Comparative Pharmacology
Head-to-head clinical analysis: ASTAGRAF XL versus MYCOPHENOLATE MOFETIL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ASTAGRAF XL versus MYCOPHENOLATE MOFETIL.
ASTAGRAF XL vs MYCOPHENOLATE MOFETIL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Calcineurin inhibitor that binds to FKBP-12, forming a complex that inhibits calcineurin, thereby preventing dephosphorylation and nuclear translocation of NFAT, which reduces T-cell activation and cytokine production (e.g., IL-2).
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.
Initial oral dose of 0.1-0.15 mg/kg/day divided every 12 hours, with subsequent adjustments based on trough levels. Typical maintenance dose 0.05-0.15 mg/kg/day.
1 g orally twice daily; intravenous infusion 1 g over 2 hours twice daily for up to 14 days.
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
Terminal elimination half-life is approximately 43 hours (range 15.8–68.6 hours) in adult kidney transplant recipients. This long half-life supports once-daily dosing. In liver transplant patients, half-life ranges from 12 to 42 hours.
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.
Primarily fecal (94.6%) via biliary elimination. Renal excretion accounts for approximately 2.4% of the dose, mainly as metabolites. Less than 1% is excreted unchanged in urine.
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.
Category C
Category D/X
Immunosuppressant, Calcineurin Inhibitor
Immunosuppressant
"Mycophenolate mofetil may decrease the cardiotoxic activities of Ouabain."