Mycophenolate Mofetil (Cellcept) and Mycophenolate Sodium (Myfortic) are strong immunomodulatory drugs that are used primarily in the treatment of transplant patients to prevent and treat rejection. It is also used in autoimmune conditions like systemic lupus erythematosus, autoimmune hepatitis, and inflammatory bowel diseases.

Mycophenolate mofetil and mycophenolate sodium Use:

• Organ transplantation:

  • Utilised in patients obtaining allogeneic renal (CellCept [mycophenolate mofetil], Myfortic [enteric-coated mycophenolate sodium]), cardiac (CellCept), or liver (CellCept) transplants as prophylactic agent against organ rejection.

Note: It is mostly combined with cyclosporine but preferred to be used combined with tacrolimus and occasionally with a mammalian goal of rapamycin inhibitor (everolimus or sirolimus).

• Myfortic can also be used to avoid organ rejection in patients getting cardiac and hepatic transplantations though not labeled for these transplantations.

• Off Label Use of Mycophenolate mofetil and mycophenolate sodium in Adults:

  • Acute graft-versus-host disease, refractory (treatment)
  • Autoimmune hepatitis (first-line agent)
  • Autoimmune hepatitis (refractory)
  • Chronic graft-versus-host disease, refractory (treatment)
  • Prevention of Graft-versus-host disease
  • Lung transplant (prevention of bronchiolitis obliterans syndrome)
  • Lung transplant (for the prevention of rejection)
  • Lupus nephritis
  • Myasthenia gravis
  • Psoriasis (moderate to severe)
  • Systemic sclerosis (scleroderma)

Mycophenolate mofetil and mycophenolate sodium dose in adults:

Note:

• Mycophenolate mofetil (CellCept) and enteric-coated mycophenolate sodium (Myfortic) are not equivalent.
• Conversion to equimolar doses is required.
• Myfortic 180 mg is considered equivalent to CellCept 250 mg.

Mycophenolate Dose in the treatment of Autoimmune hepatitis (off-label):

• CellCept: Oral:
  • Initiate with 500 mg two times a day for 3 weeks;
  • The dose is slowly increased to 1.5 to 2 g/day initially in combination with steroids;
  • In clinical trials, mycophenolate was continued for up to two years after a complete response.

Mycophenolate Dose in the treatment of refractory autoimmune hepatitis (off-label):

• CellCept:
• 2 g/day given orally in divided doses (combined with steroids and a calcineurin inhibitor).

Mycophenolate dose in Cardiac transplantation:

Oral:

• CellCept:
  • Initial: 1.5 g two times a day in addition to cyclosporine and steroids or 1 g two times a day in addition to other immunosuppressants (tacrolimus, everolimus, or sirolimus) and at first with corticosteroids.
• Myfortic (off-label use):
  • Initial: 1.08 g two times a day in addition to cyclosporine and initially with steroids.
  • Although data do not exist for combination with tacrolimus, everolimus, or sirolimus, use of lower equimolar doses (eg, 720 mg twice daily) to mycophenolate mofetil may be appropriate when used with these other immunosuppressants; higher maintenance doses of 1.08 g twice each day may be needed in some patients.

IV:

• CellCept: See oral dosing for CellCept; IV and oral doses (of mycophenolate mofetil) are equivalent.
• If converting from Myfortic to IV CellCept, convert Myfortic to equivalent CellCept oral dose first. Converting to oral therapy as soon as bearable.

Mycophenolate Dose in Liver transplantation:

Oral:

• • CellCept:
    • Initial: 1.5 g two times a day when used with cyclosporine or 1 g two times a day when used with another immunosuppressant (eg, tacrolimus).
    • Maintenance dosages differ based on concomitant immunosuppression.
  • Myfortic (off-label use):
    • 360 mg to 720 mg two times a day in combination with other immunosuppressants.
    • Higher maintenance doses of 1.08 g two times daily may be needed in some patients.

Mycophenolate Dose in the prevention of rejection and bronchiolitis obliterans syndrome in patients after Lung transplantation (off-label):

Oral:

• • CellCept:
    • Initial: 1.5 g two times daily when used in combination with cyclosporine and initially with corticosteroids or 1 g two times daily when used with other immunosuppressants (eg, tacrolimus) and primarily with corticosteroids.
    • Higher maintenance doses of 1.5 g two times each day may be needed in some patients.
  • Myfortic:
    • Initial: 1.08 g two times daily with cyclosporine and initially with corticosteroids.
    • Although data do not exist for combination with tacrolimus, everolimus, or sirolimus, usage of lower equimolar doses (eg, 720 mg twice daily) to mycophenolate mofetil may be suitable when used with these other immunosuppressants.
    • Higher maintenance doses of 1.08 g twice daily may be necessary for some patients.
• IV and oral doses (of mycophenolate mofetil) are equivalent. If converting from Myfortic to IV CellCept, change Myfortic to equivalent CellCept oral dose first. Converting to oral therapy as soon as endured.

Mycophenolate dose in the treatment of Lupus nephritis (off-label): CellCept: Oral:

• Induction:
  • 1000 mg two times a day for 6 months with a glucocorticoid or 2 to 3 g daily for 6 months with glucocorticoids.
• Maintenance:
  • 0.5 to 3 g on daily basis or 1 g two times a day or 1 to 2 g each day.

Mycophenolate Dose in the treatment of Myasthenia gravis (off-label):

• Patients who remain significantly symptomatic on pyridostigmine: CellCept:

  • Oral:
    • Initial: 500 mg two times a day;
    • Increase the dose depending on the response and endurance to a maintenance dose of 1 g to 1.5 g twice on daily basis.
    • The treatment may be added as monotherapy or in conjunction with glucocorticoids and/or pyridostigmine.
    • The onset of clinical response to mycophenolate may take up to 6 to 12 months, with a maximum effect not apparent until 1 to 2 years.

Mycophenolate Dose in the treatment of moderate to severe Psoriasis, (off-label): CellCept:

• Oral: 2 to 3 g daily.

Mycophenolate Dose in Renal transplantation:

Oral:

• CellCept:
  • Initial: 1 g two times a day.
  • The maintenance dose may vary based on concomitant immunosuppression.
  • Doses exceeding 2 g/day have been associated with an increased incidence of adverse effects but may be necessary for some patients.
• Myfortic:
  • Initial: 720 mg two times daily.
  • The maintenance doses may vary based on concomitant immunosuppression.

IV:

• CellCept: See oral dosing for CellCept; IV and oral doses (of mycophenolate mofetil) are equivalent. If converting from Myfortic to IV CellCept, convert Myfortic to equivalent
• CellCept oral dose first. Convert to oral therapy as soon as tolerated.

Mycophenolate Dose in the treatment of Systemic sclerosis (scleroderma) (off-label):

• CellCept: Oral:
  • Initial: 500 mg two times a day for 1 to 4 weeks;
  • Increase the dose to a maintenance dose of 500 to 1,500 mg twice daily as endured.
• Myfortic: Oral:
  • Initial: 360 mg twice a day for 1 week, after that 720 mg twice a day.

Mycophenolate dose in the treatment of noninfectious Uveitis (off-label use): 

• CellCept: Oral:
  • Initial: 500 mg two times a day for 14 days. The dose may be increased to a maintenance dose of 1.5 g two times a day as tolerated or
  • Initial: 500 mg two times a day for 14 days. The dose may be increased to a maintenance dose of 1000 mg two times a day as tolerated or 
  • 500 mg to 2 g/day in divided doses. Refer to protocols for further details

Mycophenolate mofetil and mycophenolate sodium dose in childrens:

Note: The IV formulation may be used for up to 14 days; convert to oral therapy as soon as tolerated. Mycophenolate mofetil (CellCept) tablets, capsules, and termination should not be interchanged with the delayed-release tablet formulation (Myfortic) due to differences in the rate of absorption. Consult institution-specific protocols.

Mycophenolate Dose in the Kidney transplantation:

• Mycophenolate mofetil (CellCept):

  • Infants ≥3 months, Children, and Adolescents:

  • Oral:
    • Suspension:
      • 600 mg/m²/dose twice daily;
      • The maximum daily dose is 2,000 mg/day.
    • Tablets or capsules:
      • BSA 1.25 m² to 1.5 m²: 750 mg twice daily.
      • BSA ≥1.5 m²: 1,000 mg twice daily.

• Mycophenolate sodium delayed-release tablets (Myfortic):

  • Children ≥5 years and Adolescents:
    • 400 mg/m²/dose twice daily;
    • The maximum daily dose: 1,440 mg/day;
    • Avoid partial tablet doses by rounding doses to the nearest whole tablet size as follows:
    • BSA <1.19 m²: Use of this formulation is not advised.
    • BSA 1.19 to 1.58 m²: 540 mg twice a day.
    • BSA >1.58 m²: 720 mg two times a day.

Note: Mycophenolate sodium delayed-release 720 mg two times a day was shown to be bioequivalent to mycophenolate mofetil 1,000 mg twice a day.

Mycophenolate Dose in the treatment of Lupus nephritis: Limited data available:

• Mycophenolate mofetil (CellCept): Children and Adolescents: Oral:

  • BSA-based dosing:

    • Induction and Maintenance:
      • 300 to 600 mg/m²/dose twice a day;
      • The maximum daily dose: 3,000 mg/day.

Mycophenolate Dose in the treatment of Nephrotic syndrome: Limited data available:

• Mycophenolate mofetil (CellCept): Children and Adolescents: Oral:

  • Frequently relapsing:

    • BSA-based dosing:
      • 600 mg/m²/dose twice daily for at least 12 months;
      • The maximum daily dose: 2,000 mg/day.
    • Weight-based dosing:
      • 5 to 18 mg/kg/dose twice daily;
      • The maximum daily dose: 2,000 mg/day for 1 to 2 years with a tapering dose of prednisone.

  • Steroid-dependent (for steroid-sparing effect):

    • BSA-based dosing:
      • 600 mg/m²/dose twice daily for at least 12 months;
      • The maximum daily dose: 2,000 mg/day.
    • Weight-based dosing:
      • 12 to 18 mg/kg/dose twice daily;
      • The maximum daily dose: 2,000 mg/day.

Dosing adjustment for toxicity:

• Hematologic:

  • If the ANC falls below 1.3 x 10 /μL or anemia develops, the dose should be reduced or the treatment should be withheld.

Pregnancy Risk Factor D

• [US Boxed Warning] Use during pregnancy can increase the risk of congenital malformations and first-trimester abortion loss.
• If safe treatments are not available, avoid them.
• It is important to educate females with reproductive potential about planning and prevention of pregnancy.
• Following exposure during pregnancy, the following congenital malformations were reported: External ear abnormalities and cleft lips and palate, cleft lip, and palate, anomalies in the distal limbs and heart, esophagus and kidney disorders, and nervous system problems.
• Mycophenolate embryopathy is a combination of the abnormalities in the eye, ear, and lip/palate has been described.
• Reports of miscarriage in the first trimester have also been made.
• Before mycophenolate therapy, females with reproductive potential (girls entering puberty or women who have not experienced clinically-established menopause) should have a negative pregnancy testing with a sensitivity >=25mL. The test should be repeated eight to ten days later.
• During follow-up visits, pregnant tests should be performed again.
• During treatment, and for six weeks following the end of therapy, it is important to use appropriate methods of contraception.
• Mycophenolate may affect the efficacy hormonal contraceptive agents.
• Effective contraception should be used by sexually active male patients and/or female partners during treatment. It should also be used for at least three months after the last dose.
• Current guidelines recommend that pregnancy should be postponed after one year without any acute rejection. This period could be modified if clinically necessary.
• Women who plan to have a baby and are currently taking mycophenolate after a kidney transplant need to switch to another medication. Mycophenolate should also be discontinued for at least six weeks before they attempt to have a child.
• Pregnant women should not use mycophenolate for psoriasis treatment.
• Women with Lupus Nephritis should not consume mycophenolate during pregnancy. If they become pregnant while on mycophenolate treatment, they should switch to another medication.
• Mycophenolate should be stopped at least six weeks before trying to conceive for women suffering from lupus, such as those who have used mycophenolate.
• American health care providers should notify the Mycophenolate Pregnancy Register (800-617-8191) if female mycophenolate exposure occurs during pregnancy.
• Transplant Pregnancy Register International (TPR), is a registry that tracks pregnancies in male transplant recipients and mothers of those recipients.
• The TPR encourages reporting of pregnancies following solid organ transplant by contacting them at 1-877955-6877 or https://www.transplantpregnancyregistry.org.

Use of mycophenolate mofetil or mycophenolate salt during breastfeeding

• Mycophenolate levels in human milk are not known.
• The manufacturer suggests that the mother decide whether to stop breastfeeding or discontinue the drug treatment due to the potential for serious adverse reactions in breastfed babies. This decision should be made taking into consideration the importance of the mother's treatment.

Mycophenolate Dose in Kidney Disease:

Note: Patients should be carefully monitored for concentration-reliant undesirable effects as renal dysfunction may lead to reduced excretion.

• Renal transplant:

  • GFR <25 mL/minute/1.73 m² in patients outside the immediate post-transplant period:
    • CellCept: Doses exceeding 1000 mg administered two times each day should be prevented; no dose modifications are needed in renal transplant patients experiencing delayed graft function postoperatively.
    • Myfortic: No dose modifications are required in renal transplant patients experiencing delayed graft function postoperatively.
  • Cardiac, lung, pancreas, or liver transplant:
    • No data available; according to the company, mycophenolate may be used in cardiac or hepatic transplant patients with acute chronic renal impairment if the potential benefit outweighs the potential risk.
  • Autoimmune disease (off-label use):
    • There have been no exact dosage adjustments identified, although the use of lower doses may be necessary.
    • Mycophenolic acid (MPA) exposure seems to be contrariwise related to renal function; monitor closely for efficacy and adverse effects, especially in patients with end-stage renal disease.
  • Hemodialysis:
    • Not removed; supplemental dose is not necessary.
  • Peritoneal dialysis:
    • Decreased mycophenolic acid (MPA) and mycophenolic acid glucuronide (MPAG) AUC values have been seen, however, there are no dosing recommendations. Consider monitoring AUC.

Mycophenolate Dose in Liver disease:

• No dosage correction is advised for renal patients with acute hepatic parenchymal disease; however, it is not presently known if dosage alterations are necessary for hepatic disease with other aetiologies.
• Expanded monitoring may be required in patients with hyperbilirubinemia and/or hypoalbuminemia; displacement or decreased number of binding sites may occur resulting in an increased concentration of MPA/MPAG free fraction.

Occurrences include concomitant use with cyclosporine and corticosteroids. In general, lower doses used in renal rejection patients had fewer undesirable effects than higher doses. Rates of adverse effects were similar for every indication, excepting those distinctive to the specific organ involved.

Common Side Effects of Mycophenolate mofetil and mycophenolate sodium:

• Cardiovascular:

  • Hypertension
  • Edema
  • Hypotension
  • Tachycardia
  • Lower Extremity Edema

• Central Nervous System:

  • Pain
  • Headache
  • Insomnia
  • Dizziness
  • Depression
  • Chills
  • Confusion
  • Drowsiness
  • Hypertonia
  • Malaise
  • Myasthenia
  • Paresthesia

• Dermatologic:

  • Skin Rash
  • Ecchymoses
  • Cellulitis

• Endocrine & Metabolic:

  • Hyperglycemia
  • Hypercholesterolemia
  • Hypomagnesemia
  • Hypokalemia
  • Hypocalcemia
  • Increased Lactate Dehydrogenase
  • Hyperkalemia
  • Acidosis
  • Weight Loss
  • Hyperuricemia
  • Hyperlipidemia
  • Hypophosphatemia

• Gastrointestinal:

  • Abdominal Pain
  • Nausea
  • Diarrhea
  • Constipation
  • Vomiting
  • Decreased Appetite
  • Dyspepsia
  • Esophagitis
  • Gastric Ulcer
  • Gastritis
  • Gastrointestinal Hemorrhage
  • Hernia Of Abdominal Cavity
  • Intestinal Obstruction
  • Stomatitis
  • Upper Abdominal Pain
  • Flatulence

• Genitourinary:

  • Urinary Tract Infection
  • Hematuria

• Hematologic & Oncologic:

  • Leukopenia
  • Anemia
  • Leukocytosis
  • Thrombocytopenia
  • Benign Skin Neoplasm
  • Disorder Of Hemostatic Components Of Blood
  • Neoplasm
  • Pancytopenia
  • Skin Carcinoma

• Hepatic:

  • Increased Liver Enzymes
  • Hepatitis
  • Increased Serum Alkaline Phosphatase

• Infection:

  • Bacterial Infection
  • Viral Infection
  • Cytomegalovirus Disease
  • Fungal Infection

• Neuromuscular & Skeletal:

  • Asthenia
  • Tremor
  • Back Pain
  • Arthralgia

• Renal:

  • Increased Serum Creatinine
  • Increased Blood Urea Nitrogen

• Respiratory:

  • Dyspnea
  • Cough
  • Pleural Effusion

• Miscellaneous:

  • Fever

Less Common Side Effects of Mycophenolate mofetil and mycophenolate sodium:

• Cardiovascular:

  • Exacerbation Of Hypertension
  • Peripheral Edema
  • Phlebitis
  • Thrombosis

• Central Nervous System:

  • Anxiety
  • Fatigue

• Dermatologic:

  • Acne Vulgaris
  • Pruritus

• Endocrine & Metabolic:

  • Diabetes Mellitus

• Gastrointestinal:

  • Abdominal Distension
  • Gastroesophageal Reflux Disease
  • Gingival Hyperplasia
  • Oral Candidiasis

• Genitourinary:

  • Urinary Retention

• Hematologic & Oncologic:

  • Lymphocele
  • Severe Neutropenia
  • Malignant Neoplasm
  • Malignant Lymphoma
  • Lymphoproliferative Disorder

• Hepatic:

  • Abnormal Hepatic Function Tests

• Infection:

  • Influenza
  • Wound Infection
  • Herpes Simplex Infection
  • Herpes Zoster Infection
  • Sepsis

• Neuromuscular & Skeletal:

  • Muscle Cramps
  • Myalgia
  • Peripheral Pain

• Ophthalmic:

  • Blurred Vision

• Renal:

  • Renal Insufficiency
  • Renal Tubular Necrosis

• Respiratory:

  • Dyspnea On Exertion
  • Nasopharyngitis
  • Pneumonia
  • Sinusitis
  • Upper Respiratory Tract Infection

Frequency of side effects not defined:

• Gastrointestinal:

  • Mucocutaneous Candidiasis

• Infection:

  • Protozoal Infection

• Respiratory:

  • Pharyngitis
  • Respiratory Tract Infection

Contraindications to Mycophenolate mofetil and mycophenolate sodium:

• Hypersensitivity to mycophenolate mofetil or mycophenolic acid, mycophenolate salt, or any other element of the formulation
• CellCept: Patients who are allergic to polysorbate80 should not receive intravenous injections.
• Canadian labeling: Additional contraindications not in the US labeling
  • Pregnancy;
  • Women with childbearing potential who are not using effective contraceptive methods.
  • Women with childbearing potential should not provide a pregnancy test results;
  • Breastfeeding

Warnings and precautions

• CNS depression:
  • CNS depression may be possible, which could impair mental or physical abilities. Patients should be aware that driving, operating machinery and other tasks that require mental alertness can put patients at risk.

• Infections [US Boxed Warning]

  • Immunosuppressant therapy can increase the risk of protozoal, viral, and bacterial infections. This includes opportunistic and viral reactivation of Hepatitis B/C.Infections can be serious and even fatal.
  • Combination immunosuppressant therapy should not be used as it may cause over-suppression of the immune system. This can increase susceptibility for infection.

• Viral infections that are new or reactivated:

  • Polyomavirus-associated nephropathy (PVAN), JC virus-associated progressive multifocal leukoencephalopathy (PML), cytomegalovirus (CMV) infections, and reactivation of hepatitis B (HBV) or hepatitis C (HCV) have been related with use.
  • Patients with new or reactivated viruses should consider a decrease in immunosuppression.
  • However, transplant recipients should consider the possibility that decreased immunosuppression could affect the functioning of the graft.
  • PVAN can be caused by activation of BK virus. This may cause deterioration in renal function and/or loss of renal grafts.
  • PML is a potentially fatal condition that can cause confusion, ataxia and cognitive deficiencies.
  • Treatment with immunosuppressants or immune function impairment can increase the risk of developing PML.
  • Patients with neurological symptoms who are receiving immunosuppressants should consult a neurologist.
  • CMV viremia and disease are more likely in transplant recipients CMV-negative at the time they receive a transplant graft from CMV seropositive donors.
  • However, there are routine advancements that can be made to limit CMV.
  • Patients infected by HBV/HCV may experience viral reactivation. These patients should be evaluated for any signs of HBV/HCV.

• Lymphoproliferative disorders: [US Boxed Warning]:

  • There is an increased risk of developing lymphoma or skin malignancy.
  • The intensity and duration of therapy are factors that increase the risk of malignancies.
  • Patients must be monitored and instructed to limit exposure to UV light/sunlight to reduce the risk of developing skin cancer. Supportive treatment should also be given if necessary.
  • EBV infection can cause post-transplant lymphoproliferative disorders in patients with immunosuppression.
  • This is most common in patients who have received transplants from immune-suppressed organs.

• Neutropenia:

  • There is a possibility of severe neutropenia (neutropenia) that may require dose reductions or interruptions (risk greater than day 31-180 after transplant).

• Pure red cell aplasia

  • PRCA, a type of anemia that can vary from subclinical to acute, has been reported in patients getting mycophenolate concomitantly with other immunosuppressive agents (eg, tacrolimus, cyclosporine, corticosteroids).
  • You may feel fatigue, lethargy or pallor.
  • Although it is not known exactly, immunosuppression or treatment with immunosuppressant therapies may be risk factors in the development of PRCA.
  • PRCA can be reversed by reducing or terminating immunosuppressive therapy.
  • However, transplant recipients should consider the risks of lower immunosuppression and rejection.

• Gastrointestinal disorders:

  • It is possible to use this product with gastric, duodenal, or GI ulcers and/or perforation.
  • Patients with active serious digestive problems should be vigilant; patients with active ulcers were not included in the clinical trials.
  • Myfortic was designed to reduce GI side effect.
  • However, studies have shown similar rates of GI side affects between Mycophenolate mofetil (and the enteric coated formulation).

• Hypoxanthine-guanine phosphoribosyltransferase deficiency:

  • Ideally, use must be prevented in patients with the rare hereditary deficiency of hypoxanthine-guanine phosphoribosyltransferase (such as Lesch-Nyhan or Kelley-Seegmiller syndrome).

• Renal impairment

  • Patients with severe renal impairment should be cautious. Toxicity may increase. Dosage adjustment may be necessary.

Mycophenolate mofetil (Cellcept) and mycophenolate sodium (Myfortic): Drug Interaction

Monitoring parameters:

• Complete blood count (weekly for the first month, twice a month during months 2 and 3, then monthly afterward through the first year);
• renal and liver function;
• signs and symptoms of organ rejection;
• signs and symptoms of bacterial, fungal, protozoal, new or reactivated viral, or opportunistic infections;
• neurological symptoms (eg, hemiparesis, confusion, cognitive deficiencies, ataxia) suggestive of PML, pregnancy test (sensitivity of ≥25 milliunits/mL;
• immediately prior to initiation and 8 to 10 days later in females of gestation potential, followed by repeat tests during therapy);
• monitor skin (for lesions suspicious of skin cancer);
• monitor for signs of lymphoma;
• monitor for signs of pure red cell aplasia or autoimmune hemolytic anemia.

How to administer Mycophenolate mofetil and mycophenolate sodium?

Oral:

• May be directed with or without food as effects of food on bioavailability are minimal.
• Oral suspension may be administered via a nasogastric tube (minimum 8 French, 1.7 mm interior diameter);
• The oral suspensions should not be mixed with other medications.
• Delayed-release tablets (Myfortic) should be swallowed whole and should not be crushed, cut, or chewed.
• If a dose is missed, administer as soon as possible.
• If it is close to the next scheduled dose, skip the missed dose and resume at the next regularly scheduled time; do not double a dose to make up for a missed dose.

IV:

• Intravenous solutions should be administered over at least 2 hours (either peripheral or central vein);
• Do not administer intravenous solution by rapid or bolus injection.

Mechanism of action of Mycophenolate mofetil and mycophenolate sodium:

MPA has a cytostatic action on both T and B lymphocytes. It inhibits inosine monophosphate hydrogenase (IMPDH), which is responsible for de novo guanosine synthesis. This pathway is essential for T and B lymphocyte proliferation.

Onset of action:

• Peak effect: The relationship between toxicity and efficacy is still being explored. However, one study found that AUCs of >40 mcg/mL/hour in 12-hour intervals were associated with efficiency and fewer episodes of rejection.

Absorption:

• Rapid and large; mycophenolic (MPA) AUC values for the early post-transplant period are lower (45% to 53%) than those of the later period (>3 month) in adults and pediatric patients.
  • Oral: Myfortic 93%

Protein binding:

• MPA: 97%, MPA 82%

Metabolism:

• Hepatic and via GI tract
• CellCept is fully hydrolyzed by the liver to mycophenolic (MPA) active metabolite; enterohepatic circulation of MPA might occur.
• MPA (inactive metabolite), is glucuronidated with MPAG (MPA).

Bioavailability:

• Oral: CellCept 94% (oral and relative to IV MMF);
• MPA concentration is a result of enterohepatic circulation
• Two 500 mg tablets were found to be bioequivalent in size to four 250 mg capsules, or 1,000 mg of oral suspension.
• Myfortic: 72%

Half-life elimination:

• CellCept: MPA:
  • Oral: 17.9 ± 6.5 hours;
  • IV: 16.6 ± 5.8 hours
• Myfortic: MPA:
  • Oral: 8 to 16 hours;
  • MPAG: 13 to 17 hours

Time to peak plasma: Oral: MPA:

• CellCept: 1 to 1.5 hours
• Myfortic: 1.5 to 2.75 hours

Excretion:

• CellCept:
  • MPA: Urine (<1%), feces (6%);
  • MPAG: Urine (87%)
• Myfortic:
  • MPA: Urine (3%), feces;
  • MPAG: Urine (>60%)

International Brand of Mycophenolate mofetil and mycophenolate sodium:

• CellCept
• CellCept Intravenous
• Myfortic
• ACH-Mycophenolate
• APO-Mycophenolate
• APO-Mycophenolic Acid
• CellCept
• CellCept IV
• CO Mycophenolate
• JAMP-Mycophenolate
• Myfortic
• MYLAN-Mycophenolate
• SANDOZ Mycophenolate Mofetil
• TEVA-Mycophenolate
• VAN-Mycophenolate
• Accempa
• Accocept
• Celguard
• Cellcept
• CellCept
• Cellmune
• Ceptolate
• Graftcept
• Imoxgen
• Imulate
• Kamyfet
• Linfonex
• Micocept
• Micoflavin
• Mofetab
• Mofetyl
• Mofilet
• Mowel
• Myclausen
• Mycofit
• Mycokem
• Mycolat
• Mycopen
• Mycotil
• Myfenax
• Myfortic
• Myora
• Myotec
• Nuodun
• Phenocept
• Suprimun
• Transfonex
• Unorem

Mycophenolate mofetil and mycophenolate sodium Brand Names in Pakistan:

• Cellcept 500 mg Tablets (Roche Pharmaceuticals)
• Myofortic 180 mg Tablets (Novartis Pharmaceuticals)
• Mygraf 500 mg Tablets (Platinum Pharmaceuticals)
• Mycolate 500 mg Tablets (CCL Pharmaceuticals)