Bosutinib

(Bosulif®)

Bosulif®

Drug updated on 12/11/2024

Dosage FormTablet (oral; 100 mg, 400 mg, 500 mg); Capsule (oral; 50 mg, 100 mg)
Drug ClassKinase inhibitors
Ongoing and
Completed Studies
ClinicalTrials.gov

Indication

  • Indicated for the treatment of adult and pediatric patients 1 year of age and older with chronic phase Ph+ chronic myelogenous leukemia (CML), newly-diagnosed or resistant or intolerant to prior therapy
  • Indicated for the treatment of adult patients with accelerated, or blast phase Ph+ chronic myelogenous leukemia (CML) with resistance or intolerance to prior therapy.

Latest News

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Summary
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  • This summary is based on the review of 10 systematic review(s)/meta-analysis(es). [1-10]
  • Second-generation tyrosine kinase inhibitors (TKIs) (dasatinib, nilotinib, radotinib) improve major molecular response (MMR) and complete cytogenetic response (CCyR) rates compared to imatinib, with imatinib 800 mg outperforming imatinib 400 mg in these measures; for third-line treatments, ponatinib achieves the highest MMR (19.0-66.7%) and CCyR (21.4-64.8%) rates, followed by asciminib, omacetaxine, and bosutinib.
  • No significant differences were observed in 5-year overall survival (OS) or progression-free survival (PFS) between imatinib and second-generation TKIs (nilotinib, dasatinib); however, second-generation TKIs improved OS at 12 months relative to imatinib.
  • New-generation tyrosine kinase inhibitors (NG-TKIs) enhance early molecular response at 3 months and reduce the rate of accelerated or blastic-phase transformations compared to imatinib.
  • No significant difference was observed in the incidence of all-grade adverse events among various TKIs; however, all TKIs were associated with serious grade 3-4 hematologic adverse events, including anemia, thrombocytopenia, and neutropenia.
  • Dasatinib showed a higher likelihood of causing anemia (54.5%), bosutinib had an increased risk of thrombocytopenia (35.3%), and imatinib was more associated with neutropenia (29.8%), while nilotinib presented lower severe hematologic adverse events.
  • Second-generation TKIs (excluding dasatinib) were linked to a higher incidence of cutaneous adverse events, such as rash, pruritus, and alopecia, compared to imatinib, with an elevated risk of hepatotoxicity, notably with radotinib (400 mg) and imatinib (800 mg).
  • There is no population type or subgroup information available in the reviewed studies.

Product Monograph / Prescribing Information

Document TitleYearSource
Bosulif (bosutinib) Prescribing Information.2023Pfizer Inc., New York, NY

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
Therapy for patients with chronic phase-chronic myeloid leukemia previously treated with ⩾2 tyrosine kinase inhibitors: a systematic literature review2023Therapeutic Advances in Hematology
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
Safety profile of bosutinib in Japanese versus non-Japanese patients with chronic myeloid leukemia: a pooled analysis2022International Journal of Hematology
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
Systematic Review and Meta-Analysis of -New-Generation Tyrosine Kinase Inhibitors versus Imatinib for Newly Diagnosed Chronic Myeloid Leukemia2020Acta Haematologica

Clinical Practice Guidelines