title: Randomized calcineurin inhibitor cross over study to measure the pharmacokinetics of co-administered enteric-coated mycophenolate sodium.
abstract: Enteric-coated mycophenolate sodium (EC-MPS) (myfortic) is an advanced formulation delivering mycophenolic acid (MPA), designed to improve MPA-related upper gastrointestinal adverse events by delaying the release of MPA until the small intestine. A randomized, calcineurin inhibitor crossover, steady-state pharmacokinetic study in stable renal transplant patients receiving EC-MPS demonstrated increased MPA exposure of 19% higher, MPA C(max,ss) 19% lower and MPA C(min,ss) approximately twofold higher with tacrolimus, than cyclosporine microemulsion. No study drug-related adverse events were recorded, but mean blood glucose concentration was higher in patients receiving tacrolimus (p = 0.031). The dose changes in relation to MPA exposure in patients is dependent on the clinical situation and may not always be warranted. These observations should be taken into consideration when switching from one calcineurin inhibitor to another, but the final dosage should be based on both this pharmacokinetic data and the clinical situation.
authors: Division of Nephrology, Department of Medicine, University of Florida College of Medicine, Gainesville, FL 32610-0224, USA. kaplab@medicine.ufl.edu
authors: Bruce
authors: B
authors: Kaplan
authors: Herwig-Ulf
authors: HU
authors: Meier-Kriesche
authors: Paula
authors: P
authors: Minnick
authors: Marie-Claude
authors: MC
authors: Bastien
authors: Romain
authors: R
authors: Sechaud
authors: Ching-Ming
authors: CM
authors: Yeh
authors: Sebastien
authors: S
authors: Balez
authors: Franck
authors: F
authors: Picard
authors: Robert
authors: R
authors: Schmouder
mesh_terms: D000328:Adult; D000368:Aged; D001786:Blood Glucose / Q000032:analysis; D065095:Calcineurin Inhibitors; D018592:Cross-Over Studies; D016572:Cyclosporine / Q000493:pharmacokinetics; D004655:Emulsions; D004791:Enzyme Inhibitors / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D016030:Kidney Transplantation; D008297:Male; D008875:Middle Aged; D009173:Mycophenolic Acid / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D012964:Sodium / Q000008:administration & dosage; D013608:Tablets, Enteric-Coated; D016559:Tacrolimus / Q000493:pharmacokinetics
chemical_list: D001786:Blood Glucose; D065095:Calcineurin Inhibitors; D004655:Emulsions; D004791:Enzyme Inhibitors; D013608:Tablets, Enteric-Coated; D016572:Cyclosporine; D012964:Sodium; D009173:Mycophenolic Acid; D016559:Tacrolimus