The aim of this study was to identify factors affecting the pharmacokinetics of mycophenolic acid (MPA) and its 7-O-glucuronide (MPAG) in systemic lupus erythematosus (SLE) patients. Thirty-one SLE patients in remission maintenance phase treated with mycophenolate mofetil (median 1500 mg/d) and prednisolone and followed-up for up to 56 months (median 13 months) were enrolled. Creatinine clearan...

Metabolism and sinusoidal/canalicular efflux of mycophenolic acid (MPA) was investigated using sandwich-cultured hepatocytes (SCHs). After applying MPA to SCHs from humans, wild-type rats, and multidrug resistance-associated protein (Mrp) 2-deficient rats, the MPA metabolites 7-O-glucuronide (MPAG) and acyl glucuronide (AcMPAG) were detected in the intracellular compartment of the SCHs. Sinusoi...

Mycophenolic acid (MPA) is an immunosuppressive agent, more and more extensively used in transplantation, rheumatology and nephrology. In this review, we will analyze the molecular mechanisms of its action, including the newest insights, in particular the inhibition of lymphocytes and the induction of tolerogenic dendritic cells (DCs) and its direct effects on non-immune cells (fibroblasts and ...

Mycophenolic acid (MPA) is a potent, selective and uncompetitive inhibitor of the inosine 5’ -monophophate dehydrogenase (IMPDH), which is the rate-limiting enzyme in the de novo synthesis of guanosine nucleotides being required during T and B lymphocyte proliferation. In this study, HPLC method was developed and validated to determine the IMPDH activity in human peripheral blood mononuclear ce...

Mycophenolate mofetil (MMF) is a prodrug immunosuppressant with a high oral bioavailability. Enterohepatic cycling of a glucuronide derivative of MMF contributes substantially to the bioavailability, but is dependent on bacterial deglucuronidation by intestinal flora. This study aims to determine whether an antibiotic regimen with activity against such organisms reduces the bioavailability of M...

BACKGROUND Despite use of a lower mycophenolate dose in Thai kidney transplant patients, acceptable graft and patient outcomes can be achieved. We therefore examined the pharmacokinetics of mycophenolic acid (MPA) by area under the curve (AUC) and investigated genetic contribution in mycophenolate metabolism in this population. METHODS Kidney transplant recipients with stable graft function w...

OBJECTIVES Neutropenia after kidney transplant is an adverse event usually treated with a dosage reduction of mycophenolic acid. We evaluated the efficacy and safety of substituting mycophenolic acid with everolimus in patients with persistent neutropenia after kidney transplant. MATERIALS AND METHODS This study was a retrospective analysis. A total of 17 patients who were initially treated w...

Immunosuppressive treatment is a prerequisite for both organ transplantation and tolerance of the allograft. However, long-term immunosuppression has been associated with a higher incidence of malignancies and infections. Immunosuppressors mainly target circulating immune cells and little is known of their "off-target" effects, such as their impact on endothelial cells (ECs). In chronic antibod...