Cobimetinib: Difference between revisions

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==Overview==
'''Cobimetinib''' (trade name '''Cotellic''') is a [[MEK inhibitor]] developed by [[Exelixis]] and [[Genentech]]. It is used in combination with [[vemurafenib]], a [[BRAF (gene)|BRAF]] inhibitor, to treat melanoma. In November 2015, the U.S. Food and Drug Administration approved cobimetinib for unresectable or metastatic melanoma with a BRAF [[V600E]] or [[V600K]] mutation, in combination with [[vemurafenib]] (Zelboraf).  Cobimetinib is not indicated for treatment of patients with wild-type BRAF melanoma.
Cobimetinib in combination with vemurafenib is reportedly priced at $17,600 per month, or about $211,000 per year and is reported to cost $15,300 monthly, or $183,600 per year.
== Medical use ==
Cobimetinib is approved for use in combination with [[vemurafenib]] (trade name Zelboraf) for the treatment of advanced [[melanoma]] that cannot be removed by surgery or which has spread to other parts of the body, provided that the melanoma has an abnormal gene, with a mutation of BRAF (either V600E or V600K).
== Adverse effects ==
Common adverse effects observed in cobimetinib and vemurafinib co-treated persons in clinical trials included diarrhea, nausea, vomiting, rash, photosensitivity, and [[pyrexia]].
== Clinical trials ==
Acquired resistance to BRAF inhibitors, such as [[vemurafenib]] and [[dabrafenib]], commonly occurs after a several months of progression-free tumor response.  Preclinical data indicated the involvement of [[MAPK]] pathways and MAPK-independent signaling in the developed resistance, suggesting dual inhibition of MEK and BRAF kinase as a strategy for increasing the longevity of tumor response seen with BRAF inhibition alone. In phase III clinical trials, the combination of cobimetinib and vemurafenib was tested in patients with BRAFV600-mutated metastic melanoma, which resulted in significant improvement in progression-free survival in patients, but also produced some increase in toxicity. The combination increased progression-free survival to an average of 12.3 months, compared to 7.2 months for vemurafenib alone. This clinical data also showed that the combination treatment resulted in 65% survival rate of patients 17 months after beginning the treatment, increased rates from the 50% of patients on vemurafenib treatment alone. Adding cobimetinib also increased the median overall survival to 25.6 months, compared to the 18 months for vemurafenib alone.
== References ==
{{reflist}}
==External links==
* [http://www.cotellic.com/hcp Cotellic (cobimetinib) Official Web Site]
* [http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206192s000lbl.pdf Highlights of prescribing information]
[[Category:Azetidines]]
[[Category:Benzamides]]
[[Category:Experimental cancer drugs]]
[[Category:Fluoroarenes]]
[[Category:Iodoarenes]]
[[Category:MEK inhibitor]]
[[Category:Piperidines]]
[[Category:Protein kinase inhibitors]]

Revision as of 19:54, 19 January 2017