Bugatinib (INN, trade name Ambrey) is an ALK tyrosine kinase inhibitor for the treatment of locally advanced or metastatic anaplastic lymphoma kinase (ALK) -positive non-small cell lung cancer (NSCLC).
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Mechanism of action
Bugitinib is a tyrosine kinase inhibitor that inhibits a variety of kinases including ALK, ROS1, insulin-like growth factor-1 receptor (IGF-1R), FLT-3, EGFR deletion and point mutation in vitro at clinically accessible concentrations. In vitro and in vivo, bugitinib inhibited ALK autophosphorylation and ALK-mediated phosphorylation of downstream signaling proteins STAT3, AKT, ERK1/2, and S6. Bugitinib also inhibited the proliferation of EML4-ALK and NPM-ALK fusion protein cell lines in vitro and inhibited the growth of EML4-ALK-positive non-small cell lung cancer xenografts in a dose-dependent manner.
Adverse reactions (side effects)
The most common adverse reactions (incidence > 25%) with bugitinib were diarrhea, nausea, vomiting, rash, cough, dyspnea, hypertension, fatigue, muscle pain, headache.
Interact with each other
The combination of bugitinib with a potent or moderate CYP3A inhibitor increases the plasma concentration of bugitinib and may increase the incidence of adverse effects. Concomitant administration of bugitinib with a potent or moderate CYP3A inducer may reduce the plasma concentration of bugitinib, which May 17/25 reduce the efficacy of bugitinib.
Bugitinib can reduce the concentration of sensitive CYP3A substrate.
