Difference between revisions of "Brigatinib (Alunbrig)"
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| − | = | + | ==General information== |
| − | + | Class/mechanism: Tyrosine kinase inhibitor (TKI); inhibits multiple kinases including anaplastic lymphoma kinase (ALK), ROS1, insulin-like growth factor-1 receptor (IGF-1R), FLT-3, and EGFR deletion and point mutations. Brigatinib inhibited growth of cells with EML4-ALK and NPM-ALK fusion proteins. Brigatinib prevents autophosphorylation of ALK and, subsequently, downstream signaling through STAT3, AKT, ERK1/2, and S6. Brigatinib inhibited cells expressing EML4-ALK, as well as mutant forms of EML4-ALK, such as as G1202R and L1196M. Brigatinib was able to inhibit some mutant forms which are associated with resistance to ALK inhibitors including [[Crizotinib (Xalkori)|crizotinib]], as well as EGFR-Del (E746-A750), ROS1-L2026M, FLT3-F691L, and FLT3-D835Y. <ref name=insert>[https://www.alunbrig.com/assets/pi.pdf Brigatinib (Alunbrig) package insert]</ref><ref>[[Media:Brigatinib.pdf | Brigatinib (Alunbrig) package insert (locally hosted backup)]]</ref><ref>[https://www.alunbrig.com/ Alunbrig manufacturer's website]</ref> | |
| + | <br>Route: PO | ||
| + | <br>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 [http://www.thomsonhc.com/home/dispatch Micromedex], [http://online.lexi.com/ Lexicomp], [http://www.utdol.com/online/content/search.do UpToDate (courtesy of Lexicomp)], or the prescribing information.<ref name="insert"></ref> | ||
| + | |||
| + | ==Diseases for which it is used== | ||
| + | *[[Non-small_cell_lung_cancer#Advanced_or_metastatic_disease.2C_ALK-positive | ALK+ non-small cell lung cancer]] | ||
| + | |||
| + | ==Patient drug information== | ||
| + | *[https://www.alunbrig.com/assets/pi.pdf Brigatinib (Alunbrig) package insert]<ref name="insert"></ref> | ||
| + | |||
| + | ==History of changes in FDA indication== | ||
| + | *4/28/2017: [https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm555841.htm FDA accelerated approval] "for the treatment of patients with metastatic [[Non-small cell lung cancer|anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer (NSCLC)]] who have progressed on or are intolerant to [[Crizotinib (Xalkori)|crizotinib]]." | ||
| + | |||
| + | ==Also known as== | ||
| + | AP26113 | ||
| + | |||
| + | ==References== | ||
| + | <references/> | ||
[[Category:Drug index]] | [[Category:Drug index]] | ||
[[Category:Chemotherapy]] | [[Category:Chemotherapy]] | ||
[[Category:Oral chemotherapy]] | [[Category:Oral chemotherapy]] | ||
| + | [[Category:Non-small cell lung cancer medications]] | ||
[[Category:Kinase inhibitors]] | [[Category:Kinase inhibitors]] | ||
[[Category:ALK inhibitors]] | [[Category:ALK inhibitors]] | ||
[[Category:EGFR inhibitors]] | [[Category:EGFR inhibitors]] | ||
| − | + | [[Category:ROS1 inhibitors]] | |
| − | [[Category: | + | [[Category:IGFR inhibitors]] |
| + | [[Category:FLT3 inhibitors]] | ||
| + | [[Category:Drugs FDA approved in 2017]] | ||
Revision as of 14:57, 29 April 2017
General information
Class/mechanism: Tyrosine kinase inhibitor (TKI); inhibits multiple kinases including anaplastic lymphoma kinase (ALK), ROS1, insulin-like growth factor-1 receptor (IGF-1R), FLT-3, and EGFR deletion and point mutations. Brigatinib inhibited growth of cells with EML4-ALK and NPM-ALK fusion proteins. Brigatinib prevents autophosphorylation of ALK and, subsequently, downstream signaling through STAT3, AKT, ERK1/2, and S6. Brigatinib inhibited cells expressing EML4-ALK, as well as mutant forms of EML4-ALK, such as as G1202R and L1196M. Brigatinib was able to inhibit some mutant forms which are associated with resistance to ALK inhibitors including crizotinib, as well as EGFR-Del (E746-A750), ROS1-L2026M, FLT3-F691L, and FLT3-D835Y. [1][2][3]
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
- 4/28/2017: FDA accelerated approval "for the treatment of patients with metastatic anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib."
Also known as
AP26113