Abstract
With the exception of organ transplant immunosuppression, the treatment of various IMPDH-dependent hyperproliferative diseases by MPA has failed due to the drugs EHC-induced GIT adverse effects. To influence its therapeutic index, novel formulations such as gastro-resistant MPA-Na (ERL080) or MPA cholestyramine combinations have been developed. Structurally novel IMPDH inhibitors have been discovered based on high throughput screening (pyridazoles) and rational design (methoxyphenyloxazoles). The clinical data on methoxyphenyloxazole derivatives such as VX-497 that is not expected to undergo EHC, will bring improved understanding of the relationship between IMPDH blockade and GIT toxicity.
Keywords: Enterohepatic Recirculation, Inosine Monophosphate Dehydrogenase, non-nucleoside agent, immunosuppressant, immunological disorders, glucuronyltransferases, phenyloxazole moiety, methoxyphenyloxazole derivative
Mini-Reviews in Medicinal Chemistry
Title: Enterohepatic Recirculation A Powerful Incentive for Drug Discovery in the Inosine Monophosphate Dehydrogenase Field
Volume: 1 Issue: 1
Author(s): Christos Papageorgiou
Affiliation:
Keywords: Enterohepatic Recirculation, Inosine Monophosphate Dehydrogenase, non-nucleoside agent, immunosuppressant, immunological disorders, glucuronyltransferases, phenyloxazole moiety, methoxyphenyloxazole derivative
Abstract: With the exception of organ transplant immunosuppression, the treatment of various IMPDH-dependent hyperproliferative diseases by MPA has failed due to the drugs EHC-induced GIT adverse effects. To influence its therapeutic index, novel formulations such as gastro-resistant MPA-Na (ERL080) or MPA cholestyramine combinations have been developed. Structurally novel IMPDH inhibitors have been discovered based on high throughput screening (pyridazoles) and rational design (methoxyphenyloxazoles). The clinical data on methoxyphenyloxazole derivatives such as VX-497 that is not expected to undergo EHC, will bring improved understanding of the relationship between IMPDH blockade and GIT toxicity.
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Papageorgiou Christos, Enterohepatic Recirculation A Powerful Incentive for Drug Discovery in the Inosine Monophosphate Dehydrogenase Field, Mini-Reviews in Medicinal Chemistry 2001; 1 (1) . https://dx.doi.org/10.2174/1389557013407269
DOI https://dx.doi.org/10.2174/1389557013407269 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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