What does bosutinib/bosutinib treat? What are its indications?

Bosutinib/Bosutinib is a tyrosine kinase inhibitor (TKI) specifically used to treat chronic myeloid leukemia (CML) and is one of five such drugs currently approved. Chronic myeloid leukemia is a malignant tumor caused by abnormal proliferation of myeloid cells in the bone marrow. The emergence of bosutinib provides a new option for the treatment of this disease.

Bosutinib forms a unique targeting combination through dual inhibition ofSrc and ABL kinases, as well as targeting of other related kinases. This mechanism not only enhances its anticancer effect but also explains the unique side effects it exhibits compared with other similar drugs. The drug was approved by the FDA in 2013 and is indicated for patients who have been treated with one or more tyrosine kinase inhibitors but still require further treatment, especially those who have an inadequate response to or are intolerant to traditional first-line drugs such as imatinib, nilotinib and dasatinib.

Although bosutinib failed to meet its primary endpoint in the initial clinical trial, preventing it from being licensed as a first-line treatment, the subsequent BFORE study showed good results in patients with chronic phase CML. The positive results of this study provide hope for the expansion of bosutinib's indications and indicate that more patients may benefit from this treatment option in the future.

In terms of side effects, bosutinib has a unique side effect profile with minimal cardiovascular and thromboembolic events and minimal long-term safety concerns, with most adverse events occurring in the first few months of treatment. On the other hand, gastrointestinal side effects of bosutinib were very common in early clinical trials evaluating bosutinib. Therefore, when treating with bosutinib, patients need to closely monitor their gastrointestinal reactions and take appropriate countermeasures.

Reference materials:https://pubmed.ncbi.nlm.nih.gov/30069626/