ICAR Presentation: IND-Directed Development of Dual-Acting Pyrimidinediones IQP-0410 and IQP-0528: Enhancement of Solubility and Metabolic Stability

April 10, 2012

A poster entitled "IND-Directed Development of Dual-Acting Pyrimidinediones IQP-0410 and IQP-0528: Enhancement of Solubility and Metabolic Stability" was presented at the 2012 International Conference for Antiviral Research (ICAR) in Sapporo, Japan. The data presented identified the pyrimidinedione compound IQP-0528 in the cyclopropyl series as the lead product for both HIV therapy and prevention based on high therapeutic index, dual mechanism of antiviral action, and enhanced genetic barrier to resistance compared to IQP-0410. Chemical modification efforts to improve solubility and eliminating the sites of rapid metabolism of IQP-0528 identified the new lead compound JDJ01. The data generated was supported by a NIH Phase II Small Business grant that was won by Dr. Buckheit in 2010.

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