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

Nippon Boehringer Ingelheim Co., Ltd.Runer Ophthalmic Drugs (Guangzhou) Co., Ltd.

Santen Pharmaceutical Co., Ltd.

+ [3]

Inactive Organization

Merck Sharp & Dohme Corp.

Boehringer Ingelheim GmbHAllergan, Inc.

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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310

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.

01 Jan 2025·Forensic Toxicology

Effects of natural environments on drug contents in nails: comparison of drug residual rates between nails and hair to determine the drug-use history of corpses in unnatural death cases using micro-segmental analysis

Article

Author: Iwata, Yuko T ; Kanamori, Tatsuyuki ; Tsujikawa, Kenji ; Kuwayama, Kenji ; Segawa, Hiroki ; Miyaguchi, Hajime ; Yamamuro, Tadashi ; Okada, Yuki

PURPOSEWe previously developed evaluation methods using micro-segmental analysis (MSA) to examine the effects of external environments on drug content in hair and nails. In this study, the effects of the natural environmental factors (water, temperature, humidity, light, and soil) on drug contents in nails were examined and compared with our previous experimental data on hair.METHODSFour hay-fever medicines were used as model drugs (fexofenadine, epinastine, cetirizine, and desloratadine) to evaluate drug stability in the nails. Reference nails containing the four medicines were collected from patients with hay fever who ingested the medicines daily for four months. The nails were exposed to various natural environments for up to four months.RESULTSThe effects of temperature, humidity, and light on drug contents in the nails were comparatively small. Soil significantly decomposed the nail surfaces and decreased the drug content of the nails (up to 17 %). Water also decreased the drug content (up to 12 %), although no apparent changes in nail surfaces were observed.CONCLUSIONSIn comparison with hair data obtained under the same environmental conditions, light affected drugs in the hair rather than in nails, whereas water and soil greatly affected drugs in the nails rather than in hair. Although the disposition of drugs incorporated in the tissues differed between nails and hair, the analytes were detected in nails and hair strands left in severe natural environments. MSA could be useful for estimating drug-use histories and personal profiles using the nails and hair of a corpse.

22 Nov 2024·Cureus

Efficacy of Epinastine Eyelid Cream in Pediatric Vernal Keratoconjunctivitis: A Case Report

Article

Author: Hashida, Noriyasu ; Mamoto, Yukinori ; Shiozaki, Daiki ; Hirose, Rina

Allergic conjunctivitis (AC) is characterized by inflammatory responses in the conjunctiva and is often complicated by atopic dermatitis and mechanical irritation. Vernal keratoconjunctivitis (VKC), a severe subtype of AC, presents unique challenges in its diagnosis and management, particularly in pediatric patients. This case report describes an eight-year-old girl with VKC who exhibited poor adherence to a prescribed regimen of 0.05% epinastine ophthalmic solution and corticosteroid eye drops, resulting in persistent symptoms. Despite initial treatment, the patient's condition included giant papillae and thickened tarsal conjunctivae that were resistant to standard therapies. Upon transitioning to 0.5% epinastine eyelid cream, the patient showed improved adherence and partial symptom resolution. However, new limbal lesions, including Horner-Trantas dots, were observed following the cessation of steroid therapy. The reintroduction of steroids led to significant improvements in conjunctival lesions and complete resolution of limbal gelatinous hyperplasia. This case underscores the potential of epinastine eyelid cream in managing VKC, particularly in patients with adherence issues, and highlights the need for careful monitoring and combination therapy in severe cases. Further studies are needed to evaluate the long-term efficacy and safety of epinastine eyelid cream. However, once-daily application of eyelid cream may serve as a viable treatment and management option for pediatric patients with VKC.

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
Conjunctivitis, Allergic	Japan	Santen Pharmaceutical Co., Ltd.	20 Sep 2013
Seasonal allergic conjunctivitis	Sweden	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	yjcepllykk(kcowwrkahu) = nqrgxhzuoj zpgmjgzgqi (zoogugkdhk, qaqannarre - curmspdxvc) View more	-	23 Sep 2014
NCT00534794 (CTgov)	Phase 4	Conjunctivitis, Allergic	79	Elestat (Elestat)	tetqvvmcsu(zbesvqvcst) = tcueczsqmw ehltfrehym (nhscktznks, gkozynzgwf - avyxhgqvty) View more	-	27 May 2009
NCT00534794 (CTgov)	Phase 4	Conjunctivitis, Allergic	79	Pataday (Pataday)	tetqvvmcsu(zbesvqvcst) = wfqnjlaudi ehltfrehym (nhscktznks, pzwfdrwsni - crkcpbpcju) View more	-	27 May 2009
ARVO2003	Not Applicable	Conjunctivitis, Allergic	14	Epinastine hydrochloride 0.05%	(qiddcwhasu) = 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 caqndzmamr (ewaoidjiig )	Positive	01 May 2003