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Sydney 2005: In Vitro Activity of a Novel Small Molecule Cyclin Dependent Kinase inhibitor, CYC202..
By Noopur Raje
04.14.05
Dr. Raje followed presented on the in vitro activity of a novel cyclin-dependent kinase inhibitor, CYC202. Cyclins are overexpressed in all MM cells. A dysregulation of cyclin D1-3 occurs in all MM cells making them susceptible to proliferative stimuli. CYC202 (selicicib or R-Roscovitine) is a purine analog that has shown activity in 19 human cancer cell lines and is currently evaluated in ongoing Phase 1 trials. Within 24 hours, CYC202 induces cytotoxicity in MM cells sensitive or resistant to conventional chemotherapy or steroids. Apoptosis is induced in MM cells in a time-and dose-dependent manner. Treatment of MM cells with combination of bortezomib and doxorubicin resulted in synergism. Dr. Raje concluded that these combinations should be further tested in clinical trials.


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