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, 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, 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

History of changes in EMA indication

  • 2018-11-22: Initial authorization

History of changes in Health Canada indication

  • 2018-07-26: Initial notice of compliance with conditions as a monotherapy for the treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or who were intolerant to an ALK inhibitor (crizotinib).
    • 2022-07-20: Conditions were met
  • 2021-03-03: New indication for the first line treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive locally advanced (not amenable to curative therapy) or metastatic non-small cell lung cancer (NSCLC).

Also known as

  • Code name: AP26113
  • Brand names: Alunbrig, Biganib, Briganix, Trepmac