Delving into the Latest Updates on Epinastine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Epinastine, Epinastine hydrochloride (JAN), エピナスチン

+ [13]

Target

H1 receptor

Action

antagonists

Mechanism

H1 receptor antagonists(Histamine H1 receptor antagonists)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesEye Diseases+ [3]

Active Indication

Conjunctivitis, AllergicSeasonal allergic conjunctivitisPsoriasis+ [7]

Inactive Indication

Dermatitis, AtopicRhinitis, Allergic, PerennialRhinitis, Allergic, Seasonal

Originator Organization

Boehringer Ingelheim GmbH

Active Organization

Runer Ophthalmic Drugs (Guangzhou) Co., Ltd.

Allergan Pharmaceuticals Ireland ULCNippon Boehringer Ingelheim Co., Ltd.

+ [3]

Inactive Organization

Merck Sharp & Dohme Corp.

Boehringer Ingelheim GmbHAllergan, Inc.

License Organization

Inspire Pharmaceuticals, Inc.

Boehringer Ingelheim GmbH

Santen Pharmaceutical Co., Ltd.

+ [2]

Drug Highest PhaseApproved

First Approval Date

Japan (01 Apr 1994),

AsthmaDermatitisEczema+ [4]

Regulation-

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Structure/Sequence

Molecular FormulaC16H16ClN3

InChIKeyVKXSGUIOOQPGAF-UHFFFAOYSA-N

CAS Registry108929-04-0

主要研究目的：以长春海悦药业股份有限公司生产的盐酸依匹斯汀片为受试制剂，以Nippon Boehringer Ingelheim Co., Ltd.持证的盐酸依匹斯汀片（商品名：Alesion，20 mg）为参比制剂，通过单中心、随机、开放、单次给药、两序列、两周期、双交叉临床研究来评价两种制剂在空腹和餐后条件下的人体生物等效性。次要研究目的：观察受试制剂和参比制剂在中国健康受试者中的安全性。

[Translation]

The main purpose of the study was to use Epinastine Hydrochloride Tablets produced by Changchun Haiyue Pharmaceutical Co., Ltd. as the test preparation and Epinastine Hydrochloride Tablets (trade name: Alesion, 20 mg) certified by Nippon Boehringer Ingelheim Co., Ltd. as the reference preparation, and to evaluate the bioequivalence of the two preparations under fasting and fed conditions through a single-center, randomized, open, single-dose, two-sequence, two-period, double-crossover clinical study. The secondary purpose of the study was to observe the safety of the test preparation and the reference preparation in healthy Chinese subjects.

Start Date07 Nov 2024

Sponsor / Collaborator

Changchun Haiyue Pharmaceutical Co., Ltd

CTR20234212

/ CompletedPhase 3

0.1%STN1011403滴眼液治疗过敏性结膜炎的多中心随机评价者盲态阳性对照试验

[Translation] A multicenter randomized evaluator-blind positive controlled trial of 0.1% STN1011403 eye drops in the treatment of allergic conjunctivitis

以中国过敏性结膜炎患者为对象，验证0.1% STN1011403 滴眼液的有效性非劣于Alesion® LX 滴眼液0.1%以及0.1%盐酸奥洛他定滴眼液，并确认安全性。

[Translation]

The efficacy of 0.1% STN1011403 eye drops was verified to be non-inferior to Alesion® LX eye drops 0.1% and 0.1% olopatadine hydrochloride eye drops in Chinese patients with allergic conjunctivitis, and the safety was confirmed.

Start Date05 Mar 2024

Sponsor / Collaborator

Santen Pharmaceutical (China) Co. Ltd.

CTR20231572

/ CompletedPhase 3

0.05%盐酸依匹斯汀滴眼液治疗中国过敏性结膜炎患者的有效性和安全性的随机、双盲、阳性药平行对照、多中心临床研究

[Translation] A randomized, double-blind, positive-drug parallel-controlled, multicenter clinical study on the efficacy and safety of 0.05% epinastine hydrochloride eye drops in the treatment of allergic conjunctivitis in Chinese patients

主要目的：以富马酸依美斯汀滴眼液为对照，评价0.05%盐酸依匹斯汀滴眼液治疗过敏性结膜炎的有效性。次要目的：评价0.05%盐酸依匹斯汀滴眼液治疗过敏性结膜炎的安全性。

[Translation]

Primary objective: To evaluate the effectiveness of 0.05% epinastine hydrochloride eye drops in the treatment of allergic conjunctivitis, using emedastine fumarate eye drops as a control. Secondary objective: To evaluate the safety of 0.05% epinastine hydrochloride eye drops in the treatment of allergic conjunctivitis.

Start Date22 May 2023

Sponsor / Collaborator

Runer Ophthalmic Drugs (Guangzhou) Co., Ltd.

100 Clinical Results associated with Epinastine Hydrochloride

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100 Translational Medicine associated with Epinastine Hydrochloride

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100 Patents (Medical) associated with Epinastine Hydrochloride

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311

Literatures (Medical) associated with Epinastine Hydrochloride

01 Apr 2025·Chemosphere

Abating a micropollutant epinastine by UV-based advanced oxidation processes: Comparison for UV/hydrogen peroxide, UV/persulfate, and UV/chlorine, impacts of bromide contents, and formation of DBPs during post-chlorination

Article

Author: Sakai, Hiroshi ; Murata, Yuichiro

Anthropogenic organic compounds, such as pharmaceuticals and personal care products, contaminate water, posing toxicological risks caused by either their parent compounds or transformation products. This study compares ultraviolet (UV)-based advanced oxidation processes (UV/hydrogen peroxide, UV/persulfate, and UV/chlorine) for the abatement of an antihistamine drug epinastine. UV light at 254 nm was irradiated upon solutions containing 10 μM epinastine and 100 μM oxidant. UV/chlorine degraded epinastine most effectively at pH 6.0-8.0; considerable contributions by reactive chlorine species and hydroxyl radicals were quantified using probe compounds. Furthermore, the degradation efficiency of the UV/chlorine treatment persisted with a halved chlorine dosage. Additionally, the types and concentrations of disinfection byproducts (DBPs) produced during UV/chlorine treatment with or without post-chlorination varied depending on the concentrations of chlorine or bromide. By comparing estimated DBP formations at a constant degradation rate of epinastine, UV/chlorine formed smaller concentrations of DBPs. Consequently, this study experimentally revealed that UV/chlorine is superior to UV/hydrogen peroxide and UV/persulfate for degrading epinastine at the possible pH and bromide content in the environment and controlling toxicological risks caused by disinfection DBPs formation by optimising chlorine dosage and UV fluence.

31 Mar 2025·Die Pharmazie

Direct comparison of the effects of first- and second-generation H₁ -receptor blockers on motor functions in mice.

Article

Author: Okamoto, Y ; Sakamoto, Y ; Enoki, Y ; Hara, R ; Tenjin, K ; Shimada, A ; Matsumoto, K ; Hori, S ; Taguchi, K ; Kizu, J ; Iketani, O

Histamine H1 receptor (H1R) antagonists are widely used to treat allergic reactions; however, their effects on the central nervous system can impair motor functions. This study investigated the impact of first-generation (diphenhydramine and d -chlorpheniramine) and second-generation (epinastine, ketotifen, bepotastine, and levocetirizine) H1R antagonists on motor functions in mice using activity wheel, balance beam, inclined screen, and rotarod tests. First-generation H1R antagonists significantly impaired motor functions, with diphenhydramine exerting stronger effects than those of d -chlorpheniramine. Among the second-generation agents, bepotastine and levocetirizine had minimal effects on all motor functions, whereas epinastine and ketotifen suppressed spontaneous movement, similar to first-generation H1R antagonists but had little effects on balance, postural stability, and coordinated movement. These findings provide valuable insights into the differential effects of first- and second-generation H1R antagonists on motor functions. These results highlight the importance of understanding individual profiles of H1R antagonists to minimize adverse effects, ensure patient safety, and improve quality of life.

28 Feb 2025·Cureus

Successful Transition From Topical Ophthalmic Drops to Cream Formulation in the Management of Mild Allergic Conjunctivitis: A Case Report

Article

Author: Fukagawa, Kazumi ; Nishio, Mai ; Shimizu, Eisuke ; Fujishima, Hiroshi ; Asai, Kazuki

This case report highlights the successful transition from epinastine eye drops to a novel epinastine eyelid cream in managing mild allergic conjunctivitis. A 33-year-old Japanese female with mild allergic conjunctivitis, previously managed with 0.1% epinastine hydrochloride eye drops, requested an alternative formulation due to daily contact lens wear. Treatment was changed to a once-daily application of 0.5% epinastine hydrochloride eyelid cream. Clinical assessment and symptom evaluation were performed at baseline and after 28 days using slit-lamp examination and the Japanese Allergic Conjunctival Disease Quality of Life Questionnaire. Following the transition, the patient's clinical signs (mild conjunctival hyperemia and moderate papillae) and subjective symptoms (itching and mild discomfort) remained stable. Slit-lamp examination showed no corneal or limbal pathology, and tear fluid immunoglobulin E (IgE) testing remained positive, consistent with mild allergic conjunctivitis. No adverse effects or cutaneous reactions were observed. This case suggests that epinastine eyelid cream may serve as an effective once-daily alternative to conventional eye drops in mild allergic conjunctivitis. While this represents the first documented successful transition between delivery methods, larger clinical trials are warranted to confirm these findings and explore applications across various presentations and severities of allergic ocular disease.

100 Deals associated with Epinastine Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D01713	Epinastine Hydrochloride	R06AX24 S01GX10	DB00751

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Seasonal allergic conjunctivitis	Czechia	Allergan Pharmaceuticals Ireland ULC	04 Mar 2003
Seasonal allergic conjunctivitis	Poland	Allergan Pharmaceuticals Ireland ULC	04 Mar 2003
Seasonal allergic conjunctivitis	Slovakia	Allergan Pharmaceuticals Ireland ULC	04 Mar 2003
Seasonal allergic conjunctivitis	Luxembourg	Allergan Pharmaceuticals Ireland ULC	04 Mar 2003
Seasonal allergic conjunctivitis	Germany	Allergan Pharmaceuticals Ireland ULC	04 Mar 2003
Seasonal allergic conjunctivitis	Ireland	Allergan Pharmaceuticals Ireland ULC	04 Mar 2003
Seasonal allergic conjunctivitis	Portugal	Allergan Pharmaceuticals Ireland ULC	04 Mar 2003
Seasonal allergic conjunctivitis	Greece	Allergan Pharmaceuticals Ireland ULC	04 Mar 2003
Seasonal allergic conjunctivitis	Denmark	Allergan Pharmaceuticals Ireland ULC	04 Mar 2003
Seasonal allergic conjunctivitis	Sweden	Allergan Pharmaceuticals Ireland ULC	04 Mar 2003
Seasonal allergic conjunctivitis	United Kingdom	Allergan Pharmaceuticals Ireland ULC	04 Mar 2003
Seasonal allergic conjunctivitis	Italy	Allergan Pharmaceuticals Ireland ULC	04 Mar 2003
Psoriasis	China	Nippon Boehringer Ingelheim Co., Ltd.	16 Jun 2000
Asthma	Japan	Nippon Boehringer Ingelheim Co., Ltd.	01 Apr 1994
Dermatitis	Japan	Nippon Boehringer Ingelheim Co., Ltd.	01 Apr 1994
Eczema	Japan	Nippon Boehringer Ingelheim Co., Ltd.	01 Apr 1994
Prurigo	Japan	Nippon Boehringer Ingelheim Co., Ltd.	01 Apr 1994
Pruritus	Japan	Nippon Boehringer Ingelheim Co., Ltd.	01 Apr 1994
Rhinitis, Allergic	Japan	Nippon Boehringer Ingelheim Co., Ltd.	01 Apr 1994
Urticaria	Japan	Nippon Boehringer Ingelheim Co., Ltd.	01 Apr 1994

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Conjunctivitis, Allergic	Phase 3	China	Runer Ophthalmic Drugs (Guangzhou) Co., Ltd.	22 May 2023
Seasonal allergic conjunctivitis	Phase 3	China	Zhaoke (Guangzhou) Ophthalmology Pharmaceutical Ltd.	10 Mar 2023
Rhinitis, Allergic, Seasonal	Preclinical	-	Merck Sharp & Dohme Corp.	18 Dec 2007
Dermatitis, Atopic	Preclinical	-	Boehringer Ingelheim GmbH	01 Jun 2001
Rhinitis, Allergic, Perennial	Preclinical	-	Boehringer Ingelheim GmbH	01 May 2000

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01363713 (CTgov)	Phase 3	Conjunctivitis, Allergic	130	DE-114	hokeulqyyi(hfxessrtbt) = qrgqiwpbgu yspkyqsuyy (gyzuanojey, bywlpxlbrm - djuznanhcy) View more	-	23 Sep 2014
NCT00534794 (CTgov)	Phase 4	Conjunctivitis, Allergic	79	Elestat (Elestat)	fpbwycxlpq(wsyflrqeys) = iyonuqmdbf zbqknlahiz (hzwzdusdwb, luzbyyfgbi - pujizagebm) View more	-	27 May 2009
NCT00534794 (CTgov)	Phase 4	Conjunctivitis, Allergic	79	Pataday (Pataday)	fpbwycxlpq(wsyflrqeys) = domvnptbpx zbqknlahiz (hzwzdusdwb, vyhiucjwql - zypfmwbiun) View more	-	27 May 2009
ARVO2003	Not Applicable	Conjunctivitis, Allergic	14	Epinastine hydrochloride 0.05%	(nwodztjgpl) = No adverse events nor any clinically relevant changes in visual acuity, biomicroscopy, ophthalmoscopy, vital signs, physical examination, or laboratory parameters were observed during the study uzkhrztcpk (afnmmuahcg )	Positive	01 May 2003