Difference between revisions of "Afatinib (Gilotrif)"

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==General information==
 
==General information==
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Class/mechanism: Irreversible tyrosine kinase inhibitor of EGFR (epidermal growth factor receptor, ErbB1), HER2 (human epidermal growth factor receptor 2, ErbB2), and HER4 (human epidermal growth factor receptor 4, ErbB4). Inhibition of tyrosine kinase autophosphorylation inhibits ErbB signaling.<ref name=insert>[http://bidocs.boehringer-ingelheim.com/BIWebAccess/ViewServlet.ser?docBase=renetnt&folderPath=/Prescribing+Information/PIs/Gilotrif/Gilotrif.pdf Afatinib (Gliotrif) package insert]</ref><ref>[[Media:Afatinib.pdf | Afatinib (Gliotrif) package insert (locally hosted backup)]]</ref><ref>[http://www.gilotrif.com/ Gliotrif manufacturer's website]</ref>
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Class/mechanism: Irreversible tyrosine kinase inhibitor of EGFR (epidermal growth factor receptor, ErbB1), HER2 (human epidermal growth factor receptor 2, ErbB2), and HER4 (human epidermal growth factor receptor 4, ErbB4). Inhibition of tyrosine kinase autophosphorylation inhibits ErbB signaling.<ref name=insert>[http://bidocs.boehringer-ingelheim.com/BIWebAccess/ViewServlet.ser?docBase=renetnt&folderPath=/Prescribing+Information/PIs/Gilotrif/Gilotrif.pdf Afatinib (Gilotrif) package insert]</ref><ref>[[:File:Afatinib.pdf | Afatinib (Gilotrif) package insert (locally hosted backup)]]</ref><ref>[http://www.gilotrif.com/ Gliotrif manufacturer's website]</ref>
  
 
Route: PO  
 
Route: PO  
 
<br>Extravasation: n/a
 
<br>Extravasation: n/a
  
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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 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>
+
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==
 
==Diseases for which it is used==
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*[[Non-small cell lung cancer]]
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*[[Head and neck cancer]]
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*[[Non-small_cell_lung_cancer,_EGFR-mutated|EGFRm NSCLC]]
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==Clinical trials==
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*[[Non-small cell lung cancer, squamous|Squamous NSCLC]]
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*[http://www.asco.org/ASCOv2/Meetings/Abstracts?&vmview=abst_detail_view&confID=114&abstractID=91942 LUX-Lung 3: A randomized, open-label, phase III study of afatinib versus pemetrexed and cisplatin as first-line treatment for patients with advanced adenocarcinoma of the lung harboring EGFR-activating mutations]
 
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*LUX-Lung 2 - Afatinib for EGFR positive lung adenocarcinoma after no more than one previous chemotherapy regimen for advanced disease<ref>Yang JC, Shih JY, Su WC, Hsia TC, Tsai CM, Ou SH, Yu CJ, Chang GC, Ho CL, Sequist LV, Dudek AZ, Shahidi M, Cong XJ, Lorence RM, Yang PC, Miller VA. Afatinib for patients with lung adenocarcinoma and epidermal growth factor receptor mutations (LUX-Lung 2): a phase 2 trial. Lancet Oncol. 2012 May;13(5):539-48. Epub 2012 Mar 26. [http://www.sciencedirect.com/science/article/pii/S1470204512700864 link to original article] [http://www.ncbi.nlm.nih.gov/pubmed/22452895 PubMed]</ref>
 
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*LUX-Lung 1 - Afatinib vs. placebo for lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy<ref>Miller VA, Hirsh V, Cadranel J, Chen YM, Park K, Kim SW, Zhou C, Su WC, Wang M, Sun Y, Heo DS, Crino L, Tan EH, Chao TY, Shahidi M, Cong XJ, Lorence RM, Yang JC. Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trial. Lancet Oncol. 2012 May;13(5):528-38. Epub 2012 Mar 26. [http://www.sciencedirect.com/science/article/pii/S1470204512700876 link to original article] [http://www.ncbi.nlm.nih.gov/pubmed/22452896 PubMed]</ref>
 
  
 
==Patient drug information==
 
==Patient drug information==
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*[http://bidocs.boehringer-ingelheim.com/BIWebAccess/ViewServlet.ser?docBase=renetnt&folderPath=/Prescribing+Information/PIs/Gilotrif/Gilotrif.pdf Afatinib (Gliotrif) package insert]<ref name="insert"></ref>
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*[http://bidocs.boehringer-ingelheim.com/BIWebAccess/ViewServlet.ser?docBase=renetnt&folderPath=/Prescribing+Information/PIs/Gilotrif/Gilotrif.pdf Afatinib (Gilotrif) package insert]<ref name="insert"></ref>
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*[http://chemocare.com/chemotherapy/drug-info/afatinib.aspx Afatinib (Gliotrif) patient drug information (Chemocare)]<ref>[http://chemocare.com/chemotherapy/drug-info/afatinib.aspx Afatinib (Gliotrif) patient drug information (Chemocare)]</ref>
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*[https://chemocare.com/druginfo/afatinib.aspx Afatinib (Gilotrif) patient drug information (Chemocare)]<ref>[https://chemocare.com/druginfo/afatinib.aspx Afatinib (Gilotrif) patient drug information (Chemocare)]</ref>
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*[http://www.uptodate.com/contents/afatinib-patient-drug-information Afatinib (Gliotrif) patient drug information (UpToDate)]<ref>[http://www.uptodate.com/contents/afatinib-patient-drug-information Afatinib (Gliotrif) patient drug information (UpToDate)]</ref>
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*[http://www.uptodate.com/contents/afatinib-patient-drug-information Afatinib (Gilotrif) patient drug information (UpToDate)]<ref>[http://www.uptodate.com/contents/afatinib-patient-drug-information Afatinib (Gilotrif) patient drug information (UpToDate)]</ref>
  
 
==History of changes in FDA indication==
 
==History of changes in FDA indication==
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*7/12/2013: [http://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm360574.htm FDA approved] for "the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test."
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*2013-07-12: [http://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm360574.htm Approved] for the [[Contexts#First-line_therapy|first-line treatment]] of patients with [[Contexts#Metastatic|metastatic]] [[Non-small_cell_lung_cancer|non-small cell lung cancer (NSCLC)]] whose tumors have [[Biomarkers#EGFR|epidermal growth factor receptor]] [[Biomarkers#Exon_19|exon 19]] [[Biomarkers#Deletion|deletion]] or [[Biomarkers#L858R|exon 21 (L858R) substitution]] mutations as detected by an FDA-approved test. ''(Based on LUX-Lung 3)''
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*2016-04-15: Approved for treatment of patients with [[Contexts#Metastatic|metastatic]], [[Non-small cell lung cancer, squamous|squamous NSCLC]] [[Contexts#Subsequent-line_therapy|progressing after]] [[Regimen_classes#Platinum-based_regimen|platinum-based chemotherapy]]. ''(Based on LUX-Lung 8)''
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*2018-01-12: Approval expanded for a broadened indication in [[Contexts#First-line_therapy|first-line treatment]] of patients with [[Contexts#Metastatic|metastatic]] [[Non-small_cell_lung_cancer|non-small cell lung cancer (NSCLC)]] whose tumors have [[Biomarkers#Non-resistant|non-resistant]] [[Biomarkers#EGFR|epidermal growth factor receptor]] mutations as detected by an FDA-approved test. ''(Based on LUX-Lung 2, LUX-Lung 3, and LUX-Lung 6)''
  
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==History of changes in EMA indication==
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*2013-09-25: Initial marketing authorization as Giotrif as monotherapy for the treatment of Epidermal Growth Factor Receptor (EGFR) TKI-naïve adult patients with locally advanced or metastatic [[Non-small_cell_lung_cancer|non-small cell lung cancer (NSCLC)]] with activating EGFR mutation(s).
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*2016-03-31: Extension of indications to include patients with locally advanced or metastatic [[Non-small cell lung cancer, squamous|Non-small cell lung cancer (NSCLC) of squamous histology]] progressing on or after platinum-based chemotherapy.
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==History of changes in Health Canada indication==
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*2013-11-01: Initial notice of compliance as monotherapy for the treatment of Epidermal Growth Factor Receptor (EGFR) tyrosine kinase inhibitor-naïve patients with metastatic (including cytologically proven pleural effusion) [[Non-small cell lung cancer, nonsquamous|adenocarcinoma of the lung]] with activating EGFR mutation(s).
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*2016-08-25: New indication for second line treatment of patients with locally advanced or metastatic [[Non-small cell lung cancer, squamous|non-small cell lung cancer (NSCLC) of squamous histology]].
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*2018-09-20: Updated indication (unclear)
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==History of changes in PMDA indication==
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*2014-01-17: Initial approval for the treatment of unresectable advanced or recurrent [[non-small cell lung cancer]] with EGFR gene mutation.
 
==Also known as==
 
==Also known as==
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2-butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-,(2E)-, (2Z)-2-butenedioate (1:2), BIBW 2992, BIBW-2992, Tomtovok, Tovok. 
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*'''Code names:''' BIBW-2992
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*'''Generic name:''' afatinib dimaleate
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*'''Brand names:''' Afanix, Gilotrif, Giotrif, Tomtovok, Tovok, Xovoltib
  
 
==References==
 
==References==
 
<references/>
 
<references/>
  
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[[Category:Drug index]]
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[[Category:Drugs]]
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[[Category:Chemotherapy]]
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[[Category:Oral medications]]
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[[Category:Oral chemotherapy]]
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[[Category:Mutation-specific medications]]
  
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[[Category:Kinase inhibitors]]
 
 
[[Category:EGFR inhibitors]]
 
[[Category:EGFR inhibitors]]
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[[Category:ERBB2 inhibitors]]
 
[[Category:ERBB4 inhibitors]]
 
[[Category:ERBB4 inhibitors]]
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[[Category:Anti-HER2 medications]]
 
  
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[[Category:Head and neck cancer medications]]
 
[[Category:Non-small cell lung cancer medications]]
 
[[Category:Non-small cell lung cancer medications]]
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[[Category:Drugs FDA approved in 2013]]
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[[Category:Non-small cell lung cancer, squamous medications]]
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[[Category:EMA approved in 2013]]
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[[Category:FDA approved in 2013]]
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[[Category:Health Canada approved in 2013]]
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[[Category:PMDA approved in 2014]]
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[[Category:WHO Essential Cancer Medicine]]

Revision as of 00:28, 9 September 2023

General information

Class/mechanism: Irreversible tyrosine kinase inhibitor of EGFR (epidermal growth factor receptor, ErbB1), HER2 (human epidermal growth factor receptor 2, ErbB2), and HER4 (human epidermal growth factor receptor 4, ErbB4). Inhibition of tyrosine kinase autophosphorylation inhibits ErbB signaling.[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

History of changes in EMA indication

  • 2013-09-25: Initial marketing authorization as Giotrif as monotherapy for the treatment of Epidermal Growth Factor Receptor (EGFR) TKI-naïve adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with activating EGFR mutation(s).
  • 2016-03-31: Extension of indications to include patients with locally advanced or metastatic Non-small cell lung cancer (NSCLC) of squamous histology progressing on or after platinum-based chemotherapy.

History of changes in Health Canada indication

  • 2013-11-01: Initial notice of compliance as monotherapy for the treatment of Epidermal Growth Factor Receptor (EGFR) tyrosine kinase inhibitor-naïve patients with metastatic (including cytologically proven pleural effusion) adenocarcinoma of the lung with activating EGFR mutation(s).
  • 2016-08-25: New indication for second line treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) of squamous histology.
  • 2018-09-20: Updated indication (unclear)

History of changes in PMDA indication

  • 2014-01-17: Initial approval for the treatment of unresectable advanced or recurrent non-small cell lung cancer with EGFR gene mutation.

Also known as

  • Code names: BIBW-2992
  • Generic name: afatinib dimaleate
  • Brand names: Afanix, Gilotrif, Giotrif, Tomtovok, Tovok, Xovoltib

References

  1. ↑ 1.0 1.1 1.2 Afatinib (Gilotrif) package insert
  2. ↑ Afatinib (Gilotrif) package insert (locally hosted backup)
  3. ↑ Gliotrif manufacturer's website
  4. ↑ Afatinib (Gilotrif) patient drug information (Chemocare)
  5. ↑ Afatinib (Gilotrif) patient drug information (UpToDate)
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