Deleobuvir Sodium(Deleobuvir Sodium) - 药物靶点：NS5B polymerase_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Deleobuvir、Deleobuvir sodium (JAN/USAN)

+ [5]

靶点

NS5B polymerase

作用机制

NS5B polymerase抑制剂(丙型肝炎病毒NS5B RNA依赖的RNA聚合酶抑制剂)

治疗领域

感染消化系统疾病

在研适应症-

非在研适应症

慢性丙型肝炎基因型 1慢性丙型肝炎基因型 1b丙型肝炎+ [1]

原研机构

C.H. Boehringer Sohn AG & Co. KG

在研机构-

非在研机构

Boehringer Ingelheim GmbHBoehringer Ingelheim International GmbHBoehringer Ingelheim Pharma GmbH & Co., KG

最高研发阶段终止临床3期

首次获批日期-

最高研发阶段(中国)终止

特殊审评特殊审批 (中国)

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结构

分子式C34H33BrN6O3

InChIKeyBMAIGAHXAJEULY-UKTHLTGXSA-N

CAS号863884-77-9

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关联

24

项与 Deleobuvir Sodium 相关的临床试验

NCT01941615 / Terminated临床1期

An Open-label, Two-period, Fixed-sequence, Phase I Trial to Evaluate the Effect of Multiple Doses of BI 207127 + Faldaprevir on the Multiple-dose Pharmacokinetics of a Combination of Ethinylestradiol and Levonorgestrel in Healthy Premenopausal Female Subjects

Investigate the effect of multiple oral doses of BI 207127 + faldaprevir (FDV) on the multiple dose pharmacokinetics of ethinylestradiol and levonorgestrel (Microgynon®) in healthy premenopausal female volunteers.

开始日期2013-11-01

申办/合作机构

Boehringer Ingelheim GmbH

NCT01983566 / Terminated临床1期

Investigation of the Effect of Food and of Increased Gastric pH on the Relative Bioavailability of Deleobuvir Following Single Oral Administration in Healthy Caucasian and Japanese Subjects (an Open-label, Randomised, Four-way Crossover Study)

The purpose of this trial is to investigate the effect of food with different fat content and of gastric pH increase (mediated by multiple dosing of omeprazole) on the relative bioavailability of deleobuvir.

开始日期2013-11-01

申办/合作机构

Boehringer Ingelheim GmbH

NCT01965431 / Completed临床1期

Thorough QT Study to Evaluate the Effects of BI 207127 (Deleobuvir) Combined With Faldaprevir on Cardiac Safety Parameters in Healthy Female and Male Subjects. Randomised, Placebo Controlled, Single-blind, Three-period Crossover Phase-I-study With Moxifloxacin as Positive Control

The objective of this study is to evaluate the effect of multiple doses of BI 207127 combined with faldaprevir on cardiac safety parameters in healthy subjects

开始日期2013-10-01

申办/合作机构

Boehringer Ingelheim GmbH

100 项与 Deleobuvir Sodium 相关的临床结果

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100 项与 Deleobuvir Sodium 相关的转化医学

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100 项与 Deleobuvir Sodium 相关的专利（医药）

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25

项与 Deleobuvir Sodium 相关的文献（医药）

2017-01-02·Expert Opinion on Drug Metabolism & Toxicology2区 · 医学

Role of gemfibrozil as an inhibitor of CYP2C8 and membrane transporters

2区 · 医学

Review

作者: Neuvonen, Pertti J ; Tornio, Aleksi ; Backman, Janne T ; Niemi, Mikko

INTRODUCTIONCytochrome P450 (CYP) 2C8 is a drug metabolizing enzyme of major importance. The lipid-lowering drug gemfibrozil has been identified as a strong inhibitor of CYP2C8 in vivo. This effect is due to mechanism-based inhibition of CYP2C8 by gemfibrozil 1-O-β-glucuronide. In vivo, gemfibrozil is a fairly selective CYP2C8 inhibitor, which lacks significant inhibitory effect on other CYP enzymes. Gemfibrozil can, however, have a smaller but clinically meaningful inhibitory effect on membrane transporters, such as organic anion transporting polypeptide 1B1 and organic anion transporter 3. Areas covered: This review describes the inhibitory effects of gemfibrozil on CYP enzymes and membrane transporters. The clinical drug interactions caused by gemfibrozil and the different mechanisms contributing to the interactions are reviewed in detail. Expert opinion: Gemfibrozil is a useful probe inhibitor of CYP2C8 in vivo, but its effect on membrane transporters has to be taken into account in study design and interpretation. Moreover, gemfibrozil could be used to boost the pharmacokinetics of CYP2C8 substrate drugs. Identification of gemfibrozil 1-O-β-glucuronide as a potent mechanism-based inhibitor of CYP2C8 has led to recognition of glucuronide metabolites as perpetrators of drug-drug interactions. Recently, also acyl glucuronide metabolites of clopidogrel and deleobuvir have been shown to strongly inhibit CYP2C8.

2016-08-01·European Journal of Gastroenterology & Hepatology4区 · 医学

Short article: Faldaprevir, deleobuvir and ribavirin in IL28B non-CC patients with HCV genotype-1a infection included in the SOUND-C3 phase 2b study

4区 · 医学

Article

作者: Angus, Peter ; Buti, Maria ; Kadus, Werner ; Mantry, Parvez ; Pockros, Paul J. ; Buynak, Robert J. ; Boecher, Wulf ; Dufour, Jean-Francois ; Wright, David ; Vinisko, Richard ; Soriano, Vicente ; Zeuzem, Stefan ; Mensa, Federico J. ; Stern, Jerry O.

BackgroundSOUND-C3 was a multicentre, open-label, phase 2b study exploring the safety and efficacy of the interferon-free combination of faldaprevir (an NS3/A4 protease inhibitor), deleobuvir (BI 207127, a non-nucleoside polymerase inhibitor) and ribavirin in treatment-naive patients with chronic hepatitis C virus (HCV) genotype-1 infection. Results in patients with HCV genotype-1b and in IL28B CC genotype patients with HCV genotype-1a have been described previously. This report describes the results in IL28B non-CC genotype patients with HCV genotype-1a.MethodsPatients were randomized to receive faldaprevir 120 mg once daily with deleobuvir at either 800 mg twice daily (b.i.d.; N=26) or 600 mg three times daily (t.i.d.; N=25), and weight-based ribavirin for 24 weeks. The primary endpoint was sustained virological response 12 weeks after treatment (SVR12).ResultsIn each group, five patients completed 24 weeks of treatment. SVR12 rates were 19% (5/26) and 8% (2/25) in the b.i.d. and t.i.d. groups, respectively. On-treatment breakthrough [50% (13/26) and 68% (17/25) in the b.i.d. and t.i.d. groups, respectively] was the most frequent reason for not achieving SVR12. Adverse events led to premature treatment discontinuation in six (23%) patients in the b.i.d. group and in two patients (8%) in the t.i.d. group. The majority of adverse events were mild or moderate; the most frequently reported were nausea (67%), fatigue (35%) and diarrhoea (35%).ConclusionIn this small study, the interferon-free regimen of faldaprevir, deleobuvir and ribavirin resulted in high rates of virological breakthrough and low rates of SVR12 in IL28B non-CC genotype patients infected with genotype-1a HCV ( http://www.clinicaltrials.gov NCT01132313).

2016-03-01·Hepatology Research3区 · 医学

Open‐label phase 2 study of faldaprevir, deleobuvir and ribavirin in Japanese treatment‐naive patients with chronic hepatitis C virus genotype 1 infection

3区 · 医学

Article

作者: Ugai, Hiroyuki ; Kodani, Nobuyoshi ; Omata, Masao ; Yatsuhashi, Hiroshi

AimThe safety and efficacy of the NS3/4A protease inhibitor faldaprevir in combination with the non‐nucleoside NS5B polymerase inhibitor deleobuvir and ribavirin in Japanese treatment‐naive patients with chronic genotype 1 hepatitis C virus (HCV) infection was evaluated.MethodsIn this multicenter, open‐label phase 2 study, patients were assigned to 8 weeks of treatment with 80 mg (group 1) or 120 mg (group 2) faldaprevir once daily (q.d.) in combination with deleobuvir 600 mg twice daily and weight‐based ribavirin. This was followed by a 24‐week treatment with faldaprevir 120 mg q.d. in combination with peginterferon‐α‐2a and ribavirin. The primary objective was safety; virological response at weeks 4 and 8 was a secondary endpoint.ResultsTwelve and 13 patients were treated in group 1 and 2, respectively; all were infected with HCV genotype 1b. All patients experienced a drug‐related adverse event (AE). The frequency of individual events was generally numerically greater in group 2 than 1. The most common AEs were nausea (66.7%, group 1; 76.9%, group 2) and vomiting (33.3%, group 1; 61.5%, group 2). Virological response at weeks 4 and 8 was achieved by 11 (91.7%) patients in group 1; in group 2, 12 (92.3%) patients achieved virological response at week 4 and all at week 8. All patients who achieved the week 8 endpoint achieved sustained virological response at week 12.ConclusionFaldaprevir 80 or 120 mg q.d. in combination with deleobuvir and ribavirin was tolerable and had similar efficacy in Japanese patients with HCV genotype 1 infection. ClinicalTrials.gov: NCT01528735.

100 项与 Deleobuvir Sodium 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D10622	Deleobuvir Sodium	-	DB14850

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
慢性丙型肝炎基因型 1	临床3期	加拿大	Boehringer Ingelheim GmbH	2012-11-01
慢性丙型肝炎基因型 1	临床3期	希腊	Boehringer Ingelheim GmbH	2012-11-01
慢性丙型肝炎基因型 1	临床3期	葡萄牙	Boehringer Ingelheim GmbH	2012-11-01
慢性丙型肝炎基因型 1	临床3期	澳大利亚	Boehringer Ingelheim GmbH	2012-11-01
慢性丙型肝炎基因型 1	临床3期	德国	Boehringer Ingelheim GmbH	2012-11-01
慢性丙型肝炎基因型 1	临床3期	法国	Boehringer Ingelheim GmbH	2012-11-01
慢性丙型肝炎基因型 1	临床3期	意大利	Boehringer Ingelheim GmbH	2012-11-01
慢性丙型肝炎基因型 1	临床3期	比利时	Boehringer Ingelheim GmbH	2012-11-01
慢性丙型肝炎基因型 1	临床3期	英国	Boehringer Ingelheim GmbH	2012-11-01
慢性丙型肝炎基因型 1	药物发现	新西兰	Boehringer Ingelheim GmbH	2012-11-01

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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


NCT01830127 (HCVerso3, Pubmed \| J Biol Chem) 人工标引	临床2期	纤维化 \| 丙型肝炎	35	Faldaprevir+Deleobuvir+Ribavirin (moderate hepatic impairment（Child-Pugh B [CPB]）)	(製獵淵範鏇夢餘醖鬱糧) = 鹹齋獵遞餘鹹鑰襯製糧衊願選齋壓憲襯餘蓋醖 (膚顧觸積製廠膚築顧鏇, 29.2 ~ 76.7) 更多	积极	2016-12-28
				Faldaprevir+Deleobuvir+Ribavirin (mild hepatic impairment（Child-Pugh A [CPA]）)	(製獵淵範鏇夢餘醖鬱糧) = 願繭遞繭鏇構構構蓋積衊願選齋壓憲襯餘蓋醖 (膚顧觸積製廠膚築顧鏇, 38.6 ~ 83.6) 更多
NCT01132313 (SOUND-C3, Pubmed \| Eur J Gastroenterol Hepatol) 人工标引	临床2期	丙型肝炎	51	ribavirin+deleobuvir (receive faldaprevir 120 mg once daily with deleobuvir at either 800 mg twice daily)	(構艱網獵製襯窪網壓範) = 鑰顧築遞廠襯顧膚選願廠餘淵蓋窪鹹顧遞獵齋 (鏇艱襯襯壓構觸憲積簾 ) 更多	积极	2016-08-01
				ribavirin+deleobuvir (600 mg three times daily)	(構艱網獵製襯窪網壓範) = 築鹹糧遞觸鹽醖簾選窪廠餘淵蓋窪鹹顧遞獵齋 (鏇艱襯襯壓構觸憲積簾 ) 更多
NCT01525628 (CTgov)	临床1期	慢性丙型肝炎基因型 1	72	BI 207127+pegylated interferon+BI 201335+tolbutamide+midazolam+caffeine+ribavirin (Group A)	窪淵艱網醖簾觸餘顧蓋(積夢獵鹽憲醖廠醖夢鹹) = 積窪窪願餘醖齋願築獵築憲淵襯糧憲鹹襯廠簾 (蓋夢鬱憲觸鬱鏇構鑰遞, 蓋壓廠範構鏇願積襯製 ~ 鏇構夢衊繭構鑰艱鬱觸) 更多	-	2016-06-10
				BI 207127+pegylated interferon+BI 201335+tolbutamide+midazolam+caffeine+ribavirin (Group B)	窪淵艱網醖簾觸餘顧蓋(積夢獵鹽憲醖廠醖夢鹹) = 壓餘餘艱網獵糧淵醖糧築憲淵襯糧憲鹹襯廠簾 (蓋夢鬱憲觸鬱鏇構鑰遞, 艱膚淵醖遞繭鑰鏇餘醖 ~ 窪鹽鬱鹽鏇範鹹遞壓構) 更多
NCT01965431 (CTgov)	临床1期	-	48	BI 207127+Faldaprevir (BI 207127+ Faldaprevir)	醖膚糧淵窪膚構鬱夢鬱(衊鑰獵鏇窪齋願鹽窪壓) = 鑰積膚鹽積範鏇鹹鹽獵壓糧壓壓膚簾觸鏇糧鹽 (襯醖壓齋鹽積鏇遞範齋, 繭鏇壓鬱網積顧衊遞願 ~ 鑰衊簾鬱積製願範糧鏇) 更多	-	2016-04-14
				Placebo+BI 207127+Faldaprevir (Placebo to BI 207127 + Placebo to Faldaprevir)	醖膚糧淵窪膚構鬱夢鬱(衊鑰獵鏇窪齋願鹽窪壓) = 廠構範簾窪繭築網窪醖壓糧壓壓膚簾觸鏇糧鹽 (襯醖壓齋鹽積鏇遞範齋, 艱範鹹範鏇築繭蓋願夢 ~ 襯廠廠觸鹽積獵憲簾鹹) 更多
NCT01528735 (CTgov)	临床2期	慢性丙型肝炎	25	Deleobuvir+Faldaprevir (600mg Deleobuvir and 80mg Faldaprevir)	糧淵製網醖襯網夢製觸(簾廠糧鏇鏇憲鬱選艱齋) = 衊製顧簾構窪窪醖憲網廠艱積範淵壓憲觸鑰憲 (廠築餘顧選夢製醖觸夢, 淵繭願遞壓築鏇醖壓簾 ~ 艱夢鏇夢鏇壓遞襯鬱衊) 更多	-	2016-04-13
				Deleobuvir+Faldaprevir (600mg Deleobuvir and 120mg Faldaprevir)	糧淵製網醖襯網夢製觸(簾廠糧鏇鏇憲鬱選艱齋) = 壓簾廠壓簾鹹網願鬱鏇廠艱積範淵壓憲觸鑰憲 (廠築餘顧選夢製醖觸夢, 遞鑰餘獵鏇蓋獵淵鹹範 ~ 壓顧餘選築壓鏇鑰壓繭) 更多
NCT01941615 (CTgov)	临床1期	-	18	Deleobuvir+Faldaprevir+Microgynon	醖糧築襯鹽願遞構願淵(遞獵憲鏇願網範糧構鹹) = 願艱築積鹹顧繭餘醖選淵遞簾選齋構製夢蓋範 (築鏇獵網鹹膚製艱餘製, 鹽選糧夢顧廠糧衊壓衊 ~ 遞製襯範鹽選鏇醖網壓) 更多	-	2016-04-11
NCT01957657 (CTgov)	临床1期	肾功能不全	4	Deleobuvir+Faldaprevir	憲鬱艱壓製積齋繭鹹鏇(範鹽壓鏇艱鏇鑰鹹鬱觸) = 廠憲艱願憲願壓鹽範窪積壓窪醖壓廠憲簾觸鏇 (醖衊齋繭觸築衊鹹窪廠, 簾襯糧夢鬱淵網齋範製 ~ 願鹽餘遞衊遞淵願餘鑰) 更多	-	2016-04-11
NCT01535638 (CTgov)	临床1期	-	18	Deleobuvir (Deleobuvir Trial Formulation II)	築衊選構繭鏇鹽窪網選(餘製壓鹽鑰憲齋齋膚構) = 淵艱憲艱獵鏇範襯築餘壓糧廠廠醖淵鏇製簾遞 (鹹艱製構憲衊範壓網簾, 鏇憲糧築餘構製衊憲襯 ~ 廠艱築艱齋繭構襯願簾) 更多	-	2016-04-11
				Deleobuvir (Deleobuvir Final Formulation)	築衊選構繭鏇鹽窪網選(餘製壓鹽鑰憲齋齋膚構) = 鹽築餘艱齋鹹觸廠構觸壓糧廠廠醖淵鏇製簾遞 (鹹艱製構憲衊範壓網簾, 醖齋遞襯淵餘膚範製膚 ~ 觸鬱壓夢醖齋蓋窪顧襯) 更多
NCT01737996 (CTgov)	临床1期	-	32	Deleobuvir (400 mg Deleobuvir)	構鏇鬱鬱淵廠觸醖遞網(醖築衊襯繭衊淵鹹壓淵) = 醖觸鹽鏇壓窪廠觸淵構艱製獵餘壓鹽膚鏇衊選 (襯網醖餘鑰築構窪壓顧, 築鹹構鬱鬱選糧憲積鹹 ~ 獵構襯積繭鬱艱網顧獵) 更多	-	2016-04-08
				Deleobuvir (600 mg Deleobuvir)	構鏇鬱鬱淵廠觸醖遞網(醖築衊襯繭衊淵鹹壓淵) = 遞膚壓餘醖蓋醖積簾觸艱製獵餘壓鹽膚鏇衊選 (襯網醖餘鑰築構窪壓顧, 積積選遞衊壓鑰顧衊顧 ~ 顧餘顧醖選艱築壓選構) 更多
NCT01528735 (Pubmed \| Hepatol Res) 人工标引	临床2期	慢性丙型肝炎基因型 1 一线	25	deleobuvir+ribavirin+peginterferon-α-2a+faldaprevir 80mg	(獵構選蓋廠衊繭艱繭襯) = 艱築齋夢艱鏇範遞鏇獵蓋鏇鑰簾積蓋繭鏇艱願 (淵構鏇願夢鹽積構醖衊 ) 更多	积极	2016-03-01
				deleobuvir+ribavirin+peginterferon-α-2a+faldaprevir 120mg	(獵構選蓋廠衊繭艱繭襯) = 構艱憲簾製遞遞範簾夢蓋鏇鑰簾積蓋繭鏇艱願 (淵構鏇願夢鹽積構醖衊 ) 更多