Clinical appraisal of tafluprost in the reduction of elevated intraocular pressure (IOP) in open-angle glaucoma and ocular hypertension

Makoto Aihara, Makoto Aihara

Abstract

An elevated intraocular pressure (IOP) is one of the most important risk factors for the development of glaucoma, which causes progressive optic neuropathy. Lowering IOP is currently the only therapeutic approach to the treatment of glaucoma. Tafluprost, a novel prostaglandin analogue, was recently launched onto the market as an ocular hypotensive agent. Tafluprost is potent in its affinity for the prostanoid FP receptor and in its intraocular lowering efficacy. Moreover, it enhances the ocular hemodynamics and has neuroprotective effects. Clinical studies have demonstrated its efficacy at decreasing intraocular pressure in patients with open-angle glaucoma or ocular hypertension.

Keywords: intraocular pressure; normal tension glaucoma; open-angle glaucoma; receptor affinity.

Figures

Figure 1
Figure 1
Structure of tafluprost.
Figure 2
Figure 2
Receptor affinities of various prostaglandin derivatives (schematic representation).
Figure 3
Figure 3
Intraocular pressure (IOP)-lowering effects of a single application of tafluprost in normotensive monkeys. Reproduced with permission from Takagi Y, Nakajima T, Shimazaki A, et al. Pharmacological characteristics of AFP-168 (tafluprost), a new prostanoid FP receptor agonist, as an ocular hypotensive drug. Exp Eye Res. 2004;78:768–776. Copyright © 2004 Elsevier. Notes: Tafluprost is indicated as AFP-168. Data represent the mean ± SEM for 12 animals. **P < 0.01 vs vehicle (Tukey–Kramer test).
Figure 4
Figure 4
Intraocular pressure (IOP)-lowering effects of once-daily multiple applications of tafluprost and latanoprost in normotensive monkeys. Reproduced with permission from Takagi Y, Nakajima T, Shimazaki A, et al. Pharmacological characteristics of AFP-168 (tafluprost), a new prostanoid FP receptor agonist, as an ocular hypotensive drug. Exp Eye Res. 2004;78:768–776. Copyright © 2004 Elsevier. Notes: Tafluprost is indicated as AFP-168. IOP change was calculated from time 0 on day 1. Drugs were instilled at 10:30 a.m. on each day from day 1 to day 5. Data represent the mean + SEM. for 10 animals. *P < 0.05; **P < 0.01 vs vehicle (Dunnett’s multiple-range test).
Figure 5
Figure 5
Effects of tafluprost on melanin formation in B16 melanoma cells. Reproduced with permission from Takagi Y, Nakajima T, Shimazaki A, et al. Pharmacological characteristics of AFP-168 (tafluprost), a new prostanoid FP receptor agonist, as an ocular hypotensive drug. Exp Eye Res. 2004;78:768–776. Copyright © 2004 Elsevier. Notes: The carbonic acid form of tafluprost is indicated as AFP-172, and that of latanoprost as PhXA85. Drugs were added to the culture medium for 4 days. Data represent the mean ± SEM from four experiments. *P < 0.05, vs vehicle (Dunnett’s multiple-range test).
Figure 6
Figure 6
Time course of intraocular pressure (IOP) change in phase II clinical study in patients with primary open angle glaucoma or ocular hypertension (noninferiority study between Tapros® and latanoprost). Notes: Data represent mean ± SD **P < 0.01, vs pre-dosing value (paired-t test). NS: not significant, comparison between Tapros® and latanoprost (Student t-test).
Figure 7
Figure 7
Time course of intraocular pressure (IOP) change in phase II clinical study in patients with normal tension glaucoma (source: Product Overview http://www.santen.co.jp/medical/common/pdf/info_package/tenpu/tapros.pdf). Notes: Data represents mean ± SD. **P < 0.01, vs pre-dosing value (paired t-test). ##P < 0.01, comparison between placebo and Tapros® (Student t-test).

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Source: PubMed

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