Comparative Pharmacology
Head-to-head clinical analysis: NEORAL versus ZORTRESS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NEORAL versus ZORTRESS.
NEORAL vs ZORTRESS
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
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.
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.
1.5 mg orally twice daily, administered with cyclosporine and corticosteroids.
None Documented
None Documented
Terminal elimination half-life: 8.4 hours (range 6–24 hours) in healthy volunteers; prolonged in hepatic impairment (up to 20 hours).
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.
Primarily biliary/fecal (94%): 94% of dose eliminated in feces via bile, 6% in urine (0.1% unchanged). Minimal renal elimination of parent drug.
Primarily fecal (~78%) with <2.5% excreted unchanged in urine. Small amount via biliary elimination.
Category C
Category C
Immunosuppressant
Immunosuppressant