奥昔卡因(Oxetacaine) - 在研适应症：恶心和呕吐，麻醉，胃食管反流_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Oxetacaine (INN)、Oxethazaine (JP17/USAN)、オキセサゼイン

+ [9]

靶点-

作用机制-

治疗领域

神经系统疾病消化系统疾病口颌疾病+ [2]

在研适应症

非在研适应症

原研机构

在研机构

非在研机构

MEDA Pharma GmbH & Co. KG

Amato Pharmaceutical Products Ltd.

最高研发阶段批准上市

首次获批日期

日本 (1962-02-27),

恶心和呕吐

最高研发阶段(中国)-

特殊审评-

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结构

分子式C28H41N3O3

InChIKeyFTLDJPRFCGDUFH-UHFFFAOYSA-N

CAS号126-27-2

关联

2

项与奥昔卡因相关的临床试验

NCT01336530 / Terminated临床3期

Clinical Trial to Assess the Efficacy of Fixed Combination Product Tepilta® in the Treatment of Radiation-induced Oesophagitis Compared to Its Active Ingredients Oxetacaine and Antacids, and to Placebo

This is a randomised, double-blind, placebo-controlled, therapeutic confirmatory multicentre trial with 4 parallel treatment groups. The design is adaptive group-sequential with two interim analyses, possible sample size re-estimation after the first or second interim analysis and drop-the-loser approach. The study design was primarily chosen to show superior efficacy of Tepilta® compared to the single components and to placebo. Evaluation of safety is a secondary objective.

开始日期2011-04-01

申办/合作机构

MEDA Pharma GmbH & Co. KG

[+3]

EUCTR2009-014441-93-DE / Not yet recruiting临床3期

Clinical trial to assess the efficacy of the fixed combination product Tepilta® in the treatment of radiation-induced oesophagitis compared to its active ingredients oxetacaine and antacids, and to placebo - Tepilta® vs. oxetacaine, antacids and placebo

开始日期2010-08-16

申办/合作机构

MEDA Pharma GmbH & Co. KG

100 项与奥昔卡因相关的临床结果

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100 项与奥昔卡因相关的转化医学

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100 项与奥昔卡因相关的专利（医药）

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64

项与奥昔卡因相关的文献（医药）

2021-10-01·Journal of Cellular Biochemistry3区 · 生物学

An integrated virtual screening and drug repurposing strategy for the discovery of new antimalarial drugs against Plasmodium falciparum phosphatidylinositol 3‐kinase

3区 · 生物学

Article

作者: Verma, Kanika ; Schneider, Kristan A. ; Bharti, Praveen K. ; Dubey, Shivangee ; Das, Aparup ; Verma, Anil K. ; Lahariya, Ayush K.

AbstractThe emergence and spread of drug resistance in Plasmodium falciparum, the parasite causing the most severe form of human malaria, is a major threat to malaria control and elimination programs around the globe. With P. falciparum having evolved widespread resistance against a number of previously widely used drugs, currently, artemisinin (ART) and its derivatives are the cornerstones of first‐line treatments of uncomplicated malaria. However, growing incidences of ART failure reflect the spread of ART‐resistant P. falciparum strains. Despite current efforts to understand the primary cause of ART resistance due to mutations in the Kelch 13 gene (PfK13), the mechanism underlying ART resistance is still not completely unclear and no feasible strategies to counteract the causes and thereby restoring the efficiency of ART have been developed. We use a polypharmacology approach to identify potential drugs that can be used for the novel purpose (target). Of note, we have designed a multimodal stratagem to identify approved drugs with a potential antimalarial activity using computational drug reprofiling. Our investigations suggest that oxetacaine, simvastatin, repaglinide, aclidinium, propafenone, and lovastatin could be repurposed for malaria control and prevention.

2020-07-01·Advanced Biosystems3区 · 生物学

Parallelized Impedance‐Based Platform for Continuous Dose‐Response Characterization of Antischistosomal Drugs

3区 · 生物学

Article

作者: Lombardo, Flavio C. ; Dupuch, Matthias A. ; Keiser, Jennifer ; Modena, Mario M. ; Hierlemann, Andreas ; Ravaynia, Paolo S. ; Biendl, Stefan

AbstractSchistosomiasis is an acute and chronic disease caused by tropical parasitic worms of the genus Schistosoma, which parasitizes annually over 200 million people worldwide. Screening of antischistosomal compounds is hampered by the low throughput and potential subjectivity of the visual evaluation of the parasite phenotypes, which affects the current drug assays. Here, an impedance‐based platform, capable of assessing the viability of Schistosoma mansoni schistosomula exposed to drugs, is presented. This automated and parallelized platform enables unbiased and continuous measurements of dose–response relationships for more than 48 h. The platform performance is established by exposure of schistosomula to three test compounds, praziquantel, oxethazaine, and mefloquine, which are known to affect the larvae phenotypes. The system is thereafter used to investigate the response of schistosomula to methiothepine, an antipsychotic compound, which causes complex drug‐induced effects. Continuous monitoring of the parasites reveals transient behavioral phenotypes and allows for extracting temporal characteristics of dose–response curves, which are essential for selecting drugs that feature high activity and fast kinetics of action. These measurements demonstrate that impedance‐based detection provides a wealth of information for the in vitro characterization of candidate antischistosomals and, represents a promising tool for the identification of new lead compounds.

2017-06-01·Journal of Pharmacy and Pharmacology3区 · 医学

Complexation of oxethazaine with 2-hydroxypropyl-β-cyclodextrin: increased drug solubility, decreased cytotoxicity and analgesia at inflamed tissues

3区 · 医学

Article

作者: Volpato, Maria C ; Cabeça, Luís F ; Yokaichiya, Fabiano ; Prado, Andressa R ; Morais Gonçalves da Silva, Camila ; Franco, Margareth Kazuyo Kobayashi Dias ; de Paula, Eneida ; Oliveira-Nascimento, Laura ; Franz-Montan, Michelle

AbstractObjectivesOxethazaine (OXZ) is one of the few local anaesthetics that provides analgesia at low pH, but presents poor solubility, cytotoxicity and no parenteral formulations. To address these issues, we aimed to prepare OXZ host-guest inclusion complex with hydroxypropyl-beta-cyclodextrin (HP-β-CD).MethodsThe inclusion complex was formed by co-solubilization, followed by a job plot analysis to determine stoichiometry of complexation and dialysis equilibrium analysis (based on UV/VIS absorption and fluorescence profiles of OXZ). Complex formation was confirmed by phase-solubility data, X-ray, Scanning Electron Microscopy and DOSY-1H-NMR experiments. In vitro cytotoxicity was analysed by MTT test in 3T3 fibroblasts. In vivo analgesia was tested by Von Frey test (inflammatory wounds – rats).Key findingsOxethazaine complexed (1 : 1 molar ratio) with HP-β-CD, as indicated by loss of OZX crystalline structure (X-ray) and strong host: guest interaction (NMR, K = 198/m), besides increased solubility. In vitro cell survival improved with the complex (IC50 OXZ = 28.9 μm, OXZ : HP-β-CD = 57.8 μm). In addition, the complex (0.1% OXZ) promoted in vivo analgesia for the same time that 2% lidocaine/epinephrine did.ConclusionOur results show that complexation improved physicochemical and biological properties of OXZ, allowing its application to inflamed tissues by parenteral routes.

100 项与奥昔卡因相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01152	奥昔卡因	C05AD06	DB12532

研发状态

批准上市

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适应症	国家/地区	公司	日期
恶心和呕吐	日本	Alfresa Pharma Corp.	1962-02-27
麻醉	-	-	-
胃食管反流	-	-	-
疼痛	-	-	-

未上市

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适应症	最高研发状态	国家/地区	公司	日期
食管炎	临床3期	德国	MEDA Pharma GmbH & Co. KG	2011-04-01
食管炎	临床3期	奥地利	MEDA Pharma GmbH & Co. KG	2011-04-01
疼痛	临床3期	日本	Amato Pharmaceutical Products Ltd.	-