Mycophenolate

Mycophenolate is an immunosuppressive agent used to prevent your body from rejecting a kidney, liver, or hear transplant. Mycophenolate is usually given with cyclosporine (Sandimmune, Neoral) and a steroid medication.

Mycophenolate is available under the following different brand names: CellCept, Myfortic, and MMF.

Dosage Forms and Strengths

Capsule

• 250 mg

Tablet

• 500 mg

Oral suspension

• 200 mg/mL

Powder for injection (adult only)

• 500 mg/mL

Tablet, delayed release

• 180 mg
• 360 mg

Dosage Considerations – Should be Given as Follows:

Kidney Transplant

Prophylaxis of organ rejection in patients receiving allogeneic renal transplants; use concomitantly with cyclosporine and corticosteroids

Adults:

• Mycophenolate mofetil (MMF): 1 g orally/intravenously every 12 hours, infused over 2 hours or more
• Mycophenolic acid (MPA): 720 mg orally every 12 hours

Pediatric:

Children under 3 months

• Safety and efficacy not established

Children over 3 monthsChildren over 3 months

• Prophylaxis of organ rejection in patients receiving allogeneic renal transplants
• MMF (suspension): 600 mg/m² orally every 12 hours; not to exceed 2 g/day
• MMF: BSA 1.25-1.5 m²: 750 mg capsule orally every 12 hours
• MMF: BSA greater than 1.5 m²: 1 g capsule/tablet orally every 12 hours
• Extended-release MPA: 400 mg/m² orally every 12 hours; not to exceed 720 mg every 12 hours

Heart Transplant

• Prophylaxis of organ rejection in patients receiving allogeneic cardiac transplants; use concomitantly with cyclosporine and corticosteroids
• MMF: 1.5 g oral/intravenous every 12 hours, infused over 2 hours or more

Liver Transplant

• Prophylaxis of organ rejection in patients receiving allogeneic hepatic transplants; use concomitantly with cyclosporine and corticosteroids
• MMF intravenous (IV): 1 g every 12 hours; infused over 2 hours or more
• MMF (oral): 1.5 g every 12 hours

Dosing Considerations

Renal Impairment

• MMF: In severe renal impairment (glomerular filtration rate [GFR] less than 25 mL/minute/1.73 m²), not to exceed 1 g every 12 hours
• No dosage adjustment needed in renal transplant patients experiencing delayed graft function postoperatively

Lupus Nephritis (Off-label)

• Induction therapy for lupus nephritis (MMF)
• Induction: 1 g orally every 12 hours with a glucocorticoid or 2-3 g for 6 months with glucocorticoids
• Maintenance: 0.5-3 g/day or 1 g orally every 12 hours or 1-2 g daily
• Administer with initial intravenous (IV) corticosteroid pulse for 3 days, then prednisone 0.5-1 mg/kg/day orally; not to exceed 10 mg/day; after a few weeks, prednisone may be tapered to lowest effective dose

Common side effects of mycophenolate include:

• High blood sugar (hyperglycemia)
• High cholesterol (hypercholesterolemia)
• Low blood magnesium (hypomagnesemia)
• Shortness of breath
• Back pain
• Increased blood urea nitrogen (BUN)
• Low white blood cell count (leukopenia, neutropenia)
• Excess fluid around the lungs
• Urinary tract infection (UTI)
• Increasing frequency of cough
• Low blood calcium (hypocalcemia)
• High blood pressure (hypertension)
• Abdominal/stomach pain or upset
• Swelling of extremities
• Anemia
• Fever
• Nausea
• High blood potassium (hyperkalemia)
• Diarrhea
• Infection
• Headache
• Melanoma
• Other malignancies
• Lymphoma
• Opportunistic infection (including herpes)
• Gastrointestinal bleeding
• Pulmonary fibrosis
• Progressive multifocal leukoencephalopathy
• Constipation
• Vomiting
• Stomach pain or upset
• Gas
• Tremor
• Trouble sleeping (insomnia)
• Numbness or tingly feeling
• Anxiety

Serious side effects of mycophenolate include

• Unusual tiredness
• Fast or irregular heartbeat
• Muscle weakness
• Easy bleeding or bruising
• Swelling of the feet or ankles
• Mental/mood changes
• Weakness on one side of the body
• Unusual change in the amount of urine

Postmarketing side effects of mycophenolate reported include:

• BK virus-associated nephropathy
• Congenital malformations, including ear, facial, cardiac and nervous system malformations and an increased incidence of first trimester pregnancy
• Colitis (sometimes caused by cytomegalovirus), pancreatitis, isolated cases of intestinal villous atrophy
• Cases of pure red cell aplasia (PRCA) and hypogammaglobulinemia reported when administered in combination with other immunosuppressive agents

This is not a complete list of side effects and other serious side effects may occur. Call your doctor for information and medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

If your doctor has directed you to use this medication for your condition, your doctor or pharmacist may already be aware of any possible drug interactions or side effects and may be monitoring you for them. Do not start, stop, or change the dosage of this medicine or any medicine before getting further information from your doctor, healthcare provider or pharmacist first.

• Severe Interactions of mycophenolate include:
  • cholestyramine
  • colestipol
• Mycophenolate has serious interactions with at least 83 different drugs.
• Mycophenolate has moderate interactions with at least 125 different drugs.
• Mild interactions of mycophenolate include:
  • bazedoxifene/conjugated estrogens
  • conjugated estrogens
  • conjugated estrogens, vaginal
  • estradiol
  • estrogens conjugated synthetic
  • estrogens esterified
  • estropipate
  • mestranol

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

Warnings

Increased susceptibility to infection as consequence of immunosuppression.

Drug should be prescribed only by healthcare providers experienced in immunosuppressive therapy and management of renal, cardiac, or hepatic transplant patients.

Patients receiving drug should be managed in facilities equipped and staffed with adequate laboratory and supportive medical resources.

Drug increases risk of developing lymphoma and risk of skin malignancy.

Myfortic and CellCept dosage form absorbed differently; not for use interchangeably.

Healthcare provider responsible for maintenance therapy should have all information required for follow-up.

Risk of first-trimester miscarriage and congenital malformations; after negative pregnancy test and follow-up, women of child-bearing age should use 2 forms of reliable contraception (hormone plus barrier) during entire course of mycophenolate therapy and continue until 6 weeks after drug discontinuation.

This medication contains mycophenolate. Do not take CellCept, Myfortic, or MMF if you are allergic to mycophenolate or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Hypersensitivity
• Intravenous (IV) formulation (CellCept) in patients allergic to polysorbate 80

Effects of Drug Abuse

• No information available

Short-Term Effects

• See "What Are Side Effects Associated with Using Mycophenolate?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Mycophenolate?"

Cautions

Pure red-cell aplasia reported in patients treated with MMF or MPA in combination with other immunosuppressive agents.

Avoid use in hypoxanthine-guanine phosphoribosyltransferase (HGPRT) deficiency (Lesch-Nyhan, Kelley-Seegmiller syndrome).

Risk of miscarriage and congenital malformations, especially external ear and other facial abnormalities including cleft lip and palate, and anomalies of the distal limbs, heart, esophagus, kidney and nervous system (see Warnings).

MMF oral suspension contains aspartame.

MPA not indicated for hepatic or cardiac transplants.

Use may be rarely associated with gastric or duodenal ulcers, gastrointestinal (GI) bleeding and/or perforation.

Safety and effectiveness of MPA for de novo pediatric renal transplant not established.

Neutropenia may occur (may require dose reduction).

Must not be administered by rapid or bolus intravenous (IV) injection.

Toxicity may increase in renal impairment; use caution.

Serious infections and viral reactivation:

• Increased risk of developing bacterial, fungal, protozoal, and new or reactivated viral infections, including opportunistic infections
• Because of danger of oversuppression of immune system, which can increase susceptibility to infection, combination immunosuppressant therapy should be used with caution
• May increase risk of new or reactivated viral infections, including polyomavirus-associated nephropathy (PVAN), JC virus-associated progressive multifocal leukoencephalopathy (PML), cytomegalovirus (CMV) infections, and reactivation of hepatitis B or C
• PVAN, especially when due to BK virus infection, is associated with serious outcomes, including deteriorating renal function and renal graft loss
• PML, which is sometimes fatal, typically presents with hemiparesis, apathy, confusion, cognitive deficiencies, and ataxia

Pregnancy and Lactation

• Use mycophenolate during pregnancy only in LIFE-THREATENING emergencies when no safer drug is available. There is positive evidence of human fetal risk.
• Mycophenolate can cause fetal harm when administered to pregnant females. Use of MMF during pregnancy is associated with an increased risk of first trimester pregnancy loss and increased risk of congenital malformations, especially external ear and other facial abnormalities including cleft lip and palate, and anomalies of distal limbs, heart, esophagus, kidney and nervous system.
• It is unknown whether mycophenolate is excreted in breast milk; avoid using mycophenolate, or do not nurse.