Difference between revisions of "Brigatinib (Alunbrig)"
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==General information== | ==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>[[File:Brigatinib.pdf | Brigatinib (Alunbrig) package insert (locally hosted backup)]]</ref><ref>[https://www.alunbrig.com/ Alunbrig manufacturer's website]</ref> | + | 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>[[:File:Brigatinib.pdf | Brigatinib (Alunbrig) package insert (locally hosted backup)]]</ref><ref>[https://www.alunbrig.com/ Alunbrig manufacturer's website]</ref> |
<br>Route: PO | <br>Route: PO | ||
<br>Extravasation: n/a | <br>Extravasation: n/a | ||
Revision as of 03:31, 20 September 2021
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: 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. (Based on ALTA)
- 5/22/2020: Approved for adult patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC). (Converted to regular approval and prior treatment requirement removed); based on ALTA-1L)
Also known as
- Code name: AP26113
- Brand names: Alunbrig, Biganib, Briganix, Trepmac