{"id":"bepotastine-besilate-ophthalmic-solution","_fda":{"id":"de111d74-c740-47b3-adc7-4b855df2c561","set_id":"de111d74-c740-47b3-adc7-4b855df2c561","openfda":{"unii":["6W18MO1QR3"],"route":["OPHTHALMIC"],"rxcui":["863038"],"spl_id":["de111d74-c740-47b3-adc7-4b855df2c561"],"brand_name":["Bepotastine Besilate Ophthalmic Solution 1.5%"],"spl_set_id":["de111d74-c740-47b3-adc7-4b855df2c561"],"package_ndc":["46708-598-10","46708-598-05"],"product_ndc":["46708-598"],"generic_name":["BEPOTASTINE BESILATE OPHTHALMIC SOLUTION 1.5%"],"product_type":["HUMAN PRESCRIPTION DRUG"],"substance_name":["BEPOTASTINE BESILATE"],"manufacturer_name":["Alembic Pharmaceuticals Limited"],"application_number":["ANDA214588"],"is_original_packager":[true]},"version":"1","pregnancy":["8.1 Pregnancy Risk Summary 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 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 5400 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 1000 mg/kg/day (5400 times higher than the maximum RHOD, on a mg/m2 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 3300 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 1000 mg/kg/day (5400 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 1000 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 Bepotastine besilate ophthalmic solution 1.5% is a sterile, topically administered drug for ophthalmic use. Each mL of bepotastine besilate ophthalmic solution 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 white or pale yellowish crystalline powder. The molecular weight of bepotastine besilate is 547.06 daltons. Bepotastine besilate ophthalmic solution is supplied as a sterile, aqueous 1.5% solution, with a pH of 6.8. The osmolality of bepotastine besilate ophthalmic solution 1.5% is approximately 290 mOsm/kg. Each mL Bepotastine besilate ophthalmic solution 1.5% contains: Active: bepotastine besilate 15 mg (equivalent to 10.7 mg bepotastine) Preservative: benzalkonium chloride 0.005% Inactives: monobasic sodium phosphate dihydrate, sodium chloride, sodium hydroxide to adjust pH, and water for injection, USP. bepotastine-structure"],"how_supplied":["16 HOW SUPPLIED/STORAGE AND HANDLING Bepotastine besilate ophthalmic solution 1.5% is supplied in a white low density polyethylene (LDPE) bottle with a white LDPE nozzle and a white high density polyethylene (HDPE) cap in the following size: 10 mL (NDC 46708-598-10) 5 mL (NDC 46708-598-05) 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 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":"20230721","clinical_studies":["14 CLINICAL STUDIES Clinical efficacy was evaluated in two conjunctival allergen challenge (CAC) studies (237 patients). 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 bepotastine besilate ophthalmic solution. The safety of bepotastine besilate ophthalmic solution 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 to 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 to 5% of subjects were eye irritation, headache, and nasopharyngitis. ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Alembic Pharmaceuticals Inc. at 1-866-210-9797 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 6.1 Clinical Trial 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 to 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 bepotastine besilate ophthalmic solution. 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 Bepotastine besilate ophthalmic solution 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."],"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 to 90% excreted unchanged in urine)."],"indications_and_usage":["1 INDICATIONS & USAGE Bepotastine besilate ophthalmic solution 1.5% is a histamine H1 receptor antagonist indicated for the treatment of itching associated with signs and symptoms of allergic conjunctivitis. Bepotastine besilate ophthalmic solution is a histamine H1 receptor antagonist indicated for the treatment of itching associated with allergic conjunctivitis."],"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: Bepotastine besilate ophthalmic solution 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 Bepotastine besilate ophthalmic solution should not be used to treat contact lens-related irritation. Bepotastine besilate ophthalmic solution should not be instilled while wearing contact lenses. Patient should remove contact lenses prior to instillation of bepotastine besilate ophthalmic solution, because benzalkonium chloride may be absorbed by soft contact lenses. Lenses may be reinserted after 10 minutes following administration of bepotastine besilate ophthalmic solution."],"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 1000 mg/kg/day (5400 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 3300 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. Concomitant Use of Contact Lenses Advise patients not to wear a contact lens if their eye is red and that bepotastine besilate ophthalmic solution should not be used to treat contact lens-related irritation. Patients should also be advised to remove contact lenses prior to instillation of bepotastine besilate ophthalmic solution, which may be reinserted after 10 minutes following administration. Rx Only Made in India. Manufactured by: Alembic Pharmaceuticals Limited Karkhadi – 391 450 Gujarat, India Issued: 04/2023"],"dosage_and_administration":["2 DOSAGE & ADMINISTRATION Instill one drop of bepotastine besilate ophthalmic solution into the affected eye(s) twice a day. Remove contact lenses prior to instillation of bepotastine besilate ophthalmic solution. Instill one drop into the affected eye(s) twice a day. (2) Remove contact lenses prior to instillation of Bepotastine besilate ophthalmic solution."],"spl_product_data_elements":["Bepotastine Besilate Ophthalmic Solution 1.5% Bepotastine Besilate Ophthalmic Solution 1.5% BEPOTASTINE BESILATE BEPOTASTINE BENZALKONIUM CHLORIDE SODIUM PHOSPHATE, MONOBASIC, DIHYDRATE SODIUM CHLORIDE SODIUM HYDROXIDE WATER"],"dosage_forms_and_strengths":["3 DOSAGE FORMS & STRENGTHS Ophthalmic solution containing bepotastine besilate 15 mg/mL (1.5%). Ophthalmic solution containing bepotastine besilate, 15 mg/mL (1.5%)."],"use_in_specific_populations":["8 USE IN SPECIFIC POPULATIONS 8.1 Pregnancy Risk Summary 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 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 5400 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 1000 mg/kg/day (5400 times higher than the maximum RHOD, on a mg/m2 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 3300 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 1000 mg/kg/day (5400 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 1000 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 bepotastine besilate ophthalmic solution 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 bepotastine besilate ophthalmic solution, and any potential adverse effects on the breastfed infant from bepotastine besilate ophthalmic solution. Animal Data Following a single 3 mg/kg oral dose (16 times the maximum RHOD, on a mg/m2 basis) of radiolabeled 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 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 Bepotastine Besilate Ophthalmic Solution 1.5% - Bottle Label -5 mL: Bepotastine Besilate Ophthalmic Solution 1.5% - Carton Label -5 mL: Bepotastine Besilate Ophthalmic Solution 1.5% - Bottle Label -10 mL: Bepotastine Besilate Ophthalmic Solution 1.5% - Carton Label -10 mL: bepotastine-bottle-5ml bepotastine-carton-5ml bepotastine-bottle-10ml bepotastine-carton-10ml"],"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 1000 mg/kg/day (5400 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 3300 times higher than that anticipated in humans at the RHOD)."]},"safety":{"boxedWarnings":[],"commonSideEffects":[{"effect":"mild taste following instillation","drugRate":"approximately 25%","_validated":true,"placeboRate":""}],"contraindications":["Bepotastine besilate ophthalmic solution 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."]},"_chembl":null,"_sources":{"trials":{"url":"https://clinicaltrials.gov/search?intr=bepotastine besilate ophthalmic solution","method":"api_direct","source":"ClinicalTrials.gov","rawText":"","confidence":1,"sourceType":"ctgov","retrievedAt":"2026-04-20T05:31:31.188951+00:00"},"aiSummary":{"url":"","method":"ai_extraction","source":"AI Strategic Summary","aiModel":"featherless","rawText":"","confidence":0.9,"sourceType":"ai_extraction","retrievedAt":"2026-04-20T05:32:08.887645+00:00"},"regulatory.ca":{"url":"","method":"api_direct","source":"Health Canada DPD","rawText":"","confidence":1,"sourceType":"health_canada_dpd","retrievedAt":"2026-04-20T05:31:36.904617+00:00"},"publicationCount":{"url":"https://pubmed.ncbi.nlm.nih.gov/?term=bepotastine besilate ophthalmic solution","method":"api_direct","source":"PubMed/NCBI","rawText":"","confidence":1,"sourceType":"pubmed","retrievedAt":"2026-04-20T05:31:37.201435+00:00"},"administration.route":{"url":"","method":"deterministic","source":"FDA Label","rawText":"","confidence":1,"sourceType":"fda_label","retrievedAt":"2026-04-20T05:31:30.081573+00:00"},"indications.approved":{"url":"","method":"ai_extraction","source":"FDA Label + AI","aiModel":"featherless","rawText":"","confidence":0.9,"sourceType":"fda_label","retrievedAt":"2026-04-20T05:32:03.732797+00:00"},"safety.boxedWarnings":{"url":"","method":"deterministic","source":"FDA Label (no boxed warning)","rawText":"","confidence":1,"sourceType":"fda_label","retrievedAt":"2026-04-20T05:31:30.081606+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":"2026-04-20T05:31:49.568190+00:00"},"mechanism.target_chembl":{"url":"","method":"api_direct","source":"ChEMBL mechanism: Histamine H1 receptor antagonist","rawText":"","confidence":1,"sourceType":"chembl","retrievedAt":"2026-04-20T05:31:38.333144+00:00"},"crossReferences.chemblId":{"url":"https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL1201759/","method":"api_direct","source":"ChEMBL (EMBL-EBI)","rawText":"","confidence":1,"sourceType":"chembl","retrievedAt":"2026-04-20T05:31:37.976765+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 to 5% of subjects were eye irritation, headache, and nasopharyngitis. ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Alembic Pharmaceuticals Inc. at 1-866-210-9797 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditio","confidence":0.95,"sourceType":"fda_label","retrievedAt":"2026-04-20T05:31:53.557720+00:00"},"safety.contraindications":{"url":"","method":"ai_extraction","source":"FDA Label + AI","aiModel":"featherless","rawText":"","confidence":0.95,"sourceType":"fda_label","retrievedAt":"2026-04-20T05:31:57.768086+00:00"},"regulatory.fda_application":{"url":"","method":"deterministic","source":"FDA Label","rawText":"ANDA214588","confidence":1,"sourceType":"fda_label","retrievedAt":"2026-04-20T05:31:30.081610+00:00"}},"_dailymed":{"setId":"de111d74-c740-47b3-adc7-4b855df2c561","title":"BEPOTASTINE BESILATE OPHTHALMIC SOLUTION 1.5% SOLUTION/ DROPS [ALEMBIC PHARMACEUTICALS LIMITED]"},"aiSummary":"Bepotastine besilate ophthalmic solution, marketed by Bausch & Lomb, is an approved treatment for allergic conjunctivitis. Its dual mechanism of action, blocking H1 receptors and inhibiting histamine release from mast cells, provides a strong therapeutic profile. The primary risk is the key composition patent expiry in 2028, which could lead to increased competition from generics.","mechanism":{"target":"H1-receptor, mast cells","modality":"Small molecule","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."},"_scrapedAt":"2026-03-28T03:58:02.728Z","_scrapedBy":"cloudflare-swarm","_wikipedia":null,"_validation":{"fieldsValidated":4,"lastValidatedAt":"2026-04-20T05:32:08.888212+00:00","fieldsConflicting":0,"overallConfidence":0.95},"indications":{"approved":[{"id":"bepotastine-besilate-ophthalmic-solution-allergic-conjunctivitis","name":"Allergic conjunctivitis","dosing":null,"approvals":[],"diseaseId":"","eligibility":"Patients with allergic conjunctivitis","pivotalTrial":null,"restrictions":[],"patientPopulation":"Patients with allergic conjunctivitis","diagnosticRequired":null,"brandNameForIndication":""}]},"trialDetails":[{"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","enrollment":22},{"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},{"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 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