Nilotinib: A review of its use in chronic myelogenous leukemia

Ting wei Lu, Ronan T Swords, Francis J. Giles, Kevin Kelly

Research output: Contribution to journalArticle

Abstract

Chronic myeloid leukemia (CML) is characterized by the reciprocal chromosomal translocation, t(9;22), forming the BCR-ABL oncogene known as the Philadelphia chromosome. The development of imatinib, a small-molecule kinase inhibitor targeted against BCR-ABL, has revolutionized the management of CML and significantly improved the prognosis and outcome and until very recently was the standard of care in patients presenting with newly diagnosed CML. Nilotinib (Tasigna®) is an orally administered kinase inhibitor made by the Novartis Pharmaceuticals Corporation that was rationally designed to bind to the ABL kinase domain of BCR-ABL resulting in enhanced BCR-ABL inhibition. It is well tolerated and has a favourable safety profile. Nilotinib has been shown to be effective in patients who have failed prior therapy with imatinib. Recently a large randomized control trial comparing imatinib and nilotinib has demonstrated that niloitinb is superior to imatinib in the frontline treatment of CML. This review summarizes the preclinical and clinical data supporting the use of nilotinib in the frontline and secondline treatment of CML.

Original languageEnglish
Pages (from-to)841-848
Number of pages8
JournalClinical Medicine Insights: Therapeutics
Volume2
DOIs
StatePublished - Jan 1 2010
Externally publishedYes

Fingerprint

Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Phosphotransferases
Philadelphia Chromosome
Genetic Translocation
Standard of Care
Oncogenes
Therapeutics
4-methyl-N-(3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-((4-pyridin-3-ylpyrimidin-2-yl)amino)benzamide
Safety
Imatinib Mesylate
Pharmaceutical Preparations

Keywords

  • CML
  • Dasatinib
  • Frontline
  • Imatinib
  • Nilotinib

ASJC Scopus subject areas

  • Medicine(all)
  • Pharmaceutical Science
  • Pharmacology

Cite this

Nilotinib : A review of its use in chronic myelogenous leukemia. / Lu, Ting wei; Swords, Ronan T; Giles, Francis J.; Kelly, Kevin.

In: Clinical Medicine Insights: Therapeutics, Vol. 2, 01.01.2010, p. 841-848.

Research output: Contribution to journalArticle

Lu, Ting wei ; Swords, Ronan T ; Giles, Francis J. ; Kelly, Kevin. / Nilotinib : A review of its use in chronic myelogenous leukemia. In: Clinical Medicine Insights: Therapeutics. 2010 ; Vol. 2. pp. 841-848.
@article{df6e24f1e89543b68b3ce8ee041648ba,
title = "Nilotinib: A review of its use in chronic myelogenous leukemia",
abstract = "Chronic myeloid leukemia (CML) is characterized by the reciprocal chromosomal translocation, t(9;22), forming the BCR-ABL oncogene known as the Philadelphia chromosome. The development of imatinib, a small-molecule kinase inhibitor targeted against BCR-ABL, has revolutionized the management of CML and significantly improved the prognosis and outcome and until very recently was the standard of care in patients presenting with newly diagnosed CML. Nilotinib (Tasigna{\circledR}) is an orally administered kinase inhibitor made by the Novartis Pharmaceuticals Corporation that was rationally designed to bind to the ABL kinase domain of BCR-ABL resulting in enhanced BCR-ABL inhibition. It is well tolerated and has a favourable safety profile. Nilotinib has been shown to be effective in patients who have failed prior therapy with imatinib. Recently a large randomized control trial comparing imatinib and nilotinib has demonstrated that niloitinb is superior to imatinib in the frontline treatment of CML. This review summarizes the preclinical and clinical data supporting the use of nilotinib in the frontline and secondline treatment of CML.",
keywords = "CML, Dasatinib, Frontline, Imatinib, Nilotinib",
author = "Lu, {Ting wei} and Swords, {Ronan T} and Giles, {Francis J.} and Kevin Kelly",
year = "2010",
month = "1",
day = "1",
doi = "10.4137/CMT.S24",
language = "English",
volume = "2",
pages = "841--848",
journal = "Clinical Medicine Insights: Therapeutics",
issn = "1179-559X",
publisher = "Libertas Academica Ltd.",

}

TY - JOUR

T1 - Nilotinib

T2 - A review of its use in chronic myelogenous leukemia

AU - Lu, Ting wei

AU - Swords, Ronan T

AU - Giles, Francis J.

AU - Kelly, Kevin

PY - 2010/1/1

Y1 - 2010/1/1

N2 - Chronic myeloid leukemia (CML) is characterized by the reciprocal chromosomal translocation, t(9;22), forming the BCR-ABL oncogene known as the Philadelphia chromosome. The development of imatinib, a small-molecule kinase inhibitor targeted against BCR-ABL, has revolutionized the management of CML and significantly improved the prognosis and outcome and until very recently was the standard of care in patients presenting with newly diagnosed CML. Nilotinib (Tasigna®) is an orally administered kinase inhibitor made by the Novartis Pharmaceuticals Corporation that was rationally designed to bind to the ABL kinase domain of BCR-ABL resulting in enhanced BCR-ABL inhibition. It is well tolerated and has a favourable safety profile. Nilotinib has been shown to be effective in patients who have failed prior therapy with imatinib. Recently a large randomized control trial comparing imatinib and nilotinib has demonstrated that niloitinb is superior to imatinib in the frontline treatment of CML. This review summarizes the preclinical and clinical data supporting the use of nilotinib in the frontline and secondline treatment of CML.

AB - Chronic myeloid leukemia (CML) is characterized by the reciprocal chromosomal translocation, t(9;22), forming the BCR-ABL oncogene known as the Philadelphia chromosome. The development of imatinib, a small-molecule kinase inhibitor targeted against BCR-ABL, has revolutionized the management of CML and significantly improved the prognosis and outcome and until very recently was the standard of care in patients presenting with newly diagnosed CML. Nilotinib (Tasigna®) is an orally administered kinase inhibitor made by the Novartis Pharmaceuticals Corporation that was rationally designed to bind to the ABL kinase domain of BCR-ABL resulting in enhanced BCR-ABL inhibition. It is well tolerated and has a favourable safety profile. Nilotinib has been shown to be effective in patients who have failed prior therapy with imatinib. Recently a large randomized control trial comparing imatinib and nilotinib has demonstrated that niloitinb is superior to imatinib in the frontline treatment of CML. This review summarizes the preclinical and clinical data supporting the use of nilotinib in the frontline and secondline treatment of CML.

KW - CML

KW - Dasatinib

KW - Frontline

KW - Imatinib

KW - Nilotinib

UR - http://www.scopus.com/inward/record.url?scp=78650726490&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=78650726490&partnerID=8YFLogxK

U2 - 10.4137/CMT.S24

DO - 10.4137/CMT.S24

M3 - Article

AN - SCOPUS:78650726490

VL - 2

SP - 841

EP - 848

JO - Clinical Medicine Insights: Therapeutics

JF - Clinical Medicine Insights: Therapeutics

SN - 1179-559X

ER -