Mycophenolate

Mycophenolate refers to immunosuppressant drugs whose active metabolite is mycophenolic acid (MPA). The two commonly used salt forms are mycophenolate mofetil (MMF; brand name CellCept) and mycophenolate sodium (brand name Myfortic). After ingestion, MMF is rapidly converted to MPA; mycophenolate sodium provides MPA as well. These agents are used to prevent organ transplant rejection and to treat certain autoimmune diseases.

Indications include prophylaxis of organ transplant rejection (kidney, heart, liver, and others) in combination with calcineurin inhibitors and corticosteroids. They are also employed for autoimmune conditions such as lupus nephritis and certain vasculitides, with use guided by disease type and prior therapies. Dosing and choice of formulation depend on indication, concomitant immunosuppressants, and renal function.

Mechanism of action: MPA inhibits inosine monophosphate dehydrogenase (IMPDH), an enzyme essential for de novo guanine nucleotide synthesis. Lymphocytes rely on this pathway, so mycophenolate suppresses T- and B-cell proliferation and function more than other cell types.

Safety and monitoring: Common adverse effects include gastrointestinal symptoms (nausea, diarrhea), leukopenia or anemia, infections, hypertension, and an increased risk of malignancies with long-term use. The drug is teratogenic and contraindicated in pregnancy; effective contraception is advised for people of reproductive potential during treatment and for a period after cessation. Regular monitoring of blood counts, kidney and liver function is recommended, and drug interactions should be reviewed with a clinician.

Interactions: Absorption can be reduced by concomitant aluminum- or magnesium-containing antacids or bile acid sequestrants. Immunosuppressants such as calcineurin inhibitors can alter MPA exposure, necessitating dose adjustments and clinical monitoring.