Difference between revisions of "Ceritinib (Zykadia)"
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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> | ||
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==Patient drug information== | ==Patient drug information== | ||
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[[Category:Kinase inhibitors]] | [[Category:Kinase inhibitors]] | ||
[[Category:ALK inhibitors]] | [[Category:ALK inhibitors]] | ||
[[Category:IGF inhibitors]] | [[Category:IGF inhibitors]] | ||
[[Category:ROS1 inhibitors]] | [[Category:ROS1 inhibitors]] | ||
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[[Category:Non-small cell lung cancer medications]] | [[Category:Non-small cell lung cancer medications]] | ||
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[[Category:Drugs FDA approved in 2014]] | [[Category:Drugs FDA approved in 2014]] | ||
Revision as of 01:45, 30 June 2014
General information
Class/mechanism: Tyrosine kinase inhibitor; inhibits anaplastic lymphoma kinase (ALK). Ceritinib prevents growth of ALK-rearranged cancer cells by inhibiting autophosphorylation of ALK and subsequent ALK-mediated phosphorylation of the downstream signaling protein STAT3. In vitro, ceritinib is 20 times as potent against ALK as compared to Crizotinib (Xalkori) and inhibits growth of cells expressing EML4-ALK and NPM-ALK fusion proteins. Ceritinib has been observed in EML4-ALK-rearranged non-small cell lung cancer xenograft models to have activity against crizotinib-sensitive and crizotinib-resistant tumors. Ceritinib also inhibits the insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1. It does not inhibit MET.[1][2][3][4]
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]
Patient drug information
History of changes in FDA indication
- 4/29/2014: FDA approved "for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib."
Also known as
LDK378.
References
- ↑ 1.0 1.1 1.2 Ceritinib (Zykadia) package insert
- ↑ Ceritinib (Zykadia) package insert (locally hosted backup)
- ↑ Zykadia manufacturer's website
- ↑ Shaw AT, Kim DW, Mehra R, Tan DS, Felip E, Chow LQ, Camidge DR, Vansteenkiste J, Sharma S, De Pas T, Riely GJ, Solomon BJ, Wolf J, Thomas M, Schuler M, Liu G, Santoro A, Lau YY, Goldwasser M, Boral AL, Engelman JA. Ceritinib in ALK-rearranged non-small-cell lung cancer. N Engl J Med. 2014 Mar 27;370(13):1189-97. link to original article PubMed