Difference between revisions of "Ceritinib (Zykadia)"
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==General information== | ==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.<ref name="insert">[http://www.pharma.us.novartis.com/product/pi/pdf/zykadia.pdf Ceritinib (Zykadia) package insert]</ref><ref>[[:File:Ceritinib.pdf | Ceritinib (Zykadia) package insert (locally hosted backup)]]</ref><ref>[http://zykadia.com Zykadia manufacturer's website]</ref><ref>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. [https://doi.org/10.1056/NEJMoa1311107 link to original article] [https://pubmed.ncbi.nlm.nih.gov/24670165/ PubMed]</ref> | + | 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.<ref name="insert">[http://www.pharma.us.novartis.com/product/pi/pdf/zykadia.pdf Ceritinib (Zykadia) package insert]</ref><ref>[[:File:Ceritinib.pdf | Ceritinib (Zykadia) package insert (locally hosted backup)]]</ref><ref>[http://zykadia.com Zykadia manufacturer's website]</ref><ref>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. [https://doi.org/10.1056/NEJMoa1311107 link to original article] [https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4079055/ link to PMC article] [https://pubmed.ncbi.nlm.nih.gov/24670165/ PubMed]</ref> |
<br>Route: PO | <br>Route: PO | ||
<br>Extravasation: n/a | <br>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 | + | 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> |
==Diseases for which it is used== | ==Diseases for which it is used== | ||
| Line 11: | Line 11: | ||
==Patient drug information== | ==Patient drug information== | ||
*[http://www.pharma.us.novartis.com/product/pi/pdf/zykadia.pdf Ceritinib (Zykadia) package insert]<ref name="insert"></ref> | *[http://www.pharma.us.novartis.com/product/pi/pdf/zykadia.pdf Ceritinib (Zykadia) package insert]<ref name="insert"></ref> | ||
| − | *[https://chemocare.com/ | + | *[https://chemocare.com/druginfo/ceritinib.aspx Ceritinib (Zykadia) patient drug information (Chemocare)]<ref>[https://chemocare.com/druginfo/ceritinib.aspx Ceritinib (Zykadia) patient drug information (Chemocare)]</ref> |
*[http://www.uptodate.com/contents/ceritinib-patient-drug-information Ceritinib (Zykadia) patient drug information (UpToDate)]<ref>[http://www.uptodate.com/contents/ceritinib-patient-drug-information Ceritinib (Zykadia) patient drug information (UpToDate)]</ref> | *[http://www.uptodate.com/contents/ceritinib-patient-drug-information Ceritinib (Zykadia) patient drug information (UpToDate)]<ref>[http://www.uptodate.com/contents/ceritinib-patient-drug-information Ceritinib (Zykadia) patient drug information (UpToDate)]</ref> | ||
==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
| − | *2014-04-29: [https://web.archive.org/web/20170213201352/http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm395299.htm Accelerated approval] for the treatment of patients with [[Biomarkers#ALK|anaplastic lymphoma kinase (ALK)]]-[[Biomarkers#Rearrangement|positive]] metastatic [[Non-small_cell_lung_cancer|non-small cell lung cancer (NSCLC)]] who have progressed on or are intolerant to [[Crizotinib (Xalkori) | crizotinib]]. ''(Based on | + | *2014-04-29: [https://web.archive.org/web/20170213201352/http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm395299.htm Accelerated approval] for the treatment of patients with [[Biomarkers#ALK|anaplastic lymphoma kinase (ALK)]]-[[Biomarkers#Rearrangement|positive]] metastatic [[Non-small_cell_lung_cancer|non-small cell lung cancer (NSCLC)]] who have progressed on or are intolerant to [[Crizotinib (Xalkori) | crizotinib]]. ''(Based on ASCEND-1)'' |
| − | *2017-05-26: [https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm560873.htm Granted regular FDA approval] for patients with metastatic [[Non-small_cell_lung_cancer|non-small cell lung cancer (NSCLC)]] whose tumors are [[Biomarkers#ALK|anaplastic lymphoma kinase (ALK)]]-[[Biomarkers#Rearrangement|positive]] as detected by an FDA-approved test. ''(Based on | + | *2017-05-26: [https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm560873.htm Granted regular FDA approval] for patients with metastatic [[Non-small_cell_lung_cancer|non-small cell lung cancer (NSCLC)]] whose tumors are [[Biomarkers#ALK|anaplastic lymphoma kinase (ALK)]]-[[Biomarkers#Rearrangement|positive]] as detected by an FDA-approved test. ''(Based on ASCEND-4)'' |
==History of changes in EMA indication== | ==History of changes in EMA indication== | ||
| Line 27: | Line 27: | ||
*2017-09-22: Revised indication for the treatment of unresectable advanced/relapsed ALK fusion gene-positive [[non-small cell lung cancer]]. | *2017-09-22: Revised indication for the treatment of unresectable advanced/relapsed ALK fusion gene-positive [[non-small cell lung cancer]]. | ||
==Also known as== | ==Also known as== | ||
| − | *'''Code name:''' | + | *'''Code name:''' LDK-378 |
*'''Brand names:''' Lucicer, Noxalk, Spexib, Zykadia | *'''Brand names:''' Lucicer, Noxalk, Spexib, Zykadia | ||
Latest revision as of 11:59, 6 July 2024
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 or the prescribing information.[1]
Diseases for which it is used
Patient drug information
- Ceritinib (Zykadia) package insert[1]
- Ceritinib (Zykadia) patient drug information (Chemocare)[5]
- Ceritinib (Zykadia) patient drug information (UpToDate)[6]
History of changes in FDA indication
- 2014-04-29: Accelerated approval 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. (Based on ASCEND-1)
- 2017-05-26: Granted regular FDA approval for patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. (Based on ASCEND-4)
History of changes in EMA indication
- 2015-05-06: Initial marketing authorization as Zykadia.
History of changes in Health Canada indication
- 2015-03-27: Initial notice of compliance with conditions as monotherapy for use in patients with anaplastic lymphoma kinase (ALK)-positive locally advanced (not amenable to curative therapy) or metastatic non-small cell lung cancer (NSCLC) who have progressed on or who were intolerant to crizotinib.
- 2018-06-06: New indication for previously untreated adult patients with anaplastic lymphoma kinase (ALK)-positive locally advanced or metastatic non-small cell lung cancer.
History of changes in PMDA indication
- 2016-03-28: Initial approval for the treatment of unresectable advanced/relapsed anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer with resistance or intolerance to crizotinib.
- 2017-09-22: Revised indication for the treatment of unresectable advanced/relapsed ALK fusion gene-positive non-small cell lung cancer.
Also known as
- Code name: LDK-378
- Brand names: Lucicer, Noxalk, Spexib, Zykadia
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 link to PMC article PubMed
- ↑ Ceritinib (Zykadia) patient drug information (Chemocare)
- ↑ Ceritinib (Zykadia) patient drug information (UpToDate)