Vemurafenib

{
  "id": "MLC-T-ONC-009207",
  "term": "Vemurafenib",
  "field": "Oncology and biomedicine",
  "definitions": [
    "A drug used to treat Erdheim-Chester disease (a very rare type of histiocytosis) and advanced melanoma that have a certain mutation (change) in the BRAF gene. It is also being studied in the treatment of other types of cancer. Vemurafenib blocks certain proteins made by the mutated BRAF gene, which may help keep cancer cells from growing. It is a type of kinase inhibitor. Also called BRAF (V600E) kinase inhibitor RO5185426, PLX4032, RG7204, and Zelboraf.",
    "An orally bioavailable, ATP-competitive, small-molecule inhibitor of BRAF(V600E) kinase with potential antineoplastic activity. Vemurafenib selectively binds to the ATP-binding site of BRAF(V600E) kinase and inhibits its activity, which may result in an inhibition of an over-activated MAPK signaling pathway downstream in BRAF(V600E) kinase-expressing tumor cells and a reduction in tumor cell proliferation. Approximately 90% of BRAF gene mutations involve a valine-to-glutamic acid mutation at residue 600 (V600E); the oncogene protein product, BRAF(V600E) kinase, exhibits a markedly elevated activity that over-activates the MAPK signaling pathway. The BRAF(V600E) gene mutation has been found to occur in approximately 60% of melanomas, and in about 8% of all solid tumors, including melanoma, colorectal, thyroid and other cancers."
  ],
  "synonyms": [
    "BRAF (V600E) kinase inhibitor RO5185426",
    "PLX4032",
    "RG7204",
    "Zelboraf",
    "BRAF(V600E) kinase inhibitor RO5185426"
  ],
  "references": [
    "NCI Dictionary of Cancer Terms",
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/vemurafenib/"
}