珠卡赛辛(Zucapsaicin) - 药物靶点：TRPV1_在研适应症：骨关节炎，疼痛，丛集性头痛_专利_临床

概要

基本信息

药物类型

小分子化药

别名

(Z)-Capsaicin、Civamide、Civanex

+ [6]

靶点

TRPV1

作用机制

TRPV1激动剂(类香草素受体激动剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

Winston Laboratories, Inc.

非在研机构-

最高研发阶段批准上市

首次获批日期

加拿大 (2010-07-15),

骨关节炎疼痛

最高研发阶段(中国)-

特殊审评孤儿药 (美国)

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结构/序列

分子式C18H27NO3

InChIKeyYKPUWZUDDOIDPM-VURMDHGXSA-N

CAS号25775-90-0

关联

23

项与珠卡赛辛相关的临床试验

NCT01341548

/ Not yet recruiting临床3期

A Phase III, Double-Blind, Randomized, Vehicle-Controlled, Parallel-Group, Multicenter Evaluation of Civamide Nasal Solution 0.01% in the Prevention of Cluster Headaches During an Episodic Cluster Headache Period

The purpose of this study is to evaluate the safety and efficacy of intranasally administered civamide nasal solution in the prevention of cluster headaches during an episodic cluster headache period.

开始日期2023-11-01

申办/合作机构

Winston Laboratories, Inc.

NCT04969198

/ Completed临床2期

UW Withdraw From Tobacco Study: Enhancing and Evaluating Tobacco Withdrawal Assessment Psychometrics and Validity

It is of considerable scientific and clinical importance to assess tobacco withdrawal accurately since withdrawal severity is highly determinant of smoking cessation success. In addition, smoking cessation pharmacotherapy produces its effects on smoking abstinence by suppressing such symptoms. However, in order to ensure that a measure of tobacco withdrawal is sensitive to severe withdrawal, it is essential to examine a period of unmedicated abstinence. The current study aims to validate, and possibly enhance, a revised Wisconsin Smoking Withdrawal Scale long and brief version for use in research and clinical settings.
Two hundred adults who smoke cigarettes daily and report a desire to quit smoking will be enrolled. This is a treatment-delay, one-group clinical trial that is intended to enhance the assessment of tobacco withdrawal amongst participants who try to quit smoking with delayed use of cessation medication. Participants will not receive any pharmacotherapy during the first 1 week of their quit attempt and will initiate 8 weeks of combination nicotine replacement therapy (C-NRT; nicotine patch + nicotine mini-lozenge) starting 1 week past the target quit day (TQD). Participants will receive 4 counseling sessions as well (1 pre-quit, 3 post-quit). Participants will complete 4 weeks of ecological momentary assessment (EMA) smartphone surveys including a 2-week baseline (starting TQD-14) and 2-week post-TQD (1-week un-medicated, 1-week using C-NRT).

开始日期2021-07-13

申办/合作机构

University of Wisconsin Madison

[+1]

NCT04882319

/ Completed临床1期

An Evaluator-blinded, Randomized Within-subject Repeat Insult Study to Evaluate Potential Skin Irritation and Sensitization of HP-5000 (Diclofenac Sodium Topical System) in Healthy Adults

This study will assess skin irritation and sensitization for HP-5000 patch in healthy subjects.

开始日期2021-06-03

申办/合作机构

Noven Pharmaceuticals, Inc.

100 项与珠卡赛辛相关的临床结果

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100 项与珠卡赛辛相关的转化医学

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100 项与珠卡赛辛相关的专利（医药）

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30

项与珠卡赛辛相关的文献（医药）

2024-04-01·Archives of Biochemistry and Biophysics

Identifying novel aryl hydrocarbon receptor (AhR) modulators from clinically approved drugs: In silico screening and In vitro validation

Article

作者: Mosa, Farag E S ; El-Kadi, Ayman O S ; El-Ghiaty, Mahmoud A ; Alqahtani, Mohammed A ; Barakat, Khaled

The aryl hydrocarbon receptor (AhR) functions as a vital ligand-activated transcription factor, governing both physiological and pathophysiological processes. Notably, it responds to xenobiotics, leading to a diverse array of outcomes. In the context of drug repurposing, we present here a combined approach of utilizing structure-based virtual screening and molecular dynamics simulations. This approach aims to identify potential AhR modulators from Drugbank repository of clinically approved drugs. By focusing on the AhR PAS-B binding pocket, our screening protocol included binding affinities calculations, complex stability, and interactions within the binding site as a filtering method. Comprehensive evaluations of all DrugBank small molecule database revealed ten promising hits. This included flibanserin, butoconazole, luliconazole, naftifine, triclabendazole, rosiglitazone, empagliflozin, benperidol, nebivolol, and zucapsaicin. Each exhibiting diverse binding behaviors and remarkably very low binding free energy. Experimental studies further illuminated their modulation of AhR signaling, and showing that they are consistently reducing AhR activity, except for luliconazole, which intriguingly enhances the AhR activity. This work demonstrates the possibility of using computational modelling as a quick screening tool to predict new AhR modulators from extensive drug libraries. Importantly, these findings hold immense therapeutic potential for addressing AhR-associated disorders. Consequently, it offers compelling prospects for innovative interventions through drug repurposing.

2021-10-01·Journal of Pharmaceutical and Biomedical Analysis3区 · 医学

LC-MS/MS determination of guanabenz E/Z isomers and its application to in vitro and in vivo DMPK profiling studies

3区 · 医学

Article

作者: Cao, Bin ; Xie, Wei ; Jiang, Rongrong ; Xie, Jiashu ; More, Swati S

Endoplasmic reticulum (ER) stress underlies a variety of disorders involving inflammation, such as diabetes, neurodegenerative diseases. Guanabenz acetate (Wytensin®, GA), a clinically approved antihypertensive drug, efficiently counteracts ER stress. The entirety of clinically used GA is the E-isomer, while the Z-isomer is known to lack significant hypotensive properties. We recently discovered that the Z-isomer retains anti-ER stress activity. Coupled with its lack of sedative effects, (Z)-GA is well positioned as a potential therapeutic for a host of ER stress-related disorders. We set forth to characterize the metabolism and pharmacokinetics (DMPK) of (Z)-GA in vitro and in vivo. Toward this end, a reliable and sensitive LC-MS/MS method for simultaneous determination of the (E)- and (Z)-guanabenz was developed. Chromatographic separation of the isomers was achieved on a C18 reverse phase column with a gradient elution. Tandem mass spectrometric detection was conducted using an AB Sciex 5500 QTrap mass spectrometer with positive electrospray ionization. Full validation of the method was performed in mouse plasma with a simple and low plasma volume protein precipitation procedure. The method demonstrated good linearity, reproducibility, and accuracy over a range of 0.5-1000 nM with minimal matrix effect and excellent extraction efficiency. In addition, the developed method was successfully applied to DMPK studies of the GA isomers in vitro and in vivo. Results of these studies revealed for the first time that the DMPK profile of (Z)-guanabenz is distinct from that of (E)-guanabenz, with higher apparent volume of distribution (V_d) and clearance, presumably due to lower plasma protein binding.

2021-06-01·Journal of Surgical Oncology3区 · 医学

Predictors and significance of histologic response to neoadjuvant therapy for gastric cancer

3区 · 医学

Article

作者: Bouvet, Michael ; Horgan, Santiago ; Lowy, Andrew M. ; Kelly, Kaitlyn J. ; Razzaque, Saqib ; Rajabnejad, Ataollah ; Valasek, Mark ; Fanta, Paul ; Vaida, Florin

AbstractBackgroundPerioperative therapy is the standard‐of‐care for locally‐advanced gastric cancer but many patients do not respond. There are currently no known factors that predict response to therapy.MethodsThis was a retrospective study aimed to evaluate treatment effect grade (TEG) in patients with locally advanced gastric cancer treated with neoadjuvant therapy and surgery at a single center. Ordinal logistic regression was performed to identify predictors of TEG, scaled from 0 to 3.ResultsFifty patients were identified. The majority were male (n = 33) and 50% were Hispanic. The most common regimens given were: 5‐fluorouracil/leucovorin, oxaliplatin, and docetaxel (n = 23, 46%), epirubicin, cis‐ or oxaliplatin, and 5‐fluorouracil/leucovorin or Xeloda (n = 8, 16%), and 5‐fluorouracil/leucovorin and oxaliplatin (n = 9, 18%). Twenty‐seven patients (55%) had complete or partial response to therapy (TEG 0–2), and 23 patients (46%) had no response (TEG 3). Of numerous variables analyzed, only race and SRC histology were associated with TEG. TEG was associated with disease free, but not disease specific survival.ConclusionsIn this cohort, 46% of patients had no histologic response to therapy. SRC histology, and possibly race, should be considered in determination of optimal multidisciplinary regimens and in amount of therapy to be given upfront, as patients with SRC histology and those of non‐Asian race are less likely to respond to standard regimens.

100 项与珠卡赛辛相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D06388	珠卡赛辛	M02AB02	DB09120

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
骨关节炎	加拿大	-	2010-07-15
疼痛	加拿大	-	2010-07-15

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
干眼综合征	临床2期	美国	Winston Laboratories, Inc.	2014-05-01
三叉神经痛	临床2期	美国	Winston Laboratories, Inc.	2014-03-01
疱疹后神经痛	临床2期	加拿大	Winston Laboratories, Inc.	2009-03-01
疱疹后神经痛	临床2期	美国	Winston Laboratories, Inc.	2009-03-01
疱疹后神经痛	临床2期	加拿大	Winston Laboratories, Inc.	2009-03-01
疱疹后神经痛	临床2期	美国	Winston Laboratories, Inc.	2009-03-01
创伤后神经痛	临床2期	加拿大	Winston Laboratories, Inc.	2009-03-01
创伤后神经痛	临床2期	美国	Winston Laboratories, Inc.	2009-03-01
膝关节炎	临床2期	-	Winston Laboratories, Inc.	2003-06-01
丛集性头痛	临床2期	美国	Winston Laboratories, Inc.	2002-01-01

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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


NCT04969198 (CTgov)	临床2期	肢端雀斑恶性黑色素瘤	232	Combination nicotine replacement therapy (Nicotine patch + nicotine mini-lozenge)	遞觸鏇積顧鏇鏇鹽簾範(鬱醖鏇膚顧窪築壓鑰齋) = 齋鑰選構鬱鏇製襯鹹簾壓鏇願醖壓顧積襯壓顧 (夢壓膚鏇製遞艱膚鬱鏇, 蓋膚壓蓋築獵觸鏇顧襯 ~ 夢鹽構膚鬱簾窪鏇築醖) 更多	-	2023-12-01
NCT01592695 (CTgov)	临床2期	酗酒 \| 抑郁症 \| 尼古丁成瘾 \| 肥胖	63	Combination pharmacotherapy - transdermal nicotine patch + nicotine gum+Bupropion Sustained Release+Nicotine replacement therapy - nicotine gum+Varenicline+Nicotine replacement therapy - transdermal nicotine patch (Tailored Intervention Group)	積鹽製鑰製鬱製願繭憲(鹽鏇鑰觸構繭選構鹽衊) = 鹹壓齋獵鑰範願獵襯網鬱蓋鏇膚齋淵鹽獵窪憲 (積築夢願構製鬱範網壓, 蓋顧鏇醖構鹽餘齋網積 ~ 鑰衊膚鑰鑰醖餘鑰積簾) 更多	-	2017-07-19
				Combination pharmacotherapy - transdermal nicotine patch + nicotine gum+Bupropion Sustained Release+Nicotine replacement therapy - nicotine gum+Varenicline+Nicotine replacement therapy - transdermal nicotine patch (Enhanced Standard of Care Group)	積鹽製鑰製鬱製願繭憲(鹽鏇鑰觸構繭選構鹽衊) = 淵糧餘鑰餘壓淵鏇鹽憲鬱蓋鏇膚齋淵鹽獵窪憲 (積築夢願構製鬱範網壓, 願廠憲醖餘網積簾築齋 ~ 網鹹糧鹽憲積簾鬱餘選) 更多
NCT01886313 (CTgov)	临床2期	疱疹后神经痛 \| 三叉神经痛	11	Civamide (Double Blind Treatment Period Civamide Nasal Spray)	製築蓋鑰簾鏇製艱糧夢(鏇淵遞繭鑰醖築選繭選) = 廠構願鹽壓壓餘獵鑰選廠夢獵餘蓋襯鏇鏇衊襯 (獵襯壓網鑰糧淵膚觸觸, 選築網願積襯遞廠憲積 ~ 遞願壓膚壓鏇廠醖醖觸) 更多	-	2017-03-01
				Placebo (Double Blind Treatment Period Placebo Nasal Spray)	製築蓋鑰簾鏇製艱糧夢(鏇淵遞繭鑰醖築選繭選) = 憲獵獵願鏇壓顧顧選獵廠夢獵餘蓋襯鏇鏇衊襯 (獵襯壓網鑰糧淵膚觸觸, 憲齋願廠鏇繭遞簾糧製 ~ 餘蓋醖簾鹹構繭淵襯積) 更多