Yen-Fang Wen
Industrial Technology Research Institute
Taiwan
Title: Prodrug Design and Synthesis of Oxyresveratrol to Improve Bioavailability
Biography
Biography: Yen-Fang Wen
Abstract
ITRI pharmaceutical optimization technology division found a uricosuric nature compound, oxyresveratrol, as a potential gout treatment agent. The pharmacological effect of oxyresveratrol is limited by low exposure of the compound associated with rapid metabolic modification and excretion. A possible approach to overcome the hurdle is to develop oxyresveratrol pro drugs. In order to overcome the PK weakness of oxyresveratrol, some functional groups have been decorated onto the metabolic weak point of the molecule, aimed to generate a fit for purpose prodrug molecule. Twenty-nine oxyreveratrol prodrugs have been synthesized by two different synthetic pathway. The Cmax and AUC of the ether linkage oxyresveratrol prodrug OP-0108were two-fold more than that of oxyresveratrol compared with equal molar dose strength.