Mycophenolate Mofetil

Holt, Curtis; Sievers, Theodore M.; Ghobrial, Rafik M.; Rossi, S; Goss, John A.; McDiarmid, Sue V.

doi:10.2165/00063030-199810050-00004

Cited by 8 publications

(4 citation statements)

References 19 publications

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“…Oral bioavailability of MPA is increased by administration of the ester prodrug MMF. MMF undergoes rapid hydrolysis to MPA followed by metabolism to MPA glucuronide. , The rapid hydrolysis of MMF occurs high up in the GI tract and is thought to be partly responsible for the observed GI side effects . In an attempt to combat the adverse effects, an enteric coated formulation of sodium mycophenolate (EC-MPS) was developed .…”

Section: Introductionmentioning

confidence: 99%

Spectroscopic Characterization of Copper(II) Binding to the Immunosuppressive Drug Mycophenolic Acid

et al. 2006

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Mycophenolic acid (MPA) is a drug that has found widespread use as an immunosuppressive agent which limits rejection of transplanted organs. Optimal use of this drug is hampered by gastrointestinal side effects which can range in severity. One mechanism by which MPA causes gastropathy may involve a direct interaction between the drug and gastric phospholipids. To combat this interaction we have investigated the potential of MPA to coordinate Cu(II), a metal which has been used to inhibit gastropathy associated with use of the NSAID indomethacin. Using a range of spectroscopic techniques we show that Cu(II) is coordinated to two MPA molecules via carboxylates and, at low pH, water ligands. The copper complex formed is stable in solution as assessed by mass spectrometry and 1H NMR diffusion experiments. Competition studies with glycine and albumin indicate that the copper-MPA complex will release Cu(II) to amino acids and proteins thereby allowing free MPA to be transported to its site of action. Transfer to serum albumin proceeds via a Cu(MPA)(albumin) ternary complex. These results raise the possibility that copper complexes of MPA may be useful in a therapeutic situation.

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Section: Introductionmentioning

confidence: 99%

Spectroscopic Characterization of Copper(II) Binding to the Immunosuppressive Drug Mycophenolic Acid

et al. 2006

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“…Studies on the use of MMF in preventing acute rejection in patients who undergo heart transplantation are ongoing. 9 …”

Section: Discussionmentioning

confidence: 99%

Comparison of MMF with prednisone in terms of rejection and duration of activity of transplant in rabbits that underwent retroperitoneal heterotopic heart transplantation: cardiovascular topic

Aygün¹,

Efe²,

Durgut³

2015

CVJA

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SummaryAimIn this study, mycophenolate mofetil (MMF) and methylprednisolone (MP) were compared in terms of rejection and duration of activity of the transplant in New Zealand rabbits that underwent retroperitoneal heart transplantation.MethodsRetroperitoneal heart transplantation was performed in New Zealand white rabbits. The animals were divided into two groups. MMF group (group 1) (10 donors, 10 recipients): 12.5 mg/kg MMF was administered orally for two days prior to the surgery; MP group (group 2) (nine donors, nine recipients): 2 mg/kg MP was administered intramuscularly for two days prior to the surgery. After the operation, we waited until all motor activity in the transplanted heart had stopped. The transplant was then removed and the recipient was sacrificed. A donor in the MP group was excluded since it died before the motor activity had stopped.ResultsNo statistically significant difference was found between the groups in terms of rejection score (p = 0.865). However, duration of motor activity was found to be statistically significantly longer in the MMF group, compared to the MP group (p = 0.013).ConclusionIn this experimental study, MMF was similar to MP in terms of rejection but had better efficacy in terms of duration of motor activity of the transplant.

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“…Mycophenolic acid (MPA) is the pharmacologically active agent of the recently introduced immunosuppressive drug mycophenolate mofetil (MMF, CellCept TM ; Behrend, 1998). In fact, MMF has never been detected systemically due to its fast hydrolysis to MPA, which is responsible for the gastrointestinal side effects and leukocytopenia observed in transplant patients (Holt et al, 1998). To alleviate the upper gastrointestinal tract problems, an enteric coated formulation of sodium mycophenolate, ERL080, (I), is currently in phase III clinical trials for the prophylaxis of transplant rejection.…”

Section: Commentmentioning

confidence: 99%