Difference between revisions of "Brigatinib (Alunbrig)"

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=Mechanism of action=
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==General information==
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From the [http://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=714373 NCI Drug Dictionary]: An orally available inhibitor of receptor tyrosine kinases anaplastic lymphoma kinase (ALK) and the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Dual ALK/EGFR inhibitor AP26113 binds to and inhibits ALK kinase and ALK fusion proteins as well as EGFR and mutant forms. This leads to the inhibition of ALK kinase and EGFR kinase, disrupts their signaling pathways and eventually inhibits tumor cell growth in susceptible tumor cells. In addition, AP26113 appears to overcome mutation-based resistance.
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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>
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<br>Route: PO
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<br>Extravasation: n/a
  
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[[Category:Drug index]]
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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 or the prescribing information.<ref name="insert"></ref>
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[[Category:Chemotherapy]]
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[[Category:Oral chemotherapy]]
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==Diseases for which it is used==
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*[[Non-small_cell_lung_cancer,_ALK-positive|ALK+ non-small cell lung cancer]]
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==Patient drug information==
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*[https://www.alunbrig.com/assets/pi.pdf Brigatinib (Alunbrig) package insert]<ref name="insert"></ref>
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==History of changes in FDA indication==
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*2017-04-28: [https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm555841.htm Accelerated approval] for the treatment of patients with metastatic [[Biomarkers#ALK|anaplastic lymphoma kinase (ALK)]]-[[Biomarkers#Rearrangement|positive]] [[Non-small_cell_lung_cancer|non-small cell lung cancer (NSCLC)]] who have progressed on or are intolerant to [[Crizotinib (Xalkori)|crizotinib]]. ''(Based on ALTA)''
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**2020-05-22: Full approval for adult patients with [[Biomarkers#ALK|anaplastic lymphoma kinase (ALK)]]-[[Biomarkers#Rearrangement|positive]] metastatic [[Non-small_cell_lung_cancer|non-small cell lung cancer (NSCLC)]]. ''(Converted to regular approval and prior treatment requirement removed); based on ALTA-1L)''
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==History of changes in EMA indication==
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*2018-11-22: Initial authorization as Alunbrig. Alunbrig is indicated as monotherapy for the treatment of adult patients with anaplastic lymphoma kinase (ALK) positive advanced [[Non-small_cell_lung_cancer|non-small cell lung cancer (NSCLC)]] previously treated with crizotinib. ''(Based on ALTA)''
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*2020-04-01: Extension of indication to include first-line treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive advanced [[Non-small_cell_lung_cancer|non-small cell lung cancer (NSCLC)]] previously not treated with an ALK inhibitor. ''(Based on ALTA-1L)''
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==History of changes in Health Canada indication==
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*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|non-small cell lung cancer (NSCLC)]] who have progressed on or who were intolerant to an ALK inhibitor (crizotinib).
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**2022-07-20: Conditions were met
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*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|non-small cell lung cancer (NSCLC)]].
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==History of changes in PMDA indication==
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*2021-01-22: Newly indicated for the treatment of unresectable advanced/recurrent anaplastic lymphoma kinase (ALK)-positive [[non-small cell lung cancer]].
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==Also known as==
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*'''Code name:''' AP-26113
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*'''Brand names:''' Alunbrig, Biganib, Briganix, Trepmac
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==References==
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<references/>
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[[Category:Drugs]]
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[[Category:Oral medications]]
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[[Category:Mutation-specific medications]]
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[[Category:Non-small cell lung cancer medications]]
  
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[[Category:Kinase inhibitors]]
 
 
[[Category:ALK inhibitors]]
 
[[Category:ALK inhibitors]]
 
[[Category:EGFR inhibitors]]
 
[[Category:EGFR inhibitors]]
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[[Category:ROS1 inhibitors]]
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[[Category:IGFR inhibitors]]
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[[Category:FLT3 inhibitors]]
  
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[[Category:Investigational]]
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[[Category:FDA approved in 2017]]
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[[Category:EMA approved in 2017]]
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[[Category:Health Canada approved in 2018]]
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[[Category:PMDA approved in 2021]]

Latest revision as of 01:06, 29 June 2024

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 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 as Alunbrig. Alunbrig is indicated as monotherapy for the treatment of adult patients with anaplastic lymphoma kinase (ALK) positive advanced non-small cell lung cancer (NSCLC) previously treated with crizotinib. (Based on ALTA)
  • 2020-04-01: Extension of indication to include first-line treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive advanced non-small cell lung cancer (NSCLC) previously not treated with an ALK inhibitor. (Based on ALTA-1L)

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).

History of changes in PMDA indication

  • 2021-01-22: Newly indicated for the treatment of unresectable advanced/recurrent anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer.

Also known as

  • Code name: AP-26113
  • Brand names: Alunbrig, Biganib, Briganix, Trepmac

References

  1. ↑ 1.0 1.1 1.2 Brigatinib (Alunbrig) package insert
  2. ↑ Brigatinib (Alunbrig) package insert (locally hosted backup)
  3. ↑ Alunbrig manufacturer's website
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