Difference between revisions of "Afatinib (Gilotrif)"
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Revision as of 15:52, 1 January 2015
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
Clinical trials
- 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
- LUX-Lung 2 - Afatinib for EGFR positive lung adenocarcinoma after no more than one previous chemotherapy regimen for advanced disease[4]
- LUX-Lung 1 - Afatinib vs. placebo for lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy[5]
Patient drug information
- Afatinib (Gliotrif) package insert[1]
- Afatinib (Gliotrif) patient drug information (Chemocare)[6]
- Afatinib (Gliotrif) patient drug information (UpToDate)[7]
History of changes in FDA indication
- 7/12/2013: 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."
Also known as
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.
References
- ↑ 1.0 1.1 1.2 Afatinib (Gliotrif) package insert
- ↑ Afatinib (Gliotrif) package insert (locally hosted backup)
- ↑ Gliotrif manufacturer's website
- ↑ 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. link to original article PubMed
- ↑ 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. link to original article PubMed
- ↑ Afatinib (Gliotrif) patient drug information (Chemocare)
- ↑ Afatinib (Gliotrif) patient drug information (UpToDate)