Difference between revisions of "Cobimetinib (Cotellic)"
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==General information== | ==General information== | ||
| − | Class/mechanism: Tyrosine kinase inhibitor, [ | + | Class/mechanism: Tyrosine kinase inhibitor, [https://en.wikipedia.org/wiki/MAP2K1 MEK1 (mitogen-activated extracellular signal regulated kinase 1)] and [https://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 | ||
| Line 8: | Line 8: | ||
==Diseases for which it is used== | ==Diseases for which it is used== | ||
*[[Melanoma,_BRAF-mutated|BRAF-mutated melanoma]] | *[[Melanoma,_BRAF-mutated|BRAF-mutated melanoma]] | ||
| + | *[[Craniopharyngioma]] | ||
| + | *[[Erdheim-Chester disease]] | ||
| + | *[[Langerhans cell histiocytosis]] | ||
| + | *[[Rosai-Dorfman-Destombes disease]] | ||
==Patient drug information== | ==Patient drug information== | ||
| − | *[ | + | *[https://www.gene.com/download/pdf/cotellic_prescribing.pdf Cobimetinib (Cotellic) package insert]<ref name="insert"></ref> |
==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
| − | *11 | + | *2015-11-10: Approved for the treatment of patients with unresectable or metastatic [[melanoma]] with a [[Biomarkers#BRAF|BRAF]] [[Biomarkers#V600E|V600E]] or [[Biomarkers#V600K|V600K mutation]], in combination with [[Vemurafenib (Zelboraf) | vemurafenib]]. ''(Based on coBRIM)'' |
| − | + | *2022-11-01: Approved for the treatment of adult patients with the family of blood diseases known as histiocytic neoplasms. These diseases include [[Erdheim-Chester disease]], [[Rosai-Dorfman-Destombes disease|Rosai-Dorfman disease]], and [[Langerhans cell histiocytosis]]. ''(Based on MSK 15-216)'' | |
| + | ==History of changes in EMA indication== | ||
| + | *2015-11-20: Initial authorization in combination with vemurafenib for the treatment of patients with unresectable or metastatic [[melanoma]] with a BRAF V600 mutation. | ||
| + | ==History of changes in Health Canada indication== | ||
| + | *2016-02-22: Initial notice of compliance | ||
==Also Known As== | ==Also Known As== | ||
| − | *'''Code names:''' GDC-0973, | + | *'''Code names:''' GDC-0973, XL-518 |
*'''Brand name:''' Cotellic | *'''Brand name:''' Cotellic | ||
| Line 26: | Line 34: | ||
[[Category:Oral medications]] | [[Category:Oral medications]] | ||
| − | + | ||
[[Category:MAP2K1 inhibitors]] | [[Category:MAP2K1 inhibitors]] | ||
[[Category:MAP2K2 inhibitors]] | [[Category:MAP2K2 inhibitors]] | ||
| + | [[Category:Craniopharyngioma medications]] | ||
| + | [[Category:Erdheim-Chester disease medications]] | ||
| + | [[Category:Langerhans cell histiocytosis medications]] | ||
[[Category:Melanoma medications]] | [[Category:Melanoma medications]] | ||
| + | [[Category:Rosai-Dorfman-Destombes disease medications]] | ||
| + | |||
| + | [[Category:EMA approved in 2015]] | ||
[[Category:FDA approved in 2015]] | [[Category:FDA approved in 2015]] | ||
| + | [[Category:Health Canada approved in 2016]] | ||
Revision as of 01:43, 26 June 2024
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
- BRAF-mutated melanoma
- Craniopharyngioma
- Erdheim-Chester disease
- Langerhans cell histiocytosis
- Rosai-Dorfman-Destombes disease
Patient drug information
History of changes in FDA indication
- 2015-11-10: 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)
- 2022-11-01: Approved for the treatment of adult patients with the family of blood diseases known as histiocytic neoplasms. These diseases include Erdheim-Chester disease, Rosai-Dorfman disease, and Langerhans cell histiocytosis. (Based on MSK 15-216)
History of changes in EMA indication
- 2015-11-20: Initial authorization in combination with vemurafenib for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600 mutation.
History of changes in Health Canada indication
- 2016-02-22: Initial notice of compliance
Also Known As
- Code names: GDC-0973, XL-518
- Brand name: Cotellic
References
Categories:
- Drugs
- Mutation-specific medications
- Oral medications
- MAP2K1 inhibitors
- MAP2K2 inhibitors
- Craniopharyngioma medications
- Erdheim-Chester disease medications
- Langerhans cell histiocytosis medications
- Melanoma medications
- Rosai-Dorfman-Destombes disease medications
- EMA approved in 2015
- FDA approved in 2015
- Health Canada approved in 2016