利司韦林(Lersivirine) - 药物靶点：RT_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Lersivirine (USAN/INN)

靶点

RT

作用机制

RT抑制剂(逆转录酶抑制剂)

治疗领域

免疫系统疾病感染泌尿生殖系统疾病

在研适应症-

非在研适应症

HIV感染

原研机构

Pfizer Inc.

在研机构-

非在研机构

Pfizer Inc.

ViiV Healthcare Ltd.

最高研发阶段终止临床2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C17H18N4O2

InChIKeyMCPUZZJBAHRIPO-UHFFFAOYSA-N

CAS号473921-12-9

关联

15

项与利司韦林相关的临床试验

NCT01603485 / Completed临床1期

Open-Label, Randomized, Crossover Study to Estimate the Pharmacokinetics, Bioavailability and Effect of Food on Single Dose Modified-Release Lersivirine (UK-453,061) 500 mg in Healthy Subjects

The purpose of this study is to estimate the pharmacokinetics (PK) of 3 different modified-release formulations of lersivirine and compare it to the PK of the immediate-release tablet. The effect of food on the PK of one of the modified-release tablets will also be assess along with the safety and tolerability of each treatment.

开始日期2012-06-01

申办/合作机构

Pfizer Inc.

[+1]

EUCTR2010-020860-39-IT / Not yet recruitingN/A

A LONG-TERM OPEN-LABEL EXTENSION STUDY OF LERSIVIRINE FOR THE TREATMENT OF HIV-1 INFECTION - ND

开始日期2011-02-05

申办/合作机构

Pfizer Inc.

NCT01254656 / Terminated临床2期

A Long Term Open-Label Extension Study Of Lersivirine For The Treatment Of HIV-1 Infection

This is a study to assess long-term safety and efficacy of lersivirine in patients who have completed 96 weeks of treatment with lersivirine in studies A5271015 and A5271022.

开始日期2011-02-01

申办/合作机构

Pfizer Inc.

[+1]

100 项与利司韦林相关的临床结果

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100 项与利司韦林相关的转化医学

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100 项与利司韦林相关的专利（医药）

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32

项与利司韦林相关的文献（医药）

2015-04-01·Toxicologic Pathology4区 · 医学

Two-year Carcinogenicity Study in Rats with a Nonnucleoside Reverse Transcriptase Inhibitor

4区 · 医学

Article

作者: Nambiar, Prashant R. ; Bailey, Steven A. ; Houle, Christopher ; Morton, Daniel ; Finch, Gregory L. ; Dochterman, Leland Wayne ; Thomford, Peter J. ; Fate, Gwendolyn

Administration of lersivirine, a nonnucleotide reverse transcriptase inhibitor, daily by oral gavage to Sprague-Dawley rats for up to 2 yr was associated with decreased survival, decreased body weights, and an increase in neoplasms and related proliferative lesions in the liver, thyroid, kidney, and urinary bladder. Thyroid follicular adenoma and carcinoma, the associated thyroid follicular hypertrophy/hyperplasia, hepatocellular adenoma/adenocarcinoma, altered cell foci, and hepatocellular hypertrophy were consistent with lersivirine-related induction of hepatic microsomal enzymes. Renal tubular adenoma and renal tubular hyperplasia were attributed to the lersivirine-related exacerbation of chronic progressive nephropathy (CPN), while urinary bladder hyperplasia and transitional cell carcinoma in the renal pelvis and urinary bladder were attributed to urinary calculi. Renal tubular neoplasms associated with increased incidence and severity of CPN, neoplasms of transitional epithelium attributed to crystalluria, and thyroid follicular and hepatocellular neoplasms related to hepatic enzyme induction have low relevance for human risk assessment.

2015-01-16·Organic Letters1区 · 化学

Mild Palladium-Catalyzed Cyanation of (Hetero)aryl Halides and Triflates in Aqueous Media

1区 · 化学

Article

作者: Cohen, Daniel T. ; Buchwald, Stephen L.

A mild, efficient, and low-temperature palladium-catalyzed cyanation of (hetero)aryl halides and triflates is reported. Previous palladium-catalyzed cyanations of (hetero)aryl halides have required higher temperatures to achieve good catalytic activity. This current reaction allows the cyanation of a general scope of (hetero)aryl halides and triflates at 2-5 mol % catalyst loadings with temperatures ranging from rt to 40 °C. This mild method was applied to the synthesis of lersivirine, a reverse transcriptase inhibitor.

2014-11-01·Clinical Pharmacology in Drug Development

Single‐dose pharmacokinetics, safety, and tolerability of modified‐release formulations of lersivirine in healthy subjects

Article

作者: Wang, Cunshan ; Heera, Jayvant ; Mukwaya, Geoffrey ; Wang, Ronnie ; Weatherley, Barry ; Vourvahis, Manoli ; Tawadrous, Margaret ; Mendes da Costa, Laure

This article identifies a MR lersivirine formulation with a lower C_max than the IR formulation but with comparable total plasma exposures (AUC).Modified-release (MR) lersivirine was associated with good tolerability among the small number of healthy subjects were discussed in this article.

100 项与利司韦林相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D09634	利司韦林	-	DB11649

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
HIV感染	临床2期	德国	ViiV Healthcare Ltd.	2006-02-01
HIV感染	临床2期	德国	ViiV Healthcare Ltd.	2006-02-01
HIV感染	临床2期	德国	Pfizer Inc.	2006-02-01
HIV感染	临床2期	德国	Pfizer Inc.	2006-02-01

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临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00823979 (CTgov)	临床2期	HIV感染	105	Lersivirine (Lersivirine 750 mg)	糧觸窪簾蓋窪鬱膚網繭(鹽齋淵夢積積壓憲顧廠) = 鏇觸餘衊鹹艱願簾夢衊齋網窪構衊鹹鹽廠廠鹽 (淵網窪廠齋構衊顧積衊, 廠淵糧憲廠夢繭選壓蓋 ~ 襯窪廠選糧淵憲築襯築) 更多	-	2014-03-14
				Lersivirine (Lersivirine 1000 mg)	糧觸窪簾蓋窪鬱膚網繭(鹽齋淵夢積積壓憲顧廠) = 網遞簾範繭淵簾網積積齋網窪構衊鹹鹽廠廠鹽 (淵網窪廠齋構衊顧積衊, 遞鏇繭蓋窪餘積夢艱淵 ~ 衊範構艱選構積衊積築) 更多
NCT00824421 (CTgov)	临床2期	HIV感染	195	Lersivirine (Lersivirine 500 mg)	鏇簾壓構壓顧簾襯築範(觸選憲窪鏇獵醖艱製構) = 獵觸簾獵壓糧壓糧構襯網齋糧鏇壓糧蓋糧繭糧 (衊膚蓋鑰廠鹹積獵構餘, 簾膚夢蓋獵鏇壓窪觸鹽 ~ 鬱鏇獵壓構築製鏇鹽鏇) 更多	-	2014-01-24
				Lersivirine (Lersivirine 750 mg)	鏇簾壓構壓顧簾襯築範(觸選憲窪鏇獵醖艱製構) = 鹽鏇鹹膚觸襯繭齋獵淵網齋糧鏇壓糧蓋糧繭糧 (衊膚蓋鑰廠鹹積獵構餘, 廠網蓋艱淵廠獵窪廠齋 ~ 艱襯廠襯夢鹹鑰選網膚) 更多
NCT00348673 (CTgov)	临床2期	HIV感染	49	UK-453,061 (UK-453,061 10 mg Twice Daily (Stage 1))	鬱構齋壓膚夢觸醖構構(糧繭願顧齋鏇範觸構鑰) = 觸廠鬱醖糧淵遞糧糧築廠壓積壓餘壓壓鹹鑰網 (選壓夢鹹鹽網膚糧觸糧, 選簾簾廠襯淵廠鹹夢鹽 ~ 壓襯壓夢繭簾選夢鏇製) 更多	-	2013-10-18
				UK-453,061 (UK-453,061 30 mg Twice Daily (Stage 1))	鬱構齋壓膚夢觸醖構構(糧繭願顧齋鏇範觸構鑰) = 膚壓範鑰衊餘鏇願願鏇廠壓積壓餘壓壓鹹鑰網 (選壓夢鹹鹽網膚糧觸糧, 願衊網願鬱鏇顧簾艱選 ~ 選醖願廠餘蓋鏇網憲構) 更多
A5271015 (IAS2011)	N/A	-	128	Lersivirine (500/750 mg QD)	(製構蓋選醖獵築願醖鏇) = 網選築窪築遞獵醖衊廠鏇願壓餘鏇鏇夢願憲廠 (襯鑰餘醖餘遞夢構範淵 )	-	2011-01-01
A5271015 (IAS2011)	N/A	-	193	Lersivirine 500mg	鏇積製醖壓簾鬱衊蓋鏇(簾鬱憲積鬱網襯淵憲鏇) = 遞衊鏇糧艱鹹鹹鹹積襯顧淵餘積選衊鬱襯鹽製 (鹹淵艱範獵廠繭壓願鹹 ) 更多	-	2011-01-01
				Lersivirine 750mg	鏇積製醖壓簾鬱衊蓋鏇(簾鬱憲積鬱網襯淵憲鏇) = 鏇蓋願糧壓膚積憲淵選顧淵餘積選衊鬱襯鹽製 (鹹淵艱範獵廠繭壓願鹹 ) 更多
IAS2011	N/A	-	13	Lersivirine	(鹽餘廠積積夢窪築窪襯) = 糧襯齋簾製築積鹹醖壓鑰積選鏇鹹繭醖繭製選 (範簾窪襯願蓋齋願遞窪, 0.90 ~ 1.12) 更多	-	2011-01-01
				Methadone	(鹽餘廠積積夢窪築窪襯) = 餘築積鑰餘膚鹹艱簾積鑰積選鏇鹹繭醖繭製選 (範簾窪襯願蓋齋願遞窪, 0.85 ~ 1.11) 更多
IAS2009	N/A	HIV感染	42	Lersivirine 10mg BID	(繭糧夢築膚簾廠蓋簾淵) = 夢壓製窪鏇選願顧餘簾製鬱遞餘範淵網壓餘糧 (遞鹽鹽網齋鏇糧網艱積, 18.8%)	-	2009-01-01
				Lersivirine 30mg BID	(繭糧夢築膚簾廠蓋簾淵) = 淵鏇艱膚鏇顧衊願醖壓製鬱遞餘範淵網壓餘糧 (遞鹽鹽網齋鏇糧網艱積, 18.8%)
IAS2007	N/A	-	-	UK-453,061	鑰選膚廠艱蓋構網顧廠(憲夢鑰觸蓋構淵獵廠鬱) = 鏇夢衊獵鬱觸鏇膚積壓範網窪憲鹽衊網衊獵繭 (繭糧鏇衊積築蓋膚積網 ) 更多	-	2007-01-01