Tolerability and efficacy of bimatoprost 0.01 % in patients with open-angle glaucoma or ocular hypertension evaluated in the Taiwanese clinical setting: the Asia Pacific Patterns from Early Access of Lumigan 0.01 % (APPEAL Taiwan) study

Abstract

BackgroundIn randomized, controlled trials of open-angle glaucoma (OAG) or ocular hypertension (OHT), bimatoprost 0.01 % improved tolerability while retaining the intraocular pressure (IOP)-lowering efficacy of bimatoprost 0.03 %. Given geographic/racial differences in glaucoma presentation, the APPEAL study assessed the occurrence and severity of hyperemia produced by bimatoprost 0.01 %, and its efficacy, in the Taiwanese clinical setting.MethodsIn this multicenter, open-label, observational study, treatment-naïve and previously treated patients with OHT or OAG received once-daily bimatoprost 0.01 % for 12 weeks. Hyperemia (primary endpoint) was graded at baseline, week 6, and week 12 using a photonumeric scale (0, +0.5, +1, +2, +3), grouped (≤ +1, none to mild; ≥ +2, moderate to severe), and reported as unchanged from baseline, improved, or worsened. IOP assessments followed the same schedule. Supplemental efficacy analyses were conducted based on previous therapies.ResultsThe intent-to-treat population (N = 312) included treatment-naïve (13.5 %) and previously treated (86.5 %) patients; mean age was 53.3 years. At baseline, 46.3 % of previously treated patients were receiving prostaglandin analog (PGA) monotherapy. At week 12, 91.2 %, 5.9 %, and 2.9 % of treatment-naïve patients exhibited unchanged, worsened, and improved hyperemia from baseline, respectively; 77.9 %, 12.9 %, and 9.2 % of previously treated patients showed no change, worsening, and improvement, respectively. There were no statistically significant shifts in hyperemia severity in either group, or in subgroups based on previous use of any PGA, any non-PGA, latanoprost, or travoprost monotherapies. In treatment-naïve patients, mean IOP reduction from baseline (18.0 ± 3.8 mm Hg) was 3.6 mm Hg at week 12 (P < 0.0001); 83.3 % had baseline IOP ≤ 21 mm Hg. In previously treated patients, mean additional IOP reduction from baseline (17.8 ± 3.9 mm Hg) was 2.6 mm Hg (P < 0.0001); similar results were observed in patient subgroups based on previous therapies.ConclusionsIn the Taiwanese clinical setting, bimatoprost 0.01 % provided significant IOP lowering in treatment-naïve patients (regardless of baseline IOP) and previously treated patients (even those with relatively low IOP on other therapies), while causing no significant changes in hyperemia from baseline.Trial registrationClinicaltrials.gov NCT01814761. Registered 18 March 2013.

Efficacy and safety of bimatoprost 0.01% formulated in tight junction modulation technology compared to marketed benzalkonium chloride preserved bimatoprost 0.01% ophthalmic solution in healthy beagle dogs

“…8 Notwithstanding the decrease in adverse events compared to the higher strength bimatoprost, the ocular surface adverse events attributable to BKC were still persistent in subsequent reports. 9 New formulation of SPARC with TMJ technology could overcome this limitation and further improve the safety outcomes. This study gives a preliminary insight into the expected benefit with the new technology.…”

“…8 Although the ocular side effects were reduced, conjunctival hyperaemia was still persistent in subsequent reports. 9 One reason could be because BKC, apart from been a preservative, is highly corrosive and its detergent effect leads to tear film instability by evaporating the aqueous layer of the tear film. A closer look at the literature also reveals that BKC causes proapoptotic changes on conjunctival cell lines, decrease in antioxidants, increase in inflammatory mediators in lens epithelial cells and DNA damage.…”

Prospective, non-interventional, multicenter study of the intraocular pressure-lowering effects of prostaglandin analog/prostamide-containing therapies in previously treated patients with open-angle glaucoma or ocular hypertension

“…However, the study was designed to reflect typical clinical settings. In addition, outcomes were reported at 8–12 weeks after initiation of study treatment, hence precluding residual carryover effects from previous treatments, as evidenced in other published studies 54–57. The fact that patients with pseudoexfoliation or pigmentary glaucoma were included in the analyses should also be considered, although it provided valuable information.…”

Aqueous humor pharmacokinetics of Benzalkonium chloride free bimatoprost formulated in tight junction modulation technology compared to Benzalkonium chloride preserved bimatoprost 0.01% ophthalmic solution in rabbit eyes

“…on PG-F2α receptors. 8 Taking this into account, a reduced strength of Bimatoprost 0.01% was developed. In order to overcome reduced efficacy, if any, because of the decreased strength, the concentration of BAK was increased 4-folds to 200ppm (0.02%) to improve permeation into ocular tissue.…”