Sodium mycophenolate

Mycophenolate sodium (62 Myfortic ) Mycophenolic acid (61) Fatty acid antibiotic NP Microbial Immuno- suppression Inhibits inosine monophosphate dehydrogenase (IMPDH) activity 215-217, 532-560... 

Mycophenolate sodium (62 Myfortic Norvatis, 2003) is an immunosuppressant drug used to prevent rejection in organ transplantation. It is a selective, noncompetitive, reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), the rate-limiting enzyme in the de novo pathway of guanosine nucleotide synthesis. Thus, mycophenolic acid (61), originally... 

Curran MP, Keating GM. (2005) Mycophenolate sodium delayed release Prevention of renal transplant rejection. Drugs 65 799-805. 

Gabardi S, Tran JL, Clarkson MR. (2003) Enteric-coated mycophenolate sodium. Ann Pharmacother 37 1685-1693. 

Salvador M, Holzer H, de Mattos A, Solhnger H, Ams W, Oppenheimer E, Maca J, Hall M. (2004) Enteric-coated mycophenolate sodium is therapeutically equivalent to mycophenolate mofetil in de novo renal transplant patients. Am J Transplant 4 231-236. 

Perry TW, Trotter IF, Christians U, Bendrick-Peart J. (2006) A single-dose pharmacokinetic study of enteric coated mycophenolate sodium, ec-mps, in liver transplant recipients. Transplantation 82 719-720. 

Budde K, Glander P, Diekmann F, Waiser J, Fritsche L, Dragun D, Neumayer H-H. (2004) Review of the immunosuppressant enteric-coated mycophenolate sodium. Expert Opin Pharmacother 5 1333-1345. 

Ingle GR, Shah T. (2005) Enteric-coated mycophenolate sodium for transplant immunosuppression. Am J Health-System Pharm (AJHP) 62 2252-2259. 

Budde K, Glander P, Grohmann J, Bauer S, Hambach P, Hepburn H, Mai I, Sandau K, Fischer W, Neumayer HH. (2004) Pharmacokinetic and pharmacodynamic comparison of mycophenolate mofetil (MMF) and enteric-coated mycophenolate sodium (EC-MPS) in maintenance renal transplant patients with tacrolimus as basic immunosuppression (P736). Transplantation 78 459 60. 

Meier-Kriesche H-U, Davies NM, Grinyo J, Heading R, Mamelok R, Wijngaard P, Oellerich M, Maes B. (2005) Mycophenolate sodium does not reduce the incidence of GI adverse effects compared with mycophenolate mofetil. Am J Transplant 5 1164. 

Calvo N, Sanchez-Fructuoso Al, Conesa J, Moreno A, Barrientos A. (2006) Renal transplant patients with gastrointestinal intolerability to mycophenolate mofetil Conversion to enteric-coated mycophenolate sodium. Transplant Proc 38 1396-2391. 

Mycophenolate mofetil is used together with cyclosporine and corticosteroids for the prophylaxis of acute organ rejection in patients undergoing allogeneic renal, or hepatic transplants. Compared with azathioprine it is more lymphocyte-specific and is associated with less bone marrow suppression, fewer opportunistic infections and lower incidence of acute rejection. More recently, the salt mycophenolate sodium has also been introduced. Mycophenolate mofetil is rapidly hydrolyzed to mycopheno-lic acid, its active metabolite. Mycophenolic acid is a reversible noncompetitive inhibitor of inosine monophosphate dehydrogenase, an important enzyme for the de novo synthesis of purines. As lymphocytes have little or no salvage pathway for purine... 

Behrend M, Braun F. Enteric-coated mycophenolate sodium tolerability profile compared with mycophenolate mofetil. Drugs 2005 65(8) 1037-1050. 

Mycophenolate sodium is an enteric-coated formulation of the sodium salt of mycophenohc acid designed to reduce the GI side effects of MMF. This formulation allows for mycophenohc acid to be released directly in the small intestine for absorption rather than in the stomach. Because mycophenohc acid is the activated form of MMF, the actions... 

Budde K, Curtis J, Knoll G, et al. Enteric-coated mycophenolate sodium can be safely administered in maintenance renal transplant patients Results of a 1-year study. Am J Transplant 2003 4 237-243. 

Granger DK. Enteric-coated mycophenolate sodium Results of two pivotal global multicenter trials. Transplant Proc 2001 33 3241-3244. 

Two further natural product-derived immunosuppressants have been introduced recently, mycophenclate scdium and everclimus (Fig. 1.7) (44). The active principle of both mycophenolate sodium and an earlier introduced form, mycophenolate mofetil (a morpholinoethyl derivative), is mycophenolic acid, obtained from several Penicillium sp. This compound is a reversible inhibitor of inosine monophosphate dehydrogenase, which is involved in guanosine nucleotide synthesis (80). 

Kaplan B, Meier-Kriesche H-U, Minnick P, Bastien M-C, Sechaud R, Yeh C-M, Balez S, Picard F, Schmouder R, Pharmacokinetics (PFQ of enteric-coated mycophenolate sodium (EC-MPS, Mycofortic) in stable renal transplant patients witiiNeoral or tacroUmus. J Am Soc Nephrol (2003) 14, 91OA,... 

Drag formulations Conversion from mycophenolate mofetil to enteric-coated mycophenolate sodium relieved gastrointestinal symptoms and improved health-related quality of life in a multicenter, open trial in renal transplant recipients who were taking both tacrolimus and mycophenolate mofetil [96 ]. 

Hwang HS, Hyoung BJ, Kim S, Oh HY, Kim YS, Kim JK, Kim YH, Kim YL, Kim CD, Shin GT, Yang CW. Improved gastrointestinal symptoms and quality of life after conversion from mycophenolate mofetil to enteric-coated mycophenolate sodium in renal transplant patients receiving tacrolimus. J Korean Med Sci 2010 25 (12) 1759-65. 

Sollinger HW, Sundberg AK, Leverson G, Voss BJ, Pirsch JD. Mycophenolate mofetil versus enteric-coated mycophenolate sodium a large, single-center comparison of dose adjustments and outcomes in kidney transplant recipients. Transplantation 2010 89(4) 446-51. 

An enteric-coated delivery system of MPA was developed with the aim that it would minimize gastrointestinal side effects [55]. Myfortic, approved by the FDA in 2004, is an enteric formulation of mycophenolate sodium (EC-MPS), which releases the active MPA moiety. The enteric coating of the tablet consists of the polymer, hypromellose phthalate combined with titanium dioxide, iron oxide yellow, and indigotine (180 mg tablet) or iron oxide red (360 mg tablet) [56]. Hypromellose phthalate is a monoph-thalic acid ester of hydroxypropyl methylcellulose which dissolves at pH 5-5.5, thereby affording delivery of MPA to the small intestine rather than the stomach. 

A. Johnston, X. He, and D.W. Holt, Bioequivalence of enteric-coated mycophenolate sodium and mycophenolate mofetil A meta-analysis of three studies in stable renal transplant recipients, Transplantation, 82 (11), 1413-1418,2006. 

A.J. Langone, L. Chan, P. Bohn, and M. Cooper, Enteric-coated mycophenolate sodium versus mycophenolate mofetil in renal transplant recipients experiencing gastrointestinal intolerance A multicenter, double-blind, randomized study. Transplantation, 91 (4), 470-... 

M.G. Kees, T. Steinke, S. Moritz, K. Rupprecht, E.M. Paulus, F. Kees, M. Bucher, and L. Faerber, Omeprazole impairs the absorption of mycophenolate mofetil but not of enteric-coated mycophenolate sodium in healthy volunteers, /. Clin. Pharmacol, 52 (8), 1265-1272,2012. 

In an open-label, multicenter trial, de novo kidney transplant recipients (KTRs) were randomised at week 7 posttransplant to remain on ciclosporin (n = 100, controls) or convert to everolimus (n = 102), both with enteric-coated mycophenolate sodium and corticosteroids. The incidence of oedema, acne, anaemia, mouth ulceration and hypercholesterolaemia was higher in the everolimus arm. Serious adverse events or infections that occurred in more than two everolimus-treated patients comprised pneumonia, lymphocele, increased plasma creatinine, sepsis, gastroenteritis, cytomegalovirus (CMV) infection, rejection and hydronephrosis. Two malignant neoplasms occurred in each group (everolimus malignant parathyroid tumour, adenocarcinoma of the prostate) [ll -]. 

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