Peringatan Keamanan

LD50

The LD50 of oral mycophenolate mofetil in rats is 250 mg/kg and >4000 mg/kg in mice.L7366

Overdose information

Possible signs and symptoms of acute overdose may consist of hematological abnormalities including leukopenia and neutropenia, and gastrointestinal symptoms.A180826,A180829,A180832

Mycophenolate mofetil

DB00688

small molecule approved investigational

Deskripsi

Mycophenolate mofetil, also known as MMF or CellCept, is a prodrug of mycophenolic acid, and classified as a reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH).A180805 This drug is an immunosuppressant combined with drugs such as Cyclosporine and corticosteroids to prevent organ rejection after hepatic, renal, and cardiac transplants.L7363 It is marketed by Roche Pharmaceuticals and was granted FDA approval for the prophylaxis of transplant rejection in 1995.A180826 In addition to the above uses, mycophenolate mofetil has also been studied for the treatment of nephritis and other complications of autoimmune diseases. Unlike another immunosuppressant class, the calcineurin inhibitors, MMF generally does not cause nephrotoxicity or fibrosis.A180799,A180805

Previously, mycophenolic acid (MPA) was administered to individuals with autoimmune diseases beginning in the 1970s, but was discontinued due to gastrointestinal effects and concerns over carcinogenicity.A180826 The new semi-synthetic 2-morpholinoethyl ester of MPA was synthesized to avoid the gastrointestinal effects associated with the administration of MPA. It demonstrates an increased bioavailability, a higher efficacy, and reduced gastrointestinal effects when compared to MPA.A180826

Struktur Molekul 2D

Berat 433.4947
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average apparent half-life of mycophenolate mofetil is 17.9 (±6.5) hours after oral administration and 16.6 (±5.8) hours after intravenous administration.[L7363]
Volume Distribusi The volume of distribution of mycophenolate mofetil is 3.6 (±1.5) to 4.0 (±1.2) L/kg.[L7363]
Klirens (Clearance) Plasma clearance of mycophenolate mofetil is 193 mL/min after an oral dose and 177 (±31) mL/min after an intravenous dose.[L7363]

Absorpsi

Mycophenolate mofetil is rapidly absorbed in the small intestine.L7363,A180898 The maximum concentration of its active metabolite, MPA, is attained 60 to 90 minutes following an oral dose.A180826 The average bioavailability of orally administered mycophenolate mofetil in a pharmacokinetic study of 12 healthy patients was 94%. In healthy volunteers, the Cmax of mycophenolate mofetil was 24.5 (±9.5)?g/mL.L7363 In renal transplant patients 5 days post-transplant, Cmax was 12.0 (±3.82) ?g/mL, increasing to 24.1 (±12.1)?g/mL 3 months after transplantation. AUC values were 63.9 (±16.2) ?g•h/mL in healthy volunteers after one dose, and 40.8 (±11.4) ?g•h/mL, and 65.3 (±35.4)?g•h/mL 5 days and 3 months after a renal transplant, respectively.L7363 The absorption of mycophenolate mofetil is not affected by food.A180826

Metabolisme

After both oral and intravenous administration mycophenolate mofetil is entirely metabolized by liver carboxylesterases 1 and 2 to mycophenolic acid (MPA), the active parent drug. It is then metabolized by the enzyme glucuronyl transferase, producing the inactive phenolic glucuronide of MPA (MPAG).L7363 The glucuronide metabolite is important, as it is then converted to MPA through enterohepatic recirculation. Mycophenolate mofetil that escapes metabolism in the intestine enters the liver via the portal vein and is transformed to pharmacologically active MPA in the liver cells.A180898N-(2-carboxymethyl)-morpholine, N-(2-hydroxyethyl)-morpholine, and the N-oxide portion of N-(2-hydroxyethyl)-morpholine are additional metabolites of MMF occurring in the intestine as a result of liver carboxylesterase 2 activity.A180898,L7363 UGT1A9 and UGT2B7 in the liver are the major enzymes contributing to the metabolism of MPA in addition to other UGT enzymes, which also play a role in MPA metabolism. The four major metabolites of MPA are 7-O-MPA-?-glucuronide (MPAG, inactive), MPA acyl-glucuronide (AcMPAG), produced by uridine 5?-diphosphate glucuronosyltransferases (UGT) activities, 7-O-MPA glucoside produced via UGT, and small amounts 6-O-des-methyl-MPA (DM-MPA) via CYP3A4/5 and CYP2C8 enzymes.A180826

Rute Eliminasi

A small amount of drug is excreted as MPA in the urine (less than 1%). When mycophenolate mofetil was given orally in a pharmacokinetic study, it was found to be 93% excreted in urine and 6% excreted in feces. Approximately 87% of the entire administered dose is found to be excreted in the urine as MPAG, an inactive metabolite.A180826,L7363

Interaksi Makanan

2 Data
  • 1. Avoid multivalent ions. Take multivalent ions such as calcium, iron, or magnesium at least 2 hours after taking this medication.
  • 2. Take on an empty stomach. Take at least 1 hour before or 2 hours after meals.

Interaksi Obat

1602 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Mycophenolate mofetil.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Mycophenolate mofetil.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Mycophenolate mofetil.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Mycophenolate mofetil.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Mycophenolate mofetil.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Mycophenolate mofetil.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Mycophenolate mofetil.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Mycophenolate mofetil.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Mycophenolate mofetil.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Mycophenolate mofetil.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Mycophenolate mofetil.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Mycophenolate mofetil.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Mycophenolate mofetil.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Mycophenolate mofetil.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Mycophenolate mofetil.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Mycophenolate mofetil.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Mycophenolate mofetil.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Mycophenolate mofetil.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Mycophenolate mofetil.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Mycophenolate mofetil.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Mycophenolate mofetil.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Mycophenolate mofetil.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Mycophenolate mofetil.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Mycophenolate mofetil.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Mycophenolate mofetil.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Mycophenolate mofetil.
Cladribine Mycophenolate mofetil may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Mycophenolate mofetil.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Mycophenolate mofetil.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Mycophenolate mofetil.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Mycophenolate mofetil.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Mycophenolate mofetil.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Mycophenolate mofetil.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Mycophenolate mofetil.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Mycophenolate mofetil.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Mycophenolate mofetil.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Mycophenolate mofetil.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Mycophenolate mofetil.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Mycophenolate mofetil.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Mycophenolate mofetil.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Mycophenolate mofetil.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Mycophenolate mofetil.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Mycophenolate mofetil.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Mycophenolate mofetil.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Mycophenolate mofetil.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Mycophenolate mofetil.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Mycophenolate mofetil.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Mycophenolate mofetil.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Mycophenolate mofetil.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Mycophenolate mofetil.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Mycophenolate mofetil.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Mycophenolate mofetil.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Mycophenolate mofetil.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Mycophenolate mofetil.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Mycophenolate mofetil.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Mycophenolate mofetil.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Mycophenolate mofetil.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Mycophenolate mofetil.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Mycophenolate mofetil.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Mycophenolate mofetil.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Mycophenolate mofetil.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Mycophenolate mofetil.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Mycophenolate mofetil.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Mycophenolate mofetil.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Mycophenolate mofetil.
Daunorubicin The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Daunorubicin.
Tretinoin The metabolism of Tretinoin can be decreased when combined with Mycophenolate mofetil.
Irinotecan The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Irinotecan.
Sulfasalazine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Sulfasalazine.
Dacarbazine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Dacarbazine.
Temozolomide The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Penicillamine.
Prednisolone The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Prednisolone.
Mechlorethamine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Azacitidine.
Carboplatin The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Carboplatin.
Methylprednisolone The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Methylprednisolone.
Dactinomycin The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Dactinomycin.
Cytarabine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Cytarabine.
Azathioprine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Azathioprine.
Doxorubicin The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Doxorubicin.
Hydroxyurea The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Hydroxyurea.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Mercaptopurine.
Thalidomide The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Flucytosine.
Capecitabine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Capecitabine.
Trilostane The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Trilostane.
Procarbazine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Procarbazine.
Arsenic trioxide The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Arsenic trioxide.
Idarubicin The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Idarubicin.
Estramustine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Estramustine.
Mitoxantrone The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Mitoxantrone.
Lomustine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Lomustine.
Dexamethasone The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Dexamethasone.
Eculizumab The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Decitabine.

Target Protein

Prostaglandin E2 receptor EP2 subtype PTGER2
Inosine-5'-monophosphate dehydrogenase 1 IMPDH1
Inosine-5'-monophosphate dehydrogenase 2 IMPDH2
6-pyruvoyl tetrahydrobiopterin synthase PTS

Referensi & Sumber

Synthesis reference: 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.
Artikel (PubMed)
  • PMID: 15570183
    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.
  • PMID: 19834629
    Villarroel MC, Hidalgo M, Jimeno A: Mycophenolate mofetil: An update. Drugs Today (Barc). 2009 Jul;45(7):521-32. doi: 10.1358/dot.2009.45.7.1384878.
  • PMID: 15803924
    Allison AC: Mechanisms of action of mycophenolate mofetil. Lupus. 2005;14 Suppl 1:s2-8.
  • PMID: 30761563
    Santiago P, Schwartz I, Tamariz L, Levy C: Systematic review with meta-analysis: mycophenolate mofetil as a second-line therapy for autoimmune hepatitis. Aliment Pharmacol Ther. 2019 Apr;49(7):830-839. doi: 10.1111/apt.15157. Epub 2019 Feb 13.
  • PMID: 20655577
    Sagcal-Gironella AC, Fukuda T, Wiers K, Cox S, Nelson S, Dina B, Sherwin CM, Klein-Gitelman MS, Vinks AA, Brunner HI: Pharmacokinetics and pharmacodynamics of mycophenolic acid and their relation to response to therapy of childhood-onset systemic lupus erythematosus. Semin Arthritis Rheum. 2011 Feb;40(4):307-13. doi: 10.1016/j.semarthrit.2010.05.007. Epub 2010 Jul 23.
  • PMID: 21278895
    Park H: The emergence of mycophenolate mofetilin dermatology: from its roots in the world of organ transplantation to its versatile role in the dermatology treatment room. J Clin Aesthet Dermatol. 2011 Jan;4(1):18-27.
  • PMID: 24987184
    Alex R, Mathew M, Arul S, Kundavaram A: Overdose of mycophenolate mofetil managed in a secondary care hospital in South India. Indian J Pharmacol. 2014 May-Jun;46(3):337-8. doi: 10.4103/0253-7613.132191.
  • PMID: 18763324
    Parfitt JR, Jayakumar S, Driman DK: Mycophenolate mofetil-related gastrointestinal mucosal injury: variable injury patterns, including graft-versus-host disease-like changes. Am J Surg Pathol. 2008 Sep;32(9):1367-72.
Menampilkan 8 dari 12 artikel.

Contoh Produk & Brand

Produk: 167 • International brands: 2
Produk
  • Accel-mycophenolate Mofetil Capsules
    Capsule • 250 mg • Oral • Canada • Generic • Approved
  • Accel-mycophenolate Mofetil Tablets
    Tablet • 500 mg • Oral • Canada • Generic • Approved
  • Ach-mycophenolate
    Tablet • 500 mg • Oral • Canada • Generic • Approved
  • Ach-mycophenolate
    Capsule • 250 mg • Oral • Canada • Generic • Approved
  • Ach-mycophenolate
    Powder, for suspension • 200 mg / mL • Oral • Canada • Generic • Approved
  • Ag-mycophenolate
    Tablet • 500 mg • Oral • Canada • Generic • Approved
  • Apo-mycophenolate
    Capsule • 250 mg • Oral • Canada • Generic • Approved
  • Apo-mycophenolate
    Tablet • 500 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 167 produk.
International Brands
  • CellCept Oral Suspension — Genentech USA, Inc.
  • CellCept Intravenous — Genentech USA, Inc.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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