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M. A. Lemp, R. Beckman, S. Weiss; Results of Phase I Tolerability LX214 (0.2%) Voclosporin Topical Solution in Healthy Volunteers and Subjects With Dry Eye Disease. Invest. Ophthalmol. Vis. Sci. 2010;51(13):6267.
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Phase 1 study results assessing tolerability of LX214 (voclosporin 0.2% topical solution-an immune-modulating agent) in healthy volunteers and subjects with Dry Eye Disease.
The Phase 1 dose-escalation study was conducted in 3 stages. Cohorts 1 and 2 each comprised 15 healthy volunteers randomized 2:1 receiving one drop of LX214 (0.02% in Cohort 1 and 0.2% in Cohort 2) or placebo at hours 0, 4, and 8 in each eye. Subjects in both cohorts were discharged at hour 12 and evaluated the next day. Cohort 3 was comprised of 5 patients with moderate to severe Dry Eye Disease. Patients self-administered treatment of LX214 0.2% bid over 14-days with examinations on Day 7 and 14. Tolerability was assessed by treatment-emergent ocular symptomatology using the Ocular Surface Disease Index (OSDI). Safety evaluations included adverse events, Snellen visual acuity, ophthalmic evaluations, intraocular pressure, vital signs, and clinical laboratory evaluations. Systemic voclosporin exposure was assessed with pharmacokinetic measurement in Cohorts 2 and 3.
30 healthy volunteers were enrolled in Cohorts 1 and 2, 14 of whom were male, 26 Caucasian, and 4 African -American. There were no statistical differences among treatment groups in symptoms and signs, at end of study. The 0.02% and 0.2% LX214 formulations were tolerated as well as placebo. 5 patients were enrolled in Cohort 3, all of whom were female; 4 were Caucasian and 1 African- American. Mean OSDI scores decreased from 62 at baseline to 42 at End of Treatment. Increases of 68% and 31% in Schirmer’s tear test scores in the right eye and left eye respectively were observed at 14 days as compared to baseline. 3/5 patients experienced one or more AEs. Maximum blood voclosporin blood concentration was 0.18 ± 0.08 ng/mL (range: 0.11-0.266ng/mL) for Cohort 2.
LX214 (0.02% and 0.2%) was well tolerated in healthy volunteers. Improvement in both symptoms and signs in patients with Dry Eye Disease was seen at 2 weeks. Systemic exposure of voclosporin was minimal.
Clinical Trial: :
www.clinicaltrials.gov NCT 00851734
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