micofenolato

Micofenolato, commonly referred to as mycophenolate, comprises immunosuppressant drugs whose active metabolite is mycophenolic acid (MPA). The main formulations are mycophenolate mofetil (MMF), a prodrug, and mycophenolate sodium (mycophenolate sodium). After oral administration, MMF is rapidly hydrolyzed to MPA, which exerts the pharmacologic effect.

The mechanism of action involves inhibition of inosine monophosphate dehydrogenase (IMPDH), the key enzyme in de novo guanine nucleotide synthesis. This preferentially affects lymphocytes, which rely on this pathway for proliferation, leading to reduced T and B cell expansion and diminished immune responses. The drug is used to prevent organ transplant rejection and, in some regimens, to treat certain autoimmune conditions.

Indications include prevention of allograft rejection in solid organ transplantation (kidney, heart, liver) as part of combination therapy with calcineurin inhibitors and corticosteroids. It is also used off-label for various autoimmune diseases, notably lupus nephritis and some severe immune-mediated conditions, though the strength of evidence varies by indication.

Pharmacokinetics and interactions: MPA exposure is influenced by formulation and concomitant immunosuppressants. Co-administration with cyclosporine can reduce MPA levels, while tacrolimus generally has less impact. Absorption can be affected by meals and by drugs that bind bile acids or reduce enterohepatic recirculation. Common drug interactions involve other immunosuppressants, anticoagulants, and vaccines.

Dosing and monitoring: Typical regimens use several hundred milligrams to 1 gram twice daily, adjusted for transplant type, co-medications, and tolerability. Dose adjustments may be needed for renal or hepatic impairment. Monitoring includes periodic complete blood counts, liver and kidney function tests, infection surveillance, and, in some protocols, MPA trough levels. Pregnancy is contraindicated due to teratogenic risk; effective contraception is required, and pregnancy should prompt discontinuation or switching therapy. Adverse effects commonly include gastrointestinal symptoms, leukopenia or anemia, infections, and rare events such as leukopenia-associated complications or malignancies with long-term use.