What type of drug is Bosutinib?

Bosutinib is a new oral targeted drug mainly used to treat Philadelphia chromosome-positive chronic myelogenous leukemia (Ph+ CML). Its mechanism of action is similar to that of other TKIs. It blocks abnormal signaling of leukemia cells by inhibiting the activity of BCR-ABL fusion protein kinase, thereby achieving the purpose of inhibiting cell growth and inducing apoptosis. However, the uniqueness of bosutinib is that it not only effectively acts on patients in the chronic phase (CP), but also shows activity in the accelerated phase (AP) and blast phase (BP). For those patients who develop resistance after using imatinib, nilotinib or dasatinib, bosutinib often becomes one of the first-choice drugs for subsequent treatment.

Currently, both the U.S. FDABosutinib and the European EMA have approved bosutinib for adult patients with newly diagnosed Ph+ CML, as well as patients with chronic phase, accelerated phase and blast crisis CML who have developed resistance or intolerance to previous TKI treatment. Its clinical positioning is a "rescue + first-line compatible" targeted drug, which can be used for first-line treatment or as an alternative after other TKIs fail.

The pharmacokinetic characteristics of bosutinib enable it to quickly reach blood drug steady state and maintain inhibitory activity in the body for a long time. Its advantage is also reflected in its high selectivity. Its precise effect on the BCR-ABL kinase target reduces interference with other cell signaling pathways, so the side effects are lighter than earlier drugs. Common reactions such as gastrointestinal discomfort and rash among patients usually appear in the early stages of medication and can be gradually relieved after adjustment or over time. From a pharmacological perspective, bosutinib is regarded as a bridge drug between the "classic TKI era" and the "precision resistance management era". Its research and development has promoted the long-term controllability of chronic myelogenous leukemia.

Reference materials:https://go.drugbank.com/drugs/DB06616