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Nilotinib

February 01, 2023

Nilotinib, sold under the brand name Tasigna marketed worldwide by Novartis, is a medication used to treat chronic myelogenous leukemia (CML) which has the Philadelphia chromosome.[2] It may be used both in initial cases of chronic phase CML as well as in accelerated and chronic phase CML that has not responded to imatinib.[2][3] It is taken by mouth.[3]

Nilotinib
Clinical data
Trade namesTasigna, others
Other namesAMN107
AHFS/Drugs.comMonograph
MedlinePlusa608002
License data
Pregnancy
category
  • AU: D
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability30%[1]
Protein binding98%[1]
MetabolismLiver (mostly CYP3A4-mediated)[1]
Elimination half-life15-17 hours[1]
ExcretionFaeces (93%)[1]
Identifiers
  • 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)- 5-(trifluoromethyl)phenyl]-3- [(4-pyridin-3-ylpyrimidin-2-yl) amino]benzamide
CAS Number
  • 641571-10-0 N (base)
PubChem CID
  • 644241
IUPHAR/BPS
  • 5697
DrugBank
  • DB04868 Y
ChemSpider
  • 559260 Y
UNII
  • F41401512X
KEGG
  • D08953 Y
ChEBI
  • CHEBI:52172 Y
ChEMBL
  • ChEMBL255863 Y
PDB ligand
  • NIL (PDBe, RCSB PDB)
CompTox Dashboard (EPA)
  • DTXSID5042663
ECHA InfoCard100.166.395
Chemical and physical data
FormulaC28H22F3N7O
Molar mass529.527 g·mol−1
3D model (JSmol)
  • Interactive image
  • Cc1ccc(cc1Nc2nccc(n2)c3cccnc3)C(=O)Nc4cc(cc(c4)n5cc(nc5)C)C(F)(F)F
  • InChI=1S/C28H22F3N7O/c1-17-5-6-19(10-25(17)37-27-33-9-7-24(36-27)20-4-3-8-32-14-20)26(39)35-22-11-21(28(29,30)31)12-23(13-22)38-15-18(2)34-16-38/h3-16H,1-2H3,(H,35,39)(H,33,36,37) Y
  • Key:HHZIURLSWUIHRB-UHFFFAOYSA-N Y
 NY (what is this?)  (verify)

Common side effects may include low platelets, low white blood cells, anemia, rashes, vomiting, diarrhea, and joint pains.[3] Other serious side effects may include QT prolongation, sudden death, pancreatitis, and liver problems.[3] It is not safe for use during pregnancy.[3] Nilotinib is a Bcr-Abl tyrosine kinase inhibitor and works by interfering with signalling within the cancer cell.[3]

Nilotinib was approved for medical use in the United States in 2007.[3] It is on the World Health Organization's List of Essential Medicines.[4]

Medical uses

Nilotinib is used to treat Philadelphia chromosome (Ph+)-positive chronic myelogenous leukaemia.[1]

Adverse effects

See also: List of adverse effects of nilotinib

Nilotinib has a number of adverse effects including headache, fatigue, gastrointestinal problems such as nausea, vomiting, diarrhea and constipation, muscle and joint pain, rash and other skin conditions, flu-like symptoms, and reduced blood cell count. Less typical side effects are those of the cardiovascular system, such as high blood pressure, various types of arrhythmia, and prolonged QT interval. Nilotinib can also affect the body's electrolyte and glucose balance.[5] Though lung-related adverse effects are rare when compared with imatinib and dasatinib, there is a case report of acute respiratory failure from diffuse alveolar hemorrhage in a people taking nilotinib.[6]

Nilotinib carries a black box warning in the United States for possible heart complications.[7][8] Contraindications include long QT syndrome, hypokalaemia, hypomagnesaemia, pregnancy, planned pregnancy, lactation and galactose/lactose intolerance.[1][9]

Cautions include:[1]

  • Myelosuppression
  • Tumour lysis syndrome
  • Liver impairment
  • History of pancreatitis
  • Check serum lipase periodically in order to detect pancreatitis
  • Total gastrectomy
  • Avoid pregnancy or impregnating women

Dose reduction has been recommended in people with liver problems which involves recommendation of lower starting dose and monitoring of any hepatic function abnormalities.[10]

Hepatitis B virus reactivation may also occur.[11]

Interactions

Nilotinib has been reported as a substrate for OATP1B1 and OATP1B3. Interaction of nilotinib with OATP1B1 and OATP1B3 may alter its hepatic disposition and can lead to transporter mediated drug-drug interactions.[10] Nilotinib is an inhibitor of OATP-1B1 transporter but not for OATP-1B3.[12]

It is a substrate for CYP3A4 and hence grapefruit juice and other CYP3A4 inhibitors[13] will increase its action and inducers like St. John's wort[14] will decrease it. Patients report that pomegranates and starfruit may also interfere.

Food should not be eaten two hours before or one hour afterwards because it unpredictably increases its bioavailability, approximately doubling it.

Pharmacology

 
Crystal structure of Abl kinase domain (blue) in complex with nilotinib (red)

Nilotinib inhibits the kinases BCR-ABL,[15] KIT, LCK, EPHA3, EPHA8, DDR1, DDR2, PDGFRB, MAPK11 and ZAK.[16]

Structurally related to imatinib,[17] It is 10–30 fold more potent than imatinib in inhibiting Bcr-Abl tyrosine kinase activity and proliferation of Bcr-Abl expressing cells.[17][18][19][20]

History

See also: Discovery and development of Bcr-Abl tyrosine kinase inhibitors

Nilotinib was developed by Novartis.[3] It was developed based on the structure of the Abl-imatinib complex to address imatinib intolerance and resistance.[21][18][19]

It was approved for medical use by the FDA in October 2007,[5] EMA in September 2009,[22] MHRA in November 2007,[23] and TGA in January 2008.[9]

Research

Parkinson's disease

There is weak evidence that nilotinib may be beneficial with Parkinson's disease (PD), with a small clinical trial suggesting it might halt progression and improve symptoms.[24] However, there were significant side effects including infection, liver function tests abnormalities, hallucinations and heart attack, and the benefit in PD disappeared at follow up after drug discontinuation, raising question as to whether it was truly a disease modifying therapy. Nilotinib is currently undergoing phase II studies for treatment of Parkinson's.[25] Scientists and medical professionals have advised caution with over-optimistic interpretation of its effects in Parkinson's due to the significant media hype surrounding the small and early clinical trial.[26][27] Dystonia and cognitive impairment have also been reported as side effects.[28]

Other

Novartis announced on April 11, 2011, that it was discontinuing a phase III trial of nilotinib as the first-line treatment of gastrointestinal stromal tumor (GIST) based on the recommendation of an independent data monitoring committee. Interim results showed Tasigna is unlikely to demonstrate superiority compared to Novartis's Gleevec (imatinib)*, the current standard of care in this setting.[29]

Low dose nilotinib is also being investigated for use in Alzheimer's disease, as well as for ALS, dementia and Huntington's disease.[30]

References

  1. ^ a b c d e f g h "Tasigna (nilotinib) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 25 January 2014.
  2. ^ a b "Nilotinib". National Cancer Institute. 1 February 2008. Retrieved 14 November 2019.
  3. ^ a b c d e f g h "Nilotinib Monograph for Professionals". Drugs.com. Retrieved 14 November 2019.
  4. ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  5. ^ a b "Complete Nilotinib information from Drugs.com". Drugs.com. Retrieved 25 January 2014.
  6. ^ Donatelli, Christopher; Chongnarungsin, Daych; Ashton, Rendell (2014). "Acute respiratory failure from nilotinib-associated diffuse alveolar hemorrhage". Leukemia & Lymphoma. 55 (10): 1–6. doi:10.3109/10428194.2014.887714. PMID 24467220. S2CID 43118790.
  7. ^ "FDA Approves Tasigna for Treatment of Philadelphia Chromosome Positive Chronic Myeloid Leukemia". U.S. Food and Drug Administration. 2007-10-30. Retrieved 2009-08-04.
  8. ^ "Prescribing information for Tasigna (nilotinib) Capsules" (PDF). NDA 022068. U.S. FDA. 2007-10-29. Retrieved 2009-08-04.
  9. ^ a b "TASIGNA® nilotinib" (PDF). TGA eBusiness Services. 21 October 2013. Retrieved 25 January 2014.
  10. ^ a b Khurana V, Minocha M, Pal D, Mitra AK (March 2014). "Role of OATP-1B1 and/or OATP-1B3 in hepatic disposition of tyrosine kinase inhibitors". Drug Metabol Drug Interact. 29 (3): 179–90. doi:10.1515/dmdi-2013-0062. PMC 4407685. PMID 24643910.
  11. ^ British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 960. ISBN 9780857113382.
  12. ^ Khurana V, Minocha M, Pal D, Mitra AK (May 2014). "Inhibition of OATP-1B1 and OATP-1B3 by tyrosine kinase inhibitors". Drug Metabol Drug Interact. 29 (4): 249–59. doi:10.1515/dmdi-2014-0014. PMC 4407688. PMID 24807167.
  13. ^ Bailey, David G; Malcolm, J; Arnold, O; David Spence, J (1998-08-01). "Grapefruit juice–drug interactions". British Journal of Clinical Pharmacology. 46 (2): 101–110. doi:10.1046/j.1365-2125.1998.00764.x. ISSN 0306-5251. PMC 1873672. PMID 9723817.
  14. ^ Komoroski, Bernard J.; Zhang, Shimin; Cai, Hongbo; Hutzler, J. Matthew; Frye, Reginald; Tracy, Timothy S.; Strom, Stephen C.; Lehmann, Thomas; Ang, Catharina Y. W. (2004-05-01). "Induction and inhibition of cytochromes P450 by the St. John's wort constituent hyperforin in human hepatocyte cultures". Drug Metabolism and Disposition. 32 (5): 512–518. doi:10.1124/dmd.32.5.512. ISSN 0090-9556. PMID 15100173.
  15. ^ Weisberg E, Manley P, Mestan J, Cowan-Jacob S, Ray A, Griffin JD (June 2006). "AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL". Br. J. Cancer. 94 (12): 1765–9. doi:10.1038/sj.bjc.6603170. PMC 2361347. PMID 16721371.
  16. ^ Manley, PW; Drueckes, P; Fendrich, G; Furet, P; Liebetanz, J; Martiny-Baron, G; Mestan, J; Trappe, J; et al. (2010). "Extended kinase profile and properties of the protein kinase inhibitor nilotinib". Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics. 1804 (3): 445–53. doi:10.1016/j.bbapap.2009.11.008. PMID 19922818.
  17. ^ a b Manley, P.; Cowan-Jacob, S.; Mestan, J. (2005). "Advances in the structural biology, design and clinical development of Bcr-Abl kinase inhibitors for the treatment of chronic myeloid leukaemia". Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics. 1754 (1–2): 3–13. doi:10.1016/j.bbapap.2005.07.040. PMID 16172030.
  18. ^ a b Jabbour, E.; Cortes, J.; Kantarjian, H. (2009). "Nilotinib for the treatment of chronic myeloid leukemia: An evidence-based review". Core Evidence. 4: 207–213. doi:10.2147/CE.S6003. PMC 2899790. PMID 20694077.
  19. ^ a b Olivieri, A.; Manzione, L. (2007). "Dasatinib: a new step in molecular target therapy". Annals of Oncology. 18 Suppl 6: vi42–vi46. doi:10.1093/annonc/mdm223. PMID 17591830.
  20. ^ Breccia, M.; Alimena, G. (2010). "Nilotinib: a second-generation tyrosine kinase inhibitor for chronic myeloid leukemia". Leukemia Research. 34 (2): 129–134. doi:10.1016/j.leukres.2009.08.031. PMID 19783301.
  21. ^ Manley, P.; Stiefl, N.; Cowan-Jacob, S.; Kaufman, S.; Mestan, J.; Wartmann, M.; Wiesmann, M.; Woodman, R.; Gallagher, N. (2010). "Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib". Bioorganic & Medicinal Chemistry. 18 (19): 6977–6986. doi:10.1016/j.bmc.2010.08.026. PMID 20817538.
  22. ^ "Tasigna : EPAR - Product Information" (PDF). European Medicines Agency. Novartis Europharm Ltd. 18 October 2013. Retrieved 25 January 2014.
  23. ^ "Tasigna 150mg Hard Capsules - Summary of Product Characteristics (SPC)". electronic Medicines Compendium. Novartis Pharmaceuticals UK Ltd. 9 September 2013. Retrieved 25 January 2014.
  24. ^ Pagan, F.; Hebron, M.; Valadez, E. H.; Torres-Yaghi, Y.; Huang, X.; Mills, R. R.; Wilmarth, B. M.; Howard, H.; Dunn, C.; Carlson, A.; Lawler, A.; Rogers, S. L.; Falconer, R. A.; Ahn, J.; Li, Z.; Moussa, C. (2016). "Nilotinib Effects in Parkinson's disease and Dementia with Lewy bodies". Journal of Parkinson's Disease. 6 (3): 503–17. doi:10.3233/JPD-160867. PMC 5008228. PMID 27434297.
  25. ^ Dash, Deepa (2019). "Anticancer Drugs for Parkinson's Disease: Is It a Ray of Hope or Only Hype?". Annals of Indian Academy of Neurology. 22 (1): 13–16. doi:10.4103/aian.AIAN_177_18. PMC 6327695. PMID 30692753.
  26. ^ Robledo, I.; Jankovic, J. (2017). "Media hype: Patient and scientific perspectives on misleading medical news". Movement Disorders. 32 (9): 1319–1323. doi:10.1002/mds.26993. PMID 28370445. S2CID 30022509.
  27. ^ Wyse, R. K.; Brundin, P.; Sherer, T. B. (2016). "Nilotinib - Differentiating the Hope from the Hype". Journal of Parkinson's Disease. 6 (3): 519–22. doi:10.3233/JPD-160904. PMC 5044778. PMID 27434298.
  28. ^ Dash, D; Goyal, V (2019). "Anticancer Drugs for Parkinson's Disease: Is It a Ray of Hope or Only Hype?". Annals of Indian Academy of Neurology. 22 (1): 13–16. doi:10.4103/aian.AIAN_177_18. PMC 6327695. PMID 30692753.
  29. ^ . Archived from the original on 2014-02-22. Retrieved 2014-02-18.
  30. ^ "Cancer drug prevents build-up of toxic brain protein". MedicalXpress.com. 10 May 2013. Retrieved 11 April 2017.

External links

  • "Nilotinib". Drug Information Portal. U.S. National Library of Medicine.

February 01, 2023
nilotinib, sold, under, brand, name, tasigna, marketed, worldwide, novartis, medication, used, treat, chronic, myelogenous, leukemia, which, philadelphia, chromosome, used, both, initial, cases, chronic, phase, well, accelerated, chronic, phase, that, responde. Nilotinib sold under the brand name Tasigna marketed worldwide by Novartis is a medication used to treat chronic myelogenous leukemia CML which has the Philadelphia chromosome 2 It may be used both in initial cases of chronic phase CML as well as in accelerated and chronic phase CML that has not responded to imatinib 2 3 It is taken by mouth 3 NilotinibClinical dataTrade namesTasigna othersOther namesAMN107AHFS Drugs comMonographMedlinePlusa608002License dataEU EMA by INN US DailyMed NilotinibPregnancycategoryAU DRoutes ofadministrationBy mouthATC codeL01EA03 WHO Legal statusLegal statusAU S4 Prescription only CA only UK POM Prescription only US only EU Rx onlyPharmacokinetic dataBioavailability30 1 Protein binding98 1 MetabolismLiver mostly CYP3A4 mediated 1 Elimination half life15 17 hours 1 ExcretionFaeces 93 1 IdentifiersIUPAC name 4 methyl N 3 4 methyl 1H imidazol 1 yl 5 trifluoromethyl phenyl 3 4 pyridin 3 ylpyrimidin 2 yl amino benzamideCAS Number641571 10 0 N base PubChem CID644241IUPHAR BPS5697DrugBankDB04868 YChemSpider559260 YUNIIF41401512XKEGGD08953 YChEBICHEBI 52172 YChEMBLChEMBL255863 YPDB ligandNIL PDBe RCSB PDB CompTox Dashboard EPA DTXSID5042663ECHA InfoCard100 166 395Chemical and physical dataFormulaC 28H 22F 3N 7OMolar mass529 527 g mol 13D model JSmol Interactive imageSMILES Cc1ccc cc1Nc2nccc n2 c3cccnc3 C O Nc4cc cc c4 n5cc nc5 C C F F FInChI InChI 1S C28H22F3N7O c1 17 5 6 19 10 25 17 37 27 33 9 7 24 36 27 20 4 3 8 32 14 20 26 39 35 22 11 21 28 29 30 31 12 23 13 22 38 15 18 2 34 16 38 h3 16H 1 2H3 H 35 39 H 33 36 37 YKey HHZIURLSWUIHRB UHFFFAOYSA N Y N Y what is this verify Common side effects may include low platelets low white blood cells anemia rashes vomiting diarrhea and joint pains 3 Other serious side effects may include QT prolongation sudden death pancreatitis and liver problems 3 It is not safe for use during pregnancy 3 Nilotinib is a Bcr Abl tyrosine kinase inhibitor and works by interfering with signalling within the cancer cell 3 Nilotinib was approved for medical use in the United States in 2007 3 It is on the World Health Organization s List of Essential Medicines 4 Contents 1 Medical uses 2 Adverse effects 3 Interactions 4 Pharmacology 5 History 6 Research 6 1 Parkinson s disease 6 2 Other 7 References 8 External linksMedical uses EditNilotinib is used to treat Philadelphia chromosome Ph positive chronic myelogenous leukaemia 1 Adverse effects EditSee also List of adverse effects of nilotinib Nilotinib has a number of adverse effects including headache fatigue gastrointestinal problems such as nausea vomiting diarrhea and constipation muscle and joint pain rash and other skin conditions flu like symptoms and reduced blood cell count Less typical side effects are those of the cardiovascular system such as high blood pressure various types of arrhythmia and prolonged QT interval Nilotinib can also affect the body s electrolyte and glucose balance 5 Though lung related adverse effects are rare when compared with imatinib and dasatinib there is a case report of acute respiratory failure from diffuse alveolar hemorrhage in a people taking nilotinib 6 Nilotinib carries a black box warning in the United States for possible heart complications 7 8 Contraindications include long QT syndrome hypokalaemia hypomagnesaemia pregnancy planned pregnancy lactation and galactose lactose intolerance 1 9 Cautions include 1 Myelosuppression Tumour lysis syndrome Liver impairment History of pancreatitis Check serum lipase periodically in order to detect pancreatitis Total gastrectomy Avoid pregnancy or impregnating women Dose reduction has been recommended in people with liver problems which involves recommendation of lower starting dose and monitoring of any hepatic function abnormalities 10 Hepatitis B virus reactivation may also occur 11 Interactions EditNilotinib has been reported as a substrate for OATP1B1 and OATP1B3 Interaction of nilotinib with OATP1B1 and OATP1B3 may alter its hepatic disposition and can lead to transporter mediated drug drug interactions 10 Nilotinib is an inhibitor of OATP 1B1 transporter but not for OATP 1B3 12 It is a substrate for CYP3A4 and hence grapefruit juice and other CYP3A4 inhibitors 13 will increase its action and inducers like St John s wort 14 will decrease it Patients report that pomegranates and starfruit may also interfere Food should not be eaten two hours before or one hour afterwards because it unpredictably increases its bioavailability approximately doubling it Pharmacology Edit Crystal structure of Abl kinase domain blue in complex with nilotinib red Nilotinib inhibits the kinases BCR ABL 15 KIT LCK EPHA3 EPHA8 DDR1 DDR2 PDGFRB MAPK11 and ZAK 16 Structurally related to imatinib 17 It is 10 30 fold more potent than imatinib in inhibiting Bcr Abl tyrosine kinase activity and proliferation of Bcr Abl expressing cells 17 18 19 20 History EditSee also Discovery and development of Bcr Abl tyrosine kinase inhibitors Nilotinib was developed by Novartis 3 It was developed based on the structure of the Abl imatinib complex to address imatinib intolerance and resistance 21 18 19 It was approved for medical use by the FDA in October 2007 5 EMA in September 2009 22 MHRA in November 2007 23 and TGA in January 2008 9 Research EditParkinson s disease Edit There is weak evidence that nilotinib may be beneficial with Parkinson s disease PD with a small clinical trial suggesting it might halt progression and improve symptoms 24 However there were significant side effects including infection liver function tests abnormalities hallucinations and heart attack and the benefit in PD disappeared at follow up after drug discontinuation raising question as to whether it was truly a disease modifying therapy Nilotinib is currently undergoing phase II studies for treatment of Parkinson s 25 Scientists and medical professionals have advised caution with over optimistic interpretation of its effects in Parkinson s due to the significant media hype surrounding the small and early clinical trial 26 27 Dystonia and cognitive impairment have also been reported as side effects 28 Other Edit Novartis announced on April 11 2011 that it was discontinuing a phase III trial of nilotinib as the first line treatment of gastrointestinal stromal tumor GIST based on the recommendation of an independent data monitoring committee Interim results showed Tasigna is unlikely to demonstrate superiority compared to Novartis s Gleevec imatinib the current standard of care in this setting 29 Low dose nilotinib is also being investigated for use in Alzheimer s disease as well as for ALS dementia and Huntington s disease 30 References Edit a b c d e f g h Tasigna nilotinib dosing indications interactions adverse effects and more Medscape Reference WebMD Retrieved 25 January 2014 a b Nilotinib National Cancer Institute 1 February 2008 Retrieved 14 November 2019 a b c d e f g h Nilotinib Monograph for Professionals Drugs com Retrieved 14 November 2019 World Health Organization 2019 World Health Organization model list of essential medicines 21st list 2019 Geneva World Health Organization hdl 10665 325771 WHO MVP EMP IAU 2019 06 License CC BY NC SA 3 0 IGO a b Complete Nilotinib information from Drugs com Drugs com Retrieved 25 January 2014 Donatelli Christopher Chongnarungsin Daych Ashton Rendell 2014 Acute respiratory failure from nilotinib associated diffuse alveolar hemorrhage Leukemia amp Lymphoma 55 10 1 6 doi 10 3109 10428194 2014 887714 PMID 24467220 S2CID 43118790 FDA Approves Tasigna for Treatment of Philadelphia Chromosome Positive Chronic Myeloid Leukemia U S Food and Drug Administration 2007 10 30 Retrieved 2009 08 04 Prescribing information for Tasigna nilotinib Capsules PDF NDA 022068 U S FDA 2007 10 29 Retrieved 2009 08 04 a b TASIGNA nilotinib PDF TGA eBusiness Services 21 October 2013 Retrieved 25 January 2014 a b Khurana V Minocha M Pal D Mitra AK March 2014 Role of OATP 1B1 and or OATP 1B3 in hepatic disposition of tyrosine kinase inhibitors Drug Metabol Drug Interact 29 3 179 90 doi 10 1515 dmdi 2013 0062 PMC 4407685 PMID 24643910 British national formulary BNF 76 76 ed Pharmaceutical Press 2018 p 960 ISBN 9780857113382 Khurana V Minocha M Pal D Mitra AK May 2014 Inhibition of OATP 1B1 and OATP 1B3 by tyrosine kinase inhibitors Drug Metabol Drug Interact 29 4 249 59 doi 10 1515 dmdi 2014 0014 PMC 4407688 PMID 24807167 Bailey David G Malcolm J Arnold O David Spence J 1998 08 01 Grapefruit juice drug interactions British Journal of Clinical Pharmacology 46 2 101 110 doi 10 1046 j 1365 2125 1998 00764 x ISSN 0306 5251 PMC 1873672 PMID 9723817 Komoroski Bernard J Zhang Shimin Cai Hongbo Hutzler J Matthew Frye Reginald Tracy Timothy S Strom Stephen C Lehmann Thomas Ang Catharina Y W 2004 05 01 Induction and inhibition of cytochromes P450 by the St John s wort constituent hyperforin in human hepatocyte cultures Drug Metabolism and Disposition 32 5 512 518 doi 10 1124 dmd 32 5 512 ISSN 0090 9556 PMID 15100173 Weisberg E Manley P Mestan J Cowan Jacob S Ray A Griffin JD June 2006 AMN107 nilotinib a novel and selective inhibitor of BCR ABL Br J Cancer 94 12 1765 9 doi 10 1038 sj bjc 6603170 PMC 2361347 PMID 16721371 Manley PW Drueckes P Fendrich G Furet P Liebetanz J Martiny Baron G Mestan J Trappe J et al 2010 Extended kinase profile and properties of the protein kinase inhibitor nilotinib Biochimica et Biophysica Acta BBA Proteins and Proteomics 1804 3 445 53 doi 10 1016 j bbapap 2009 11 008 PMID 19922818 a b Manley P Cowan Jacob S Mestan J 2005 Advances in the structural biology design and clinical development of Bcr Abl kinase inhibitors for the treatment of chronic myeloid leukaemia Biochimica et Biophysica Acta BBA Proteins and Proteomics 1754 1 2 3 13 doi 10 1016 j bbapap 2005 07 040 PMID 16172030 a b Jabbour E Cortes J Kantarjian H 2009 Nilotinib for the treatment of chronic myeloid leukemia An evidence based review Core Evidence 4 207 213 doi 10 2147 CE S6003 PMC 2899790 PMID 20694077 a b Olivieri A Manzione L 2007 Dasatinib a new step in molecular target therapy Annals of Oncology 18 Suppl 6 vi42 vi46 doi 10 1093 annonc mdm223 PMID 17591830 Breccia M Alimena G 2010 Nilotinib a second generation tyrosine kinase inhibitor for chronic myeloid leukemia Leukemia Research 34 2 129 134 doi 10 1016 j leukres 2009 08 031 PMID 19783301 Manley P Stiefl N Cowan Jacob S Kaufman S Mestan J Wartmann M Wiesmann M Woodman R Gallagher N 2010 Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib Bioorganic amp Medicinal Chemistry 18 19 6977 6986 doi 10 1016 j bmc 2010 08 026 PMID 20817538 Tasigna EPAR Product Information PDF European Medicines Agency Novartis Europharm Ltd 18 October 2013 Retrieved 25 January 2014 Tasigna 150mg Hard Capsules Summary of Product Characteristics SPC electronic Medicines Compendium Novartis Pharmaceuticals UK Ltd 9 September 2013 Retrieved 25 January 2014 Pagan F Hebron M Valadez E H Torres Yaghi Y Huang X Mills R R Wilmarth B M Howard H Dunn C Carlson A Lawler A Rogers S L Falconer R A Ahn J Li Z Moussa C 2016 Nilotinib Effects in Parkinson s disease and Dementia with Lewy bodies Journal of Parkinson s Disease 6 3 503 17 doi 10 3233 JPD 160867 PMC 5008228 PMID 27434297 Dash Deepa 2019 Anticancer Drugs for Parkinson s Disease Is It a Ray of Hope or Only Hype Annals of Indian Academy of Neurology 22 1 13 16 doi 10 4103 aian AIAN 177 18 PMC 6327695 PMID 30692753 Robledo I Jankovic J 2017 Media hype Patient and scientific perspectives on misleading medical news Movement Disorders 32 9 1319 1323 doi 10 1002 mds 26993 PMID 28370445 S2CID 30022509 Wyse R K Brundin P Sherer T B 2016 Nilotinib Differentiating the Hope from the Hype Journal of Parkinson s Disease 6 3 519 22 doi 10 3233 JPD 160904 PMC 5044778 PMID 27434298 Dash D Goyal V 2019 Anticancer Drugs for Parkinson s Disease Is It a Ray of Hope or Only Hype Annals of Indian Academy of Neurology 22 1 13 16 doi 10 4103 aian AIAN 177 18 PMC 6327695 PMID 30692753 Global Novartis News Archive Archived from the original on 2014 02 22 Retrieved 2014 02 18 Cancer drug prevents build up of toxic brain protein MedicalXpress com 10 May 2013 Retrieved 11 April 2017 External links Edit Nilotinib Drug Information Portal U S National Library of Medicine Portal Medicine Retrieved from https en wikipedia org w index php title Nilotinib amp oldid 1136544330, wikipedia, wiki, book, books, library,

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