April 2010
Volume 51, Issue 13
Free
ARVO Annual Meeting Abstract  |   April 2010
Ocular Hypotensive Efficacy and Safety of the Rho Kinase Inhibitor AR-12286 in Patients With Elevated Intraocular Pressure
Author Affiliations & Notes
  • R. D. Williams
    Center for Clinical Research, Louisville, Kentucky
  • G. D. Novack
    PharmaLogic Development Inc, San Rafael, California
  • T. van Haarlem
    Aerie Pharmaceuticals, Inc, Bridgewater, New Jersey
  • C. Kopczynski
    Aerie Pharmaceuticals, Inc, Research Triangle Park, North Carolina
  • AR-12286 Phase 2a Study Group
    Center for Clinical Research, Louisville, Kentucky
  • Footnotes
    Commercial Relationships  R.D. Williams, None; G.D. Novack, Inspire Pharmaceuticals, Inc, I; Aerie Pharmaceuticals, Inc., C; Inspire Pharmaceuticals, Inc, C; Santen Pharmaceutical Co., C; T. van Haarlem, Aerie Pharmaceuticals, Inc., E; C. Kopczynski, Aerie Pharmaceuticals, Inc, E.
  • Footnotes
    Support  None.
Investigative Ophthalmology & Visual Science April 2010, Vol.51, 1633. doi:https://doi.org/
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      R. D. Williams, G. D. Novack, T. van Haarlem, C. Kopczynski, AR-12286 Phase 2a Study Group; Ocular Hypotensive Efficacy and Safety of the Rho Kinase Inhibitor AR-12286 in Patients With Elevated Intraocular Pressure. Invest. Ophthalmol. Vis. Sci. 2010;51(13):1633. doi: https://doi.org/.

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      © ARVO (1962-2015); The Authors (2016-present)

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Abstract

Purpose: : To evaluate the ocular hypotensive efficacy and safety of 0.05%, 0.1% and 0.25% AR-12286 Ophthalmic Solutions in patients diagnosed with ocular hypertension or glaucoma. AR-12286 is a highly selective Rho kinase inhibitor designed to lower intraocular pressure by improving trabecular outflow.

Methods: : Parallel comparison, vehicle-controlled, double-masked, 3-week randomized clinical trial. Subjects (n=89) with elevated intraocular pressure (IOP) were randomly assigned to receive either one of three concentrations of AR-12286 or its vehicle. Dosing was q.d. AM x 7 days, then q.d. PM x 7 days, then b.i.d. x 7 days. Primary and secondary efficacy endpoints were mean IOP at each diurnal time point (8 AM, 10 AM, 12 PM, and 4 PM) and mean change in IOP from baseline, respectively.

Results: : All three concentrations of AR-12286 produced statistically and clinically significant reductions in mean IOP that were dose-dependent, with peak effects occurring 2 to 4 hours after dosing. Mean IOP at peak effect ranged from 17.6 to 18.7 mm Hg (-6.8 to -4.4 mm Hg) for the three concentrations. The largest IOP reductions were produced by 0.25% AR-12286 after b.i.d. dosing (up to -6.8 mm Hg; 28%). The 0.25% concentration had a long duration of effect, with q.d. PM dosing producing highly significant IOP reductions throughout the following day (-5.4 to -4.2 mm Hg). The only adverse event of note was trace (+0.5) to moderate (+2) conjunctival hyperemia that was transient, typically lasting 4 hours or less. After q.d. PM dosing, hyperemia was seen in less than 10% of patients.

Conclusions: : AR-12286 provided clinically and statistically significant ocular hypotensive efficacy in patients with ocular hypertension and glaucoma. The only safety finding of note was a transient, self-resolving ocular hyperemia. The top of the dose response for AR-12286 was not established; higher doses could provide greater efficacy, especially when administered q.d. PM.

Clinical Trial: : www.clinicaltrials.gov NCT00902200

Keywords: intraocular pressure • trabecular meshwork • clinical (human) or epidemiologic studies: treatment/prevention assessment/controlled clinical trials 
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