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Latanoprostene Bunod

Class: Prostaglandin Analogs
Chemical Name: 4-(Nitrooxy) butyl (5Z)-7-{(1R,2R,3R,5S)-3,5- dihydroxy-2-[(3R)-3-hydroxy-5-phenylpentyl] cyclopentyl}hept-5-enoate
Molecular Formula: C27H41NO8
CAS Number: 860005-21-6
Brands: Vyzulta

Medically reviewed by Last updated on Nov 2, 2020.


Ocular hypotensive agent; synthetic analog of prostaglandin F (PGF).1 2 3 4 5 6 7 8 11

Uses for Latanoprostene Bunod

Ocular Hypertension and Glaucoma

Reduction of elevated IOP in patients with open-angle glaucoma or ocular hypertension.1 3

Once-daily latanoprostene bunod 0.024% ophthalmic solution appears to be more effective than or at least as effective as twice-daily timolol 0.5% ophthalmic solution in reducing IOP in adults with open-angle glaucoma or ocular hypertension.4 5 8 9 10

When selecting an initial ocular hypotensive agent, consider extent of the required IOP reduction, coexisting medical conditions, and drug characteristics (e.g., dosing frequency, adverse effects, cost).130 132 With single-agent regimens, the reduction in IOP is approximately 25–33% with topical prostaglandin analogs; 20–25% with topical β-adrenergic blocking agents, α-adrenergic agonists, or miotic (parasympathomimetic) agents; 20–30% with oral carbonic anhydrase inhibitors; 18% with topical rho kinase inhibitors; and 15–20% with topical carbonic anhydrase inhibitors.130 131

A prostaglandin analog frequently is considered for initial therapy in the absence of other considerations (e.g., contraindications, cost considerations, intolerance, adverse effects, patient refusal) because of relatively greater activity, once-daily administration, and low frequency of systemic adverse effects; however, ocular adverse effects can occur.130 131 132 134

Goal is to maintain an IOP at which visual field loss is unlikely to substantially reduce quality of life during the patient's lifetime.130 132

Reduction of pretreatment IOP by ≥25% shown to slow progression of primary open-angle glaucoma.130 131 Set an initial target IOP (based on extent of optic nerve damage and/or visual field loss, baseline IOP at which damage occurred, rate of progression, life expectancy, and other considerations) and reduce IOP toward this goal.130 131 132 Adjust target IOP up or down as needed over course of disease.130 131 132

Combination therapy with drugs from different therapeutic classes often required to control IOP.131 133

Latanoprostene Bunod Dosage and Administration


Ophthalmic Administration

Apply topically to the affected eye(s).1 3

Avoid contaminating solution container.1 (See Bacterial Keratitis under Cautions.)

Remove contact lenses prior to administration of each dose;1 may reinsert contact lenses 15 minutes after the dose.1 (See Use with Contact Lenses under Cautions.)

If more than one topical ophthalmic drug used, administer the drugs at least 5 minutes apart.1



Ocular Hypertension and Glaucoma

Latanoprostene bunod 0.024% ophthalmic solution: One drop into conjunctival sac of affected eye(s) once daily in the evening.1

More frequent dosing may diminish the IOP-lowering effect of the drug.1

If target IOP not achieved, may initiate additional or alternative ocular hypotensive agents.130 131 133 (See Ocular Hypertension and Glaucoma under Uses.)

Special Populations

No special population dosage recommendations.1

Cautions for Latanoprostene Bunod


  • Manufacturer states none known.1



Increased pigmentation of the iris and periorbital tissue (eyelid) reported with prostaglandin analogs, including latanoprostene bunod.1 Pigmentation expected to increase as long as latanoprostene bunod is administered.1 Following discontinuance of the drug, pigmentation of the iris is likely to be permanent, while pigmentation of periorbital tissue likely to be reversible in most patients.1 Long-term effects of increased pigmentation unknown.1

Increased pigmentation of the iris may not be evident until after several months to years of therapy.1

May continue latanoprostene bunod in patients who develop noticeably increased iris pigmentation; however, examine such patients regularly.1

Eyelash Changes

Possible gradual change in eyelashes and vellus hair in the treated eye, including increased length, thickness, pigmentation, and number of eyelashes and/or misdirected growth of eyelashes.1 3 Usually reversible upon discontinuance of the drug.1

Intraocular Inflammation

Use with caution in patients with a history of intraocular inflammation (e.g., iritis/uveitis); generally do not use in patients with active intraocular inflammation since therapy may exacerbate the condition.1

Macular Edema

Macular edema, including cystoid macular edema, reported with prostaglandin analogs.1

Use with caution in aphakic patients, in pseudophakic patients with torn posterior lens capsule, and in those with known risk factors for macular edema.1

Bacterial Keratitis

Bacterial keratitis reported with use of multiple-dose containers of topical ophthalmic preparations.1 These containers were inadvertently contaminated by patients who, in most cases, had concurrent corneal disease or disruption of the ocular epithelial surface.1

Improper handling of ophthalmic solutions can result in contamination of the solution by common bacteria known to cause ocular infections.1 Serious damage to the eye and subsequent loss of vision may result from using contaminated ophthalmic solutions.1 (See Advice to Patients.)

Use with Contact Lenses

Remove contact lenses prior to administration of each dose since the preparation contains benzalkonium chloride preservative;1 may reinsert contact lenses 15 minutes after the dose.1

Specific Populations


No data available regarding use in pregnant women.1

Has caused miscarriages, abortions, and fetal harm in rabbits.1 No treatment-related teratogenic effects observed in rats.1


Not known if distributed into milk following topical application to the eye.1 Data not available on effects of the drug on the breast-fed child or on milk production.1

Consider benefits of breast-feeding along with importance of the drug to the woman and any potential adverse effects on the breast-fed child from the drug.1

Pediatric Use

Use in pediatric patients <16 years of age not recommended because of potential safety concerns related to increased pigmentation following long-term use.1 (See Pigmentation under Cautions.)

Geriatric Use

No overall differences in safety and efficacy relative to younger adults.1

Common Adverse Effects

Conjunctival hyperemia,1 3 4 5 eye irritation,1 eye pain,1 instillation site pain.1

Interactions for Latanoprostene Bunod

No formal drug interaction studies to date.1 2 Interactions not expected because of limited systemic exposure following topical application to the eye.2

Latanoprostene Bunod Pharmacokinetics



Prodrug; absorbed through the cornea following ocular instillation and hydrolyzed to active metabolites, latanoprost acid (prostaglandin agonist) and butanediol mononitrate (nitric oxide donor).1 4 5 7 8 9 10 11

Following once-daily topical application of latanoprostene bunod 0.024% to the eyes for 28 days, no quantifiable plasma concentrations of latanoprostene bunod or butanediol mononitrate observed;1 low plasma concentrations of latanoprost acid detected.1 2 10

Mean time to peak plasma concentrations of latanoprost acid occur approximately 5 minutes following administration of the prodrug.1 2 10 Mean maximal plasma concentrations of latanoprost acid observed above the lower limit of quantitation (30 pg/mL) were 59.1 and 51.1 pg/mL on days 1 and 28, respectively.1


Reduction in IOP generally occurs within 1–3 hours after ocular instillation and peaks within 11–13 hours.1



Not known whether the drug or its metabolites distribute into milk in humans following topical ocular administration.1



Prodrug; metabolized in the eye by cellular esterases to latanoprost acid and butanediol mononitrate.1 2 3 5 7

Elimination of latanoprost acid from human plasma is rapid; plasma concentrations dropped below the lower limit of quantitation (30 pg/mL) in most individuals by 15 minutes following administration of the prodrug.1 2

Systemically, latanoprost acid is further metabolized in the liver to the 1,2-dinor and 1,2,3,4-tetranor metabolites via fatty acid β-oxidation.1 2 Butanediol mononitrate is metabolized to 1,4-butanediol and nitric oxide; the 1,4-butanediol metabolite is further oxidized to succinic acid and enters the tricarboxylic acid cycle.1 3





Unopened bottles: 2–8°C; protect from light and freezing.1 During shipment, may be maintained at up to 40°C for ≤14 days.1

Opened bottles: 2–25°C for 8 weeks.1


  • Synthetic analog of prostaglandin F (PGF).1 3 4 5 11

  • Lowers IOP via dual mechanism of action from effects of 2 active moieties (i.e., latanoprost acid [prostaglandin agonist] and butanediol mononitrate [nitric oxide donor]).1 4 5 7 8 9 10 11

  • Increases aqueous humor outflow within both the trabecular meshwork and uveoscleral pathway.1 2 4 5 7

  • Latanoprost acid increases aqueous humor outflow via the uveoscleral pathway; butanediol mononitrate releases nitric oxide inducing relaxation of the trabecular meshwork and Schlemm’s canal, resulting in further increases in aqueous humor outflow.1 2 4 5 7 8 11

Advice to Patients

  • Importance of not exceeding once-daily dosing; more frequent administration may paradoxically decrease IOP-lowering effect of latanoprostene bunod.1

  • Importance of learning and adhering to proper administration techniques to avoid contaminating the ophthalmic solution with common bacteria that can cause ocular infections; instruct patients to avoid contact of tip of the container with the eyes or surrounding structures, fingers, or any other surface.1 Serious damage to the eye and subsequent loss of vision may result from using contaminated ophthalmic solutions.1

  • Importance of patients immediately informing a clinician before continuing therapy if they develop a new ocular condition (e.g., trauma, infection) or ocular reaction (particularly conjunctivitis, eyelid reactions), experience a sudden decrease in visual acuity, or have ocular surgery.1

  • Importance of removing contact lenses prior to administration of each dose since the ophthalmic solution contains benzalkonium chloride preservative; may reinsert contact lenses 15 minutes after the dose.1

  • If using more than one ophthalmic preparation, importance of administering the preparations at least 5 minutes apart.1

  • Risk of permanent increase in brown pigmentation of the iris; risk of darkening of the skin around the eyes (eyelid), which usually is reversible after discontinuance of latanoprostene bunod.1

  • Risk of changes in eyelashes and vellus hair in the treated eye.1 Potential for disparity between eyes in length, thickness, pigmentation, or number of eyelashes or vellus hairs and/or direction of eyelash growth.1 Eyelash changes usually reversible after discontinuance of therapy.1

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)


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.

Latanoprostene Bunod


Dosage Forms


Brand Names






Bausch & Lomb

AHFS DI Essentials™. © Copyright 2021, Selected Revisions November 2, 2020. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.


1. Bausch & Lomb. Vyzulta (latanoprostene bunod ophthalmic solution 0.024%) prescribing information. Bridgewater, NJ; 2019 May.

2. US Food and Drug Administration. Center for Drug Evaluation and Research: Application number 207795Orig1s000: Clinical pharmacology and biopharmaceutics review (s). From FDA website.

3. Kawase K, Vittitow JL, Weinreb RN et al. Long-term Safety and Efficacy of Latanoprostene Bunod 0.024% in Japanese Subjects with Open-Angle Glaucoma or Ocular Hypertension: The JUPITER Study. Adv Ther. 2016; 33:1612-27.

4. Weinreb RN, Scassellati Sforzolini B, Vittitow J et al. Latanoprostene Bunod 0.024% versus Timolol Maleate 0.5% in Subjects with Open-Angle Glaucoma or Ocular Hypertension: The APOLLO Study. Ophthalmology. 2016; 123:965-73.

5. Medeiros FA, Martin KR, Peace J et al. Comparison of Latanoprostene Bunod 0.024% and Timolol Maleate 0.5% in Open-Angle Glaucoma or Ocular Hypertension: The LUNAR Study. Am J Ophthalmol. 2016; 168:250-259.

6. Weinreb RN, Ong T, Scassellati Sforzolini B et al. A randomised, controlled comparison of latanoprostene bunod and latanoprost 0.005% in the treatment of ocular hypertension and open angle glaucoma: the VOYAGER study. Br J Ophthalmol. 2015; 99:738-45.

7. Cavet ME, Vollmer TR, Harrington KL et al. Regulation of Endothelin-1-Induced Trabecular Meshwork Cell Contractility by Latanoprostene Bunod. Invest Ophthalmol Vis Sci. 2015; 56:4108-16.

8. Aliancy J, Stamer WD, Wirostko B. A Review of Nitric Oxide for the Treatment of Glaucomatous Disease. Ophthalmol Ther. 2017; 6:221-232.

9. Liu JHK, Slight JR, Vittitow JL et al. Efficacy of Latanoprostene Bunod 0.024% Compared With Timolol 0.5% in Lowering Intraocular Pressure Over 24 Hours. Am J Ophthalmol. 2016; 169:249-257.

10. Kaufman PL. Latanoprostene bunod ophthalmic solution 0.024% for IOP lowering in glaucoma and ocular hypertension. Expert Opin Pharmacother. 2017; 18:433-444.

11. Lu LJ, Tsai JC, Liu J. Novel Pharmacologic Candidates for Treatment of Primary Open-Angle Glaucoma. Yale J Biol Med. 2017; 90:111-118.

130. Prum BE Jr, Rosenberg LF, Gedde SJ et al. Primary open-angle glaucoma preferred practice pattern guideline [published corrigendum appears in Ophthalmology. 2018; 125: 949]. San Francisco, CA: American Academy of Ophthalmology; 2015. From the American Academy of Ophthalmology website.

131. Liebmann JM, Lee JK. Current therapeutic options and treatments in development for the management of primary open-angle glaucoma. Am J Manag Care. 2017; 23(15 Suppl):S279-S292.

132. Weinreb RN, Aung T, Medeiros FA. The pathophysiology and treatment of glaucoma: a review. JAMA. 2014; 311:1901-11.

133. Gupta D, Chen PP. Glaucoma. Am Fam Physician. 2016; 93:668-74.

134. Inoue K. Managing adverse effects of glaucoma medications. Clin Ophthalmol. 2014; 8:903-13.