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

作用方式

激动剂

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IIT

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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52

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.

2023-07-01·Radiation Physics and Chemistry

Determination of the molecular structure and spectroscopic properties of capsaicin

作者: Alim, Zuhal ; Sakar, Erdem ; Alim, Bunyamin ; Cinar, Mehmet

In this study, the ground state mol. structure and spectroscopic features of cis- and trans-forms of capsaicin were investigated using DFT (B3LYP) invoking 6-311++G(d,p) basis set.The optimized geometry of capsaicin was determined for the isolated mol. in a vacuum, and then the vibrational spectra (IR and Raman) obtained, and the assignments of fundamental vibrational modes were done.By applying the GIAO method, proton and carbon chem. shifts were computed for the gas and solvated phases.Besides using the TD-DFT, the Hirshfeld surface and Mol. electrostatic potential surfaces were obtained and evaluated to understand the electronic properties.The total and partial d. of state (TDOS and PDOS) spectra were also examinedAll obtained computational results were compared with the previously reported exptl. data.A high accuracy was obtained for the ground state geometrical structure, and thus, the vibrational frequencies especially lie on the finger print region are predicted also with a high correlation.Similarly, the optimization of chem. shift values calculated by considering solvent effects with exptl. data were found as high R² values of 0.9953 and 0.9455 for C and H atoms, resp.This comparison shows that the DFT method precisely predicts capsaicin′s mol. and spectroscopic characteristics.

2023-04-10·Journal of chemical information and modeling

Phyto4Health: Database of Phytocomponents from Russian Pharmacopoeia Plants.

Article

作者: Ionov, Nikita ; Poroikov, Vladimir ; Druzhilovskiy, Dmitry ; Filimonov, Dmitry

Medicinal plants growing in Russia are a rich source of biologically active compounds. However, the evaluation of the hidden pharmacological potential of these compounds by in silico methods is complicated by the lack of specialized databases. We have created a database of 3128 phytocomponents from 268 medical plants included in the Russian Pharmacopoeia. The information about the compounds was supplemented with their physical-chemical characteristics and biological activity profiles estimated using the PASS software. Comparison with phytocomponents of medicinal plants from five other countries showed that the similarity of phytocomponents in our database is rather small. The uniqueness of the contents significantly enriches and provides easy access to the necessary information. The Phyto4Health data are freely available at http://www.way2drug.com/p4h/.

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
三叉神经痛	临床1期	美国	Winston Laboratories, Inc.	2014-03-01
疱疹后神经痛	临床1期	美国	Winston Laboratories, Inc.	2009-03-01
疱疹后神经痛	临床1期	加拿大	Winston Laboratories, Inc.	2009-03-01
干眼综合征	药物发现	美国	Winston Laboratories, Inc.	2014-05-01
疱疹后神经痛	药物发现	美国	Winston Laboratories, Inc.	2009-03-01
疱疹后神经痛	药物发现	加拿大	Winston Laboratories, Inc.	2009-03-01
创伤后神经痛	药物发现	加拿大	Winston Laboratories, Inc.	2009-03-01
创伤后神经痛	药物发现	美国	Winston Laboratories, Inc.	2009-03-01
膝关节炎	药物发现	-	Winston Laboratories, Inc.	2003-06-01
丛集性头痛	药物发现	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)	鏇範廠遞憲餘鏇蓋鑰壓(築鏇構範衊齋遞選鏇網) = 鏇醖蓋顧鬱窪壓選淵窪淵構夢鑰廠壓製襯淵顧 (襯餘蓋選遞廠壓鹽繭積, 齋蓋壓衊鬱網膚餘鏇醖 ~ 壓窪鏇構淵構艱築鏇膚) 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)	觸顧廠淵鑰壓醖鹽獵築(鑰鬱憲獵觸鏇廠壓積夢) = 網鏇築窪衊蓋醖鏇艱鹹襯製積鏇願願艱製鹹鹽 (製壓鏇壓糧積襯齋築齋, 遞願構醖襯願蓋壓齋蓋 ~ 網鹹簾艱醖鏇醖淵壓襯) 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)	觸顧廠淵鑰壓醖鹽獵築(鑰鬱憲獵觸鏇廠壓積夢) = 觸衊夢窪鑰網壓遞簾鹽襯製積鏇願願艱製鹹鹽 (製壓鏇壓糧積襯齋築齋, 醖壓襯遞醖積鑰選繭艱 ~ 繭構糧壓壓積艱鹹餘鏇) 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)	觸築鑰鏇襯觸顧繭夢衊(鏇積網衊鹽鹽遞鹽糧餘) = 餘淵簾鏇網鏇積鹽憲網衊簾蓋醖鹹範蓋獵願積 (遞鹹窪糧淵鑰壓憲簾繭, 獵範遞蓋窪蓋網膚蓋構 ~ 簾淵製網醖襯遞構廠繭) 更多	-	2017-03-01
				Placebo (Double Blind Treatment Period Placebo Nasal Spray)	觸築鑰鏇襯觸顧繭夢衊(鏇積網衊鹽鹽遞鹽糧餘) = 築齋廠選膚襯衊壓鹽鬱衊簾蓋醖鹹範蓋獵願積 (遞鹹窪糧淵鑰壓憲簾繭, 淵膚膚壓觸鏇夢築鏇繭 ~ 顧艱築構遞淵遞齋壓艱) 更多