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D. Edwards, David S Boyer, Peter K Kaiser, Jeffrey S. Heier, Ben Askew; First-in human study of SF0166 Topical Ophthalmic Solution in patients with diabetic macular edema. Invest. Ophthalmol. Vis. Sci. 2018;59(9):1961. doi: https://doi.org/.
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© ARVO (1962-2015); The Authors (2016-present)
To study the safety, tolerability and preliminary efficacy of SF0166 Topical Ophthalmic Solution (SF0166) in patients with diabetic macular edema (DME). SF0166 is a novel, highly potent and selective, small molecule inhibitor of the integrin alpha-v-beta-3 (αvβ3), an endothelial cell surface receptor that modulates cellular response to vascular endothelial growth factor (VEGF). SF0166 has been shown to distribute to the choroid and retina in substantial concentrations after eye-drop administration in animals.
The safety and exploratory efficacy of SF0166 was assessed in a Phase I/II, randomized, double-masked, multicenter study in patients with DME. Eligible patients with active DME were randomized 1:1 to self-administer an eye-drop, containing either 1.25 or 2.5 mg SF0166, twice a day for 28 days. Following completion of the treatment period, patients were followed for another 28-day period for safety and efficacy monitoring. Clinical assessments included spectral domain optical coherence tomography (SD-OCT), visual acuity, slit-lamp biomicroscopy, intraocular pressure (IOP), ophthalmoscopy and dilated fundus exam, fluorescein angiography, and adverse event (AE) collection.
A total of 44 patients (44 eyes) were randomized, 40 of which completed the study. During the study, ocular adverse events (AEs) were reported for 7 patients, all of which were mild and only one event (red eye OU) was deemed possibly related to study treatment. Six unrelated, non-ocular serious adverse events were reported during the study, all of which were typical for the diabetic population. Twenty-seven non-serious, non-ocular AEs were reported.Evidence of biologic activity was seen by decreases in central retinal thickness (CRT) by SD-OCT in 15 (38%) of completed patients at Day 28, and in 22 (55%) at Day 56, roughly equally distributed between the two dose groups. Nine patients showed at least a 1-line improvement in vision, however, visual acuity changes, in general, were not well correlated with retinal thickness changes.
SF0166 Topical Ophthalmic Solution was well tolerated and no safety signals or trends were observed. Further, a number of patients experienced reductions in retinal thickness showing that SF0166 has biological activity when delivered as an eye drop. These results support the further clinical development of SF0166.
This is an abstract that was submitted for the 2018 ARVO Annual Meeting, held in Honolulu, Hawaii, April 29 - May 3, 2018.
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