Six-Month Clinical Outcome of Cyclosporine Microemulsion Formulation (Sigmasporin Microral) in Stable Renal Transplant Patients Previously Maintained on Sandimmun Neoral

Abstract The trial objective was to investigate the feasibility and safety of conversion to a generic microemulsion cyclosporine in stable renal transplant patients premaintained on Neoral. We enrolled 75 patients from seven centers in five Middle Eastern countries monitored them for 6 months after conversion to Sigmasporin Microral. Readings at 0, 0.5, 1, 2, 3, 4.5, and 6 months included cyclosporine blood level, serum creatinine, liver enzymes, lipid profile, blood sugar, blood pressure and adverse events. Patients included 54 men and 21 women of mean age 38.9 ± 10.7 years at 30.3 ± 29.3 months post-transplantation maintained on Sigmasporin Microral dose of 2.8 ± 1.0 mg/kg per day; they were observed to be stable throughout the study period as reflected by the therapeutic blood C 0 level of 181.6 ± 102.1 and C 2 of 759.2 ± 384.4. Their absorption profile as represented by C 2 /C 0 was 4.9 ± 2.8, and C 2 /cyclosporine dose of 282.3 ± 128.8. An average serum creatinine level of 116.1 ± 29.5 μmol/L denoted stable graft function and their liver enzymes did not change during the study. No new-onset cases of hypertension, diabetes mellitus, or hyperlipidemia were reported among the patients. Graft function was stable for all patients, except for two incidences of mild acute rejection and two of mild cyclosporine nephrotoxicity; graft and patient survival rates were both 100%. Results of this 6-month study showed that Sigmasporin Microral was effective to maintain stable renal function in kidney transplant patients converted from Neoral with similar safety and tolerability profiles as those reported in the literature.