{"id":"epinastine","rwe":[{"pmid":"41561388","year":"2026","title":"Melkersson-Rosenthal syndrome with facial swelling and palsy and associated diagnostic challenges: A case report.","finding":"","journal":"Medicine international","studyType":"Clinical Study"},{"pmid":"40959436","year":"2025","title":"A case report of eruptive pruritic papular porokeratosis with atopic dermatitis treated with upadacitinib: a novel therapeutic perspective.","finding":"","journal":"Frontiers in medicine","studyType":"Clinical Study"},{"pmid":"30000206","year":"2006","title":"Epinastine.","finding":"","journal":"","studyType":"Clinical Study"},{"pmid":"40786375","year":"2025","title":"Epinastine Eyelid Cream as a Practical Option for Patients With Glaucoma on Multidrug Topical Therapy: A Case Report.","finding":"","journal":"Cureus","studyType":"Clinical Study"},{"pmid":"40733076","year":"2025","title":"Topical Percutaneous Drug Delivery for Allergic Diseases: A Novel Strategy for Site-Directed Pharmacologic Modulation.","finding":"","journal":"Pharmaceutics","studyType":"Clinical Study"}],"_fda":{"id":"a873a505-bb9c-4430-8921-8d800df991c7","set_id":"0d4ee45c-e58f-4b7c-b389-898f5c27f54d","openfda":{"upc":["0370069008010"],"unii":["GFM415S5XL"],"route":["OPHTHALMIC"],"rxcui":["860654"],"spl_id":["a873a505-bb9c-4430-8921-8d800df991c7"],"brand_name":["EPINASTINE HYDROCHLORIDE"],"spl_set_id":["0d4ee45c-e58f-4b7c-b389-898f5c27f54d"],"package_ndc":["70069-008-01"],"product_ndc":["70069-008"],"generic_name":["EPINASTINE HYDROCHLORIDE"],"product_type":["HUMAN PRESCRIPTION DRUG"],"substance_name":["EPINASTINE HYDROCHLORIDE"],"manufacturer_name":["Somerset Therapeutics, LLC"],"application_number":["ANDA090951"],"is_original_packager":[true]},"version":"7","description":["11 DESCRIPTION Epinastine HCl Ophthalmic Solution 0.05% is a clear, colorless, sterile isotonic solution containing epinastine HCl, an antihistamine and an inhibitor of histamine release from the mast cell for topical administration to the eyes. Epinastine HCl is represented by the following structural formula: C 16 H 15 N 3 HCl Mol. Wt. 285.78 Chemical Name: 3-Amino-9,13b-dihydro-1H-dibenz[c,f]imidazo [1,5-a]azepine hydrochloride Each mL contains: Active: epinastine HCl 0.05% (0.5 mg/mL) equivalent to epinastine 0.044% (0.44 mg/mL); Preservative: benzalkonium chloride 0.01%; Inactives: edetate disodium; water for injection; sodium chloride; sodium phosphate, monobasic; and sodium hydroxide and/or hydrochloric acid (to adjust pH). Epinastine HCl has a pH of approximately 7 and an osmolality range of 250 to 310 mOsm/kg. Molecular Structure"],"how_supplied":["16 HOW SUPPLIED/STORAGE AND HANDLING Epinastine HCl ophthalmic solution 0.05% is supplied sterile in opaque white LDPE plastic bottles with dropper tips and white polypropylene caps as follows: 5 mL in 10 mL bottle; individually packaged NDC 70069- 008 -01 Storage: Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) (See USP Controlled Room Temperature). Keep bottle tightly closed and out of the reach of children."],"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 effectiveness in pediatric patients below the age of 2 years have not been established."],"effective_time":"20250322","nursing_mothers":["8.3 Nursing Mothers A study in lactating rats revealed excretion of epinastine in the breast milk. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when epinastine HCl ophthalmic solution is administered to a nursing woman."],"clinical_studies":["14 CLINICAL STUDIES Epinastine HCl 0.05% has been shown to be significantly superior to vehicle for improving ocular itching in patients with allergic conjunctivitis in clinical studies using two different models: (1) conjunctival antigen challenge (CAC) where patients were dosed and then received antigen instilled into the inferior conjunctival fornix; and (2) environmental field studies where patients were dosed and evaluated during allergy season in their natural habitat. Results demonstrated a rapid onset of action for epinastine HCl 0.05% within 3 to 5 minutes after conjunctival antigen challenge. Duration of effect was shown to be 8 hours, making a twice daily regimen suitable. This dosing regimen was shown to be safe and effective for up to 8 weeks, without evidence of tachyphylaxis."],"pharmacokinetics":["12.3 Pharmacokinetics Fourteen subjects, with allergic conjunctivitis, received one drop of epinastine HCl ophthalmic solution in each eye twice daily for seven days. On day seven, average maximum epinastine plasma concentrations of 0.04±0.014 ng/mL were reached after about two hours indicating low systemic exposure. While these concentrations represented an increase over those seen following a single dose, the day 1 and day 7 Area Under the Curve (AUC) values were unchanged indicating that there is no increase in systemic absorption with multiple dosing. Epinastine is 64% bound to plasma proteins. The total systemic clearance is approximately 56 L/hr and the terminal plasma elimination half-life is about 12 hours. Epinastine is mainly excreted unchanged. About 55% of an intravenous dose is recovered unchanged in the urine with about 30% in feces. Less than 10% is metabolized. The renal elimination is mainly via active tubular secretion."],"adverse_reactions":["6 ADVERSE REACTIONS The most common ocular adverse reactions (incidence occurring in approximately 1% to 10% of epinastine HCl-treated eyes were burning sensation in the eye, folliculosis, hyperemia, and pruritus. The most common non-ocular adverse reactions, occurring in 10% epinastine HCl-treated eyes, were infection (cold symptoms and upper respiratory infections). To report SUSPECTED ADVERSE REACTIONS, contact Somerset Therapeutics, LLC at +1 800-417-9175 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Studies Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice. The most frequently reported ocular adverse reactions occurring in approximately 1 to 10% of patients were burning sensation in the eye, folliculosis, hyperemia, and pruritus. The most frequently reported non-ocular adverse reactions were infection (cold symptoms and upper respiratory infections), seen in approximately 10% of patients, and headache, rhinitis, sinusitis, increased cough, and pharyngitis, seen in approximately 1 to 3% of patients. Some of these reactions were similar to the underlying disease being studied. 6.2 Postmarketing Experience The following reactions have been identified during postmarketing use of epinastine HCl in clinical practice. Because they are reported voluntarily from a population of unknown size, estimates of frequency cannot be made. The reactions, which have been chosen for inclusion due to either their seriousness, frequency of reporting, possible causal connection to epinastine HCl, or a combination of these factors, include: lacrimation increased."],"contraindications":["4 CONTRAINDICATIONS None None"],"mechanism_of_action":["12.1 Mechanism of Action Epinastine is a topically active, direct H 1 -receptor antagonist and an inhibitor of the release of histamine from the mast cell. Epinastine is selective for the histamine H 1 -receptor and has affinity for the histamine H 2 -receptor. Epinastine also possesses affinity for the ɑ 1 , ɑ 2 -, and 5-HT 2 -receptors."],"clinical_pharmacology":["12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Epinastine is a topically active, direct H 1 -receptor antagonist and an inhibitor of the release of histamine from the mast cell. Epinastine is selective for the histamine H 1 -receptor and has affinity for the histamine H 2 -receptor. Epinastine also possesses affinity for the ɑ 1 , ɑ 2 -, and 5-HT 2 -receptors. 12.3 Pharmacokinetics Fourteen subjects, with allergic conjunctivitis, received one drop of epinastine HCl ophthalmic solution in each eye twice daily for seven days. On day seven, average maximum epinastine plasma concentrations of 0.04±0.014 ng/mL were reached after about two hours indicating low systemic exposure. While these concentrations represented an increase over those seen following a single dose, the day 1 and day 7 Area Under the Curve (AUC) values were unchanged indicating that there is no increase in systemic absorption with multiple dosing. Epinastine is 64% bound to plasma proteins. The total systemic clearance is approximately 56 L/hr and the terminal plasma elimination half-life is about 12 hours. Epinastine is mainly excreted unchanged. About 55% of an intravenous dose is recovered unchanged in the urine with about 30% in feces. Less than 10% is metabolized. The renal elimination is mainly via active tubular secretion."],"indications_and_usage":["1 INDICATIONS AND USAGE Epinastine HCl ophthalmic solution is an H 1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis. Epinastine HCl ophthalmic solution is indicated for the prevention of itching associated with allergic conjunctivitis."],"warnings_and_cautions":["5 WARNINGS AND PRECAUTIONS To minimize the risk of contamination, do not touch dropper tip to any surface. Keep bottle tightly closed when not in use. ( 5.1 ) Epinastine HCl should not be used to treat contact lens-related irritation. ( 5.2 ) Remove contact lenses prior to instillation of epinastine HCl.( 5.2 ) 5.1 Contamination of Tip and Solution Patients should be instructed to avoid allowing the tip of the dispensing container to contact the eye, surrounding structures, fingers, or any other surface in order to avoid contamination of the solution by common bacteria known to cause ocular infections. Serious damage to the eye and subsequent loss of vision may result from using contaminated solutions. Bottle should be kept tightly closed when not in use. 5.2 Use with Contact Lenses Patients should be advised not to wear a contact lens if their eye is red. Epinastine HCl ophthalmic solution should not be used to treat contact lens-related irritation. The preservative in epinastine HCl, benzalkonium chloride, may be absorbed by soft contact lenses. Contact lenses should be removed prior to instillation of epinastine HCl ophthalmic solution and may be reinserted after 10 minutes following its administration. 5.3 Topical Ophthalmic Use Only Epinastine HCl ophthalmic solution is for topical ophthalmic use only and not for injection or oral use."],"nonclinical_toxicology":["13 NONCLINICAL TOXICOLOGY 13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility In 18-month or 2-year dietary carcinogenicity studies in mice or rats, respectively, epinastine was not carcinogenic at doses up to 40 mg/kg [approximately 30,000 times higher than the MROHD, assuming 100% absorption in humans and animals]. Epinastine in newly synthesized batches was negative for mutagenicity in the Ames / Salmonella assay and in vitro chromosome aberration assay using human lymphocytes. Positive results were seen with early batches of epinastine in two in vitro chromosomal aberration studies conducted in the 1980s with human peripheral lymphocytes and with V79 cells, respectively. Epinastine was negative in the in vivo clastogenicity studies, including the mouse micronucleus assay and chromosome aberration assay in Chinese hamsters. Epinastine was also negative in the cell transformation assay using Syrian hamster embryo cells, V79/HGPRT mammalian cell point mutation assay, and in vivo / in vitro unscheduled DNA synthesis assay using rat primary hepatocytes. Epinastine had no effect on fertility of male rats. Decreased fertility in female rats was observed at an oral dose up to approximately 90,000 times the MROHD."],"information_for_patients":["17 PATIENT COUNSELING INFORMATION 17.1 Sterility of Dropper Tip Patients should be advised not to touch dropper tip to any surface, as this may contaminate the contents [ see WARNINGS AND PRECAUTIONS, (5.1)] 17.2 Concomitant Use of Contact Lenses Patients should be advised not to wear a contact lens if their eye is red. Patients should be advised that epinastine HCl should not be used to treat contact lens-related irritation. Patients should also be advised to remove contact lenses prior to instillation of epinastine HCl. The preservative in epinastine HCl ophthalmic solution, benzalkonium chloride, may be absorbed by soft contact lenses. Lenses may be reinserted after 10 minutes following administration of epinastine HCl. 17.3 Topical Ophthalmic Use Only For topical ophthalmic administration only."],"spl_unclassified_section":["Manufactured for: Somerset Therapeutics, LLC Somerset, NJ 08873 Customer Care # 1-800-417-9175 Made in India Code No.:KR/DRUGS/KTK/28/289/97 ST-EPN11/P/06 1201003"],"dosage_and_administration":["2 DOSAGE AND ADMINISTRATION The recommended dosage is one drop in each eye twice a day. The recommended dosage is one drop in each eye twice a day. Treatment should be continued throughout the period of exposure (i.e., until the pollen season is over or until exposure to the offending allergen is terminated), even when symptoms are absent."],"spl_product_data_elements":["EPINASTINE HYDROCHLORIDE EPINASTINE HYDROCHLORIDE EPINASTINE HYDROCHLORIDE EPINASTINE BENZALKONIUM CHLORIDE EDETATE DISODIUM SODIUM CHLORIDE SODIUM PHOSPHATE, MONOBASIC SODIUM HYDROXIDE HYDROCHLORIC ACID WATER Clear Solution"],"dosage_forms_and_strengths":["3 DOSAGE FORMS AND STRENGTHS Ophthalmic solution containing 0.5 mg/mL epinastine HCl. Solution containing 0.5 mg/mL epinastine HCl."],"use_in_specific_populations":["8 USE IN SPECIFIC POPULATIONS 8.1 Pregnancy: In an embryofetal developmental study in pregnant rats, maternal toxicity with no embryofetal effects was observed at an oral dose that was approximately 150,000 times the maximum recommended ocular human dose (MROHD) of 0.0014 mg/kg/day on a mg/kg basis. Total resorptions and abortion were observed in an embryofetal study in pregnant rabbits at an oral dose that was approximately 55,000 times the MROHD. In both studies, no drug-induced teratogenic effects were noted. Epinastine reduced pup body weight gain following an oral dose to pregnant rats that was approximately 90,000 times the MROHD. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, epinastine HCl ophthalmic solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. 8.3 Nursing Mothers A study in lactating rats revealed excretion of epinastine in the breast milk. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when epinastine HCl ophthalmic solution is administered to a nursing woman. 8.4 Pediatric Use Safety and effectiveness in pediatric patients below the age of 2 years have not been established. 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 Container label Carton label Container label Carton label"]},"tags":[{"label":"Adrenergic Receptor Agonist","category":"class"},{"label":"Small Molecule","category":"modality"},{"label":"Histamine H1 receptor","category":"target"},{"label":"HRH1","category":"gene"},{"label":"SLC47A1","category":"gene"},{"label":"SLC22A2","category":"gene"},{"label":"R06AX24","category":"atc"},{"label":"Ophthalmic","category":"route"},{"label":"Solution","category":"form"},{"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":"Ocular Itching","category":"indication"},{"label":"Allergan","category":"company"},{"label":"Approved 2000s","category":"decade"},{"label":"Histamine Agents","category":"pharmacology"},{"label":"Histamine Antagonists","category":"pharmacology"},{"label":"Histamine H1 Antagonists","category":"pharmacology"},{"label":"Neurotransmitter Agents","category":"pharmacology"}],"phase":"marketed","safety":{"boxedWarnings":[],"safetySignals":[{"date":"","signal":"TREATMENT FAILURE","source":"FDA FAERS","actionTaken":"317 reports"},{"date":"","signal":"PYREXIA","source":"FDA FAERS","actionTaken":"60 reports"},{"date":"","signal":"DRUG INEFFECTIVE","source":"FDA FAERS","actionTaken":"54 reports"},{"date":"","signal":"DIARRHOEA","source":"FDA FAERS","actionTaken":"48 reports"},{"date":"","signal":"DECREASED APPETITE","source":"FDA FAERS","actionTaken":"46 reports"},{"date":"","signal":"PNEUMONIA","source":"FDA FAERS","actionTaken":"42 reports"},{"date":"","signal":"RASH","source":"FDA FAERS","actionTaken":"37 reports"},{"date":"","signal":"ANAEMIA","source":"FDA FAERS","actionTaken":"36 reports"},{"date":"","signal":"MALAISE","source":"FDA FAERS","actionTaken":"35 reports"},{"date":"","signal":"HEPATIC FUNCTION ABNORMAL","source":"FDA FAERS","actionTaken":"32 reports"}],"commonSideEffects":[{"effect":"infection","drugRate":"10%","severity":"common","_validated":true},{"effect":"burning sensation in the eye","drugRate":"10%","severity":"common","_validated":true},{"effect":"folliculosis","drugRate":"10%","severity":"common","_validated":true},{"effect":"hyperemia","drugRate":"10%","severity":"common","_validated":true},{"effect":"pruritus","drugRate":"10%","severity":"common","_validated":true},{"effect":"headache","drugRate":"reported","severity":"unknown"},{"effect":"rhinitis","drugRate":"reported","severity":"unknown"},{"effect":"sinusitis","drugRate":"reported","severity":"unknown"},{"effect":"increased cough","drugRate":"reported","severity":"unknown"},{"effect":"pharyngitis","drugRate":"reported","severity":"unknown"},{"effect":"lacrimation increased","drugRate":"reported","severity":"unknown"}],"specialPopulations":{"Pregnancy":"Because animal reproduction studies are not always predictive of human response, epinastine HCl ophthalmic solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. In an embryofetal developmental study in pregnant rats, maternal toxicity with no embryofetal effects was observed at an oral dose that was approximately 150,000 times the maximum recommended ocular human dose (MROHD) of 0.0014 mg/kg/day on mg/kg basis. Total resorptions and abortion were observed in an embryofetal study in pregnant rabbits at an oral dose that was approximately 55,000 times the MROHD. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when epinastine HCl ophthalmic solution is administered to nursing woman.","Geriatric use":"No overall differences in safety or effectiveness have been observed between elderly and younger patients.","Paediatric use":"Safety and effectiveness in pediatric patients below the age of years have not been established."}},"trials":[],"aliases":[],"company":"AbbVie","patents":[],"pricing":[{"market":"United States","source":"CMS National Average Drug Acquisition Cost (NADAC)","asOfDate":"2024-01-03","unitCost":"$14.4520/ML","priceType":"NADAC","sourceUrl":"https://data.medicaid.gov/dataset/4j6z-xnwq","annualCost":"$5,203","description":"EPINASTINE HCL 0.05% EYE DROPS","retrievedDate":"2026-04-07"}],"_sources":{"trials":{"url":"https://clinicaltrials.gov/search?intr=EPINASTINE","method":"api_direct","source":"ClinicalTrials.gov","rawText":"","confidence":1,"sourceType":"ctgov","retrievedAt":"2026-04-20T03:13:08.621942+00:00"},"regulatory.ca":{"url":"","method":"api_direct","source":"Health Canada DPD","rawText":"","confidence":1,"sourceType":"health_canada_dpd","retrievedAt":"2026-04-20T03:13:15.235464+00:00"},"regulatory.us":{"url":"","method":"api_direct","source":"FDA Drugs@FDA","rawText":"","confidence":1,"sourceType":"fda_drugsfda","retrievedAt":"2026-04-20T03:13:07.253421+00:00"},"publicationCount":{"url":"https://pubmed.ncbi.nlm.nih.gov/?term=EPINASTINE","method":"api_direct","source":"PubMed/NCBI","rawText":"","confidence":1,"sourceType":"pubmed","retrievedAt":"2026-04-20T03:13:15.948798+00:00"},"administration.route":{"url":"","method":"deterministic","source":"FDA Label","rawText":"","confidence":1,"sourceType":"fda_label","retrievedAt":"2026-04-20T03:13:06.337650+00:00"},"indications.approved":{"url":"","method":"ai_extraction","source":"FDA Label + AI","aiModel":"featherless","rawText":"","confidence":0.9,"sourceType":"fda_label","retrievedAt":"2026-04-20T03:13:26.872069+00:00"},"safety.boxedWarnings":{"url":"","method":"deterministic","source":"FDA Label (no boxed warning)","rawText":"","confidence":1,"sourceType":"fda_label","retrievedAt":"2026-04-20T03:13:06.337737+00:00"},"safety.safetySignals":{"url":"https://api.fda.gov/drug/event.json","method":"api_direct","source":"FDA FAERS","rawText":"","confidence":1,"sourceType":"fda_faers","retrievedAt":"2026-04-20T03:13:17.432559+00:00"},"mechanism.target_chembl":{"url":"","method":"api_direct","source":"ChEMBL mechanism: Histamine H1 receptor antagonist","rawText":"","confidence":1,"sourceType":"chembl","retrievedAt":"2026-04-20T03:13:16.494041+00:00"},"crossReferences.chemblId":{"url":"https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL1200491/","method":"api_direct","source":"ChEMBL (EMBL-EBI)","rawText":"","confidence":1,"sourceType":"chembl","retrievedAt":"2026-04-20T03:13:16.404329+00:00"},"regulatory.fda_application":{"url":"","method":"deterministic","source":"FDA Label","rawText":"ANDA090951","confidence":1,"sourceType":"fda_label","retrievedAt":"2026-04-20T03:13:06.337752+00:00"}},"allNames":"elestat","offLabel":[],"synonyms":["alesion","epinastine","(+/-)-Epinastine","epinastine hydrochloride","epinastine HCl"],"timeline":[{"date":"2003-01-01","type":"neutral","source":"FDA Orange Book","milestone":"Rights transferred from ALLERGAN to Allergan"},{"date":"2003-10-16","type":"positive","source":"DrugCentral","milestone":"FDA approval (Allergan)"},{"date":"2016-12-07","type":"neutral","source":"FDA Orange Book","milestone":"Generic entry — 5 manufacturers approved"},{"date":"2019-09-20","type":"positive","source":"DrugCentral","milestone":"PMDA approval (Santen Pharmaceutical Co., Ltd.)"}],"aiSummary":"Elestat (EPINASTINE) is a small molecule adrenergic receptor agonist that targets the histamine H1 receptor. It was originally developed by Allergan and is currently owned by the same company. FDA approved in 2003, it is used to treat allergic conjunctivitis and ocular itching. Elestat is off-patent, with six generic manufacturers available. Key safety considerations include its 12-hour half-life.","approvals":[{"date":"2003-10-16","orphan":false,"company":"ALLERGAN","regulator":"FDA"},{"date":"2019-09-20","orphan":false,"company":"Santen Pharmaceutical Co., Ltd.","regulator":"PMDA"}],"brandName":"Elestat","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},{"indication":"Ocular Itching","otherDrugs":[{"name":"antazoline","slug":"antazoline","company":"Novartis"},{"name":"naphazoline","slug":"naphazoline","company":"Novartis"},{"name":"nedocromil","slug":"nedocromil","company":"King Pharms"},{"name":"pheniramine","slug":"pheniramine","company":"Alcon"}],"globalPrevalence":null}],"mechanism":{"target":"Histamine H1 receptor","novelty":"Follow-on","targets":[{"gene":"HRH1","source":"DrugCentral","target":"Histamine H1 receptor","protein":"Histamine H1 receptor"},{"gene":"SLC47A1","source":"DrugCentral","target":"Multidrug and toxin extrusion protein 1","protein":"Multidrug and toxin extrusion protein 1"},{"gene":"SLC22A2","source":"DrugCentral","target":"Solute carrier family 22 member 2","protein":"Solute carrier family 22 member 2"},{"gene":"SLC47A2","source":"DrugCentral","target":"Multidrug and toxin extrusion protein 2","protein":"Multidrug and toxin extrusion protein 2"},{"gene":"KCNH2","source":"DrugCentral","target":"Potassium voltage-gated channel subfamily H member 2","protein":"Potassium voltage-gated channel subfamily H member 2"},{"gene":"HTR2A","source":"DrugCentral","target":"5-hydroxytryptamine receptor 2A","protein":"5-hydroxytryptamine receptor 2A"},{"gene":"ADRA1A","source":"DrugCentral","target":"Alpha-1A adrenergic receptor","protein":"Alpha-1A adrenergic receptor"},{"gene":"ADRA2A","source":"DrugCentral","target":"Alpha-2A adrenergic receptor","protein":"Alpha-2A adrenergic receptor"},{"gene":"HRH2","source":"DrugCentral","target":"Histamine H2 receptor","protein":"Histamine H2 receptor"},{"gene":"ABCB1","source":"DrugCentral","target":"Multidrug resistance protein 1","protein":"Multidrug resistance protein 1"}],"moaClass":"Adrenergic Agonists","modality":"Small Molecule","drugClass":"Adrenergic Receptor Agonist","explanation":"Epinastine is topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from the mast cell. Epinastine is selective for the histamine H1-receptor and has affinity for the histamine H2-receptor. Epinastine also possesses affinity for the 1, 2-, and 5-HT2-receptors.","oneSentence":"Elestat works by binding to the histamine H1 receptor, blocking the action of histamine and reducing allergic symptoms.","technicalDetail":"Elestat (EPINASTINE) is a selective histamine H1 receptor antagonist that competitively inhibits the binding of histamine to its receptor, thereby reducing the symptoms of allergic conjunctivitis and ocular itching."},"commercial":{"launchDate":"2003","_launchSource":"DrugCentral (FDA 2003-10-16, ALLERGAN)"},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/1027","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=EPINASTINE","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=EPINASTINE","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":"2026-03-30T10:58:40.763563","_validation":{"fieldsValidated":1,"lastValidatedAt":"2026-04-20T03:13:27.137306+00:00","fieldsConflicting":0,"overallConfidence":0.95},"biosimilars":[],"competitors":[{"drugName":"cyproheptadine","drugSlug":"cyproheptadine","fdaApproval":"1961-10-17","genericCount":31,"patentStatus":"Off-patent — generic available","relationship":"same-class"},{"drugName":"antazoline","drugSlug":"antazoline","fdaApproval":"1990-04-30","relationship":"same-class"},{"drugName":"triprolidine","drugSlug":"triprolidine","fdaApproval":"1983-05-17","genericCount":6,"patentStatus":"Off-patent — generic available","relationship":"same-class"},{"drugName":"azatadine","drugSlug":"azatadine","fdaApproval":"1977-03-29","patentStatus":"Unknown","relationship":"same-class"},{"drugName":"astemizole","drugSlug":"astemizole","fdaApproval":"1988-12-31","relationship":"same-class"},{"drugName":"terfenadine","drugSlug":"terfenadine","fdaApproval":"","relationship":"same-class"},{"drugName":"loratadine","drugSlug":"loratadine","fdaApproval":"1993-04-12","genericCount":29,"patentStatus":"Off-patent — generic available","relationship":"same-class"},{"drugName":"ketotifen","drugSlug":"ketotifen","fdaApproval":"1999-07-02","patentExpiry":"Mar 27, 2028","patentStatus":"Patent 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