Z-338 - Cerep

More documents

Recommendations

Info

Introduction Z-338 is a novel gastroprokinetic agent, which is synthesized by Zeria Pharmaceutical Co., Ltd (Fig. 1). Z-338 is under development for the treatment of functional dyspepsia, and is now in clinical trials. The purpose of the study was to evaluate possible involvement of cytochrome P450 (CYP) enzyme(s) and UDP-glucuronosyltransferase (UGT) enzyme(s) responsible for metabolizing Z-338. Potential interactions of Z-338 with CYP enzymes were also investigated, and we compared its inhibitory potentials with cisapride and Z-338 analog, ID951551.
CYP2C8 (>>CYP3A4 or 1A1) MeO O N H S N O N H N H MeO O N H S N O N H N MeO OH Z-338 deisopropyl metabolite MeO MeO MeO O OMe OH N H Z-338 S N N H ID951551 O N UGT1A9 (>>UGT1A8) MeO MeO CYP2C8 (>CYP3A4 or 1A1) MeO MeO O OGlu N H O OMe S N H N S N O O N H Z-338 glucuronide ID951551 deisopropyl metabolite N H N N H OCH 3 H 3 CO CYP3A4 OCH 3 H 3 CO F O(CH 2 ) 3 N NHCO NH 2 HN NHCO NH 2 Cisapride Cl N-dealkylcisapride Cl Fig.1 Metabolic Scheme of Z-338, ID951551 and Cisapride
Page 1: Involvement of CYP2C8 and UGT1A9 in
Page 5 and 6: Method: In vitro inhibition study T
Page 7 and 8: CYP1A1 CYP1A2 CYP2A6 CYP2B6 CYP2C8
Page 9 and 10: Rate (pmol/min/mg protein) 160 140
Page 11 and 12: Table 3 Inhibition constants (K i v
Page 13: Conclusion Z-338 is predominantly m

Z-338 - Cerep

You also want an ePaper? Increase the reach of your titles

Delete template?

Save as template?