Breakpoint cluster region Abelson (Bcr-Abl) tyrosine kinase (TK) is a constitutively activated cytoplasmic TK and is the underlying cause of chronic myeloid leukemia (CML). To date, imatinib represents the frontline treatment for CML therapy. The development of resistance has prompted the search for novel Bcr-Abl inhibitors. Areas covered: This review presents a short overview of drugs already approved for CML therapy and of the compds. that are in clin. trials. The body of the article deals with Bcr-Abl inhibitors patented since 2008, focusing on their chem. features. Expert opinion: The search for Bcr-Abl inhibitors is very active. We believe that a no. of patented compds. could enter clin. trials and some could be approved for CML therapy in the next few years. Overall, Bcr-Abl inhibitors constitute a very appealing research field that can be expected to expand further.
Bcr-Abl tyrosine kinase inhibitors: A patent review
DESOGUS, ANDREA;SCHENONE, SILVIA;BRULLO, CHIARA;MUSUMECI, FRANCESCA
2015-01-01
Abstract
Breakpoint cluster region Abelson (Bcr-Abl) tyrosine kinase (TK) is a constitutively activated cytoplasmic TK and is the underlying cause of chronic myeloid leukemia (CML). To date, imatinib represents the frontline treatment for CML therapy. The development of resistance has prompted the search for novel Bcr-Abl inhibitors. Areas covered: This review presents a short overview of drugs already approved for CML therapy and of the compds. that are in clin. trials. The body of the article deals with Bcr-Abl inhibitors patented since 2008, focusing on their chem. features. Expert opinion: The search for Bcr-Abl inhibitors is very active. We believe that a no. of patented compds. could enter clin. trials and some could be approved for CML therapy in the next few years. Overall, Bcr-Abl inhibitors constitute a very appealing research field that can be expected to expand further.
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