April 2011
Volume 52, Issue 14
Free
ARVO Annual Meeting Abstract  |   April 2011
Pharmacodynamic Modeling of 24-Hour Intraocular Pressure Lowering for Taprenepag Isopropyl (PF-04217329), a Selective EP2 Receptor Agonist, as Monotherapy and in Combination with Latanaprost
Author Affiliations & Notes
  • Dana J. Nickens
    Global Pharmacometrics, Pfizer Inc, San Diego, California
  • J Mandema
    Quantitative Solutions, Menlo Park, California
  • S Raber
    Global Pharmacometrics, Pfizer Inc, San Diego, California
  • R A. Schachar
    Global Pharmacometrics, Pfizer Inc, San Diego, California
  • M Zhang
    Global Pharmacometrics, Pfizer Inc, San Diego, California
  • Footnotes
    Commercial Relationships  Dana J. Nickens, Pfizer (E); J. Mandema, Quantative Solutions (C); S. Raber, Pfizer (E); R. A. Schachar, Pfizer (E); M. Zhang, Pfizer (E)
  • Footnotes
    Support  Research supported by Pfizer Inc.
Investigative Ophthalmology & Visual Science April 2011, Vol.52, 225. doi:
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      Dana J. Nickens, J Mandema, S Raber, R A. Schachar, M Zhang; Pharmacodynamic Modeling of 24-Hour Intraocular Pressure Lowering for Taprenepag Isopropyl (PF-04217329), a Selective EP2 Receptor Agonist, as Monotherapy and in Combination with Latanaprost. Invest. Ophthalmol. Vis. Sci. 2011;52(14):225.

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

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Abstract

Purpose: : Characterize the 24 hr time course in IOP reduction for taprenepag (TAP) as mono-therapy and combined with latanoprost and to compare the IOP reduction of TAP with other single and dual combination agents as found in available published reports.

Methods: : A randomized, single-center, crossover trial of TAP 0.01% qAM for 14 days in subjects with glaucoma or ocular hypertension was conducted. IOP was measured at 2 hour intervals for 24 hr. A time-matched 24 hr baseline IOP was taken prior to each crossover period. Using a longitudinal pharmacodynamic (PD) model of individual subjects’ data, IOP reduction from baseline was estimated. Data from the trial was added to a previously reported meta-analysis (IOVS 2010, 51:E-Abst 172) in order to compare with an earlier TAP trial and a model-based meta-analysis (MBMA) of prostaglandin analogs.

Results: : Of 31 subjects randomized, 29 were available for the analyses. For the longitudinal PD model: (1) the magnitude of IOP reduction was directly related to baseline IOP (p<0.0001); (2) For similar baseline IOP, TAP + latanoprost significantly reduced IOP more than TAP alone (p=0.002) and was consistent over the 24 hr time course (p=0.51); (3) the effect of baseline IOP on IOP reduction was significantly different between TAP alone and TAP + latanoprost (p=0.028), resulting in a larger difference between mono and combination therapy at higher baseline values. For the MBMA: (1) time of maximum effect for TAP was estimated to be greatest between 11-14 hours after administration; (2) maximum effect for TAP mono-therapy after ≥14 days of treatment (baseline IOP = 25 mmHg) and 12 hours after qPM administration was estimated to be -6.27 [-7.27 to -5.27; 90% CI]; (3) IOP reduction with TAP mono-therapy was comparable to prostaglandin analogs (4) TAP + latanoprost had a higher average IOP reducing effect than a prostaglandin + timolol.

Conclusions: : TAP reduces IOP consistently throughout the day and night. TAP + latanoprost reduces IOP more than prostaglandins or prostaglandin + timolol. The difference is expected to be larger at higher baselines.

Clinical Trial: : http://www.clinicaltrials.gov NCT00934089

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