selpercatinib

{
  "id": "MLC-T-ONC-007648",
  "term": "selpercatinib",
  "field": "Oncology and biomedicine",
  "definitions": [
    "A drug used to treat certain types of non-small cell lung cancer in adults and certain types of thyroid cancer or other solid tumor in adults and children aged 2 years and older. It is used in patients whose cancer has an abnormal RET gene. It is also being studied in the treatment of other types of cancer. Selpercatinib blocks certain proteins, including those made by the RET fusion gene or the mutated RET gene. Blocking these proteins may help keep cancer cells from growing. Selpercatinib is a type of tyrosine kinase inhibitor. Also called Retevmo.",
    "An orally bioavailable selective inhibitor of wild-type, mutant and fusion products involving the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET), with potential antineoplastic activity. Upon oral administration, selpercatinib selectively binds to and targets wild-type RET as well as various RET mutants and RET-containing fusion products. This results in an inhibition of cell growth of tumors cells that exhibit increased RET activity. In addition, selpercatinib targets, binds to and inhibits vascular endothelial growth factor receptor 1 (VEGFR1) and 3 (VEGFR3), and fibroblast growth factor receptor 1 (FGFR1), 2 (FGFR2), and 3 (FGFR3). RET overexpression, activating mutations, and fusions result in the upregulation and/or overactivation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and progression of these cancers."
  ],
  "synonyms": [
    "Retevmo",
    "RET inhibitor LOXO-292",
    "RET kinase inhibitor LOXO-292",
    "WHO 10967"
  ],
  "references": [
    "NCI Dictionary of Cancer Terms",
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/selpercatinib/"
}