Santen Applies for Manufacturing and Marketing Approval in Japan for STN1013800 (oxymetazoline hydrochloride), Eye Drops for Treatment of Acquired Blepharoptosis

December 26, 2024 - Osaka, Japan - Santen Pharmaceutical Co., Ltd. (hereinafter Santen) announced today that it has filed an application in Japan for manufacturing and marketing approval of STN1013800 (generic name: oxymetazoline hydrochloride) for the treatment of acquired blepharoptosis. The application was filed on December 26, 2024.

Blepharoptosis is a condition that causes the upper eyelid to droop, making it difficult to see. Symptoms include loss of upper visual field, stiff shoulders, headaches, and fatigue, all of which can interfere with everyday activities and lead to a decreased quality of life. ¹ Blepharoptosis can be classified into congenital and acquired forms. Acquired blepharoptosis has a variety of causes, and it is said that it can occur as a result of degeneration of the levator aponeurosis due to aging or the prolonged use of contact lenses. ^2,3,4,5 The treatment for most cases of blepharoptosis is surgery.

It has been reported that oxymetazoline acts as an agonist for α₁ and α₂ receptors. ⁶ Oxymetazoline acts on the α-adrenergic receptors of Müller’s muscle, which is one of the muscle tissues involved in raising the upper eyelid, and causes Müller’s muscle to contract, thus raising the upper eyelid. ⁷

In a Phase 3, placebo-controlled, randomized, double-masked study conducted in Japan, the efficacy and safety of 0.1% STN1013800 once daily and twice daily was evaluated in patients with acquired blepharoptosis. There was a statistically significant improvement in the primary endpoint—a change in MRD-1 (Marginal Reflex Distance-1, the margin between the upper eyelid and the center of the pupil)*—in the 0.1% STN1013800 once-daily group versus the placebo group, demonstrating the superiority of the drug over the placebo eye drop solution.

Santen’s Chief Medical Officer, Peter Sallstig commented: “Outside of the United States, surgery is currently the only approved treatment for blepharoptosis. Surgery carries various risks, including postoperative complications, making it particularly challenging to actively diagnose and treat patients with mild to moderate conditions. As a company specialized in ophthalmology, Santen is pursuing research and development in areas of ocular disease that have not previously been treatable with eye drops. We aim to make STN1013800 a new treatment option to address the needs of patients with blepharoptosis in Japan.”

References

1. Battu VK, et al. Am J Ophthalmol. 1996;121(6):677-686.
2. Custer PL. et al. Ophthalmology. 3rd ed. St. Louis, Mo: Mosby Elsevier; 2008. p. 1397-1403.
3. Van den Bosch WA, et al. Ophthalmology. 1992;99(12):1759-65.
4. Kersten, RC, et al. Ophthalmology. 1995;102(6):924-8.
5. Reddy AK, et al. Ophthalmology. 2007;114(12):2370.
6. Haenisch B, et al. Fundam Clin Pharmacol. 2010;24(6):729-39.
7. Slonim CB, et. al. JAMA Ophthalmol. 2020 ;138(11):1168-75.

• In this clinical study, MRD-1 was defined as the distance from the center of the pupil to the upper eyelid margin identified in the anterior segment image.

About STN1013800
In July 2020, Santen entered into an exclusive license agreement with Osmotica Pharmaceuticals plc (due to a company name change, currently known as RVL Pharmaceuticals plc), covering the continued development, registration, and commercialization rights for RVL-1201, a 0.1% oxymetazoline hydrochloride ophthalmic solution in Japan, China, other Asian countries, and EMEA. Santen has been developing the product as STN1013800.
In the United States, RVL Pharmaceuticals plc product UPNEEQ^® (oxymetazoline hydrochloride ophthalmic solution 0.1%) is the first and only ophthalmic solution approved by the U.S. Food and Drug Administration (FDA) for the treatment of acquired blepharoptosis in adults.

About Santen
As a specialized company dedicated to eye health, Santen aspires to contribute to the realization of “Happiness with Vision” by providing products and services to patients, consumers, and medical professionals around the world. Since its establishment, and guided by its CORE PRINCIPLE, “Tenki ni sanyo suru,” Santen has been committed to helping people maintain and improve their eye health for more than 130 years. Santen is engaged in the global research and development, manufacturing, and sales and marketing of pharmaceutical products in the field of eye care, supporting the eye health of approximately 50 million people in more than 60 countries and regions worldwide. Santen’s mission is to provide essential and significant value to patients and society in the prevention, diagnosis, and treatment of eye diseases through products and services created from its expertise in the ophthalmology field and from the patient's perspective. To create a future in which as many patients as possible can lead happy and fulfilling lives, Santen is committed to doing its utmost to realize a society in which people around the world can experience “Happiness with Vision.”
For more information, please visit Santen’s website https://www.santen.com/en.

Contact
Corporate Communications
Santen Pharmaceutical Co., Ltd.
E-mail: communication@santen.com