NEO-1940(NEO-1940) - 药物靶点：CB1R x CB2_在研适应症：焦虑症，恶病质，癌症疼痛_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

CB1R x CB2

作用机制

CB1激动剂(大麻素受体CB1激动剂)、CB2激动剂(大麻素受体CB2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

非在研机构

最高研发阶段临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C20H29F2N3O2S

InChIKeyZAGGGZCIFUQHOH-UHFFFAOYSA-N

CAS号881413-29-2

关联

2

项与 NEO-1940 相关的临床试验

NCT00689780 / Completed临床1期

A Phase I, Multi-Centre, Randomised, Double-blind, Placebo-controlled Study to Investigate the Safety, Tolerability and Pharmacokinetics of AZD1940, Including an Interaction Study, After Administration of Oral Multiple Ascending Doses in Adult Subjects With Chronic Low Back Pain

A Phase I, Multi-Centre, Randomised, Double-blind, Placebo-controlled Study to Investigate the Safety, Tolerability and Pharmacokinetics of AZD1940, Including an Interaction Study, After Administration of Oral Multiple Ascending Doses in Adult Subjects with Chronic Low Back Pain

开始日期2008-03-01

申办/合作机构

AstraZeneca PLC

NCT00659490 / Completed临床2期

A Randomised, Double Blind, Placebo-Controlled Study to Investigate the Analgesic Efficacy of a Single Dose of AZD1940, in Patients Undergoing Impacted Mandibular Third Molar Extraction

The primary aim of this study is to investigate if AZD1940 can relieve the pain induced by the surgical removal of one lower wisdom-tooth. This will be done by comparing the effect of AZD1940 to placebo ("inactive substance") on pain. A number of patients will instead receive the common painkiller naproxen for comparison purposes. Rescue medication, acetaminophen, will be allowed if a need for additional painkillers would arise. A number of patients will receive Naproxen as control.

开始日期2008-02-01

申办/合作机构

AstraZeneca PLC

100 项与 NEO-1940 相关的临床结果

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100 项与 NEO-1940 相关的转化医学

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100 项与 NEO-1940 相关的专利（医药）

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4

项与 NEO-1940 相关的文献（医药）

2022-06-01·British Journal of Oral and Maxillofacial Surgery4区 · 医学

Cannabis and orofacial pain: a systematic review

4区 · 医学

Review

作者: Tan, H ; Gadiwalla, Y ; Grossman, S

The naturally occurring cannabis plant has played an established role in pain management throughout recorded history. However, in recent years, both natural and synthetic cannabis-based products for medicinal use (CBPM) have gained increasing worldwide attention due to growing evidence supporting their use in alleviating chronic inflammatory and neuropathic pain associated with an array of conditions. In view of these products' growing popularity in both the medical and commercial fields, we carried out a systematic review to ascertain the effects of cannabis and its synthetically derived products on orofacial pain and inflammation. The application of topical dermal cannabidiol formulation has shown positive findings such as reducing pain and improving muscle function in patients suffering from myofascial pain. Conversely, two orally-administered synthetic cannabinoid receptor agonists (AZD1940 and GW842166) failed to demonstrate significant analgesic effects following surgical third molar removal. There is a paucity of literature pertaining to the effects of cannabis-based products in the orofacial region; however, there is a wealth of high-quality evidence supporting their use for treating chronic nociceptive and neuropathic pain conditions in other areas. Further research is warranted to explore and substantiate the therapeutic role of CBPMs in the context of orofacial pain and inflammation. As evidence supporting their use expands, healthcare professionals should pay close attention to outcomes and changes to legislation that may impact and potentially benefit their patients.

2013-04-01·Nuclear Medicine and Biology4区 · 医学

Radiolabeling of the cannabinoid receptor agonist AZD1940 with carbon-11 and PET microdosing in non-human primate

4区 · 医学

Article

作者: Katarina Varnäs ; Balázs Gulyás ; Magnus Schou ; Christer Halldin ; Lars Farde ; Aurelija Jucaite

INTRODUCTIONN-(2-tert-butyl-1-((4,4-difluorocyclohexyl)methyl)-1H-benzo[d]imidazol-5-yl)ethanesulfonamide (AZD1940) is a candidate drug for treatment of neuropathic pain. As part of the preclinical evaluation of AZD1940, a microdosing study with positron emission tomography (PET) was conducted to assess brain exposure.METHODSAZD1940 was radiolabeled with carbon-11 in the benzimidazole moiety. The radioactive precursor, lithium [(11)C]pivalate was obtained via (11)C-carboxylation of tert-butyl lithium. The target compound, [(11)C]AZD1940, was in turn obtained by the microwave assisted reaction between lithium [(11)C]pivalate and the o-phenylene diamine analog of AZD1940 (N-(3-amino-4-((4,4-difluorocyclohexyl)methylamino)phenyl)ethanesulfonamide) in neat phosphorous oxychloride. A brain PET measurement was performed in cynomolgus monkey.RESULTSThe overall radiochemical yield of final formulated radiochemically pure (>99%) [(11)C]AZD1940 was 0.4% (uncorrected for decay) and the specific radioactivity was 13GBq/μmol at time of administration (58min after end of bombardment). After intravenous injection to cynomolgus monkey, the maximum concentration of radioactivity detected in the brain region of interest was 0.7% of the total injected radioactivity. The regional distribution of radioactivity within brain was homogenous.CONCLUSIONSAZD1940 was radiolabelled with carbon-11 and its brain exposure, assessed using PET, was relatively low in comparison to peripheral organ exposure.

2013-01-01·Scandinavian Journal of Pain

Why we are proud to publish well-performed negative clinical studies?

Article

作者: Kalso, Eija ; Kontinen, Vesa

In the present issue of the Scandinavian Journal of Pain the aper “Evaluation of the analgesic efficacy of AZD1940, a novel annabinoid agonist, onpost-operative pain after lower thirdmolar xtraction” by Jarkko Kalliomaki et al. [1] describes the effect of peripherally active CB1/CB2-receptor agonist in the most comonly used model of postoperative pain. The compound is novel, he methodology is impeccable, the paper is very well written, and he topic is hot, and yet everyone in the business knows that it is ard to get it published. And this is only because the drug was not ffective. Most researchers have at some point struggled to publish negative study.

100 项与 NEO-1940 相关的药物交易

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研发状态

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
焦虑症	临床1期	-	Neomed Institute	-
恶病质	临床1期	-	Neomed Institute	-
癌症疼痛	临床1期	-	Neomed Institute	-
恶心	临床1期	-	Neomed Institute	-
入睡和睡眠障碍	临床1期	-	Neomed Institute	-
腰痛	临床前	瑞典	AstraZeneca PLC	2008-03-01
疼痛	临床前	美国	AstraZeneca PLC	2008-02-01

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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


NCT00659490 (CTgov)	临床2期	疼痛	151	AZD1940 (AZD1940)	醖鬱選窪壓範餘糧獵鏇(糧觸艱鑰壓膚鏇願鏇繭) = 糧夢獵夢製鏇簾餘壓膚願窪廠鹹顧製製鬱襯範 (餘繭醖憲壓築簾夢願鏇, 膚獵鹽築顧簾蓋獵構襯 ~ 積鹽憲簾鑰鏇壓網築構) 更多	-	2012-03-26
				Placebo (Placebo)	醖鬱選窪壓範餘糧獵鏇(糧觸艱鑰壓膚鏇願鏇繭) = 觸鹹糧窪膚遞憲憲艱積願窪廠鹹顧製製鬱襯範 (餘繭醖憲壓築簾夢願鏇, 網鏇廠鹹鹽範襯齋窪壓 ~ 簾遞蓋艱襯衊構糧願鑰) 更多