Bosutinib in the treatment of patients with Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia: an overview

Shen, Ann Q.; Wilson, Nicole M.; Gleason, S L; Khoury, H. Jean

doi:10.1177/2040620713510481

Cited by 13 publications

(4 citation statements)

References 8 publications

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“…The most commonly reported adverse reactions of bosutinib include gastrointestinal symptoms (abdominal pain, diarrhea, nausea, and vomiting), thrombocytopenia, anemia, and hepatic failure [ 2 ]. Cutaneous adverse reactions secondary to bosutinib include non-specific manifestations such as edema or rash that occur in approximately 22% of the patients [ 2 , 3 ].…”

Section: Discussionmentioning

confidence: 99%

Bosutinib-Induced Stevens-Johnson Syndrome and Evidence of Tolerance to a Structurally Dissimilar Tyrosine Kinase Inhibitor

Avila-Castano¹,

Morgenstern-Kaplan²,

Carrillo-Martín³

et al. 2022

Cureus

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Bosutinib is a breakpoint cluster region-Abelson gene (BCR-ABL) tyrosine kinase inhibitor (TKI) used for the treatment of chronic myeloid leukemia (CML). Patients on TKIs may develop severe cutaneous adverse reactions (SCARs). A 73-year-old female with CML treated with a second-generation TKI (bosutinib) was evaluated after developing fever and a maculopapular exanthema with skin-peeling affecting her lips, oral mucosa, and genitals 10 days after starting the medication. She required hospitalization, bosutinib discontinuation, and management with intravenous corticosteroids and antibiotics. Patch testing was contraindicated due to the severity of the reaction. The patient was subsequently challenged with first-generation TKI along with careful observation without any adverse reactions. She has not reported any adverse reactions while on therapy in the last two years. In patients who have suffered from SCARs, the suspected triggers must be avoided in all instances. In some cases, the underlying condition limits the use of alternative agents, but low-concentration patch testing may help guide alternative therapies within the same medication group. There appears to be a low cross-reactivity among generational TKIs, and our patient benefited from treatment with a structurally dissimilar alternative TKI for her CML.

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Section: Discussionmentioning

confidence: 99%

Bosutinib-Induced Stevens-Johnson Syndrome and Evidence of Tolerance to a Structurally Dissimilar Tyrosine Kinase Inhibitor

Avila-Castano¹,

Morgenstern-Kaplan²,

Carrillo-Martín³

et al. 2022

Cureus

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“…The major circulating metabolites identified in plasma were oxydechlorinated (M2) bosutinib (19% of parent exposure) and N -desmethylated (M5) bosutinib (25% of parent exposure), with bosutinib N -oxide (M6) a minor circulating metabolite. All the metabolites were inactive [ 20 ].…”

Section: Pharmacokinetic Datamentioning

confidence: 99%

Bosutinib for Chronic Myeloid Leukemia

Breccia

Binotto

2015

Rare Cancers Ther

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In recent years the availability of several tyrosine kinase inhibitors (TKI) in the therapeutic armamentarium for chronic myeloid leukemia has dramatically changed the objectives and expectations of healthcare providers and patients. For many, but not all, patients the forerunner of TKI, imatinib, is still an excellent treatment option. Unfortunately, nearly 30–40% of imatinib-treated patients discontinue therapy in the long-term, because of failure and/or intolerance. Second-generation tyrosine kinase inhibitors are more potent drugs which are suitable for treatment of approximately 50% of patents for whom imatinib is unsuitable, and with high success and rapid responses. Bosutinib, an orally bioavailable Src/Abl tyrosine kinase inhibitor, has proved to be effective in vitro against resistant chronic myeloid leukemia cells that do not harbor the T315I or V299L ABL kinase domain mutations. During clinical development the manageable safety profile of bosutinib have become evident for both simple and more advanced treatment. In this review we summarize preclinical and clinical data for bosutinib and discuss its ideal field of action in comparison with other TKI.

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“…In the second-line studies, grade 3 or 4 thrombocytopenia, neutropenia, and anemia occurred in 25%, 19%, and 8% of patients, respectively. The majority of these patients could be managed with dose reductions or dose interruptions 10,46. In the BELA trial, grade 3 or 4 thrombocytopenia, neutropenia, and anemia occurred in 14%, 6%, and 11% of bosutinib-treated patients, respectively 45.…”

Section: Long-term Efficacy Side Effects Safety and Tolerability Omentioning

confidence: 99%

“…The majority of these patients could be managed with dose reductions or dose interruptions. 10 , 46 In the BELA trial, grade 3 or 4 thrombocytopenia, neutropenia, and anemia occurred in 14%, 6%, and 11% of bosutinib-treated patients, respectively. 45 Again, because of the lack of c-kit inhibition by bosutinib, one would expect lower rates of myelosuppression with bosutinib when compared with other second-generation TKIs.…”

Section: Long-term Efficacy Side Effects Safety and Tolerability Omentioning

confidence: 99%

Clinical advances in the management of chronic myelogenous leukemia: focus on bosutinib and patient considerations

Sweet¹,

Pinilla‐Ibarz²,

Zhang³

2014

PPA

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The treatment for chronic myeloid leukemia has changed significantly over the past 15 years, and as of now, there are five BCR-ABL1 (breakpoint cluster region-Abelson murine leukemia viral oncogene homolog 1) tyrosine kinase inhibitors that have gained approval for treatment of this disease. All five are very effective drugs, and the decision surrounding which to use in specific patients is based on numerous factors. Bosutinib is one of the newer tyrosine kinase inhibitors to gain approval, and has been studied in the first-line setting as well as after failure of other tyrosine kinase inhibitors. It is an SRC-ABL1 (steroid receptor co-activator-ABL1) inhibitor that works in the presence of most kinase domain mutations. The primary side effects of bosutinib are gastrointestinal upsets. In the appropriate clinical setting, bosutinib can be considered a valuable addition to the armamentarium of treatments available for chronic myeloid leukemia.

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Bosutinib in the treatment of patients with Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia: an overview

Cited by 13 publications

References 8 publications

Bosutinib-Induced Stevens-Johnson Syndrome and Evidence of Tolerance to a Structurally Dissimilar Tyrosine Kinase Inhibitor

Bosutinib-Induced Stevens-Johnson Syndrome and Evidence of Tolerance to a Structurally Dissimilar Tyrosine Kinase Inhibitor

Bosutinib for Chronic Myeloid Leukemia

Clinical advances in the management of chronic myelogenous leukemia: focus on bosutinib and patient considerations

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