Difference between revisions of "Cobimetinib (Cotellic)"
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==General information== | ==General information== | ||
− | Class/mechanism: Tyrosine kinase inhibitor, [http://en.wikipedia.org/wiki/MAP2K1 MEK1 (mitogen-activated extracellular signal regulated kinase 1)] and [http://en.wikipedia.org/wiki/MAP2K2 MEK2] inhibitor. Cobimetinib inhibits the mitogen-activated protein kinase (MAPK)/extracellular signal-related kinase (ERK) pathway by inhibiting MEK1 and MEK2. Cancers with BRAF V600E and K mutations have constitutive activation of the BRAF pathway, which includes MEK1 and MEK2. Inhibiting MEK1 and MEK2 results in inhibition of ERK and cellular proliferation.<ref name=insert>[https://www.gene.com/download/pdf/cotellic_prescribing.pdf Cobimetinib (Cotellic) package insert]</ref><ref>[[ | + | Class/mechanism: Tyrosine kinase inhibitor, [http://en.wikipedia.org/wiki/MAP2K1 MEK1 (mitogen-activated extracellular signal regulated kinase 1)] and [http://en.wikipedia.org/wiki/MAP2K2 MEK2] inhibitor. Cobimetinib inhibits the mitogen-activated protein kinase (MAPK)/extracellular signal-related kinase (ERK) pathway by inhibiting MEK1 and MEK2. Cancers with BRAF V600E and K mutations have constitutive activation of the BRAF pathway, which includes MEK1 and MEK2. Inhibiting MEK1 and MEK2 results in inhibition of ERK and cellular proliferation.<ref name=insert>[https://www.gene.com/download/pdf/cotellic_prescribing.pdf Cobimetinib (Cotellic) package insert]</ref><ref>[[File:Cobimetinib.pdf | Cobimetinib (Cotellic) package insert (locally hosted backup)]]</ref> |
<br>Route: PO | <br>Route: PO | ||
<br>Extravasation: n/a | <br>Extravasation: n/a |
Revision as of 00:10, 20 September 2021
General information
Class/mechanism: Tyrosine kinase inhibitor, MEK1 (mitogen-activated extracellular signal regulated kinase 1) and MEK2 inhibitor. Cobimetinib inhibits the mitogen-activated protein kinase (MAPK)/extracellular signal-related kinase (ERK) pathway by inhibiting MEK1 and MEK2. Cancers with BRAF V600E and K mutations have constitutive activation of the BRAF pathway, which includes MEK1 and MEK2. Inhibiting MEK1 and MEK2 results in inhibition of ERK and cellular proliferation.[1][2]
Route: PO
Extravasation: n/a
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]
Diseases for which it is used
Patient drug information
History of changes in FDA indication
- 11/10/2015: Approved for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, in combination with vemurafenib. (Based on coBRIM)
Also Known As
- Code names: GDC-0973, XL518
- Brand name: Cotellic