Comparative Pharmacology
Head-to-head clinical analysis: MYCOPHENOLATE MOFETIL versus ZORTRESS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: MYCOPHENOLATE MOFETIL versus ZORTRESS.
MYCOPHENOLATE MOFETIL vs ZORTRESS
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Mycophenolate mofetil is a prodrug that is rapidly hydrolyzed to mycophenolic acid (MPA), a potent, selective, uncompetitive, and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), which inhibits the de novo pathway of guanosine nucleotide synthesis. This inhibition preferentially blocks proliferation of T- and B-lymphocytes, as they are critically dependent on this pathway, thereby suppressing cell-mediated immune responses and antibody formation.
Inhibits mammalian target of rapamycin (mTOR) by binding to FKBP-12, blocking cell cycle progression from G1 to S phase, thereby suppressing cytokine-driven T-cell proliferation.
1 g orally twice daily; intravenous infusion 1 g over 2 hours twice daily for up to 14 days.
1.5 mg orally twice daily, administered with cyclosporine and corticosteroids.
None Documented
None Documented
Clinical Note
moderateMycophenolate mofetil + Digitoxin
"Mycophenolate mofetil may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateMycophenolate mofetil + Deslanoside
"Mycophenolate mofetil may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateMycophenolate mofetil + Acetyldigitoxin
"Mycophenolate mofetil may decrease the cardiotoxic activities of Acetyldigitoxin."
Clinical Note
moderateMycophenolate mofetil + Ouabain
The terminal elimination half-life of mycophenolic acid (MPA) is approximately 8-16 hours in healthy volunteers and renal transplant patients. In patients with renal impairment, the half-life may be prolonged due to accumulation of MPAG. The half-life supports twice-daily dosing.
Terminal elimination half-life is approximately 10-15 hours in renal transplant patients. In de novo liver transplant patients, half-life is ~13 hours. The effective half-life supports twice-daily dosing.
Mycophenolate mofetil is extensively metabolized to mycophenolic acid (MPA), which is primarily eliminated in urine as MPA glucuronide (MPAG). Approximately 87% of the dose is excreted in urine as MPAG, with less than 1% as unchanged MPA. Fecal excretion accounts for about 6% of the dose, mainly as MPAG. Biliary excretion contributes to enterohepatic recirculation of MPA, enhancing its exposure.
Primarily fecal (~78%) with <2.5% excreted unchanged in urine. Small amount via biliary elimination.
Category D/X
Category C
Immunosuppressant
Immunosuppressant
"Mycophenolate mofetil may decrease the cardiotoxic activities of Ouabain."