Drug updated on 11/1/2024
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 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 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 |