Comparative Pharmacology
Head-to-head clinical analysis: CELLCEPT versus NEORAL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CELLCEPT versus NEORAL.
CELLCEPT vs NEORAL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Mycophenolate mofetil is a reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), inhibiting de novo purine synthesis in T and B lymphocytes, thereby suppressing lymphocyte proliferation.
Cyclosporine, the active ingredient in Neoral, is a calcineurin inhibitor. It binds to cyclophilin, forming a complex that inhibits calcineurin, thereby preventing dephosphorylation and nuclear translocation of NF-AT (nuclear factor of activated T-cells). This inhibits transcription of interleukin-2 and other cytokines, reducing T-cell activation and proliferation.
Oral: 1-2 g daily in two divided doses. Intravenous: 1-2 g daily in two divided doses as a 2-hour infusion.
Initial dose 10-15 mg/kg/day orally divided q12h, then taper by 5% weekly to maintenance of 3-5 mg/kg/day divided q12h. For psoriasis: 2.5 mg/kg/day orally divided q12h. For rheumatoid arthritis: 2.5-5 mg/kg/day orally divided q12h. Administer consistently with or without food.
None Documented
None Documented
Terminal elimination half-life of MPA is approximately 17.9 ± 6.5 hours in renal transplant patients. Clinical significance: dosing interval of 12 hours maintains therapeutic levels.
Terminal elimination half-life: 8.4 hours (range 6–24 hours) in healthy volunteers; prolonged in hepatic impairment (up to 20 hours).
Mycophenolic acid (MPA) is primarily excreted in urine as mycophenolic acid glucuronide (MPAG) (87% of dose); <1% excreted as unchanged MPA. Fecal excretion accounts for approximately 6% of dose.
Primarily biliary/fecal (94%): 94% of dose eliminated in feces via bile, 6% in urine (0.1% unchanged). Minimal renal elimination of parent drug.
Category C
Category C
Immunosuppressant
Immunosuppressant