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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Selective immunosuppressants
mycophenolic acid
L04AA06
Forms & Strengths
- Delayed-release tablets (as sodium salt): 180 mg, 360 mg
- Oral suspension (as mofetil prodrug): 200 mg/mL
- Capsules (as mofetil prodrug): 250 mg
- Tablets (as mofetil prodrug): 500 mg
- Intravenous injection (as mofetil prodrug): 500 mg/vial
Adult Dosing
- Renal transplantation: 720 mg orally twice daily (mycophenolate sodium) or 1 g to 1.5 g orally/IV twice daily (mycophenolate mofetil).
- Cardiac transplantation: 1.5 g orally/IV twice daily (mycophenolate mofetil).
- Hepatic transplantation: 1 g orally twice daily or 1 g IV twice daily (mycophenolate mofetil).
Pediatric Dosing
- Renal transplantation (children $\ge$ 3 months): 600 mg/m² orally twice daily (mycophenolate mofetil), up to 1 g twice daily.
- Pediatric dosing for mycophenolate sodium is less established; conversion based on surface area and equivalent MPA exposure.
Indications
- Prophylaxis of organ rejection in adult and pediatric patients receiving allogeneic renal, cardiac, or hepatic transplants.
- Off-label: Lupus nephritis, rheumatoid arthritis, psoriasis, and other autoimmune conditions.
Mechanism of Action
- Reversible, non-competitive inhibitor of inosine monophosphate dehydrogenase (IMPDH).
- Rate-limiting step in de novo guanosine nucleotide synthesis.
- Selectively inhibits proliferation of T and B lymphocytes more than other cell types.
Contraindications
- Hypersensitivity to mycophenolic acid, mycophenolate mofetil, or any component of the drug formulation.
- Pregnancy (due to increased risk of first-trimester pregnancy loss and congenital malformations).
Adverse Reactions
- Gastrointestinal: Diarrhea, nausea, vomiting, abdominal pain, GI tract ulceration/hemorrhage.
- Hematologic: Leukopenia, anemia, thrombocytopenia, neutropenia.
- Infections: Increased risk of opportunistic infections (CMV, BK virus, fungal infections).
- Malignancies: Increased risk of lymphomas and skin malignancies.
Drug Interactions
- Antacids with magnesium/aluminum hydroxide: Decrease absorption of mycophenolic acid; avoid coadministration.
- Sevelamer and bile acid sequestrants (e.g., cholestyramine): Reduce MPA AUC by interfering with enterohepatic recirculation.
- Acyclovir, ganciclovir, or valganciclovir: Compete for renal tubular secretion, potentially increasing concentrations of both drugs.
- Azathioprine: Should not be administered concomitantly due to potential bone marrow suppression and overlapping toxicity.
Curated Content: Needs Vetting Before Put to Clinical Use