About: Mycophenolate mofetil     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • Mycophenolate mofetil is the 2-morpholinoethyl ester of mycophenolic acid (MPA), an immunosuppressive agent, inosine monophosphate dehydrogenase (IMPDH) inhibitor. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Woodroffe R, Yao GL, Meads C, Bayliss S, Ready A, Raftery J, Taylor RS: Clinical and cost-effectiveness of newer immunosuppressive regimens in renal transplantation: a systematic review and modelling study. Health Technol Assess. 2005 May;9(21):1-179, iii-iv. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15899149 # FDA label # Picard N, Cresteil T, Premaud A, Marquet P: Characterization of a phase 1 metabolite of mycophenolic acid produced by CYP3A4/5. Ther Drug Monit. 2004 Dec;26(6):600-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15570183 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
  • investigational (en)
http://linked.open...drugbank/halfLife
  • The mean elimination half-life for mycophenolic acid (the active metabolite) ranges from 8-16 hours, while that of the MPAG metabolite ranges from 13-17 hours. (en)
http://linked.open...ugbank/indication
  • For the prophylaxis of organ rejection in patients receiving allogeneic renal, cardiac or hepatic transplants. Mycophenolate mofetil should be used concomitantly with cyclosporine and corticosteroids. (en)
http://linked.open...bank/manufacturer
sameAs
Title
  • Mycophenolate mofetil (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Mycophenolate mofetil is hydrolyzed to form mycophenolic acid (MPA), which is the active metabolite. MPA is a potent, selective, uncompetitive, and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and therefore inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation into DNA. Because T- and B-lymphocytes are critically dependent for their proliferation on de novo synthesis of purines, whereas other cell types can utilize salvage pathways, MPA has potent cytostatic effects on lymphocytes. MPA inhibits proliferative responses of T- and B-lymphocytes to both mitogenic and allospecific stimulation. Addition of guanosine or deoxyguanosine reverses the cytostatic effects of MPA on lymphocytes. MPA also suppresses antibody formation by B-lymphocytes. MPA prevents the glycosylation of lymphocyte and monocyte glycoproteins that are involved in intercellular adhesion to endothelial cells and may inhibit recruitment of leukocytes into sites of inflammation and graft rejection. Mycophenolate mofetil did not inhibit early events in the activation of human peripheral blood mononuclear cells, such as the production of interleukin-1 (IL-1) and interleukin-2 (IL-2), but did block the coupling of these events to DNA synthesis and proliferation. (en)
http://linked.open...drugbank/packager
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • Negligible amount of drug is excreted as MPA (< 1% of dose) in the urine. When orally administered, mycophenolate mofetil was completely recovered with 93% of the dose found in the urine and 6% found in feces. 87% of the administered dose is excreted in the urine as MPAG. (en)
http://linked.open.../drugbank/synonym
  • Cellcept (en)
  • MMF (en)
  • Mycophenolic acid morpholinoethyl ester (en)
  • RS 61443 (en)
  • 2-Morpholinoethyl (e)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-5-phthalanyl)-4-methyl-4-hexenoate (en)
http://linked.open...drugbank/toxicity
  • Oral (LD50): Acute: 352 mg/kg [Rat], 1000 mg/kg [Mouse], and &gt;6000 mg/kg [Rabbit]. Possible signs and symptoms of acute overdose could include the following: hematological abnormalities such as leukopenia and neutropenia, and gastrointestinal symptoms such as abdominal pain, diarrhea, nausea and vomiting, and dyspepsia. (en)
http://linked.open...umeOfDistribution
  • * 3.6 ±1.5 L/kg [intravenous, healthy subjects, MPA] * 4 ±1.2 L/kg [oral administration, healthy subjects, MPA] (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • Take on empty stomach: 1 hour before or 2 hours after meals. (en)
  • Do not take calcium, aluminium, magnesium or iron supplements within 2 hours of taking this medication. (en)
http://linked.open...nk/proteinBinding
  • MPA (the active metabolite), at clinically relevant concentrations, is over 98% bound to plasma albumin. The phenolic glucuronide of MPA, mycophenolic acid glucuronide (MPAG) has 82% protein bound. (en)
http://linked.open...ynthesisReference
  • Roger C. Fu, De-Mei Leung, Jeffrey S. Fleitman, Michele C. Rizzolio, Andrew R. Miksztal, "Process for preparing pharmaceutical compositions containing crystalline anhydrous mycophenolate mofetil salts." U.S. Patent US5545637, issued November, 1988. (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open.../Water-Solubility
http://linked.open...ogy/drugbank/logP
http://linked.open...ogy/drugbank/logS
http://linked.open...nd-Acceptor-Count
http://linked.open...-Bond-Donor-Count
http://linked.open...drugbank/InChIKey
http://linked.open...urface-Area--PSA-
http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
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