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[摘要]:SNS-032 (formerly BMS-387032) is a small-molecule cyclin-dependent kinase (CDK) inhibitor currently in phase I clinical trials for the treatment of B-cell malignancies and advanced solid tumors. Preclinical studies have shown that SNS-032 is a specific and potent inhibitor of CDK2, 7 and 9 which induces cell cycle arrest and apoptosis in tumor cell lines. It was shown to inhibit in vitro angiogenesis and prostaglandin E-2 (PGE(2)) production, both strongly associated with tumorigenesis. Phase I clinical trials support the safety and tolerability of SNS-032 as evaluated in dose-escalation studies. The compound is currently administered by i.v. infusion but has shown promising potential for oral delivery. |
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