Bosutinib

(Bosulif®)

Bosulif®

Drug updated on 11/1/2024

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 TKIs (dasatinib, nilotinib, radotinib) improve MMR (major molecular response) and CCyR (complete cytogenetic response) 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 OS or PFS between imatinib and second-generation TKIs (nilotinib, dasatinib); however, second-generation TKIs improved OS at 12 months relative to imatinib.
  • 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