Ocuphire Extends US Patent Protection for Late-Stage Drug Candidate for Reversal of Mydriasis by 5 More Years Into 2039

Ocuphire Pharma, Inc. recently announced the issuance of US Patent No. 11,400,077. The patent provides added intellectual property protection for the company’s late-stage product candidate, Nyxol (phentolamine mesylate), with claims directed to methods for treating mydriasis using phentolamine mesylate. The patent is eligible for listing in the US FDA Orange Book and has a term extending into year 2039.

“We are very pleased with the issuance of this new patent for Nyxol, which extends our intellectual property protection in the US by an additional 5 years into 2039,” said Mina Sooch, MBA, Founder and CEO of Ocuphire Pharma. “Last year, we were granted a new US Patent for presbyopia extending our existing patent estate into year 2039 and now we are very pleased with the issuance of this new patent for Nyxol in reversal of mydriasis. As we own the worldwide rights to Nyxol for all indications, this added protection will position us to maximize the commercial value of Nyxol for at least 15 years in reversal of mydriasis as we plan to submit an NDA to the FDA later this year. If approved, Nyxol could be launched in the second half of 2023.”

Ocuphire owns all of the worldwide rights to Nyxol for all indications. Ocuphire’s patent estate for Nyxol includes patents and patent applications for phentolamine mesylate formulations and methods of using phentolamine mesylate. Ocuphire’s patent estate for Nyxol contains nine issued US patents, eight pending US non-provisional patent applications, as well as issued patents in Australia, Canada, Europe, Japan, and Mexico and pending patent applications in Australia, Canada, Europe, Japan, and other foreign countries. Ocuphire’s first set of US and foreign patents expire in year 2034, while Ocuphire’s second set of US patents expire in year 2039. Patents, if granted based on Ocuphire’s pending foreign patent applications, would expire in year 2039.

An estimated 100 million eye dilations are conducted every year in the US to examine the back of the eye either for routine check-ups, disease monitoring or surgical procedures across all eye care practice groups. Depending on the individual and the color of their eyes, the pharmacologically-induced dilation can last anywhere from 6 to 24 hours in adults. Dilated eyes have heightened sensitivity to light and an inability to focus on near objects, causing difficulty reading, working and driving. Currently, there are no approved or available treatment options to safely reverse mydriasis. If approved, Nyxol has the potential to be the only FDA-approved drug for the reversal of mydriasis, uniquely modulating the pupil by blocking or ‘relaxing’ the α1 receptors found only on the iris dilator muscle. This mechanism is differentiated from other miotics in that Nyxol moderately reduces the pupil size without engaging the ciliary muscle, resulting in favorable safety and tolerability seen across 12 completed trials in 3 indications by avoiding accommodative ciliary spasm, associated headaches and browaches, narrow angle closure, or risk of retinal detachment.

Ocuphire is a publicly traded, clinical-stage ophthalmic biopharmaceutical company focused on developing and commercializing small-molecule therapies for the treatment of refractive and retinal eye disorders. The company’s lead product candidate, Nyxol eye drops (0.75% phentolamine ophthalmic solution), is a once-daily, preservative-free eye drop formulation of phentolamine mesylate, a non-selective alpha-1 and alpha-2 adrenergic antagonist designed to reduce pupil size, and is being developed for several indications, including reversal of pharmacologically-induced mydriasis (RM), presbyopia and dim light or night vision disturbances (NVD), and has been studied in 12 completed clinical trials. Ocuphire has reported positive data from MIRA-2 and MIRA-3 registration trials and MIRA-4 pediatric safety trial for the treatment of RM. Ocuphire also reported positive topline data from the VEGA-1 Phase 2 trial of Nyxol for treatment of presbyopia, both Nyxol as a single agent and Nyxol with low dose pilocarpine (LDP) 0.4% as adjunctive therapy. The company recently reported positive topline results from LYNX-1 Phase 3 trial of Nyxol for NVD. Ocuphire’s second product candidate, APX3330, is an oral tablet designed to inhibit angiogenesis and inflammation pathways relevant to retinal and choroidal vascular diseases, such as diabetic retinopathy (DR) and diabetic macular edema (DME) and has been studied in 11 Phase 1 and 2 trials. The Company announced in March the completion of enrollment in the ZETA-1 Phase 2b clinical trial of APX3330 to treat DR/DME. Please visit www.clinicaltrials.gov to learn more about Ocuphire’s ongoing APX3330 Phase 2b trial in DR/DME ZETA-1 (NCT04692688) and completed Nyxol trials: Phase 3 registration trial in NVD LYNX-1 (NCT04638660), Phase 3 registration trials in RM MIRA-2 (NCT04620213) and MIRA-3 (NCT05134974), MIRA-4 Phase 3 pediatric safety study (NCT05223478), and Phase 2 trial in presbyopia VEGA-1 (NCT04675151). As part of its strategy, Ocuphire will continue to explore opportunities to acquire additional ophthalmic assets and seek strategic partners for late-stage development, regulatory preparation, and commercialization of drugs in key global markets. For more information, visit www.ocuphire.com.