Drug updated on 12/11/2024
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.
Latest News
Summary
- 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 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 |
European LeukemiaNet 2020 recommendations for treating chronic myeloid leukemia | 2020 | Leukemia |
The New ELN Recommendations for Treating CML | 2020 | Journal of Clinical Medicine |