Bosutinib is a second-generation tyrosine kinase inhibitor (TKI) approved for use in patients with newly diagnosed Philadelphia chromosome (Ph)-positive chronic phase (CP) chronic myeloid leukemia (CML), as well as Ph-positive CP, accelerated phase, or blast phase (with chemotherapy) CML resistant or intolerant to prior therapy. Clinical trials have shown bosutinib is effective as first-line therapy for patients with CML as well as in later lines of therapy after prior TKI failure. Bosutinib has an established safety profile; however, as with all TKIs approved for the treatment of CML, there are adverse events (AEs) that require management. The safety profile of bosutinib is characterized by gastrointestinal, hematological, hepatic, and skin toxicities. Many of these AEs can be managed with dose adjustment strategies. In this podcast, the authors summarize data from some recent bosutinib publications and discuss implications for optimizing bosutinib treatment of patients with CML. Podcast Video (MP4 210846 KB).
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1007/s11523-024-01123-3 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Bosutinib for the Treatment of CML-Using it Safely: a Podcast.
Target Oncol
January 2025
Division of Hematology and SCT, Georgia Cancer Centre, Augusta, GA, USA.
Bosutinib is a second-generation tyrosine kinase inhibitor (TKI) approved for use in patients with newly diagnosed Philadelphia chromosome (Ph)-positive chronic phase (CP) chronic myeloid leukemia (CML), as well as Ph-positive CP, accelerated phase, or blast phase (with chemotherapy) CML resistant or intolerant to prior therapy. Clinical trials have shown bosutinib is effective as first-line therapy for patients with CML as well as in later lines of therapy after prior TKI failure. Bosutinib has an established safety profile; however, as with all TKIs approved for the treatment of CML, there are adverse events (AEs) that require management.
View Article and Find Full Text PDFDisrupted target binding with acryloyl group as potential Bcr-Abl/C-Src dual kinase inhibitor optimization strategies with maintained antitumor activity.
Bioorg Med Chem Lett
January 2025
National Taiwan University, School of Pharmacy, College of Medicine, Taipei 100 Taiwan. Electronic address:
Current CML treatments often suffer from undesired side effects. Herein we report the computation-assisted optimization of Bcr-Abl/C-Src dual kinase inhibitor. We surmised the improved toxicity profile was achieved via disrupted ligand-target binding.
View Article and Find Full Text PDFIntegrating machine learning and structure-based approaches for repurposing potent tyrosine protein kinase Src inhibitors to treat inflammatory disorders.
Sci Rep
January 2025
State Key Laboratory of Chemical Resources Engineering, Beijing University of Chemical Technology, Beijing, 100029, People's Republic of China.
Tyrosine-protein kinase Src plays a key role in cell proliferation and growth under favorable conditions, but its overexpression and genetic mutations can lead to the progression of various inflammatory diseases. Due to the specificity and selectivity problems of previously discovered inhibitors like dasatinib and bosutinib, we employed an integrated machine learning and structure-based drug repurposing strategy to find novel, targeted, and non-toxic Src kinase inhibitors. Different machine learning models including random forest (RF), k-nearest neighbors (K-NN), decision tree, and support vector machine (SVM), were trained using already available bioactivity data of Src kinase targeting compounds.
View Article and Find Full Text PDFCaught in the Crossfire: Unmasking the Silent Renal Threats of Tyrosine Kinase Inhibitors in Chronic Myeloid Leukemia.
Cancers (Basel)
December 2024
Department of Hematology and Bone Marrow Transplant, National Center for Cancer Care and Research, Doha P.O. Box 3050, Qatar.
Background: Renal adverse drug reactions (ADRs) associated with tyrosine kinase inhibitors (TKIs) in the treatment of chronic myeloid leukemia (CML) are relatively rare, and there is currently no standardized protocol for their management. Therefore, this study aimed to summarize renal ADRs related to TKIs use in CML and propose an evidence-based approach to monitor and manage these ADRs.
Methods: A systematic literature review was performed to identify renal ADRs associated with TKIs in CML.
Asciminib versus bosutinib following 2 or more prior therapies in chronic myeloid leukemia: a plain language summary of the ASCEMBL study.
Future Oncol
January 2025
dPrincess Margaret Cancer Centre, University Health Network, University of Toronto, Toronto, Canada.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!