盐酸左卡巴斯汀(Levocabastine Hydrochloride) - 药物靶点：H1 receptor_在研适应症：季节性过敏性鼻炎，变应性结膜炎_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Histimet、Levocabastine、Levocabastine Hydrochloride Nasal Spray

+ [13]

靶点

H1 receptor

作用机制

H1 receptor拮抗剂(组胺H1受体拮抗剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

Johnson & Johnson Consumer NV

Santen Pharmaceutical Co., Ltd.Janssen Pharmaceutical KK

非在研机构

GSK Plc

Novartis Pharmaceuticals Corp.

最高研发阶段批准上市

首次获批日期

美国 (1993-11-10),

变应性结膜炎常年性变应性鼻炎

最高研发阶段(中国)批准上市

特殊审评-

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结构

分子式C26H29FN2O2

InChIKeyZCGOMHNNNFPNMX-KYTRFIICSA-N

CAS号79516-68-0

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关联

7

项与盐酸左卡巴斯汀相关的临床试验

NCT04002349 / Unknown statusN/A

Study of Medication for Nonallergic Rhinitis (NAR) Based on Cluster Analysis

Chronic rhinitis (CR) is one of the most common nasal mucosal diseases in the world. In China, about 140 million people suffer from this disease. Chronic rhinitis can lead to severe economic and social burden, as well as the potential risk of developing other chronic diseases such as asthma and chronic sinusitis. Therefore, it is of great significance to explore the classification and treatment strategies of chronic rhinitis in order to improve the health level of Chinese people.

开始日期2019-07-01

申办/合作机构

北京同仁医院管理有限公司

[+1]

KCT0004672 / CompletedN/AIIT

Double blind, randomized controlled study to evaluate the efficacy and safety of extract of leaves of Dendropanax morbiferous H. Lev on the glucose metabolism

开始日期2018-07-23

申办/合作机构-

JPRN-UMIN000017531 / RecruitingIIT

Evaluation of the effect of the antiepiletic levetiracetum on seizure control and expression of MGMT in patients with gliomas (Phase II clinical trial) - LEV for Glioma

开始日期2014-10-06

申办/合作机构-

100 项与盐酸左卡巴斯汀相关的临床结果

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100 项与盐酸左卡巴斯汀相关的转化医学

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100 项与盐酸左卡巴斯汀相关的专利（医药）

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298

项与盐酸左卡巴斯汀相关的文献（医药）

2024-07-01·Journal of Pharmacological and Toxicological Methods

Evaluation methods using tear volume in a conjunctivitis mice model

Article

作者: Kai, Haruki ; Sugimoto, Yukio ; Haraoka, Noriaki

Allergic conjunctival disease is an immune-mediated inflammatory disease of the conjunctiva. To develop clinically useful drugs, it is necessary to develop quantitative evaluation methods that reflect the clinical symptoms in experimental animal models. Allergic conjunctivitis model mice were systemically sensitised with ovalbumin (OVA) administered intraperitoneally and locally sensitised with OVA eye drops between day 14-28. Next, conjunctivitis induced by ocular administration of OVA solution to sensitised mice was evaluated based on tear volume. Additionally, we evaluated increase in tear volume induced by direct ocular instillation of histamine, compound 48/80, and carrageenan. An increase in antigen-induced tear volume was observed in the mice model. Additionally, direct instillation of histamine, compound 48/80, and carrageenan increased tear volume. Furthermore, levocabastine inhibited the increase in tear volume in antigen-induced allergic conjunctivitis and histamine- and compound 48/80-induced conjunctivitis models. In contrast, betamethasone suppressed carrageenan-induced tear volume but not histamine- or compound 48/80-induced tear volume. Histamine may be involved in increased tear volume in allergic conjunctivitis. Betamethasone is not directly involved in the action of histamine and is thought to suppress increase in tear volume. Evaluation of tear volume in a conjunctivitis mice model is highly quantitative; therefore, it is possible to evaluate drug efficacy. This is considered a useful index compared with conventional methods.

2024-03-23·Journal of Biomolecular Structure and Dynamics

In-silico identification of novel DDI2 inhibitor in glioblastoma via repurposing FDA approved drugs using molecular docking and MD simulation study

Article

作者: Majumder, Ranabir ; Mandal, Mahitosh ; Roy, Pritam Kumar

Glioblastoma, the most severe form of brain tumor and a leading cause of death within a year of diagnosis, is characterized by excessive protein synthesis and folding in the lumen of the endoplasmic reticulum (ER), leading to increased ER stress in the cells of GBM tissues. To mitigate this stress the cancer cells have intelligently adopted a plethora of response mechanisms and Unfolded Protein Response (UPR) is one of those. To bear with this exhaustive situation cells upregulate a strong protein degradation system in form of 26S proteasome and blocking of proteasomal gene synthesis may be a potential therapeutic action against GBM. Proteasomal gene synthesis is exclusively dependent on the transcription factor Nuclear respiratory factor 1 (NRF1) and its activating enzyme DNA damage inducible 1 homolog 2 (DDI2). Here in this study, we performed molecular docking against DDI2 with the 20 FDA-approved drugs and identified Alvimopan and Levocabastine as the top two compounds with the best binding score along with the standard drug Nelfinavir. MD simulation (100 ns) of these protein-ligand docked complexes reveals that the stability and compactness of Alvimopan are high in comparison with Nelfinavir. Our in-silico (Molecular docking and Molecular dynamics simulation) studies pointed out that Alvimopan may be repurposed as a DDI2 inhibitor and can be used as a potential anticancer agent for the treatment of brain tumors.Communicated by Ramaswamy H. Sarma.

2024-02-01·Toxicology and Applied Pharmacology

Levocabastine ameliorates cyclophosphamide-induced cardiotoxicity in Swiss albino mice: Targeting TLR4/NF-κB/NLRP3 signaling pathway

Article

作者: Alam, M Mumtaz ; Najmi, Abul Kalam ; Akram, Wasim ; Haque, Syed Ehtaishamul

Cyclophosphamide (CP), although a potent anti-cancer drug, causes cardiotoxicity as a side effect that limits its use. Hence, a specific medicine that can lower cardiotoxicity and be utilised as an adjuvant in cancer treatment is very much needed. In this light, we intended to assess the protective potential of levocabastine (LEV) on CP-induced cardiotoxicity in Swiss albino mice. Mice were administered LEV (50 and 100 μg/kg, i.p.) daily for 14 days and CP at 200 mg/kg, intraperitoneally once on the 7th day. On the 15th day, mice were weighed, blood withdrawn then sacrificed and hearts were removed to estimate various biochemical and histopathological parameters. CP 200 mg/kg significantly increased cardiac troponin T, LDH, CK-MB, interleukin-1β, IL-6, TNF-α, TBARS, nitrite, and decreased CAT, GSH, and SOD levels, thus, manifested cardiac damage, inflammation, oxidative stress, and nitrative stress, cumulatively causing cardiotoxicity. CP also elevated the expression of various markers including cleaved caspase-3, NF-κB, TLR4, NLRP3, and fibrotic lesions in cardiac tissues, whereas decreased hematological parameters (RBCs, platelets, and Hb) to confirm cardiotoxicity. LEV and fenofibrate (FF) treatment reversed these changes towards normal and showed a significant protective effect against CP. The results showed the protective role of LEV in restoring CP-induced cardiotoxicity in terms of inflammation, apoptosis, oxidative stress, cardiac injury and histopathological damage. Thus, levocabastine can be used as an adjuvant to cyclophosphamide in cancer treatment but a thorough study with various animal cancer models is further needed to establish the fact.

100 项与盐酸左卡巴斯汀相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01717	盐酸左卡巴斯汀	R01AC02 S01GX02	DB01106

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
季节性过敏性鼻炎	中国	Johnson & Johnson Consumer NV	2018-07-24
变应性结膜炎	日本	Santen Pharmaceutical Co., Ltd.	2000-09-22
变应性结膜炎	日本	Janssen Pharmaceutical KK	2000-09-22

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
季节性常年性变应性鼻炎	药物发现	加拿大	GSK Plc	2013-10-01
季节性常年性变应性鼻炎	药物发现	奥地利	GSK Plc	2013-10-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01949051 (CTgov)	临床2期	季节性常年性变应性鼻炎	78	placebo (Placebo)	遞餘醖觸窪範繭醖鑰艱(壓艱積鬱願糧製簾襯衊) = 餘壓獵艱夢鏇壓襯夢壓廠觸繭範鹽醖糧鏇蓋齋 (廠簾鹹餘範選築鑰廠範, 淵鹽窪顧餘襯鬱獵窪壓 ~ 淵糧艱淵觸觸廠鹹醖醖) 更多	-	2014-09-25
				Levocabastine (Levocabastine 200µg OD)	遞餘醖觸窪範繭醖鑰艱(壓艱積鬱願糧製簾襯衊) = 憲餘鹽願蓋艱糧積蓋願廠觸繭範鹽醖糧鏇蓋齋 (廠簾鹹餘範選築鑰廠範, 鹽願憲簾廠鬱鹹蓋製糧 ~ 糧選鹹窪齋鏇衊夢鏇餘) 更多
ARVO2007	N/A	结膜疾病 ICAM-1 \| VLA-4 \| VCAM-1	-	Levocabastine	醖簾襯遞糧繭網壓壓壓(積繭顧製顧繭襯鏇積憲) = 網醖壓窪繭糧觸簾鹹鏇餘鹽夢壓糧構繭遞鏇顧 (網網窪鑰壓顧夢鬱鬱鏇 )	-	2007-05-01
ARVO2003	N/A	季节性过敏性结膜炎	-	Epinastine HCl 0.05%	(壓鬱艱膚膚繭鬱醖願糧) = 襯窪網獵築網簾襯夢鹹糧蓋遞構構窪廠繭餘壓 (遞衊範餘範獵願網築淵 )	积极	2003-05-01
				Levocabastine 0.05%	(壓鬱艱膚膚繭鬱醖願糧) = 夢範願繭襯繭艱壓鏇觸糧蓋遞構構窪廠繭餘壓 (遞衊範餘範獵願網築淵 )