The Exelixis pipeline includes our lead compounds, cabozantinib and cobimetinib, as well as other programs that are the subject of partnerships and collaborations with other biopharmaceutical companies. An additional wholly-owned compound, XL888, is the subject of ongoing clinical research through our Investigator-Sponsored Trial program. Safety and efficacy for these compounds in the unapproved uses or indications described below have not yet been established.
Exelixis focuses its internal development efforts primarily upon cabozantinib, a targeted agent that inhibits the activity of receptor tyrosine kinases including MET, VEGF Receptors, AXL, and RET. These receptor tyrosine kinases are involved in both normal cellular function and in pathologic processes such as oncogenesis, metastasis, tumor angiogenesis, and maintenance of the tumor microenvironment. Exelixis discovered cabozantinib, internally and maintains exclusive rights to commercialize the product in the United States and Canada, and also in Japan, where it is seeking a commercial partner. Per an agreement announced in February 2016, Exelixis has granted Ipsen exclusive commercialization rights for current and future indications outside of those territories. Both companies will collaborate on the development of cabozantinib for current and future indications as well.
For information on approved uses of cabozantinib, please visit our Medicines page.
Cobimetinib, an Exelixis-discovered compound, is a selective inhibitor of MEK, part of the RAS/RAF/MEK/ERK pathway that is frequently dysregulated in human tumors. Cobimetinib is being developed by Genentech (a member of the Roche Group) under a collaboration agreement with Exelixis and is the subject of a broad clinical development program in combination with a variety of investigational and approved therapies.
Cobimetinib is commercially available in the United States for the treatment of unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, in combination with vemurafenib, where it is marketed as COTELLIC® for that use. COTELLIC is also approved in the European Union, Switzerland and Canada for the treatment of people with BRAF V600 mutation-positive advanced melanoma. For more information on COTELLIC, including important safety information, please click here.
XL888 is a highly potent, orally bioavailable ATP-competitive inhibitor of HSP90, a molecular chaperone protein that affects the activity and stability of a range of key regulatory proteins, including kinases such as BRAF, MET, and VEGFR2. Exelixis discovered XL888 and owns the compound exclusively.
We have established multiple partnerships and collaborations with other leading pharmaceutical and biopharmaceutical companies. These partnerships are designed to advance the development of a variety of potential therapies for cancer and other serious diseases.