Exelixis
Encyclopedia
Exelixis is a genomics
Genomics
Genomics is a discipline in genetics concerning the study of the genomes of organisms. The field includes intensive efforts to determine the entire DNA sequence of organisms and fine-scale genetic mapping efforts. The field also includes studies of intragenomic phenomena such as heterosis,...

-based drug discovery company located in South San Francisco, Ca. It works on the development of anti-cancer therapies. Exelixis has several compounds in various stages of FDA approval including :
  • XL147 that targets phosphoinositide-3 kinase (PI3K); and
  • XL765, which targets PI3K and mTOR, kinases in the PI3K signaling pathway.
  • XL880
    Foretinib
    Foretinib is an experimental drug candidate for the treatment of cancer. It was discovered by Exelixis and is under development by GlaxoSmithKline. It is currently in Phase II clinical trials....

     (foretinib)


The company also has various compounds in phase 1 clinical trials, including
  • XL518, a small molecule inhibitor of the MEK
    MEK
    MEK or Mek may refer to:* In chemistry and industry methyl ethyl ketone, a solvent, used also to weld some plastics* The Iranian guerilla-cum-opposition group Mujahideen-e Khalq* Mek, a comic mini series by Warren Ellis...

    ;
  • XL228, which targets insulin-like growth factor type 1 receptor, an RTK in a range of human tumors;
  • XL139 that targets Hedgehog; XL413, a small molecule inhibitor of the serine-threonine kinase CDC7;
  • XL888, a synthetic inhibitor of HSP90
    Hsp90
    Hsp90 is a molecular chaperone and is one of the most abundant proteins expressed in cells. It is a member of the heat shock protein family, which is upregulated in response to stress...

    , a chaperone protein that promotes the activity and stability of a range of regulatory proteins, including kinases.


Its lead compound, XL184, is currently in a number of clinical trials for prostate, ovarian, brain, melanoma, breast, non-small cell lung, hepatocellular, kidney, and medullary thyroid cancer. XL184 was recently designated orphan-drug status by the FDA and given the generic name, cabozantinib. Cabozantinib
Cabozantinib
Cabozantinib is a small molecule inhibitor of the tyrosine kinases Met and VEGFR2, and has been shown to reduce tumor growth, metastasis, and angiogenesis.It is being developed by Exelixis Inc....

is an inhibitor of the tyrosine kinases Met and VEGFR2, and has been shown to abrogate tumor growth, metastasis, and angiogenesis.
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