OMIDENEPAG: Omlonti, Eybelis

 

OMLONTI 0.002% (EYBELIS) eye drops is a new drug approved by FDA recently, for treatment of open angle glaucoma and ocular hypertension.

The drug has been developed jointly by Santen Pharmaceutical Co., Ltd. and UBE Corporation of Japan.

Omidenepag isopropyl, the active pharmaceutical ingredient in OMLONTI, is a relatively selective prostaglandin EP2 receptor agonist.

It increases aqueous humor drainage through the conventional (or trabecular) and uveoscleral outflow pathways, and the only product of this kind with this pharmacological action.

The FDA approval for OMLONTI was based on data from 12 clinical studies conducted in multiple global locations. Notably, a U.S. Phase 3 study confirmed OMLONTI to be non-inferior to timolol, the standard of care. Two different Phase 3 studies conducted in Japan and Asia showed OMLONTI to be non-inferior to latanoprost, another standard of care.

OMLONTI appears as a clear, colorless solution. It is supplied as a sterile, isotonic, buffered aqueous solution of omidenepag isopropyl with a target pH of 5.8 and an osmolality of approximately 285 mOsmol/kg.

Each mL of OMLONTI contains: 

Active: 0.02 mg of omidenepag isopropyl. Preservative: 0.005% benzalkonium chloride. Inactive ingredients: glycerin, polyoxyl 35 castor oil, sodium citrate, citric acid monohydrate, edetate disodium, sodium hydroxide and/or hydrochloric acid (to adjust pH), and water for injection.

Recommended Dosage:

The recommended dosage is one drop in the affected eye(s) once daily in the evening.

Side effects:

The most common adverse reactions seen with OMLONTI are conjunctival hyperemia (9%), photophobia (5%), vision blurred (4%), dry eye (3%), instillation site pain (3%), eye pain (2%), ocular hyperemia (2%), punctate keratitis (2%), headache (2%), eye irritation (1%), and visual impairment (1%).

The pigmentation change is due to increased melanin content in the melanocytes rather than to an increase in the number of melanocytes. After discontinuation of OMLONTI, pigmentation of the iris is likely to be permanent, while pigmentation of the periorbital tissue and eyelash changes are likely to be reversible.

Iris color change may not be noticeable for several months to years. Typically, the brown pigmentation around the pupil spreads concentrically towards the periphery of the iris and the entire iris or parts of the iris become more brownish.

OMLONTI may gradually change eyelashes and vellus hair in the treated eye. These changes include increased length, thickness, and the number of lashes or hairs. Eyelash changes are usually reversible upon discontinuation of treatment.

OMLONTI can induce ocular inflammation and should be used with caution in patients with active ocular inflammation, including iritis/uveitis.

OMLONTI can induce macular edema. It should be used with caution in aphakic patients, in pseudophakic patients, or in patients with known risk factors for macular edema.

Risk during pregnancy:

There are no available data on the use of OMLONTI in pregnant women. In animal reproduction studies, subcutaneous administration of omidenepag isopropyl to pregnant rabbits throughout the period of organogenesis produced fetal skeletal anomalies at a dose of 24 times the clinical dose, based on estimated plasma Cmax. Omidenepag isopropyl was not teratogenic in rats when administered subcutaneously at 1 mg/kg/day, 2,452 times the clinical dose, based on estimated plasma Cmax.

Risk during lactation:

Systemic exposure to omidenepag following topical ocular administration is low. it is not known whether measurable levels of omidenepag would be present in maternal milk following topical ocular administration. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for OMLONTI and any unknown potential adverse effects on the breast-fed child from OMLONTI.

Effect on male/female fertility:

There are no data on the effects of OMLONTI on human fertility. No impairment of fertility has been reported in animals receiving omidenepag isopropyl subcutaneously at doses up to 2,452 times the clinical dose based on estimated plasma Cmax.

Pediatric Use:

The safety and effectiveness of OMLONTI have not been established in pediatric patients.