De. Yocum et al., Microemulsion formulation of cyclosporin (Sandimmun Neoral (R)) vs Sandimmun (R): Comparative safety, tolerability and efficacy in severe active rheumatoid arthritis, RHEUMATOLOG, 39(2), 2000, pp. 156-164
Objective. To compare the safety, tolerability and efficacy of the new oral
microemulsion formulation of cyclosporin A (CyA, Sandimmun Neoral(R)) and
the original CyA formulation (Sandimmun(R)), in patients with severe active
rheumatoid arthritis (RA), over a 12-month period.
Methods. In this double-blind. multicentre study. patients were randomized
to treatment with Neoral or Sandimmun. starting with 2.5 mg/kg/day, with do
se adjustments after 4 weeks. Primary efficacy criteria included patients'
assessment of disease activity. Pharmacokinetic and safety assessments were
performed at regular intervals.
Results. Compared with Sandimmun, Neoral showed a consistent trend towards
greater clinical efficacy from week 12 onwards, including a significant dif
ference in patients' assessment of disease activity at the study end-points
. A significantly lower increase in dose from baseline was observed with Ne
oral at week 24. Pharmacokinetic assessments at week 24 showed increased ab
sorption and decreased variability with Neoral. No differences in safety we
re found between treatment groups.
Conclusion. These observations indicate that Neoral is as safe and at least
as effective as Sandimmun and have important implications for patient mana
gement given the increasing role for CyA in the treatment of severe, active