous Cell Carcinoma; Solid tumours; Squamous Cell Carcinoma of Head and Neck; Triple Negative Breast Neoplasms; Ureteral Neoplasms; Uterine Cervical Neoplasms; Uveal melanoma | Details |
| MRX-2843 | UNC-2371; UNC-2025; MRX-2843 | Phase 2 Clinical | University Of North Carolina At Chapel Hill | Carcinoma, Non-Small-Cell Lung; Leukemia; Leukemia, Myeloid, Acute; Lung Neoplasms; Neoplasm Metastasis; Neoplasms; Neoplastic Processes; Pathologic Processes; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Solid tumours | Details |
| Merestinib | 5OGS5K699E; LY-2801653 | Phase 2 Clinical | Eli Lilly And Company | Biliary Tract Neoplasms; Bone metastases; Breast Neoplasms; Carcinoma, Non-Small-Cell Lung; Cholangiocarcinoma; Colorectal Neoplasms; Gallbladder Neoplasms; Leukemia, Myeloid, Acute; Lymphoma, Mantle-Cell; Lymphoma, Non-Hodgkin; Microsatellite instability-high cancer; Neoplasm Metastasis; Neoplasms; Pancreatic Neoplasms; Skin Melanoma; Solid tumours | Details |
| Tamnorzatinib | ONO-7475 | Phase 2 Clinical | Ono Pharmaceutical Co Ltd | Carcinoma, Non-Small-Cell Lung; Leukemia; Leukemia, Myeloid, Acute; Myelodysplastic Syndromes; Pancreatic Neoplasms; Solid tumours | Details |
| Adrixetinib | Q-702 | Phase 2 Clinical | Lead Discovery Center GmbH, Max Planck Institute of Biochemistry, Vichem Chemie | Blastic Plasmacytoid Dendritic Cell Neoplasm; Carcinoma, Hepatocellular; Central Nervous System Lymphoma; Erdheim-Chester Disease; Esophageal Neoplasms; Graft vs Host Disease; Hematologic Neoplasms; Histiocytic Sarcoma; Histiocytosis, Langerhans-Cell; Histiocytosis, Sinus; Leukemia, Lymphocytic, Chronic, B-Cell; Leukemia, Lymphoid; Leukemia, Myeloid, Acute; Leukemia, Myelomonocytic, Chronic; Lymphoma; Lymphoma, Follicular; Lymphoma, T-Cell, Cutaneous; Lymphoma, T-Cell, Peripheral; Myelodysplastic Syndromes; Neoplasm Metastasis; Neoplasms; Neoplasms, Plasma Cell; Solid tumours; Stomach Neoplasms; Uterine Cervical Neoplasms; Waldenstrom Macroglobulinemia | Details |
| INCB-081776 | INCB-81776; INCB-081776 | Phase 1 Clinical | Incyte Corp | Solid tumours; Squamous Cell Carcinoma of Head and Neck | Details |
| Nifitinib Tosilate | Phase 1 Clinical | Sichuan University, Yangzijiang Pharmaceutical Group Sichuan Hairong Pharmaceutical Co Ltd | Carcinoma, Non-Small-Cell Lung | Details | |
| NPS-1034 | HOPE-777; KDDF-201111-02 | Neopharma Ltd | 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| Cabozantinib S-malate | XL-184; BMS-907351; RO7047650; RO-7047650 | Approved | Exelixis Inc | Cometriq, Cabometyx | United States | Thyroid Neoplasms; Carcinoma, Neuroendocrine | Exelixis Inc | 2012-11-29 | Adenocarcinoma, Clear Cell; Adenocarcinoma, Follicular; Adenoma, Islet Cell; Adrenal Cortex Neoplasms; Adrenocortical Carcinoma; Astrocytoma; Bile Duct Neoplasms; Bone metastases; Brain metastases; Brain Neoplasms; Breast Neoplasms; Carcinoma, Adenosquamous; Carcinoma, Endometrioid; Carcinoma, Hepatocellular; Carcinoma, Merkel Cell; Carcinoma, Neuroendocrine; Carcinoma, Non-Small-Cell Lung; Carcinoma, Ovarian Epithelial; Carcinoma, Papillary; Carcinoma, Renal Cell; Carcinoma, Squamous Cell; Carcinoma, Transitional Cell; Central Nervous System Neoplasms; Cholangiocarcinoma; Colorectal Neoplasms; Endometrial Neoplasms; Fallopian Tube Neoplasms; Gastroenteropancreatic neuroendocrine tumor; Glioblastoma; Glioma; Gliosarcoma; Hepatic Insufficiency; Hepatoblastoma; HIV Infections; Kidney Neoplasms; Leiomyosarcoma; Leukemia, Myeloid, Acute; Lymphoma; Medullary thyroid cancer (MTC); Melanoma; Meningioma; Multiple Myeloma; Neoplasm Metastasis; Neoplasms; Neoplasms, Germ Cell and Embryonal; Neuroblastoma; Neuroendocrin | Details |