We conducted a clinical study in China on the efficacy and safety of
mizoribine (MZR) in
lupus nephritis. Eleven subjects with
proteinuria (≥2 g/day) who had undergone renal biopsy confirming a diagnosis of
lupus nephritis (class III: 1 subject; class IV: 6 subjects; class V: 4 subjects) were enrolled. Nine of the subjects were treatment- naive patients who received
remission induction therapy, and the other two were switched from
cyclophosphamide (CTX) or
mycophenolate mofetil due to lack of efficacy. MZR 150 mg was administered once a day. After 6 months, the remission rate was 72.7% (2 subjects achieved complete remission, and 9 partial remission). After 3 and 6 months, significant reductions (p < 0.01) were obtained in 24-h
proteinuria (g/day). In the subjects switched to MZR due to lack of efficacy with CTX, the dose was increased from MZR 150-200 mg due to inadequate improvement in
proteinuria, and this dose escalation resulted
in complete remission after 6 months. It is believed that this kind of dose escalation is one possible treatment option for
lupus nephritis. In this study, no adverse events occurred in any of the subjects. We therefore concluded that this first use in China as
remission induction therapy in
lupus nephritis patients of MZR, which is recognized as an effective maintenance
therapy in Japan, was effective. The results also suggest that MZR could be effective in patients for whom other drugs have been insufficiently effective.