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Suliman Al-Fayoumi, Suresh Mallikaarjun, Shiva Patel, Amy Eisenfeld, John W. Chandler, Ryo Kubota; A Phase I Dose-Ranging Study of ACU-4429, a Novel Visual Cycle Modulator, in Healthy Volunteers. Invest. Ophthalmol. Vis. Sci. 2012;53(14):2043.
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To evaluate the safety, tolerability, and pharmacokinetics of ACU-4429, a novel visual cycle modulator, following once daily oral administration for 14 days in healthy volunteers in a randomized, double-masked, dose-ranging, placebo-controlled study.
Escalating doses of ACU-4429 (5-40 mg) or placebo (3:1 ratio) were administered orally to 40 fasted healthy volunteers (8 subjects/dose level) once daily for 14 days.
Mean age was 38 years (range 25-55 years); 80% were males. The incidence of ocular adverse events (AEs) increased in a dose-dependent manner; all participants exposed to ≥20 mg ACU-4429 reported mild, drug-related ocular AEs and numerous D-28 color vision testing abnormal results; all ocular AEs and abnormal results resolved within 7-10 days of study completion. ACU-4429 Tmax was 3.5-5 hrs and t1/2 was 4.6-7.9 hrs. Mean Cmax and AUC0-24 generally increased proportionately to dose on study Days 1 and 14. No accumulation of ACU-4429 or any of the major metabolites was observed following multiple once-daily administration for 14 days.
Once-daily ACU-4429 was safe and well-tolerated when administered for 14 days to healthy volunteers. ACU-4429 was rapidly absorbed and eliminated after oral dosing. Drug-related ocular AEs were mild and occurred more often with increasing doses of ACU-4429; all ocular AEs resolved within 7-10 days of study completion.
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