title: Pharmacological and clinical profile of lenvatinib (E-7080) in the treatment of advanced, radioiodine-refractory, differentiated thyroid cancer.
abstract: After the pathogenesis of thyroid carcinomas was better understood and the role of molecular alterations in RET, BRAF and RET/PTC rearrangement was revealed, several trials using multikinase inhibitors were developed during the last decade for the treatment of recurrent radioactive iodine (RAI)-refractory differentiated thyroid cancer (DTC), achieving a remarkable success. Sorafenib became the first drug approved for this indication in more than two decades after a significant improvement in the progression-free survival was demonstrated. Lenvatinib (E-7080), an orally active inhibitor of multiple receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFR) 1, 2 and 3, proto-oncogene tyrosine-protein kinase receptor Ret and mast/stem cell growth factor receptor Kit, yielded highly promising early clinical data, even when given after progression on first-line therapy. The phase III SELECT trial recently demonstrated the impressive clinical activity of the drug in RAI-refractory thyroid cancer, leading to the drug's approval by the regulatory agencies and potentially making lenvatinib the most effective drug available to date for the treatment of the disease.
authors.affiliation: Division of Medical Oncology and Hematology, James Graham Brown Cancer Center, University of Louisville, Louisville, Kentucky, USA.
authors.forename: M
authors.initials: M
authors.lastname: Hegazi
authors.affiliation: Division of Medical Oncology and Hematology, James Graham Brown Cancer Center, University of Louisville, Louisville, Kentucky, USA.
authors.forename: A
authors.initials: A
authors.lastname: Azadi
authors.affiliation: Division of Medical Oncology and Hematology, James Graham Brown Cancer Center, University of Louisville, Louisville, Kentucky, USA.
authors.forename: D
authors.initials: D
authors.lastname: Jain
authors.affiliation: Division of Medical Oncology and Hematology, James Graham Brown Cancer Center, University of Louisville, Louisville, Kentucky, USA.
authors.forename: R
authors.initials: R
authors.lastname: Redman
authors.affiliation: Division of Medical Oncology and Hematology, James Graham Brown Cancer Center, University of Louisville, Louisville, Kentucky, USA. capere06@louisville.edu.
authors.forename: C A
authors.initials: CA
authors.lastname: Perez
mesh_terms: D000970:Antineoplastic Agents / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D006801:Humans; D007457:Iodine Radioisotopes / Q000627:therapeutic use*; D010671:Phenylurea Compounds / Q000627:therapeutic use*; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D000090063:Proto-Oncogene Mas; D011804:Quinolines / Q000627:therapeutic use*; D013964:Thyroid Neoplasms / Q000188:drug therapy*
chemical_list: D000970:Antineoplastic Agents; D007457:Iodine Radioisotopes; C000715470:MAS1 protein, human; D010671:Phenylurea Compounds; D047428:Protein Kinase Inhibitors; D000090063:Proto-Oncogene Mas; D011804:Quinolines; C531958:lenvatinib
keywords: Angiogenesis inhibitors; Lenvatinib; Thyroid cancer