Enterohepatic Recirculation A Powerful Incentive for Drug Discovery in the Inosine Monophosphate Dehydrogenase Field

Author: Papageorgiou C.

Source: Mini Reviews in Medicinal Chemistry, Volume 1, Number 1, May 2001 , pp. 71-77(7)

Publisher: Bentham Science Publishers

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; Enterohepatic recirculation; non-nucleoside agent; immunosuppressant; immunological disorders; glucuronyltransferases; phenyloxazole moiety; methoxyphenyloxazole derivative

Language: English

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1389557013407269

Publication date: 2001-05-01

• The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines.
  
  The scope of Mini-Reviews in Medicinal Chemistry will cover all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies.
  
  Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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