Omidenepag Isopropyl
Brand name: Omlonti
Drug class: Antiglaucoma Agents, Miscellaneous
Chemical name: propan-2-yl 2-[[6-[[(4-pyrazol-1-ylphenyl)methyl-pyridin-3-ylsulfonylamino]methyl]pyridin-2-yl]amino]acetate
Molecular formula: C26H28N6O4S
CAS number: 1187451-19-9
Introduction
Omidenepag isopropyl, a relatively selective prostaglandin E2 (EP2) receptor agonist, is an antiglaucoma agent.
Uses for Omidenepag Isopropyl
Omidenepag isopropyl has the following uses:
Omidenepag isopropyl 0.002% ophthalmic solution is indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension.
Omidenepag Isopropyl Dosage and Administration
General
Omidenepag isopropyl is available in the following dosage form(s) and strength(s):
Ophthalmic solution containing 0.002% (0.02 mg/mL) of omidenepag isopropyl.
Dosage
It is essential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:
Adults
Dosage and Administration
The recommended dosage is one drop in the affected eye(s) once daily in the evening.
Cautions for Omidenepag Isopropyl
Contraindications
-
None.
Warnings/Precautions
Pigmentation
Omidenepag isopropyl ophthalmic solution is a prodrug of omidenepag, a relatively selective prostaglandin E2 (EP2) receptor agonist. Pigmentation is expected to increase as long as omidenepag isopropyl ophthalmic solution is administered. 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 omidenepag isopropyl, pigmentation of the iris is likely to be permanent, while pigmentation of the periorbital tissue and eyelash changes are likely to be reversible in most patients. Patients who receive prostaglandin analogs, including omidenepag isopropyl, should be informed of the possibility of increased pigmentation, including permanent changes. The long-term effects of increased pigmentation are not known.
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. Neither nevi nor freckles of the iris appear to be affected by treatment. While treatment with omidenepag isopropyl ophthalmic solution can be continued in patients who develop noticeably increased iris pigmentation, these patients should be examined regularly.
Eyelash Changes
Omidenepag isopropyl 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.
Ocular Inflammation
Ocular inflammation has been reported in patients taking omidenepag isopropyl. Omidenepag isopropyl should be used with caution in patients with active ocular inflammation, including iritis/uveitis.
Macular Edema
Macular edema, including cystoid macular edema, has been reported during clinical trials in patients with pseudophakia receiving omidenepag isopropyl. Omidenepag isopropyl should be used with caution in aphakic patients, in pseudophakic patients, or in patients with known risk factors for macular edema.
Risk of Contamination and Potential Injury to the Eye
Advise patients to avoid touching the tip of the bottle to the eye or any surface, as this may contaminate the solution. Advise patients to not touch the tip to their eye to avoid the potential for injury to the eye.
Specific Populations
Pregnancy
There are no available data on the use of omidenepag isopropyl 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.
An embryofetal development study was conducted in pregnant rabbits administered omidenepag isopropyl once daily by subcutaneous injection at 0.008, 0.08, or 0.8 mg/kg/day from gestation Day 6 to 18, a period which covers implantation and the period of organogenesis in rabbits. Fetal skeletal anomalies (thoracic misaligned centrum and hemivertebra, fused sternebra, absent rib) were observed at 0.008 mg/kg/day (24 times the maximum recommended human ocular dose [MRHOD], based on estimated plasma Cmax). Additional fetal skeletal anomalies were observed at 0.08 mg/kg (absent thoracic arch, fused rib) and 0.8 mg/kg (misaligned and misshapen cervical vertebrae), corresponding to 256 times and 3,696 times the MRHOD based on estimated plasma Cmax, respectively. Increases in preimplantation loss and post-implantation loss were observed at 0.8 mg/kg/day. The rabbit maternal, No Observed Adverse Effect Level [NOAEL] was 0.8 mg/kg/day.
An embryofetal development study was conducted in pregnant rats administered omidenepag isopropyl once daily by subcutaneous injection at 0.01, 0.1, or 1 mg/kg/day from gestation Day 6 to 17, to target the period of organogenesis. Omidenepag isopropyl was not found to have any effect on embryo-fetal development in rats at up to 1 mg/kg/day (2,452 times the MRHOD based on estimated plasma Cmax). The rat maternal NOAEL was 1 mg/kg/day. In a pre/postnatal development study, treatment of pregnant rats with omidenepag isopropyl subcutaneously from gestation day 6 to lactation day 20 at 0.01, 0.1, or 1 mg/kg/day resulted in no adverse effects. The NOAEL for pre- and postnatal development was 1 mg/kg/day (2,452 times the MRHOD based on estimated plasma Cmax).
Lactation
There are no data on the presence of omidenepag isopropyl in human milk, the effects on the breastfed infant, or the effects on milk production. However, systemic exposure to omidenepag following topical ocular administration is low and 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 omidenepag isopropyl and any unknown potential adverse effects on the breast-fed child from omidenepag isopropyl.
Females and Males of Reproductive Potential
There are no data on the effects of omidenepag isopropyl 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 omidenepag isopropyl have not been established in pediatric patients.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and other adult patients.
Common Adverse Effects
The most common adverse reactions with incidence ≥ 1% 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%).
Drug Interactions
Specific Drugs
It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:
Please see product labeling for drug interaction information.
Actions
Mechanism of Action
Omidenepag is a relatively selective prostaglandin E2 (EP2) receptor agonist which decreases intraocular pressure (IOP). The exact mechanism of action is unknown at this time. Elevated IOP represents a major risk factor for glaucomatous field loss. The higher the level of IOP, the greater the likelihood of optic nerve damage and visual field loss.
Advice to Patients
-
Advise the patient to read the FDA-approved patient labeling (Instructions for Use).
-
Patients should be advised about the potential for increased brown pigmentation of the iris, which may be permanent. Patients should also be informed about the possibility of eyelid skin darkening, which is usually reversible after discontinuation of omidenepag isopropyl.
-
Patients should also be informed of the possibility of eyelash and vellus hair changes in the treated eye during treatment with omidenepag isopropyl. These changes may result in a disparity between eyes in length, thickness, pigmentation, number of eyelashes or vellus hairs, and/or direction of eyelash growth. Eyelash changes are usually reversible upon discontinuation of treatment.
-
Advise patients to avoid touching the tip of the bottle to the eye or any surface, as this may contaminate the solution. Advise patients to not touch the tip to their eye to avoid the potential for injury to the eye. The product should be refrigerated before opening, and once it is opened, it can be stored at room temperature for up to 31 days.
-
Advise patients that if they develop a new ocular condition (e.g., trauma, infection, or inflammation), experience a sudden decrease in visual acuity, have ocular surgery, or develop any ocular reactions, particularly conjunctivitis and eyelid reactions, they should immediately seek their physician's advice concerning the continued use of omidenepag isopropyl.
-
Contact lenses should be removed prior to administration of the solution. Lenses may be reinserted 15 minutes after administration.
-
Advise patients that if more than one topical ophthalmic drug is being used, the drugs should be administered at least five (5) minutes apart.
Additional Information
AHFSfirstRelease™. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Routes |
Dosage Forms |
Strengths |
Brand Names |
Manufacturer |
---|---|---|---|---|
Ophthalmic |
Solution |
0.002% |
Omlonti |
Santen Incorporated |
AHFS Drug Information. © Copyright 2023, Selected Revisions October 26, 2022. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
Reload page with references included
More about omidenepag isopropyl ophthalmic
- Check interactions
- Side effects
- Dosage information
- During pregnancy
- Drug class: ophthalmic glaucoma agents