Peringatan Keamanan

There are anecdotal reports of deliberate or accidental overdoses with mycophenolic acid; however, not all patients have experienced related adverse reactions. In those cases where adverse reactions have been reported, reactions fall within the safety profile of its class of drugs. A mycophenolic acid overdose could lead to the oversuppression of the immune system and increase the susceptibility to infection.L42165 It may be appropriate to interrupt or discontinue mycophenolic acid if blood dyscrasias occur. Some of the signs and symptoms associated with mycophenolic acid overdose are hematological abnormalities, such as leukopenia and neutropenia, and gastrointestinal symptoms, such as abdominal pain, diarrhea, nausea and vomiting, and dyspepsia.L42165

Carcinogenicity studies of 104 weeks done in rats and mice, suggest that mycophenolate sodium does not induce the formation of tumours. Rats were given up to 9 mg/kg of mycophenolate sodium, which corresponded to 0.6-1.2 times the systemic exposure observed in renal transplant patients, while mice were given 180 mg/kg, an equivalent of 0.6 times the mycophenolate sodium therapeutic dose.L42165 The genotoxicity of mycophenolate sodium was confirmed by the mouse lymphoma/thymidine kinase assay, the micronucleus test in V79 Chinese hamster cells, and the in vivo mouse micronucleus assay. Mycophenolate mofetil, a prodrug of mycophenolic acid, had a similar genotoxic profile. At daily oral doses as high as 18 mg/kg and 20 mg/kg, mycophenolate sodium had no effect on male and female rat fertility, respectively.L42165 The oral LD50 of mycophenolic acid is 352 mg/kg in rats and 1000 mg/kg in mice.L42180

Mycophenolic acid

DB01024

small molecule approved investigational

Deskripsi

Mycophenolic acid is a potent immunosuppressant agent that inhibits de novo purine biosynthesis.L42165 It was derived from Penicillium stoloniferum, and has also shown antibacterial, antifungal and antiviral properties.A249170. Mycophenolic acid is used in immunosuppressive regimens as part of a triple therapy that includes a calcineurin inhibitor (ciclosporin or tacrolimus) and prednisolone.A249175 This regimen can be used in place of the older anti-proliferative azathioprine due to its stronger immunosuppressive potency.A249180 However, mycophenolic acid treatment is more expensive and requires therapeutic drug monitoring to optimize efficacy and minimize toxicity.A249180,A249185 Mycophenolic acid is available as enteric-coated tablets of delayed-release, in an effort to improve upper gastrointestinal adverse events by delaying mycophenolic acid release until it reaches the small intestine.A249190 Mycophenolate mofetil, a prodrug of mycophenolic acid, is also prescribed to transplant recipients to prevent organ rejection.L42020

Struktur Molekul 2D

Berat 320.3371
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean elimination half-life of mycophenolic acid ranges between 8 and 16 hours, while the mean elimination half-life of mycophenolic acid glucuronide, its major metabolite, ranges between 13 and 17 hours.[L42165]
Volume Distribusi At steady state, the volume of distribution of mycophenolic acid is 54 L. At the elimination phase, the volume of distribution of mycophenolic acid is 112 L.[L42165]
Klirens (Clearance) The mean clearance of mycophenolic acid is 140 mL/min. The mean renal clearance of its metabolite, mycophenolic acid glucuronide, is 15.5 mL/min.[L42165]

Absorpsi

Between 360 mg and 2,160 mg, mycophenolic acid follows a linear and dose-proportional pharmacokinetic profile. The enteric-coating of mycophenolic acid tablets prevents release under acidic conditions (stomach, pH < 5). However, enteric-coated mycophenolic acid tablets are highly soluble in neutral pH conditions such as those in the intestine.L42165 In renal transplant patients, the median delay (Tlag) in the rise of mycophenolic acid concentration ranged between 0.25 and 1.25 hours, and the Tmax ranged between 1.5 and 2.75 hours. Adult renal transplant patients on cyclosporine given mycophenolic acid had a Tmax of 2 h, a Cmax of 26.1 ?g/mL, and an AUC0-12 of 66.5 ?g?h/mL. Stable pediatric (5-16 years old) renal transplant patients had a Cmax and AUC 33% and 18% higher than the ones detected in adults.L42165 In stable renal transplant patients treated with cyclosporine, the gastrointestinal absorption and absolute bioavailability of delayed-release tablets of mycophenolic acid were 93% and 72%, respectively.L42165 Following the administration of a high-fat meal (55 g fat, 1000 calories), the AUC of mycophenolic acid (enteric-coated tablets, 720 mg) was comparable to the one detected during fasting. However, a high-fat meal can lead to a 33% decrease of the Cmax, a 3.5-hour delay in the Tlag (range of -6 to 18 hours), and a 5.0-hour delay in the Tmax (range of -9 to 20 hours). To avoid variability in the absorption of mycophenolic acid, this drug should be taken on an empty stomach.L42165

Metabolisme

Mycophenolic acid is mainly metabolized by glucuronyl transferase to form glucuronidated metabolites. Mycophenolic acid glucuronide (MPAG), the major metabolite of mycophenolic acid, does not display pharmacological activity. However, the acyl glucuronide minor metabolite has a pharmacological activity similar to mycophenolic acid. The AUC ratio of mycophenolic acid:MPAG:acyl glucuronide is approximately 1:24:0.28 at a steady state.L42165

Rute Eliminasi

In stable renal transplant patients, approximately 60% of mycophenolic acid is eliminated in the urine as mycophenolic acid glucuronide (MPAG), while 3% is eliminated unchanged.L42165 MPAG is also secreted in the bile and is available for deconjugation by gut flora. The mycophenolic acid that results from MPAG deconjugation may be reabsorbed and produce a second peak 6-8 hours after administration.L42165

Interaksi Makanan

1 Data
  • 1. Take on an empty stomach. Take mycophenolic acid at least 1 hour before or 2 hours after eating.

Interaksi Obat

1261 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Mycophenolic acid.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Mycophenolic acid.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Mycophenolic acid.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Mycophenolic acid.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Mycophenolic acid.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Mycophenolic acid.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Mycophenolic acid.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Mycophenolic acid.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Mycophenolic acid.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Mycophenolic acid.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Mycophenolic acid.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Mycophenolic acid.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Mycophenolic acid.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Mycophenolic acid.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Mycophenolic acid.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Mycophenolic acid.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Mycophenolic acid.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Mycophenolic acid.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Mycophenolic acid.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Mycophenolic acid.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Mycophenolic acid.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Mycophenolic acid.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Mycophenolic acid.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Mycophenolic acid.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Mycophenolic acid.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Mycophenolic acid.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Mycophenolic acid.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Mycophenolic acid.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Mycophenolic acid.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Mycophenolic acid.
Cladribine Mycophenolic acid may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Mycophenolic acid.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Mycophenolic acid.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Mycophenolic acid.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Mycophenolic acid.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Mycophenolic acid.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Mycophenolic acid.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Mycophenolic acid.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Mycophenolic acid.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Mycophenolic acid.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Mycophenolic acid.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Mycophenolic acid.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Mycophenolic acid.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Mycophenolic acid.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Mycophenolic acid.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Mycophenolic acid.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Mycophenolic acid.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Mycophenolic acid.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Mycophenolic acid.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Mycophenolic acid.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Mycophenolic acid.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Mycophenolic acid.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Mycophenolic acid.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Mycophenolic acid.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Mycophenolic acid.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Mycophenolic acid.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Mycophenolic acid.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Mycophenolic acid.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Mycophenolic acid.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Mycophenolic acid.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Mycophenolic acid.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Mycophenolic acid.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Mycophenolic acid.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Mycophenolic acid.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Mycophenolic acid.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Mycophenolic acid.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Mycophenolic acid.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Mycophenolic acid.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Mycophenolic acid.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Mycophenolic acid.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Mycophenolic acid.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Mycophenolic acid.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Mycophenolic acid.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Mycophenolic acid.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Mycophenolic acid.
Etoposide The risk or severity of adverse effects can be increased when Etoposide is combined with Mycophenolic acid.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Mycophenolic acid.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Mycophenolic acid.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Mycophenolic acid.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Mycophenolic acid.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Mycophenolic acid.
Sirolimus The risk or severity of adverse effects can be increased when Sirolimus is combined with Mycophenolic acid.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Mycophenolic acid.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Mycophenolic acid.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Mycophenolic acid.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Mycophenolic acid.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Mycophenolic acid.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Mycophenolic acid.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Mycophenolic acid.
Doxorubicin The risk or severity of adverse effects can be increased when Doxorubicin is combined with Mycophenolic acid.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Mycophenolic acid.
Busulfan The risk or severity of adverse effects can be increased when Busulfan is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Mercaptopurine.
Thalidomide The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Flucytosine.
Capecitabine The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Capecitabine.
Trilostane The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Trilostane.

Target Protein

Inosine-5'-monophosphate dehydrogenase 2 IMPDH2
Inosine-5'-monophosphate dehydrogenase 1 IMPDH1

Referensi & Sumber

Synthesis reference: Bernard J. Abbott, John G. Whitney, "Method of preparing mycophenolic acid glucoside." U.S. Patent US4234684, issued January, 1976.
Artikel (PubMed)
  • PMID: 9308561
    Kitchin JE, Pomeranz MK, Pak G, Washenik K, Shupack JL: Rediscovering mycophenolic acid: a review of its mechanism, side effects, and potential uses. J Am Acad Dermatol. 1997 Sep;37(3 Pt 1):445-9. doi: 10.1016/s0190-9622(97)70147-6.
  • PMID: 12752309
    Shaw LM, Korecka M, Venkataramanan R, Goldberg L, Bloom R, Brayman KL: Mycophenolic acid pharmacodynamics and pharmacokinetics provide a basis for rational monitoring strategies. Am J Transplant. 2003 May;3(5):534-42. doi: 10.1034/j.1600-6143.2003.00079.x.
  • PMID: 26633102
    Wagner M, Earley AK, Webster AC, Schmid CH, Balk EM, Uhlig K: Mycophenolic acid versus azathioprine as primary immunosuppression for kidney transplant recipients. Cochrane Database Syst Rev. 2015 Dec 3;(12):CD007746. doi: 10.1002/14651858.CD007746.pub2.
  • PMID: 31332670
    Kiang TKL, Ensom MHH: Exposure-Toxicity Relationships of Mycophenolic Acid in Adult Kidney Transplant Patients. Clin Pharmacokinet. 2019 Dec;58(12):1533-1552. doi: 10.1007/s40262-019-00802-z.
  • PMID: 15163278
    Budde K, Glander P, Diekmann F, Waiser J, Fritsche L, Dragun D, Neumayer HH: Review of the immunosuppressant enteric-coated mycophenolate sodium. Expert Opin Pharmacother. 2004 Jun;5(6):1333-45. doi: 10.1517/14656566.5.6.1333.

Contoh Produk & Brand

Produk: 66 • International brands: 2
Produk
  • Apo-mycophenolic Acid
    Tablet, delayed release • 180 mg • Oral • Canada • Generic • Approved
  • Apo-mycophenolic Acid
    Tablet, delayed release • 360 mg • Oral • Canada • Generic • Approved
  • Jamp Mycophenolic Acid
    Tablet, delayed release • 360 mg • Oral • Canada • Generic • Approved
  • Jamp Mycophenolic Acid
    Tablet, delayed release • 180 mg • Oral • Canada • Generic • Approved
  • Mar-mycophenolic Acid
    Tablet, delayed release • 180 mg • Oral • Canada • Generic • Approved
  • Mar-mycophenolic Acid
    Tablet, delayed release • 360 mg • Oral • Canada • Generic • Approved
  • Mycophenolic Acid
    Tablet, delayed release • 180 mg/1 • Oral • US • Generic • Approved
  • Mycophenolic Acid
    Tablet, delayed release • 360 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 66 produk.
International Brands
  • Melbex
  • Myfortic — Novartis Pharmaceuticals Corporation

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul