{"id":"bepotastine","rwe":[{"pmid":"41724883","year":"2026","title":"Risk of injury associated with the sedative potential of second-generation antihistamines: A nationwide retrospective cohort study.","finding":"","journal":"British journal of clinical pharmacology","studyType":"Clinical Study"},{"pmid":"41315830","year":"2025","title":"A fluorescence-off based approach for sensitive determination of bepotastine in pharmaceutical and biological matrices considering human safety aspects: sustainability assessment.","finding":"","journal":"Scientific reports","studyType":"Clinical Study"},{"pmid":"41146419","year":"2025","title":"BINOL-3,3'-Dicarboxylic Acid: Resolution for the Key Intermediate of (S)-bepotastine.","finding":"","journal":"Chirality","studyType":"Clinical Study"},{"pmid":"30000754","year":"2006","title":"Bepotastine.","finding":"","journal":"","studyType":"Clinical Study"},{"pmid":"40938791","year":"2025","title":"Comparative Effectiveness and Safety of Second-Generation Antihistamines Treatments for Chronic Urticaria: A Network Meta-Analysis.","finding":"","journal":"International archives of allergy and immunology","studyType":"Clinical Study"}],"_fda":{"id":"a4c88d72-eb17-446a-9da5-6bcf1263377f","set_id":"68bbf6a0-c4b5-47c1-8a1c-08220fbdbce6","openfda":{"unii":["6W18MO1QR3"],"route":["OPHTHALMIC"],"rxcui":["863038","863042"],"spl_id":["a4c88d72-eb17-446a-9da5-6bcf1263377f"],"brand_name":["Bepreve"],"spl_set_id":["68bbf6a0-c4b5-47c1-8a1c-08220fbdbce6"],"package_ndc":["24208-629-02","24208-629-01","24208-629-03"],"product_ndc":["24208-629"],"generic_name":["BEPOTASTINE BESILATE"],"product_type":["HUMAN PRESCRIPTION DRUG"],"substance_name":["BEPOTASTINE BESYLATE"],"manufacturer_name":["Bausch & Lomb Incorporated"],"application_number":["NDA022288"],"is_original_packager":[true]},"version":"14","pregnancy":["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). Oral administration of bepotastine besilate to pregnant rats throughout organogenesis produced skeletal anomalies at 1,000 mg/kg/day (5,400 times higher than the maximum RHOD, on a mg/m 2 basis), a dose that also produced maternal toxicity and lethality. No teratogenic effects were observed in rats at maternal doses up to 200 mg/kg/day (corresponding to an estimated blood plasma concentration 3,300 times higher than that anticipated in humans at the maximum RHOD). A maternal NOAEL was observed at 10 mg/kg/day (54 times higher than the maximum RHOD, on a mg/m 2 basis). Following a single 3 mg/kg oral dose in rats (16 times higher than the maximum RHOD, on a mg/m 2 basis), the concentration of radio-labeled bepotastine besilate was similar in fetal liver and maternal blood plasma. The concentration in other fetal tissues was one-third to one-tenth the concentration in maternal blood plasma. In a pre/postnatal development study, oral administration of bepotastine besilate to rats during the perinatal and lactation periods produced an increase in stillbirths and decreased growth and development in offspring at a maternal dose of 1,000 mg/kg/day (5,400 times higher than the maximum RHOD, on a mg/m 2 basis). There were no observed adverse effects on offspring of rats treated with 100 mg/kg/day (540 times higher than the maximum RHOD, on a mg/m 2 basis). Effects on parturition and maternal lethality were observed at 100 mg/kg/day and 1,000 mg/kg/day, respectively. A maternal NOAEL was observed at 10 mg/kg/day (54 times higher than the maximum RHOD, on a mg/m 2 basis)."],"description":["11 DESCRIPTION BEPREVE (bepotastine besilate ophthalmic solution) 1.5% is a sterile, topically administered drug for ophthalmic use. Each mL of BEPREVE contains 15 mg bepotastine besilate. Bepotastine besilate is designated chemically as (+) -4-[[(S)-p-chloro-alpha -2-pyridylbenzyl]oxy]-1-piperidine butyric acid monobenzenesulfonate. The chemical structure for bepotastine besilate is: Bepotastine besilate is a white to pale yellowish-white crystalline powder. The molecular weight of bepotastine besilate is 547.06 daltons. BEPREVE ophthalmic solution is supplied as a sterile, aqueous 1.5% solution, with an approximate pH of 6.8. The osmolality of BEPREVE (bepotastine besilate ophthalmic solution) 1.5% is approximately 295 mOsm/kg. Each mL of BEPREVE (bepotastine besilate ophthalmic solution) 1.5% contains: • Active: bepotastine besilate 15 mg (equivalent to 10.7 mg bepotastine) • Inactives: monobasic sodium phosphate dihydrate, sodium chloride, sodium hydroxide to adjust pH, and water for injection, USP • Preservative: benzalkonium chloride 0.005% Chemical Structure"],"how_supplied":["16 HOW SUPPLIED/STORAGE AND HANDLING BEPREVE (bepotastine besilate ophthalmic solution) 1.5% is supplied in a white low density polyethylene bottle with a sterile linear low density polyethylene controlled dropper tip and a white polypropylene cap in the following sizes: NDC 24208-629-02 5 mL Bottle NDC 24208-629-01 10 mL Bottle Storage: Store at 15°C to 25°C (59°F to 77°F)."],"geriatric_use":["8.5 Geriatric Use No overall differences in safety or effectiveness have been observed between elderly and younger patients."],"pediatric_use":["8.4 Pediatric Use Safety and efficacy of BEPREVE (bepotastine besilate ophthalmic solution) 1.5% have not been established in pediatric patients under 2 years of age. Efficacy in pediatric patients under 10 years of age was extrapolated from clinical trials conducted in pediatric patients greater than 10 years of age and from adults."],"effective_time":"20220831","clinical_studies":["14 CLINICAL STUDIES Clinical efficacy was evaluated in two conjunctival allergen challenge (CAC) studies (237 patients). BEPREVE (bepotastine besilate ophthalmic solution) 1.5% was more effective than its vehicle for relieving ocular itching induced by an ocular allergen challenge, both at a CAC 15 minutes post-dosing and a CAC 8 hours post-dosing of BEPREVE. The safety of BEPREVE was evaluated in a randomized clinical study of 861 subjects over a period of 6 weeks."],"pharmacokinetics":["12.3 Pharmacokinetics 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. Maximum plasma concentrations for the 1% and 1.5% strengths were 5.1 ± 2.5 ng/mL and 7.3 ± 1.9 ng/mL, respectively. Plasma concentrations at 24 hours post-instillation were below the quantifiable limit (2 ng/mL) in 11/12 subjects in the two dose groups. Distribution: The extent of protein binding of bepotastine is approximately 55% and independent of bepotastine concentration. Metabolism: In vitro metabolism studies with human liver microsomes demonstrated that bepotastine is minimally metabolized by CYP450 isozymes. In vitro studies demonstrated that bepotastine besilate does not inhibit the metabolism of various cytochrome P450 substrates via inhibition of CYP3A4, CYP2C9, and CYP2C19. The effect of bepotastine besilate on the metabolism of substrates of CYP1A2, CYP2C8, and CYP2D6 was not studied. Bepotastine besilate has a low potential for drug interaction via inhibition of CYP3A4, CYP2C9, and CYP2C19. Excretion: The main route of elimination of bepotastine besilate is urinary excretion (with approximately 75-90% excreted unchanged in urine)."],"adverse_reactions":["6 ADVERSE REACTIONS 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.","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."],"contraindications":["4 CONTRAINDICATIONS 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. ( 4 )"],"mechanism_of_action":["12.1 Mechanism of Action Bepotastine is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from mast cells."],"clinical_pharmacology":["12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Bepotastine is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from mast cells. 12.3 Pharmacokinetics 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. Maximum plasma concentrations for the 1% and 1.5% strengths were 5.1 ± 2.5 ng/mL and 7.3 ± 1.9 ng/mL, respectively. Plasma concentrations at 24 hours post-instillation were below the quantifiable limit (2 ng/mL) in 11/12 subjects in the two dose groups. Distribution: The extent of protein binding of bepotastine is approximately 55% and independent of bepotastine concentration. Metabolism: In vitro metabolism studies with human liver microsomes demonstrated that bepotastine is minimally metabolized by CYP450 isozymes. In vitro studies demonstrated that bepotastine besilate does not inhibit the metabolism of various cytochrome P450 substrates via inhibition of CYP3A4, CYP2C9, and CYP2C19. The effect of bepotastine besilate on the metabolism of substrates of CYP1A2, CYP2C8, and CYP2D6 was not studied. Bepotastine besilate has a low potential for drug interaction via inhibition of CYP3A4, CYP2C9, and CYP2C19. Excretion: The main route of elimination of bepotastine besilate is urinary excretion (with approximately 75-90% excreted unchanged in urine)."],"indications_and_usage":["1 INDICATIONS AND USAGE 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. ( 1 )"],"warnings_and_cautions":["5 WARNINGS AND PRECAUTIONS • 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.","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."],"nonclinical_toxicology":["13 NONCLINICAL TOXICOLOGY 13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis Long-term dietary studies in mice and rats were conducted to evaluate the carcinogenic potential of bepotastine besilate. Bepotastine besilate did not significantly induce neoplasms in mice receiving a nominal dose of up to 200 mg/kg/day for 21 months, or in rats receiving a nominal dose of up to 97 mg/kg/day for 24 months. These dose levels correspond to systemic exposures approximately 350 and 200 times higher than that achieved at the RHOD, respectively. The no observable adverse effect level for bepotastine besilate based on nominal dose levels in carcinogenicity tests were 18.7 to 19.9 mg/kg/day in mice and 9.6 to 9.8 mg/kg/day in rats (corresponding to systemic exposures approximately 60 and 20 times higher than that anticipated in humans at RHOD, respectively). Mutagenesis There was no evidence of genotoxicity in the Ames test (mutagenicity), in CHO cells (chromosome aberration), in mouse hepatocytes (unscheduled DNA synthesis), or in the mouse micronucleus test. Impairment of Fertility Oral administration of bepotastine to male and female rats at doses up to 1,000 mg/kg/day (5,400 times higher than the maximum RHOD, on a mg/m 2 basis) resulted in reduction in fertility index and surviving fetuses. Oral administration of bepotastine besilate produced no observed adverse effects on fertility or reproduction in rats at oral doses up to 200 mg/kg/day (corresponding to an estimated blood plasma concentration 3,300 times higher than that anticipated in humans at the RHOD)."],"information_for_patients":["17 PATIENT COUNSELING INFORMATION • Sterility of Dropper Tip Advise patients not to touch the dropper tip to any surface, as this may contaminate the solution and to keep the bottle tightly closed when not in use. Distributed by: Bausch & Lomb Americas Inc. Bridgewater, NJ 08807 USA Manufactured by: Bausch & Lomb Incorporated Tampa, FL 33637 USA Under license from: Senju Pharmaceutical Co., Ltd. Osaka, Japan 541-0046 U.S. Patent Numbers: 8,784,789 and 8,877,168 BEPREVE is a trademark of Bausch & Lomb Incorporated or its affiliates. © 2022 Bausch & Lomb Incorporated or its affiliates 9291104 (folded) 9291004 (flat)"],"dosage_and_administration":["2 DOSAGE AND ADMINISTRATION 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 )"],"spl_product_data_elements":["Bepreve bepotastine besilate BENZALKONIUM CHLORIDE SODIUM PHOSPHATE, MONOBASIC, DIHYDRATE SODIUM CHLORIDE SODIUM HYDROXIDE WATER BEPOTASTINE BESYLATE BEPOTASTINE"],"dosage_forms_and_strengths":["3 DOSAGE FORMS AND STRENGTHS Ophthalmic solution containing bepotastine besilate 15 mg/mL (1.5%). Ophthalmic solution containing bepotastine besilate, 15 mg/mL (1.5%). ( 3 )"],"use_in_specific_populations":["8 USE IN SPECIFIC POPULATIONS 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). Oral administration of bepotastine besilate to pregnant rats throughout organogenesis produced skeletal anomalies at 1,000 mg/kg/day (5,400 times higher than the maximum RHOD, on a mg/m 2 basis), a dose that also produced maternal toxicity and lethality. No teratogenic effects were observed in rats at maternal doses up to 200 mg/kg/day (corresponding to an estimated blood plasma concentration 3,300 times higher than that anticipated in humans at the maximum RHOD). A maternal NOAEL was observed at 10 mg/kg/day (54 times higher than the maximum RHOD, on a mg/m 2 basis). Following a single 3 mg/kg oral dose in rats (16 times higher than the maximum RHOD, on a mg/m 2 basis), the concentration of radio-labeled bepotastine besilate was similar in fetal liver and maternal blood plasma. The concentration in other fetal tissues was one-third to one-tenth the concentration in maternal blood plasma. In a pre/postnatal development study, oral administration of bepotastine besilate to rats during the perinatal and lactation periods produced an increase in stillbirths and decreased growth and development in offspring at a maternal dose of 1,000 mg/kg/day (5,400 times higher than the maximum RHOD, on a mg/m 2 basis). There were no observed adverse effects on offspring of rats treated with 100 mg/kg/day (540 times higher than the maximum RHOD, on a mg/m 2 basis). Effects on parturition and maternal lethality were observed at 100 mg/kg/day and 1,000 mg/kg/day, respectively. A maternal NOAEL was observed at 10 mg/kg/day (54 times higher than the maximum RHOD, on a mg/m 2 basis). 8.2 Lactation Risk Summary There are no data on the presence of BEPREVE in human milk, the effects on the breastfed infant or the effects on milk production. The developmental and health benefits of breastfeeding should be considered, along with the mother’s clinical need for BEPREVE, and any potential adverse effects on the breastfed infant from BEPREVE. Animal Data Following a single 3 mg/kg oral dose (16 times the maximum RHOD, on a mg/m2 basis) of radio-labeled bepotastine besilate to nursing rats 11 days after delivery, the maximum concentration of radioactivity in milk was 0.40 mcg-eq/mL 1 hour after administration; at 48 hours after administration, the radioactivity concentration was below detection limits. The milk radioactivity concentration was higher than the maternal blood plasma radioactivity concentration at each time of measurement. It is not known whether bepotastine besilate would be present in maternal milk following topical ocular administration. 8.4 Pediatric Use Safety and efficacy of BEPREVE (bepotastine besilate ophthalmic solution) 1.5% have not been established in pediatric patients under 2 years of age. Efficacy in pediatric patients under 10 years of age was extrapolated from clinical trials conducted in pediatric patients greater than 10 years of age and from adults. 8.5 Geriatric Use No overall differences in safety or effectiveness have been observed between elderly and younger patients."],"package_label_principal_display_panel":["PACKAGE/LABEL PRINCIPAL DISPLAY PANEL NDC 24208-629-02 BEPREVE ® (bepotastine besilate ophthalmic solution) 1.5% Sterile 5 mL Rx only FOR TOPICAL OPHTHALMIC USE BAUSCH + LOMB 9528502 AB52107 5ML CARTON"],"carcinogenesis_and_mutagenesis_and_impairment_of_fertility":["13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis Long-term dietary studies in mice and rats were conducted to evaluate the carcinogenic potential of bepotastine besilate. Bepotastine besilate did not significantly induce neoplasms in mice receiving a nominal dose of up to 200 mg/kg/day for 21 months, or in rats receiving a nominal dose of up to 97 mg/kg/day for 24 months. These dose levels correspond to systemic exposures approximately 350 and 200 times higher than that achieved at the RHOD, respectively. The no observable adverse effect level for bepotastine besilate based on nominal dose levels in carcinogenicity tests were 18.7 to 19.9 mg/kg/day in mice and 9.6 to 9.8 mg/kg/day in rats (corresponding to systemic exposures approximately 60 and 20 times higher than that anticipated in humans at RHOD, respectively). Mutagenesis There was no evidence of genotoxicity in the Ames test (mutagenicity), in CHO cells (chromosome aberration), in mouse hepatocytes (unscheduled DNA synthesis), or in the mouse micronucleus test. Impairment of Fertility Oral administration of bepotastine to male and female rats at doses up to 1,000 mg/kg/day (5,400 times higher than the maximum RHOD, on a mg/m 2 basis) resulted in reduction in fertility index and surviving fetuses. Oral administration of bepotastine besilate produced no observed adverse effects on fertility or reproduction in rats at oral doses up to 200 mg/kg/day (corresponding to an estimated blood plasma concentration 3,300 times higher than that anticipated in humans at the RHOD)."]},"tags":[{"label":"Histamine-1 Receptor Antagonist","category":"class"},{"label":"Small Molecule","category":"modality"},{"label":"Histamine H1 receptor","category":"target"},{"label":"HRH1","category":"gene"},{"label":"Ophthalmic","category":"route"},{"label":"Solution/ Drops","category":"form"},{"label":"Off-Patent","category":"patent"},{"label":"Generic Available","category":"availability"},{"label":"Mature","category":"status"},{"label":"Allergic conjunctivitis","category":"indication"},{"label":"Bausch And Lomb Inc","category":"company"},{"label":"Approved 2000s","category":"decade"},{"label":"Anti-Allergic Agents","category":"pharmacology"}],"phase":"marketed","safety":{"boxedWarnings":[],"safetySignals":[{"llr":80.839,"date":"","count":38,"signal":"Hepatic function abnormal","source":"DrugCentral FAERS","actionTaken":"Reported 38 times (LLR=81)"},{"llr":39.471,"date":"","count":28,"signal":"Interstitial lung disease","source":"DrugCentral FAERS","actionTaken":"Reported 28 times (LLR=39)"},{"llr":36.075,"date":"","count":34,"signal":"Platelet count decreased","source":"DrugCentral FAERS","actionTaken":"Reported 34 times (LLR=36)"},{"llr":35.79,"date":"","count":14,"signal":"Erythema multiforme","source":"DrugCentral FAERS","actionTaken":"Reported 14 times (LLR=36)"},{"llr":31.322,"date":"","count":17,"signal":"Drug eruption","source":"DrugCentral FAERS","actionTaken":"Reported 17 times (LLR=31)"},{"llr":30.047,"date":"","count":22,"signal":"Neutrophil count decreased","source":"DrugCentral FAERS","actionTaken":"Reported 22 times (LLR=30)"},{"llr":27.278,"date":"","count":11,"signal":"Pemphigoid","source":"DrugCentral FAERS","actionTaken":"Reported 11 times (LLR=27)"},{"llr":27.207,"date":"","count":4,"signal":"Nasal turbinate abnormality","source":"DrugCentral FAERS","actionTaken":"Reported 4 times (LLR=27)"},{"llr":26.618,"date":"","count":19,"signal":"Liver disorder","source":"DrugCentral FAERS","actionTaken":"Reported 19 times (LLR=27)"},{"llr":24.657,"date":"","count":7,"signal":"Hypopituitarism","source":"DrugCentral FAERS","actionTaken":"Reported 7 times (LLR=25)"},{"llr":23.639,"date":"","count":5,"signal":"Syphilis","source":"DrugCentral FAERS","actionTaken":"Reported 5 times (LLR=24)"},{"llr":22.721,"date":"","count":4,"signal":"Dermatophytosis of nail","source":"DrugCentral FAERS","actionTaken":"Reported 4 times (LLR=23)"}],"commonSideEffects":[{"effect":"mild taste following instillation","drugRate":"approximately 25%","_validated":true,"placeboRate":""}],"contraindications":["BEPREVE is contraindicated in patients with a history of hypersensitivity reactions to bepotastine or any of the other ingredients.","Hypersensitivity to any component of this product."],"specialPopulations":{"Lactation":"There are no data on the presence of bepotastine besilate in human milk, the effects on the breastfed infant or the effects on milk production. The developmental and health benefits of breastfeeding should be considered, along with the mothers clinical need for bepotastine besilate ophthalmic solution, and any potential adverse effects on the breastfed infant from bepotastine besilate ophthalmic solution.","Pregnancy":"There are no available human data for the use of Bepotastine Besilate Ophthalmic Solution 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 mg/m2 basis).","Geriatric use":"No overall differences in safety or effectiveness have been observed between elderly and younger patients.","Paediatric use":"Safety and efficacy of bepotastine besilate ophthalmic solution, 1.5% have not been established in pediatric patients under 2 years of age. Efficacy in pediatric patients under 10 years of age was extrapolated from clinical trials conducted in pediatric patients greater than 10 years of age and from adults."}},"trials":[],"aliases":[],"company":"Bausch Health","patents":[],"pricing":[{"market":"United States","source":"CMS National Average Drug Acquisition Cost (NADAC)","asOfDate":"2024-01-03","unitCost":"$19.3224/ML","priceType":"NADAC","sourceUrl":"https://data.medicaid.gov/dataset/4j6z-xnwq","annualCost":"$6,956","description":"BEPOTASTINE 1.5% EYE DROP","retrievedDate":"2026-04-07"}],"_fixedAt":"2026-03-30T16:56:24.299330","_sources":{"trials":{"url":"https://clinicaltrials.gov/search?intr=BEPOTASTINE","method":"api_direct","source":"ClinicalTrials.gov","rawText":"","confidence":1,"sourceType":"ctgov","retrievedAt":"2026-04-20T02:06:19.571577+00:00"},"regulatory.ca":{"url":"","method":"api_direct","source":"Health Canada DPD","rawText":"","confidence":1,"sourceType":"health_canada_dpd","retrievedAt":"2026-04-20T02:06:26.693609+00:00"},"publicationCount":{"url":"https://pubmed.ncbi.nlm.nih.gov/?term=BEPOTASTINE","method":"api_direct","source":"PubMed/NCBI","rawText":"","confidence":1,"sourceType":"pubmed","retrievedAt":"2026-04-20T02:06:27.068372+00:00"},"administration.route":{"url":"","method":"deterministic","source":"FDA Label","rawText":"","confidence":1,"sourceType":"fda_label","retrievedAt":"2026-04-20T02:06:18.466078+00:00"},"safety.boxedWarnings":{"url":"","method":"deterministic","source":"FDA Label (no boxed warning)","rawText":"","confidence":1,"sourceType":"fda_label","retrievedAt":"2026-04-20T02:06:18.466101+00:00"},"mechanism.oneSentence":{"url":"","method":"ai_extraction","source":"FDA Label + AI","aiModel":"featherless","rawText":"12.1 Mechanism of Action Bepotastine is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from mast cells.","confidence":0.95,"sourceType":"fda_label","retrievedAt":"2026-04-20T02:06:37.577148+00:00"},"crossReferences.chemblId":{"url":"https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL1201758/","method":"api_direct","source":"ChEMBL (EMBL-EBI)","rawText":"","confidence":1,"sourceType":"chembl","retrievedAt":"2026-04-20T02:06:27.970953+00:00"},"safety.commonSideEffects":{"url":"","method":"ai_extraction","source":"FDA Label + AI","aiModel":"featherless","rawText":"6 ADVERSE REACTIONS 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, ","confidence":0.95,"sourceType":"fda_label","retrievedAt":"2026-04-20T02:06:41.549297+00:00"},"safety.contraindications":{"url":"","method":"ai_extraction","source":"FDA Label + AI","aiModel":"featherless","rawText":"","confidence":0.95,"sourceType":"fda_label","retrievedAt":"2026-04-20T02:06:45.817334+00:00"},"regulatory.fda_application":{"url":"","method":"deterministic","source":"FDA Label","rawText":"NDA022288","confidence":1,"sourceType":"fda_label","retrievedAt":"2026-04-20T02:06:18.466112+00:00"}},"allNames":"bepreve","offLabel":[],"synonyms":["bepotastine","bepotastine besilate","bepreve","bepotastine besylate"],"timeline":[{"date":"2009-01-01","type":"neutral","source":"FDA Orange Book","milestone":"Rights transferred from BAUSCH AND LOMB INC to Bausch And Lomb Inc"},{"date":"2009-09-08","type":"positive","source":"DrugCentral","milestone":"FDA approval (Bausch And Lomb Inc)"},{"date":"2023-04-05","type":"neutral","source":"FDA Orange Book","milestone":"Generic entry — 3 manufacturers approved"}],"aiSummary":"Bepotastine (Bepreve) is a small molecule histamine-1 receptor antagonist developed by Bausch and Lomb Inc. It targets the histamine H1 receptor to treat allergic conjunctivitis. Bepreve is a generic medication, off-patent since there are no active Orange Book patents. It was FDA approved in 2009 for its approved indications. As a generic medication, it is available from multiple manufacturers.","brandName":"Bepreve","ecosystem":[{"indication":"Allergic conjunctivitis","otherDrugs":[{"name":"acrivastine","slug":"acrivastine","company":"Auxilium Pharms Inc"},{"name":"alcaftadine","slug":"alcaftadine","company":"Allergan"},{"name":"alimemazine","slug":"alimemazine","company":"Allergan Herbert"},{"name":"antazoline","slug":"antazoline","company":"Novartis"}],"globalPrevalence":null}],"mechanism":{"target":"H1-receptor, mast cells","novelty":"Follow-on","targets":[{"gene":"HRH1","source":"DrugCentral","target":"Histamine H1 receptor","protein":"Histamine H1 receptor","isPrimary":true,"activityType":"","activityValue":null}],"modality":"Small molecule","drugClass":"Histamine-1 Receptor Antagonist","explanation":"Bepotastine works by directly blocking H1 receptors, which prevents the effects of histamine. Additionally, it stops mast cells from releasing histamine, reducing allergic symptoms.","oneSentence":"Bepotastine blocks H1 receptors and inhibits histamine release from mast cells.","technicalDetail":"Bepotastine is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from mast cells."},"commercial":{"launchDate":"2009","_launchSource":"DrugCentral (FDA 2009-09-08, BAUSCH AND LOMB INC)"},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/341","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=BEPOTASTINE","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=BEPOTASTINE","fields":["publications"],"source":"PubMed/NCBI"},{"id":4,"url":"https://www.fda.gov/drugs/drug-approvals-and-databases/orange-book-data-files","fields":["patents","exclusivity","genericManufacturers"],"source":"FDA Orange Book"}],"_enrichedAt":"2026-03-30T08:59:48.737735","_validation":{"fieldsValidated":2,"lastValidatedAt":"2026-04-20T02:06:46.711093+00:00","fieldsConflicting":0,"overallConfidence":0.95},"biosimilars":[],"competitors":[{"drugName":"acrivastine","drugSlug":"acrivastine","fdaApproval":"1994-03-25","relationship":"same-target"},{"drugName":"alcaftadine","drugSlug":"alcaftadine","fdaApproval":"2010-07-28","patentExpiry":"Mar 19, 2027","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"alimemazine","drugSlug":"alimemazine","fdaApproval":"","relationship":"same-target"},{"drugName":"amitriptyline","drugSlug":"amitriptyline","fdaApproval":"1961-04-07","genericCount":33,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"amoxapine","drugSlug":"amoxapine","fdaApproval":"1980-09-22","genericCount":3,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"antazoline","drugSlug":"antazoline","fdaApproval":"1990-04-30","relationship":"same-target"},{"drugName":"aripiprazole","drugSlug":"aripiprazole","fdaApproval":"2002-11-15","patentExpiry":"Sep 24, 2033","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"aripiprazole lauroxil","drugSlug":"aripiprazole-lauroxil","fdaApproval":"2015-10-05","patentExpiry":"Sep 8, 2035","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"asenapine","drugSlug":"asenapine","fdaApproval":"2009-08-13","patentExpiry":"Sep 22, 2033","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"astemizole","drugSlug":"astemizole","fdaApproval":"1988-12-31","relationship":"same-target"}],"dataSources":[{"url":"https://data.medicaid.gov/dataset/4j6z-xnwq","name":"CMS National Average Drug Acquisition Cost (NADAC)","fields":["pricing"],"retrievedDate":"2026-04-07"}],"genericName":"bepotastine","indications":{"approved":[{"name":"Allergic conjunctivitis","source":"DrugCentral","snomedId":473460002,"regulator":"FDA"}],"offLabel":[],"pipeline":[]},"_fixedFields":["primaryTarget"],"currentOwner":"Bausch And Lomb Inc","drugCategory":"mature","labelChanges":[],"patentStatus":"Off-patent — no active Orange Book patents","relatedDrugs":[{"drugId":"acrivastine","brandName":"acrivastine","genericName":"acrivastine","approvalYear":"1994","relationship":"same-target"},{"drugId":"alcaftadine","brandName":"alcaftadine","genericName":"alcaftadine","approvalYear":"2010","relationship":"same-target"},{"drugId":"alimemazine","brandName":"alimemazine","genericName":"alimemazine","approvalYear":"","relationship":"same-target"},{"drugId":"amitriptyline","brandName":"amitriptyline","genericName":"amitriptyline","approvalYear":"1961","relationship":"same-target"},{"drugId":"amoxapine","brandName":"amoxapine","genericName":"amoxapine","approvalYear":"1980","relationship":"same-target"},{"drugId":"antazoline","brandName":"antazoline","genericName":"antazoline","approvalYear":"1990","relationship":"same-target"},{"drugId":"aripiprazole","brandName":"aripiprazole","genericName":"aripiprazole","approvalYear":"2002","relationship":"same-target"},{"drugId":"aripiprazole-lauroxil","brandName":"aripiprazole lauroxil","genericName":"aripiprazole lauroxil","approvalYear":"2015","relationship":"same-target"},{"drugId":"asenapine","brandName":"asenapine","genericName":"asenapine","approvalYear":"2009","relationship":"same-target"},{"drugId":"astemizole","brandName":"astemizole","genericName":"astemizole","approvalYear":"1988","relationship":"same-target"}],"trialDetails":[{"nctId":"NCT01840605","phase":"PHASE3","title":"A Confirmatory Study of TAU-284 in Pediatric Patients With Atopic Dermatitis","status":"COMPLETED","sponsor":"Tanabe Pharma Corporation","startDate":"2013-03","conditions":["Dermatitis","Atopic"],"enrollment":303,"completionDate":"2013-11"},{"nctId":"NCT01861522","phase":"PHASE3","title":"The Confirmatory Study of TAU-284 in Pediatric Patients With Perennial Allergic Rhinitis","status":"COMPLETED","sponsor":"Tanabe Pharma Corporation","startDate":"2013-04","conditions":["Perennial Allergic Rhinitis"],"enrollment":473,"completionDate":"2013-12"},{"nctId":"NCT01425632","phase":"PHASE3","title":"A Confirmatory Study of TAU-284 in Pediatric Patients With Perennial Allergic Rhinitis","status":"COMPLETED","sponsor":"Tanabe Pharma Corporation","startDate":"2011-08","conditions":["Perennial Allergic Rhinitis"],"enrollment":490,"completionDate":"2011-12"},{"nctId":"NCT01900054","phase":"PHASE3","title":"A Long-Term Study of TAU-284 in Pediatric Patients With Perennial Allergic Rhinitis","status":"COMPLETED","sponsor":"Tanabe Pharma Corporation","startDate":"2013-06","conditions":["Perennial Allergic Rhinitis"],"enrollment":58,"completionDate":"2013-11"},{"nctId":"NCT04693429","phase":"PHASE1","title":"Clinical Study for the Evaluation of Safety and Tolerability of PRO-172 Ophthalmic Solution+","status":"COMPLETED","sponsor":"Laboratorios Sophia S.A de C.V.","startDate":"2020-09-24","conditions":["Safety","Tolerability","Ocular Surface","Ocular Comfort"],"enrollment":22,"completionDate":"2020-12-08"},{"nctId":"NCT04877678","phase":"PHASE4","title":"Effects of Second-generation Antihistamine Bepotastine on Cough Outcomes in Cough Patients With Allergic Rhinitis","status":"COMPLETED","sponsor":"Asan Medical Center","startDate":"2021-10-01","conditions":["Allergic Rhinitis","Cough"],"enrollment":50,"completionDate":"2022-10-31"},{"nctId":"NCT04776096","phase":"PHASE4","title":"Efficacy and Toxicity of Bepotastine 1,5% PF vs Olopatadine 0,2% With BAK on Allergic Conjunctivitis Treatment","status":"COMPLETED","sponsor":"Laboratorios Poen","startDate":"2021-03-10","conditions":["Allergic Conjunctivitis"],"enrollment":97,"completionDate":"2022-08-18"},{"nctId":"NCT01277341","phase":"PHASE2","title":"Safety and Efficacy of Bepotastine Besilate Nasal Spray in the Treatment of Seasonal Allergic Rhinitis","status":"COMPLETED","sponsor":"Bausch & Lomb Incorporated","startDate":"2010-12","conditions":["Seasonal Allergic Rhinitis"],"enrollment":601,"completionDate":"2011-05"},{"nctId":"NCT01578278","phase":"PHASE2","title":"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","status":"COMPLETED","sponsor":"Bausch & Lomb Incorporated","startDate":"2011-12","conditions":["Seasonal Allergic Rhinitis"],"enrollment":606,"completionDate":"2012-08"},{"nctId":"NCT01753739","phase":"PHASE2","title":"Bepotastine Besilate Nasal Sprays in the Treatment of Seasonal Allergic Rhinitis (SAR)","status":"COMPLETED","sponsor":"Bausch & Lomb Incorporated","startDate":"2013-01","conditions":["Seasonal Allergic Rhinitis"],"enrollment":617,"completionDate":"2013-05"},{"nctId":"NCT01222299","phase":"PHASE1,PHASE2","title":"Safety, Pharmacokinetics, and Efficacy of Bepotastine Besilate Nasal Product After Ragweed Pollen Exposure in an Environmental Chamber","status":"COMPLETED","sponsor":"Bausch & Lomb Incorporated","startDate":"2010-05","conditions":["Seasonal Allergic Rhinitis"],"enrollment":89,"completionDate":"2010-08"},{"nctId":"NCT01174823","phase":"PHASE2","title":"Safety and Efficacy of Bepotastine Besilate Ophthalmic Solution in Seasonal Allergic Conjunctivitis Patients","status":"COMPLETED","sponsor":"Bausch & Lomb Incorporated","startDate":"2010-06","conditions":["Allergic Conjunctivitis"],"enrollment":245,"completionDate":"2010-12"},{"nctId":"NCT01346371","phase":"PHASE4","title":"The Effect of BEPREVE 1.5% on Tear Film Osmolarity and Tear Film Lipid Layer","status":"COMPLETED","sponsor":"Minnesota Eye Consultants, P.A.","startDate":"2011-05","conditions":["Allergic Conjunctivitis"],"enrollment":40,"completionDate":"2012-09"},{"nctId":"NCT03932435","phase":"NA","title":"Bioequivalence Test of \"Dong-a Bepotastine Besilate Tab\" and \"Twolion Tab\"","status":"COMPLETED","sponsor":"Dong-A ST Co., Ltd.","startDate":"2019-04-23","conditions":["Healthy"],"enrollment":32,"completionDate":"2019-05-28"},{"nctId":"NCT04097951","phase":"PHASE1","title":"HDDO-1801 Intervention Trial","status":"UNKNOWN","sponsor":"Hyundai Pharmaceutical Co., LTD.","startDate":"2019-11-08","conditions":["Respiratory Disease"],"enrollment":36,"completionDate":"2020-02-28"},{"nctId":"NCT01443442","phase":"PHASE4","title":"Bepreve vs. Alrex in Subjects With Moderate to Severe Allergic Conjunctivitis","status":"COMPLETED","sponsor":"Southern California College of Optometry at Marshall B. Ketchum University","startDate":"2011-10","conditions":["Allergic Conjunctivitis"],"enrollment":23,"completionDate":"2012-12"},{"nctId":"NCT01339507","phase":"","title":"A Patient Reported Ocular Comfort Assessment Comparing Bepreve to Lastacaft","status":"COMPLETED","sponsor":"Cunningham, Derek N., O.D., P.A.","startDate":"2011-04","conditions":["Allergic Conjunctivitis"],"enrollment":25,"completionDate":"2011-06"},{"nctId":"NCT02332044","phase":"PHASE1","title":"Drug Interaction Study Between Erdosteine and Bepotastine Besilate in Healthy Adult Volunteers","status":"COMPLETED","sponsor":"Daewoong Pharmaceutical Co. LTD.","startDate":"2014-04","conditions":["Healthy"],"enrollment":36,"completionDate":"2015-01"},{"nctId":"NCT01450176","phase":"NA","title":"Comparing Patient Satisfaction With Pataday or Bepreve","status":"COMPLETED","sponsor":"McCabe Vision Center","startDate":"2011-09","conditions":["Eye Allergies"],"enrollment":30,"completionDate":"2011-12"},{"nctId":"NCT01925313","phase":"PHASE1","title":"A Randomized, Open Label, Three-Treatment, Three-Period, Six-Sequence Crossover Study To Compare Safety and Pharmacokinetic Properties of CJ-30044 and Bepotastine Besilate and To Investigate Food-effect on Pharmacokinetics of CJ-30044 in Healthy Adult Male Volunteers","status":"COMPLETED","sponsor":"HK inno.N Corporation","startDate":"2012-12","conditions":["Healthy"],"enrollment":30,"completionDate":"2013-05"},{"nctId":"NCT01897428","phase":"PHASE1","title":"PK Comparisons of Bepotastine Besilate 10 mg and Bepotastine Salicylate 9.64 mg","status":"COMPLETED","sponsor":"Korea University Anam Hospital","startDate":"2011-04","conditions":["Allergic Rhinitis","Urticaria","Pruritus"],"enrollment":26,"completionDate":"2011-08"},{"nctId":"NCT00424398","phase":"PHASE2,PHASE3","title":"Evaluation of the Onset and Duration of Action of Bepotastine Besilate Ophthalmic Solution in Acute Allergic Conjunctivitis","status":"COMPLETED","sponsor":"Bausch & Lomb Incorporated","startDate":"2007-02","conditions":["Conjunctivitis, Allergic"],"enrollment":107,"completionDate":""},{"nctId":"NCT00586625","phase":"PHASE3","title":"Safety Study for Bepotastine Besilate Ophthalmic Solution in Normal Volunteers","status":"COMPLETED","sponsor":"Bausch & Lomb Incorporated","startDate":"2007-10","conditions":["Allergic Conjunctivitis"],"enrollment":861,"completionDate":""},{"nctId":"NCT00586664","phase":"PHASE3","title":"Efficacy and Safety Study of Bepotastine Besilate Ophthalmic Solution in Allergic Conjunctivitis","status":"COMPLETED","sponsor":"Bausch & Lomb Incorporated","startDate":"2007-10","conditions":["Allergic Conjunctivitis"],"enrollment":130,"completionDate":"2008-06"},{"nctId":"NCT01337557","phase":"PHASE4","title":"Use of BEPREVE (Bepotastine Besilate Ophthalmic Solution) 1.5% for Allergic Conjunctivitis and Contact Lenses","status":"UNKNOWN","sponsor":"Hom, Milton M., OD, FAAO","startDate":"2011-05","conditions":["Allergic Conjunctivitis"],"enrollment":24,"completionDate":"2011-11"},{"nctId":"NCT01128556","phase":"PHASE4","title":"The Evaluation of Bepreve on the Measurement of Wheal and Flare Response From Histamine Skin Prick Testing","status":"COMPLETED","sponsor":"North Texas Institute for Clinical Trials","startDate":"2010-04","conditions":["Histamine Responsive Allergy Patients"],"enrollment":30,"completionDate":"2010-06"}],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"administration":{"route":"Ophthalmic","formulation":"Solution/ Drops","formulations":[{"form":"SOLUTION/ DROPS","route":"OPHTHALMIC","productName":"Bepotastine Besilate"},{"form":"SOLUTION/ DROPS","route":"OPHTHALMIC","productName":"Bepotastine Besilate Ophthalmic Solution 1.5%"},{"form":"SOLUTION/ DROPS","route":"OPHTHALMIC","productName":"BEPREVE"},{"form":"SOLUTION/ DROPS","route":"OPHTHALMIC","productName":"Bepreve"},{"form":"SOLUTION/ DROPS","route":"OPHTHALMIC","productName":"Bepotastine Besilate"}]},"_patentsChecked":true,"crossReferences":{"NUI":"N0000181653","MMSL":"167734","NDDF":"010865","UNII":"HYD2U48IAS","VUID":"4029223","CHEBI":"CHEBI:71204","VANDF":"4029223","INN_ID":"7648","RXNORM":"658552","UMLSCUI":"C2698371","chemblId":"CHEMBL1201758","ChEMBL_ID":"CHEMBL1201758","KEGG_DRUG":"D01654","DRUGBANK_ID":"DB04890","PUBCHEM_CID":"164522","SNOMEDCT_US":"443616002","IUPHAR_LIGAND_ID":"7466","SECONDARY_CAS_RN":"190786-44-8","MESH_SUPPLEMENTAL_RECORD_UI":"C108476"},"formularyStatus":[],"_enricherVersion":"v2","developmentCodes":[],"ownershipHistory":[{"period":"2009-","companyName":"Bausch And Lomb Inc","relationship":"Original Developer"}],"publicationCount":96,"therapeuticAreas":["Other"],"biosimilarFilings":[],"originalDeveloper":"Bausch And Lomb Inc","recentPublications":[{"date":"2026 Feb 22","pmid":"41724883","title":"Risk of injury associated with the sedative potential of second-generation antihistamines: A nationwide retrospective cohort study.","journal":"British journal of clinical pharmacology"},{"date":"2025 Nov 28","pmid":"41315830","title":"A fluorescence-off based approach for sensitive determination of bepotastine in pharmaceutical and biological matrices considering human safety aspects: sustainability assessment.","journal":"Scientific reports"},{"date":"2025 Nov","pmid":"41146419","title":"BINOL-3,3'-Dicarboxylic Acid: Resolution for the Key Intermediate of (S)-bepotastine.","journal":"Chirality"},{"date":"2006","pmid":"30000754","title":"Bepotastine.","journal":""},{"date":"2025 Sep 12","pmid":"40938791","title":"Comparative Effectiveness and Safety of Second-Generation Antihistamines Treatments for Chronic Urticaria: A Network Meta-Analysis.","journal":"International archives of allergy and immunology"}],"companionDiagnostics":[],"genericManufacturers":4,"_genericFilersChecked":true,"genericManufacturerList":["Alembic","Apotex","Mylan","Somerset Theraps Llc"],"status":"approved","companyName":"Bausch And Lomb Inc","companyId":"bausch","modality":"Small molecule","firstApprovalDate":"2009","enrichmentLevel":4,"visitCount":1,"regulatoryByCountry":[{"country_code":"CA","regulator":"Health Canada","status":"approved","approval_date":null,"mah":"","brand_name_local":"","application_number":""},{"country_code":"US","regulator":"FDA","status":"approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null}],"trialStats":{"total":0,"withResults":0},"validation":{"fieldsValidated":2,"lastValidatedAt":"2026-04-20T02:06:46.711093+00:00","fieldsConflicting":0,"overallConfidence":0.95},"verificationStatus":"verified","dataCompleteness":{"mechanism":true,"indications":true,"safety":true,"trials":true,"score":4}}