Difference between revisions of "Nilotinib (Tasigna)"
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==General information== | ==General information== | ||
− | Class/mechanism: Tyrosine kinase inhibitor of Bcr-Abl, the constitutively active tyrosine kinase resulting from the Philadelphia chromosome abnormality in CML. Nilotinib binds to the inactive conformation of the Abl kinase domain and stabilizes it.<ref name="insert">[https://www.pharma.us.novartis.com/sites/www.pharma.us.novartis.com/files/tasigna.pdf Nilotinib (Tasigna) package insert]</ref><ref>[[ | + | Class/mechanism: Tyrosine kinase inhibitor of Bcr-Abl, the constitutively active tyrosine kinase resulting from the Philadelphia chromosome abnormality in CML. Nilotinib binds to the inactive conformation of the Abl kinase domain and stabilizes it.<ref name="insert">[https://www.pharma.us.novartis.com/sites/www.pharma.us.novartis.com/files/tasigna.pdf Nilotinib (Tasigna) package insert]</ref><ref>[[:File:Nilotinib.pdf | Nilotinib (Tasigna) package insert (locally hosted backup)]]</ref><ref>[http://tasigna.com Tasigna manufacturer's website]</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 such as | + | 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, [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 established== | |
+ | *[[Chronic myeloid leukemia]] | ||
==Diseases for which it is used== | ==Diseases for which it is used== | ||
− | |||
*[[Hypereosinophilic syndrome]] | *[[Hypereosinophilic syndrome]] | ||
*[[B-cell_acute_lymphoblastic_leukemia,_Ph-positive|Ph+ B-cell ALL]] | *[[B-cell_acute_lymphoblastic_leukemia,_Ph-positive|Ph+ B-cell ALL]] | ||
Line 18: | Line 18: | ||
==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
− | *10 | + | *2007-10-29: Granted accelerated approval for the treatment of chronic phase and accelerated phase [[Biomarkers#BCR-ABL1|Philadelphia chromosome positive]] [[Chronic myeloid leukemia |chronic myelogenous leukemia (CML)]] in adult patients resistant to or intolerant to prior therapy that included [[Imatinib (Gleevec)]]. ''(Based on A2101)'' |
− | * | + | **2011-01-14: Converted to regular approval for the treatment of chronic phase and accelerated phase [[Biomarkers#BCR-ABL1|Philadelphia chromosome positive]] [[Chronic myeloid leukemia |chronic myelogenous leukemia (CML)]] in adult patients resistant to or intolerant to prior therapy that included [[Imatinib (Gleevec)]]. |
− | *12 | + | *2010-06-17: Granted accelerated approval for the treatment of newly diagnosed adult patients with [[Biomarkers#BCR-ABL1|Philadelphia chromosome positive]] [[Chronic myeloid leukemia |chronic myeloid leukemia]] (Ph+ CML) in chronic phase. ''(Approval extended to first-line setting; based on ENESTnd) |
− | * | + | **2015-01-27: Converted to regular approval. |
− | + | *2017-12-22: FDA label updated: Patients with newly diagnosed [[Biomarkers#BCR-ABL1 |Ph+]] [[Chronic myeloid leukemia |CML]] in the chronic phase (CP) and resistant or intolerant Ph+ CML-CP patients who have achieved a sustained molecular response (MR4.5) may be considered for discontinuation after at least three years of nilotinib. To be considered for discontinuation, patients must have typical BCR-ABL transcripts. An FDA-authorized test with a detection limit below at least MR4.5 must be used to determine discontinuation eligibility. Patients must be frequently monitored by this test to detect possible loss of remission. ''(Based on ENESTfreedom and ENESTop)'' | |
− | * | + | *2018-03-22: FDA approved for pediatric patients 1 year of age or older with newly diagnosed [[Biomarkers#BCR-ABL1 |Philadelphia chromosome positive]] [[Chronic myeloid leukemia |chronic myeloid leukemia]] in chronic phase (Ph+ CML-CP). ''(Approval extended to pediatric setting; based on DIALOG) |
+ | *2018-03-22: FDA approved for pediatric patients 1 year of age or older with [[Biomarkers#BCR-ABL1|Ph+]] [[Chronic myeloid leukemia |CML]]-CP resistant or intolerant to prior [[Regimen_classes#Tyrosine_kinase_inhibitor_therapy|tyrosine-kinase inhibitor (TKI) therapy]]. ''(Approval extended to pediatric setting; based on CAMN107A2120) | ||
+ | |||
+ | ==History of changes in EMA indication== | ||
+ | *2007-11-19: Initial authorization | ||
+ | ==History of changes in Health Canada indication== | ||
+ | *2008-09-09: Initial notice of compliance with conditions | ||
+ | *2011-11-30: Conditions were met | ||
+ | ==History of changes in PMDA indication== | ||
+ | *2009-01-21: Initial approval for the treatment of imatinib-resistant, chronic phase and accelerated phase [[Chronic myeloid leukemia|chronic myelogenous leukemia]]. | ||
+ | *2010-12-21: New additional indications and a new dosage for the treatment of chronic- or accelerated-phase [[Chronic myeloid leukemia|chronic myelocytic leukaemia]]. | ||
==Also known as== | ==Also known as== | ||
− | *'''Code name:''' | + | *'''Code name:''' AMN-107 |
*'''Brand name:''' Tasigna | *'''Brand name:''' Tasigna | ||
Line 44: | Line 54: | ||
[[Category:B-cell acute lymphoblastic leukemia medications]] | [[Category:B-cell acute lymphoblastic leukemia medications]] | ||
− | [[Category:Chronic | + | [[Category:Chronic myeloid leukemia medications]] |
[[Category:Hypereosinophilic syndrome medications]] | [[Category:Hypereosinophilic syndrome medications]] | ||
[[Category:Systemic mastocytosis medications]] | [[Category:Systemic mastocytosis medications]] | ||
+ | [[Category:EMA approved in 2007]] | ||
[[Category:FDA approved in 2007]] | [[Category:FDA approved in 2007]] | ||
+ | [[Category:Health Canada approved in 2008]] | ||
+ | [[Category:PMDA approved in 2009]] | ||
[[Category:WHO Essential Cancer Medicine]] | [[Category:WHO Essential Cancer Medicine]] |
Latest revision as of 12:13, 29 June 2024
General information
Class/mechanism: Tyrosine kinase inhibitor of Bcr-Abl, the constitutively active tyrosine kinase resulting from the Philadelphia chromosome abnormality in CML. Nilotinib binds to the inactive conformation of the Abl kinase domain and stabilizes it.[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 established
Diseases for which it is used
Patient drug information
- Nilotinib (Tasigna) package insert[1]
- Nilotinib (Tasigna) patient drug information (Chemocare)[4]
- Nilotinib (Tasigna) patient drug information (UpToDate)[5]
History of changes in FDA indication
- 2007-10-29: Granted accelerated approval for the treatment of chronic phase and accelerated phase Philadelphia chromosome positive chronic myelogenous leukemia (CML) in adult patients resistant to or intolerant to prior therapy that included Imatinib (Gleevec). (Based on A2101)
- 2011-01-14: Converted to regular approval for the treatment of chronic phase and accelerated phase Philadelphia chromosome positive chronic myelogenous leukemia (CML) in adult patients resistant to or intolerant to prior therapy that included Imatinib (Gleevec).
- 2010-06-17: Granted accelerated approval for the treatment of newly diagnosed adult patients with Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase. (Approval extended to first-line setting; based on ENESTnd)
- 2015-01-27: Converted to regular approval.
- 2017-12-22: FDA label updated: Patients with newly diagnosed Ph+ CML in the chronic phase (CP) and resistant or intolerant Ph+ CML-CP patients who have achieved a sustained molecular response (MR4.5) may be considered for discontinuation after at least three years of nilotinib. To be considered for discontinuation, patients must have typical BCR-ABL transcripts. An FDA-authorized test with a detection limit below at least MR4.5 must be used to determine discontinuation eligibility. Patients must be frequently monitored by this test to detect possible loss of remission. (Based on ENESTfreedom and ENESTop)
- 2018-03-22: FDA approved for pediatric patients 1 year of age or older with newly diagnosed Philadelphia chromosome positive chronic myeloid leukemia in chronic phase (Ph+ CML-CP). (Approval extended to pediatric setting; based on DIALOG)
- 2018-03-22: FDA approved for pediatric patients 1 year of age or older with Ph+ CML-CP resistant or intolerant to prior tyrosine-kinase inhibitor (TKI) therapy. (Approval extended to pediatric setting; based on CAMN107A2120)
History of changes in EMA indication
- 2007-11-19: Initial authorization
History of changes in Health Canada indication
- 2008-09-09: Initial notice of compliance with conditions
- 2011-11-30: Conditions were met
History of changes in PMDA indication
- 2009-01-21: Initial approval for the treatment of imatinib-resistant, chronic phase and accelerated phase chronic myelogenous leukemia.
- 2010-12-21: New additional indications and a new dosage for the treatment of chronic- or accelerated-phase chronic myelocytic leukaemia.
Also known as
- Code name: AMN-107
- Brand name: Tasigna
References
- Drugs
- Oral medications
- Mutation-specific medications
- Bcr-Abl inhibitors
- CSF1R inhibitors
- DDR inhibitors
- KIT inhibitors
- PDGFR inhibitors
- B-cell acute lymphoblastic leukemia medications
- Chronic myeloid leukemia medications
- Hypereosinophilic syndrome medications
- Systemic mastocytosis medications
- EMA approved in 2007
- FDA approved in 2007
- Health Canada approved in 2008
- PMDA approved in 2009
- WHO Essential Cancer Medicine