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Mycophenolate Mofetil

Immunological Chemotherapy Prescription
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Indications

Graftcept (mycophenolate mofetil) is used together with corticosteroids and either ciclosporin or tacrolimus. It is indicated for the prophylaxis of acute organ rejection, and for the treatment of first or refractory organ rejection, in patients who have received an allogeneic renal transplant. The same combination is also indicated for prophylaxis of acute organ rejection after an allogeneic cardiac transplant. The third use is prophylaxis of acute organ rejection after an allogeneic hepatic transplant. Graftcept is also indicated for induction and maintenance therapy of patients with Class III-V lupus nephritis, diagnosed according to the International Society of Nephrology/Renal Pathology Society classification.

⚠️ Always consult a registered physician before taking any medicine.

Pharmacology

Mechanism of Action: Mycophenolate mofetil is the 2-morpholinoethyl ester of mycophenolic acid (MPA). MPA is a potent, selective, uncompetitive and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and it therefore inhibits the de novo pathway of guanosine nucleotide synthesis. The way MPA inhibits the enzymatic activity of IMPDH appears to be related to its ability to structurally mimic both the nicotinamide adenine dinucleotide cofactor and a catalytic water molecule. This prevents the oxidation of IMP to xanthose-5'-monophosphate, which is the committed step in de novo guanosine nucleotide biosynthesis. MPA has more potent cytostatic effects on lymphocytes than on other cells because T and B lymphocytes depend critically on de novo purine synthesis for their proliferation, whereas other cell types can rely on salvage pathways instead.

Pharmacodynamics: Mycophenolic acid, the active metabolite of mycophenolate mofetil, is a non-competitive, reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH). Inhibiting IMPDH blocks the de novo synthesis of guanosine nucleotides, which are necessary substrates for DNA and RNA synthesis. Unlike other cell types, which can use the salvage pathway, B and T lymphocytes depend on the de novo pathway to generate guanosine. Data from in vitro studies show that mycophenolic acid and/or mycophenolate mofetil inhibit mixed lymphocyte responses and human peripheral blood lymphocyte proliferation induced by a variety of mitogens and antigens. Mycophenolic acid reduces intracellular pools of guanosine triphosphate (GTP) and deoxyguanosine triphosphate (dGTP) in mitogen-stimulated human peripheral blood monocytes or T lymphocytic cell lines, but it has no effect on GTP concentrations in human neutrophils.

Pregnancy & Breastfeeding

Mycophenolate Mofetil should not be used during pregnancy or while breastfeeding. It has not been established as safe for use during labor and delivery either.

⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.

Dosage Reference

⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.

Adults: Transplant patients Standard dosage for prophylaxis of renal rejection Adults: 1 g of Mycophenolate Mofetil by mouth twice a day (a daily dose of 2 g) is recommended for renal transplant patients. Children (aged 3 months to 18 years): Patients with a body surface area of 1.25 to 1.5 m2 may be prescribed Mycophenolate Mofetil tablets at 750 mg twice daily (1.5 g daily dose). Patients with a body surface area above 1.5 m2 may be prescribed the tablets at 1 gm twice daily (2 g daily dose). Standard dosage for prophylaxis of cardiac rejection Adults: 1.5 g by mouth twice a day (a daily dose of 3 g) is recommended for cardiac transplant patients. Each dose should be given over not less than 2 hours. Children: no data are available for paediatric cardiac transplant patients. Standard dosage for prophylaxis of hepatic rejection Adults: 1.5 g by mouth twice a day (a daily dose of 3 g) is recommended for hepatic transplant patients. Children: no data are available for paediatric hepatic transplant patients. Standard dosage for treatment of first or refractory renal rejection Adults: 1.5 g by mouth twice a day (a daily dose of 3 g) is recommended for managing first or refractory rejection. Children: no data are available for treating first or refractory renal rejection in paediatric renal transplant patients. Lupus nephritis patients Standard dosage for induction therapy Adults: 750 mg to 1.5 g by mouth twice a day (a daily dose of up to 3 g) is recommended. Children: 600 mg/m2 by mouth twice a day, up to a maximum of 2 g daily, is recommended. Standard dosage for maintenance therapy Adults: 500 mg to 1 g by mouth twice a day is recommended. Children: 300 mg/m2 by mouth twice a day is recommended. Mycophenolate Mofetil should be used together with corticosteroids. Doses should be introduced gradually and adjusted according to the clinical response. Therapeutic drug monitoring can help avoid sub-therapeutic exposure (Cmin ≥3.0 mg/L or inter-dose AUC ≥35 h*mg/L).

Side Effects & Interactions

Side Effects

No side-effect data recorded yet.