Nilotinib

(Tasigna®)

Nilotinib

Drug updated on 12/11/2024

Dosage FormCapsules (oral; 50 mg, 150 mg, and 200 mg)
Drug ClassKinase inhibitors
Ongoing and
Completed Studies
ClinicalTrials.gov

Indication

  • Indicated for the treatment of adult and pediatric patients greater than or equal to 1 year of age with newly diagnosed Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase
  • Indicated for the treatment of adult patients with chronic phase (CP) and accelerated phase (AP) Ph+ CML resistant to or intolerant to prior therapy that included imatinib
  • Indicated for the treatment of pediatric patients greater than or equal to 1 year of age with Ph+ CML-CP and CML-AP resistant or intolerant to prior tyrosine-kinase inhibitor (TKI) therapy.

Latest News

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Summary
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  • This summary is based on the review of 11 systematic review(s)/meta-analysis(es). [1-11]
  • Second-generation TKIs (dasatinib, nilotinib, radotinib) achieved higher rates of Major Molecular Response (MMR) and Complete Cytogenetic Response (CCyR) compared to imatinib, with imatinib 800 mg performing better than imatinib 400 mg. New-generation TKIs (NG-TKIs) also showed increased early molecular response rates, including at the 3-month mark.
  • Studies comparing second-generation TKIs (dasatinib, nilotinib) to imatinib showed no significant differences in 5-year Overall Survival (OS) or Progression-Free Survival (PFS), though NG-TKIs indicated higher OS at 12 months compared to imatinib.
  • NG-TKIs were associated with lower rates of Chronic Myeloid Leukemia (CML)-related death and progression to the accelerated phase or blast crisis compared to imatinib.
  • Second-generation TKIs consistently outperformed imatinib in achieving MMR and CCyR.
  • All TKIs caused severe hematologic adverse events (AEs), with dasatinib showing a higher likelihood for anemia, bosutinib for thrombocytopenia, imatinib for neutropenia, and nilotinib displaying a relatively better safety profile regarding severe hematologic AEs. The prevalence of hematologic AEs was highest for dasatinib and lowest for nilotinib.
  • Second-generation TKIs had a higher risk of cutaneous AEs (rash and pruritus) and increased hepatotoxicity (alanine transaminase (ALT) and aspartate aminotransferase (AST) levels) compared to imatinib. Nilotinib was associated with a significantly higher risk of cardiovascular events, including coronary artery disease, acute coronary syndrome, cerebrovascular accidents, and peripheral arterial occlusive disease, with a higher incidence of hypertension compared to imatinib.
  • Malformation rates in offspring of fathers who did not discontinue TKI treatment before conception were comparable to the general population, though data on nilotinib were limited.
  • The effectiveness outcomes for Chronic Myeloid Leukemia (CML) patients indicate that second-generation TKIs show favorable rates of MMR and CCyR, while patients in accelerated CML phases experience significantly higher rates of hematologic adverse events, particularly when treated with nilotinib, which also poses increased risks for those with pre-existing cardiovascular conditions.

Product Monograph / Prescribing Information

Document TitleYearSource
Tasigna (nilotinib) Prescribing Information.2024Novartis Pharmaceuticals Corporation, East Hanover, NJ

Systematic Reviews / Meta-Analyses

Document TitleYearSource
Comparative efficacy and safety of first-line tyrosine kinase inhibitors in chronic myeloid leukemia: a systematic review and network meta-analysis2024Translational Cancer Research
Comparison of cutaneous adverse events between second-generation tyrosine kinase inhibitors and imatinib for chronic myeloid leukemia: a systematic review and meta-analysis2023Acta Oncologica
Hematological Adverse Events with Tyrosine Kinase Inhibitors for Chronic Myeloid Leukemia: A Systematic Review with Meta-Analysis2023Cancers
Cardiovascular adverse events in chronic myeloid leukemia patients treated with nilotinib or imatinib: A systematic review, meta-analysis and integrative bioinformatics analysis2022Frontiers in Cardiovascular Medicine
Arterial Hypertension and Tyrosine Kinase Inhibitors in Chronic Myeloid Leukemia: A Systematic Review and Meta-Analysis2021Frontiers in Pharmacology
Comparison of Hepatotoxicity Associated With New BCR-ABL Tyrosine Kinase Inhibitors vs Imatinib Among Patients With Chronic Myeloid Leukemia: A Systematic Review and Meta-analysis2021JAMA Network Open
Pregnancy outcomes of women whom spouse fathered children after tyrosine kinase inhibitor therapy for chronic myeloid leukemia: A systematic review2020PLoS One
First-line imatinib vs second- and third-generation TKIs for chronic-phase CML: a systematic review and meta-analysis2020Blood Advances
Relapse Prevention with Tyrosine Kinase Inhibitors after Allogeneic Transplantation for Philadelphia Chromosome-Positive Acute Lymphoblast Leukemia: A Systematic Review2020Biology of Blood and Marrow Transplantation
Systematic Review and Meta-Analysis of -New-Generation Tyrosine Kinase Inhibitors versus Imatinib for Newly Diagnosed Chronic Myeloid Leukemia2020Acta Haematologica
Utility of Therapeutic Drug Monitoring of Imatinib, Nilotinib, and Dasatinib in Chronic Myeloid Leukemia: A Systematic Review and Meta-analysis2019Clinical Therapeutics

Clinical Practice Guidelines