Analogs, formulations and derivatives of imatinib: A patent review

The Bcr-Abl inhibitor imatinib was approved in 2001 for chronic myeloid leukemia therapy, and dramatically changed the lives of patients affected by this disease. Since it also inhibits platelet derived growth factor receptor (PDGFR) and c-Kit, imatinib is used for various other tumors caused by abnormalities of one or both these two enzymes. This review presents an overview on imatinib formulations and derivs., synthetic methodologies and therapeutic uses that have appeared in the patent literature since 2008. Innovative imatinib formulations, such as nanoparticles contg. the drug, will improve its bioavailability. Moreover, oral solns. or high imatinib content tablets or capsules will improve patient compliance. Some solid formulations and innovative syntheses that have appeared in the last few years will reduce the cost of the drug, offering big advantages for poor countries. Some recently patented efficacious imatinib derivs. are in preclin. studies and could enter clin. trials in the next few years. Overall, Bcr-Abl inhibitors constitute a very appealing research field that can be expected to expand further.