Bepotastine

Bepotastine is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from mast cells.

• BEPREVE ® (bepotastine besilate ophthalmic solution) 1.5% is a histamine H 1 receptor antagonist indicated for the treatment of itching associated with signs and symptoms of allergic conjunctivitis. BEPREVE is a histamine H1 receptor antagonist indicated for the treatment of itching associated with allergic conjunctivitis.ICD-10: H10.9

• BEPREVE is contraindicated in patients with a history of hypersensitivity reactions to bepotastine or any of the other ingredients [see Adverse Reactions ( 6.2 )] . Hypersensitivity to any component of this product.contraindicated

Instill one drop of BEPREVE into the affected eye(s) twice a day. Remove contact lenses prior to instillation of BEPREVE. • Instill one drop into the affected eye(s) twice a day. ( 2 ) • Remove contact lenses prior to instillation of BEPREVE. ( 2 )

• Contamination of Solution: Do not touch the dropper tip to any surface. Keep bottle tightly closed when not in use. ( 5.1 ) • Contact Lens Wear: BEPREVE should not be used to treat contact lens-related irritation. ( 5.2 ) 5.1 Contamination of Tip and Solution To minimize contaminating the dropper tip and solution, advise the patient not to touch the eyelids or surrounding areas with the dropper tip of the bottle and to keep the bottle tightly closed when not in use. 5.2 Contact Lens Wear BEPREVE should not be used to treat contact lens-related irritation. BEPREVE should not be instilled while wearing contact lenses. Patient should remove contact lenses prior to instillation of BEPREVE, because benzalkonium chloride may be absorbed by soft contact lenses. Lenses may be reinserted after 10 minutes following administration of BEPREVE.

The most common adverse reaction occurring in approximately 25% of patients was a mild taste following instillation. Other adverse reactions which occurred in 2-5% of subjects were eye irritation, headache, and nasopharyngitis. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Bausch & Lomb Incorporated at 1-800-553-5340 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. The most common reported adverse reaction occurring in approximately 25% of subjects was a mild taste following instillation. Other adverse reactions occurring in 2-5% of subjects were eye irritation, headache, and nasopharyngitis. 6.2 Post-Marketing Experience Hypersensitivity reactions have been reported rarely during the post-marketing use of BEPREVE. Because these reactions are reported voluntarily from a population of unknown size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. The hypersensitivity reactions may include itching, body rash, and swelling of lips, tongue and/or throat.

8.1 Pregnancy Risk Summary There are no available human data for the use of BEPREVE during pregnancy to inform any drug-associated risks. Oral administration of bepotastine besilate to pregnant rats or rabbits during organogenesis or during the pre/postnatal period did not produce adverse embryofetal or offspring effects at clinically relevant systemic exposures. Maternal toxicity was observed in the rabbits at the lowest dose administered, 20 mg/kg/day (215 times the maximum recommended human ophthalmic dose, RHOD, on a mg/m 2 basis) [see Data ] . The background risk of major birth defects and miscarriage for the indicated population is unknown. However, the background risk in the U.S. general population of major birth defects is 2 to 4%, and of miscarriage is 15 to 20%, of clinically recognized pregnancies. Data Animal Data In embryofetal development studies, oral administration of bepotastine besilate to pregnant rabbits throughout organogenesis did not produce teratogenic effects at maternal doses up to 500 mg/kg/day (approximately 5,400 times the maximum RHOD, on a mg/m 2 basis). A maternal no observed adverse effect level (NOAEL) was not identified in this study due to spontaneous abortion observed at the lowest dose tested, 20 mg/kg/day (approximately 215 times higher than the maximum RHOD, on a mg/m 2 basis).

Metabolism

Absorption: The extent of systemic exposure to bepotastine following topical ophthalmic administration of bepotastine besilate 1% and 1.5% ophthalmic solutions was evaluated in 12 healthy adults. Following one drop of 1% or 1.5% bepotastine besilate ophthalmic solution to both eyes four times daily (QID) for 7 days, bepotastine plasma concentrations peaked at approximately 1 to 2 hours post-instillation.

• Sep 8, 2009NDANDA022288Bausch And Lomb Inc
• Mar 18, 2019ANDAANDA206220Mylan
• Apr 5, 2023ANDAANDA214588Alembic
• Aug 14, 2024ANDAANDA217770Somerset Theraps Llc

1. 1Drug Ineffective436.8%
2. 2Headache355.5%
3. 3Eye Irritation325.0%
4. 4Fatigue314.9%
5. 5Nausea314.9%
6. 6Pain284.4%
7. 7Diarrhoea274.3%
8. 8Pruritus274.3%
9. 9Treatment Failure264.1%
10. 10Dyspnoea253.9%
11. 11Asthma243.8%
12. 12Arthralgia233.6%
13. 13Malaise233.6%
14. 14Dysgeusia223.5%
15. 15Off Label Use203.2%

The 10 most recently updated of 26 ClinicalTrials.gov registrations naming Bepotastine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Confirmatory Study of TAU-284 in Pediatric Patients With Atopic Dermatitis
  Completed · Phase 3 · Interventional · 303 enrolled · Tanabe Pharma Corporation
  NCT01840605updated 2026-01-08
• The Confirmatory Study of TAU-284 in Pediatric Patients With Perennial Allergic Rhinitis
  Completed · Phase 3 · Interventional · 473 enrolled · Tanabe Pharma Corporation
  NCT01861522updated 2026-01-08
• A Long-Term Study of TAU-284 in Pediatric Patients With Perennial Allergic Rhinitis
  Completed · Phase 3 · Interventional · 58 enrolled · Tanabe Pharma Corporation
  NCT01900054updated 2026-01-07
• A Confirmatory Study of TAU-284 in Pediatric Patients With Perennial Allergic Rhinitis
  Completed · Phase 3 · Interventional · 490 enrolled · Tanabe Pharma Corporation
  NCT01425632updated 2026-01-07
• Clinical Study for the Evaluation of Safety and Tolerability of PRO-172 Ophthalmic Solution+
  Completed · Phase 1 · Interventional · 22 enrolled · Laboratorios Sophia S.A de C.V.
  NCT04693429updated 2025-07-16
• Effects of Second-generation Antihistamine Bepotastine on Cough Outcomes in Cough Patients With Allergic Rhinitis
  Completed · Phase 4 · Interventional · 50 enrolled · Asan Medical Center
  NCT04877678updated 2023-01-05
• Efficacy and Toxicity of Bepotastine 1,5% PF vs Olopatadine 0,2% With BAK on Allergic Conjunctivitis Treatment
  Completed · Phase 4 · Interventional · 97 enrolled · Laboratorios Poen
  NCT04776096updated 2022-12-15
• Bepotastine Besilate-corticosteroid Nasal Spray Combination Compared to Placebo, Bepotastine Besilate Nasal Spray, and Corticosteroid Nasal Spray in the Treatment of Patients With Seasonal Allergic Rhinitis
  Completed · Phase 2 · Interventional · 606 enrolled · Bausch & Lomb Incorporated
  NCT01578278updated 2020-10-05
• Bepotastine Besilate Nasal Sprays in the Treatment of Seasonal Allergic Rhinitis (SAR)
  Completed · Phase 2 · Interventional · 617 enrolled · Bausch & Lomb Incorporated
  NCT01753739updated 2020-10-05
• Safety and Efficacy of Bepotastine Besilate Nasal Spray in the Treatment of Seasonal Allergic Rhinitis
  Completed · Phase 2 · Interventional · 601 enrolled · Bausch & Lomb Incorporated
  NCT01277341updated 2020-10-05

Frequently asked questions

How does Bepotastine work?

Bepotastine is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from mast cells.

What is Bepotastine used for?

According to FDA labeling, Bepotastine carries indications including: BEPREVE ® (bepotastine besilate ophthalmic solution) 1.5% is a histamine H 1 receptor antagonist indicated for the treatment of itching associated with signs and symptoms of allergic conjunctivitis. BEPREVE is a histamine H1 receptor antagonist indicated for the treatment of itching associated with allergic conjunctivitis.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Bepotastine?

Bepotastine is classified as Histamine-1 Receptor Antagonist, Histamine H1 Receptor Antagonists, Decreased Histamine Activity.

What are the brand names for Bepotastine?

Bepotastine is marketed under brand names including Bepreve.

What are the contraindications for Bepotastine?

Bepotastine labeling lists contraindications including: BEPREVE is contraindicated in patients with a history of hypersensitivity reactions to bepotastine or any of the other ingredients [see Adverse Reactions ( 6.2 )] . Hypersensitivity to any component of this product.. Always consult the full prescribing information and a clinician.