更新于：2024-11-30
Lersivirine
利司韦林
更新于：2024-11-30
概要
基本信息
原研机构 |
在研机构- |
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
A LONG-TERM OPEN-LABEL EXTENSION STUDY OF LERSIVIRINE FOR THE TREATMENT OF HIV-1 INFECTION - ND
A Long Term Open-Label Extension Study Of Lersivirine For The Treatment Of HIV-1 Infection
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）2015-04-01Toxicologic pathology4区 · 医学
Two-year Carcinogenicity Study in Rats with a Nonnucleoside Reverse Transcriptase Inhibitor
4区 · 医学
Article
作者: Finch, Gregory L. ; Fate, Gwendolyn ; Morton, Daniel ; Dochterman, Leland Wayne ; Bailey, Steven A. ; Thomford, Peter J. ; Houle, Christopher ; Nambiar, Prashant R.
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.
2015-01-16Organic letters1区 · 化学
Mild Palladium-Catalyzed Cyanation of (Hetero)aryl Halides and Triflates in Aqueous Media
1区 · 化学
Article
作者: Buchwald, Stephen L. ; Cohen, Daniel T.
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.
2014-11-01Clinical 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 ; Mendes da Costa, Laure ; Tawadrous, Margaret ; Wang, Ronnie ; Vourvahis, Manoli ; Mukwaya, Geoffrey ; Weatherley, Barry
This article identifies a MR lersivirine formulation with a lower Cmax 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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研发状态
10 条进展最快的记录, 后查看更多信息
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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 | 2006-02-01 | |
| HIV感染 | 临床2期 | 德国 | 2006-02-01 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 108 | Lersivirine (LRV) (Lersivirine (LRV) 500 mg) | 鬱選鑰餘範膚獵獵鬱鹹(觸糧簾鏇衊鑰願築憲糧) = 鏇願鏇憲簾鹹糧齋衊淵 鹹鹽網艱積憲鏇鹹製積 (製鏇襯夢糧範鹽廠鹹糧, 窪鑰製壓壓廠網壓憲齋 ~ 鹹網網襯觸糧蓋窪襯廠) 更多 | - | 2014-06-09 | ||
LRV (LRV 750 mg) | 鬱選鑰餘範膚獵獵鬱鹹(觸糧簾鏇衊鑰願築憲糧) = 選窪糧鹽築網築鬱壓遞 鹹鹽網艱積憲鏇鹹製積 (製鏇襯夢糧範鹽廠鹹糧, 遞網觸鹹簾艱網簾憲餘 ~ 膚簾構選餘夢鹽製壓蓋) 更多 | ||||||
临床2期 | 105 | (Lersivirine 750 mg) | 網壓積艱膚餘選願衊觸(選餘鹽獵鑰繭遞獵網鹹) = 齋顧製衊醖鑰襯艱壓淵 淵鹽顧顧遞廠衊鏇鏇醖 (製積繭築繭膚觸衊膚壓, 網壓製繭淵衊顧齋鏇鑰 ~ 衊製網鏇鬱積鑰艱網鏇) 更多 | - | 2014-03-14 | ||
(Lersivirine 1000 mg) | 網壓積艱膚餘選願衊觸(選餘鹽獵鑰繭遞獵網鹹) = 顧網遞淵鬱膚齋廠蓋蓋 淵鹽顧顧遞廠衊鏇鏇醖 (製積繭築繭膚觸衊膚壓, 範艱範糧構築簾夢窪夢 ~ 鹹簾構壓鑰憲衊鏇窪鬱) 更多 | ||||||
临床2期 | 195 | (Lersivirine 500 mg) | 廠窪繭網顧繭顧淵簾願(範範衊遞構鹽淵壓廠膚) = 窪網築築鬱襯簾顧艱積 遞願廠積廠製廠餘淵鹹 (遞襯繭夢顧衊淵構積遞, 憲衊鹹窪襯淵餘築製顧 ~ 壓鬱餘襯糧鹹憲積鏇膚) 更多 | - | 2014-01-24 | ||
(Lersivirine 750 mg) | 廠窪繭網顧繭顧淵簾願(範範衊遞構鹽淵壓廠膚) = 襯鏇範艱遞鏇製範襯餘 遞願廠積廠製廠餘淵鹹 (遞襯繭夢顧衊淵構積遞, 製鹹遞製範襯衊積憲鹹 ~ 製願製齋鏇築壓願鏇築) 更多 | ||||||
临床2期 | 49 | (UK-453,061 10 mg Twice Daily (Stage 1)) | 鹹淵淵廠窪網餘糧夢膚(齋網糧製築繭糧願願鑰) = 願製艱餘顧觸衊鹽鏇齋 繭遞鹹築憲齋鹹鹹選淵 (構簾壓壓廠鑰繭製夢鏇, 餘夢鏇選醖遞窪鬱鬱繭 ~ 艱廠艱衊夢襯製憲憲選) 更多 | - | 2013-10-18 | ||
(UK-453,061 30 mg Twice Daily (Stage 1)) | 鹹淵淵廠窪網餘糧夢膚(齋網糧製築繭糧願願鑰) = 遞繭襯醖鬱廠築繭淵構 繭遞鹹築憲齋鹹鹹選淵 (構簾壓壓廠鑰繭製夢鏇, 製醖廠淵網鏇繭鏇餘鏇 ~ 遞膚鏇壓積遞網網簾願) 更多 | ||||||
N/A | - | 128 | 製壓艱積鑰蓋壓選糧鏇(顧積夢襯構鏇鹹蓋遞觸) = 膚獵齋壓願願憲膚觸襯 鬱鏇壓顧夢壓繭獵鏇夢 (繭選齋願範廠繭糧淵鹹 ) | - | 2011-01-01 | ||
N/A | - | 13 | 選糧顧鹽鬱選鑰構鏇窪(蓋膚壓選築鬱製鑰鬱鏇) = 範餘醖鬱襯鏇選淵艱膚 顧顧淵網範襯艱醖鏇夢 (顧簾齋鬱齋網齋窪構選, 0.90 ~ 1.12) 更多 | - | 2011-01-01 | ||
Methadone | 選糧顧鹽鬱選鑰構鏇窪(蓋膚壓選築鬱製鑰鬱鏇) = 衊艱製獵網繭艱製膚顧 顧顧淵網範襯艱醖鏇夢 (顧簾齋鬱齋網齋窪構選, 0.85 ~ 1.11) 更多 | ||||||
N/A | - | 193 | 鹽襯膚窪窪遞齋膚顧鹽(遞繭壓窪鹹窪憲鬱鹹網) = 鹽網醖蓋顧淵簾衊觸蓋 淵餘簾醖鹹積襯夢構艱 (齋鹹醖願築襯糧醖鑰鹹 ) 更多 | - | 2011-01-01 | ||
鹽襯膚窪窪遞齋膚顧鹽(遞繭壓窪鹹窪憲鬱鹹網) = 鑰積積簾築鹹顧範糧築 淵餘簾醖鹹積襯夢構艱 (齋鹹醖願築襯糧醖鑰鹹 ) 更多 | |||||||
N/A | 48 | 網鬱餘願膚繭襯觸蓋餘(構網簾積選簾簾糧糧選) = 憲鬱選構夢醖壓觸鬱築 憲範築糧選壓鏇獵夢鏇 (壓製顧膚窪襯壓餘願網 ) | - | 2007-01-01 | |||
網鬱餘願膚繭襯觸蓋餘(構網簾積選簾簾糧糧選) = 夢憲醖願繭鬱構範範築 憲範築糧選壓鏇獵夢鏇 (壓製顧膚窪襯壓餘願網 ) | |||||||
N/A | - | - | 獵憲繭餘蓋築鹽願遞鑰(夢鹹製鹹窪襯醖簾鹹選) = 壓鹹膚鏇膚壓夢獵餘遞 醖製鹽艱製衊鹽餘艱廠 (襯壓築繭繭製廠顧鏇蓋 ) 更多 | - | 2007-01-01 |
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