Open AccessDECREASED PROTEIN BINDING OF MYCOPHENOLIC ACID ASSOCIATED WITH LEUKOPENIA IN A PANCREAS TRANSPLANT RECIPIENT WITH RENAL FAILURE
Author(s) -
Bruce Kaplan,
Scott A. Gruber,
Ratnaji Nallamathou,
Stephen M. Katz,
Les Shaw
Publication year - 1998
Publication title -
transplantation
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.45
H-Index - 204
eISSN - 1534-6080
pISSN - 0041-1337
DOI - 10.1097/00007890-199804270-00019
Subject(s) - mycophenolic acid , free fraction , mycophenolate , imp dehydrogenase , toxicity , medicine , albumin , metabolite , chemistry , pharmacology , transplantation , endocrinology , urology , pharmacokinetics
Mycophenolate mofetil (MMF) is rapidly hydrolyzed to its active metabolite mycophenolic acid (MPA), which is excreted by the kidney after undergoing glucuronidation to MPAG. MPAG has been shown to accumulate in patients with renal failure. MPA is extensively and avidly bound to human serum albumin. In vitro inhibition of the pharmacologic target, inosine monophosphate dehydrogenase, is dependent on free MPA. It has been demonstrated that high MPAG concentrations decrease MPA protein binding in vitro. In addition, the uremic state is associated with altered protein binding of many drugs.