Drug updated on 4/15/2024
| Dosage Form | Tablet (oral; 100 mg, 400 mg, 500 mg); Capsule (oral; 50 mg, 100 mg) |
| Drug Class | Kinase 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.
Summary
- Bosutinib (Bosulif) is indicated for the treatment of adult patients with chronic, accelerated, or blast phase Ph+ chronic myelogenous leukemia (CML), particularly those resistant or intolerant to previous therapy. It also serves as a treatment option for newly-diagnosed chronic phase Ph+ CML.
- The information was derived from 10 studies focusing on the safety and efficacy of bosutinib compared to other tyrosine kinase inhibitors in treating different phases of CML.
- In terms of effectiveness post-2nd line therapy setting, bosutinib showed lower major molecular response and complete cytogenetic response rates at 6 months compared to ponatinib and asciminib. This suggests that these drugs might offer better efficacy in this patient population.
- Safety profiles varied among TKIs; while patients treated with second-generation TKIs like bosutinib experienced higher incidences of cutaneous adverse events than those receiving imatinib, it had a lower incidence rate for hematological adverse events such as anemia, neutropenia, and thrombocytopenia when compared to dasatinib, but higher than imatinib and nilotinib. However, bosutinib presented with the highest incidence rate for gastrointestinal adverse events, notably diarrhea, indicating a significant burden relative to other TKIs.
- There's an increased risk associated with hypertension among patients treated with second and third-generation TKIs, including Bosulif, which is even more pronounced in the case of Ponatinib. Similarly, there are increased risks related to hepatotoxicity observed amongst new generation TKIs, including Bosulif, when compared against Imatinib.
- Economic evaluations suggested that newer tyrosine kinase inhibitors were mostly cost-effective only as second-line agents, due largely because generics were available primarily for the imatinib regimen.
Product Monograph / Prescribing Information
| Document Title | Year | Source |
|---|---|---|
| Bosulif (bosutinib) Prescribing Information. | 2023 | Pfizer Inc., New York, NY |
Systematic Reviews / Meta-Analyses
Clinical Practice Guidelines
| Document Title | Year | Source |
|---|---|---|
| Practical recommendations for the manipulation of kinase inhibitor formulations to age-appropriate dosage forms. | 2022 | Pharmaceutics |
| Discordance between child‐pugh and National Cancer Institute classifications for hepatic dysfunction: implications on dosing recommendations for oncology compounds. | 2021 | The Journal of Clinical Pharmacology |
| Chronic myeloid leukemia, version 2.2021, NCCN clinical practice guidelines in oncology. | 2020 | Journal of the National Comprehensive Cancer Network |
| A British society for haematology guideline on the diagnosis and management of chronic myeloid leukaemia. | 2020 | British Journal of Haematology |