A5004615988- Hepatitis C virus research
- Hepatitis B Virus Studies
- Atrial Fibrillation Management and Outcomes
- Inflammatory mediators and NSAID effects
- Liver Disease Diagnosis and Treatment
- Pharmacogenetics and Drug Metabolism
- Statistical Methods in Clinical Trials
- Receptor Mechanisms and Signaling
- Venous Thromboembolism Diagnosis and Management
- Drug Transport and Resistance Mechanisms
- Antiplatelet Therapy and Cardiovascular Diseases
- Hormonal and reproductive studies
- Acute Myocardial Infarction Research
- Cardiac electrophysiology and arrhythmias
- Pharmacovigilance and Adverse Drug Reactions
- Drug-Induced Hepatotoxicity and Protection
- Heart Failure Treatment and Management
- Liver Diseases and Immunity
- HIV/AIDS drug development and treatment
- Pharmacological Effects and Toxicity Studies
- Statistical Methods and Inference
- Optimal Experimental Design Methods
- Health Systems, Economic Evaluations, Quality of Life
- Radiation Dose and Imaging
- Immunodeficiency and Autoimmune Disorders
Boehringer Ingelheim (Germany)
2006-2017
Inserm
2014
Hôpital Beaujon
2014
Boehringer Ingelheim (United States)
2014
Délégation Paris 7
2014
Université Paris Cité
2014
Boehringer Ingelheim (Denmark)
2012
Boehringer Ingelheim (Australia)
2012
Idera Pharmaceuticals (United States)
2011
World Water Watch
2011
Dabigatran etexilate is an oral low‐molecular‐weight direct thrombin inhibitor. Following administration, dabigatran rapidly converted to its active form, dabigatran. The authors investigated the absorption, distribution, and elimination of a single 150‐mg dose capsule formulation in healthy volunteers patients undergoing total hip replacement. In open‐label, 3‐way crossover study, was administered 18 male fasted state, after administration food with coadministration proton pump inhibitor,...
BILN-2061, a specific and potent peptidomimetic inhibitor of the HCV NS3 protease, has recently been shown to markedly lower serum hepatitis C virus (HCV)-RNA levels in patients chronically infected with genotype 1 three 2-day proof principle studies. The aim current study was assess antiviral efficacy BILN-2061 genotypes 2 3 infection. efficacy, pharmacokinetics, tolerability 500 mg twice-daily given as monotherapy for days 10 non-genotype (genotype 2: n = 3; 3: =7) minimal liver fibrosis...
Aim To investigate the effect of P ‐glycoprotein inhibitor verapamil on pharmacokinetics and pharmacodynamics dabigatran etexilate ( DE ). Method In this two part multiple crossover trial in 40 healthy subjects, 150 mg was given alone or with at different doses, duration treatment (single vs. dosing), formulations, timings (before, concurrently after Primary pharmacokinetic endpoints were determined from concentrations total (unconjugated plus conjugated). Pharmacodynamic clotting time....
Empagliflozin is an orally available, selective inhibitor of sodium glucose cotransporter 2. In this study, single oral doses empagliflozin from 0.5 to 800 mg were not associated with any clinically significant safety concerns in healthy male volunteers. The incidence adverse events (AEs) was similar subjects receiving placebo (22.2%) or (25.0%) the rising dose part study and after 50 under fed (28.6%) fasted conditions. most frequent AE headache. No relevant changes laboratory...
This study examined the effects of CYP3A/P-glycoprotein inducer, rifampicin, on pharmacokinetics dabigatran following oral administration prodrug, etexilate.This was an open-label, fixed-sequence, four-period in healthy volunteers. Subjects received a single dose etexilate 150 mg day 1, rifampicin 600 once daily days 2-8, and doses 9, 16 23.Twenty-four subjects were treated, whom 22 all treatments. Relative to reference (single alone; treatment A), 7 (treatment B) decreased geometric mean...
Abstract Faldaprevir (BI 201335) is a potent, hepatitis C virus (HCV) NS3/4A protease inhibitor with pharmacokinetic properties supportive of once-daily (QD) dosing. Four hundred and twenty-nine HCV genotype (GT)-1 treatment-naïve patients without cirrhosis were randomized 1:1:2:2 to receive 24 weeks pegylated interferon alfa-2a ribavirin (PegIFN/RBV) in combination placebo, faldaprevir 120 mg QD 3 days PegIFN/RBV lead-in (LI), 240 LI, or followed by an additional PegIFN/RBV. Patients the...
BackgroundBILB 1941 is a potent and specific non-nucleoside inhibitor of the hepatitis C virus (HCV) RNA polymerase in vitro.MethodsIn double-blind sequential group comparison, 96 male HCV genotype 1 patients with minimal to mild liver fibrosis (Ishak or Metavir score 0–2) were randomized (8 active treatment 2 placebo per dose group) treated 10–450 mg BILB every 8 h over 5 days. Viral load (VL) was measured using Roche Cobas TaqMan® assays.ResultsVL decreased by ≥1 log10 IU/ml 2/8, 1/8, 2/7,...
Abstract Faldaprevir (BI 201335) is a potent, hepatitis C virus (HCV) NS3/4A protease inhibitor. In all, 290 noncirrhotic HCV genotype (GT)-1 patients with prior null (<1 log10 viral load [VL] drop at any time on treatment) or partial response (≥1 VL but never undetectable were randomized 2:1:1 to receive 48 weeks of peginterferon alfa-2a and ribavirin (PegIFN/RBV) in combination faldaprevir 240 mg once daily (QD) 3 days PegIFN/RBV lead-in (LI), QD without LI, twice (BID) LI. Patients the...
1. In a randomized, double‐blind trial we compared the inhibition of platelet‐vessel wall interactions in whole blood ex vivo. There were four groups 24 healthy volunteers each whom treated orally for 3.5 days with either 200 mg dipyridamole (sustained release preparation), 25 acetylsalicylic acid, both drugs combined or placebo twice daily. 2. The mean area all platelets/aggregates was reduced by 6.2% +/− 4.2% (+/− s.e. mean) (n = 23), 19.8% 6.7% 22), 53.7% 4.9% acid 23) and 71.4% 3.7%...
Faldaprevir (BI 201335) and deleobuvir 207127) are direct-acting antiviral agents under development for the treatment of chronic HCV infection. This article describes final results Phase Ib SOUND-C1 study that evaluated interferon-free oral combination faldaprevir, ribavirin in 32 treatment-naive patients infected with genotype 1.Patients were randomized to receive 400 mg (n=15) or 600 (n=17) three times daily plus faldaprevir 120 once weight-based 4 weeks. Interferon-free therapy was...
Faldaprevir, an investigational agent for hepatitis C virus treatment, is well tolerated but associated with rapidly reversible, dose-dependent, clinically benign, unconjugated hyperbilirubinemia. Multidisciplinary preclinical and clinical studies were used to characterize mechanisms underlying this In vitro, faldaprevir inhibited key processes involved in bilirubin clearance: UDP glucuronosyltransferase (UGT) 1A1 (UGT1A1) (IC<sub>50</sub> 0.45 <i>µ</i>M), which conjugates bilirubin, hepatic...
Meloxicam is a new enol carboxamide nonsteroidal antiinflammatory drug (NSAID). Preclinical studies have indicated that it possesses high potency and low ulcerogenic potency. This open, randomized, crossover study was conducted to examine the effects of aspirin, antacid Maalox (Rhone‐Poulenc Rorer, Cologne, Germany), cimetidine on pharmacokinetics bioavailability single oral dose meloxicam 30 mg in healthy male volunteers. Plasma concentrations were determined subjected noncompartmental...
Deleobuvir (BI 207127) is an investigational oral nonnucleoside inhibitor of hepatitis C virus (HCV) NS5B RNA polymerase. Antiviral activity, virology, pharmacokinetics, and safety were assessed in HCV genotype 1-infected patients receiving 5 days' deleobuvir monotherapy. In this double-blind phase 1b study, treatment-naive (TN; n = 15) treatment-experienced (TE; 45) without cirrhosis received placebo or at 100, 200, 400, 800, 1,200 mg every 8 h (q8h) for days. Patients with (n 13) 400 600...
We analysed viral kinetics from a 2-day treatment with BILN 2061, serine protease inhibitor of hepatitis C virus, in patients chronically infected genotype 1 virus. The efficiency (E), describing inhibition production, was above 99.45% all minor or moderate fibrosis receiving doses 200mg and 500 mg twice daily larger than previous studies for interferon-based treatments. However, epsilon slightly smaller cirrhosis given markedly 25 mg. Estimates clearance infected-cell loss support...
1 The pharmacokinetics and tolerability of a new nonsteroidal anti‐inflammatory drug (NSAID), meloxicam, administered i.m., were investigated in two studies conducted healthy male volunteers. Study was an open, placebo‐controlled design which 32 volunteers randomized to single ascending i.m. dose meloxicam (5, 10, 20, 30 mg) or placebo. 2 had way crossover 12 received i.v. doses (15 mg). Meloxicam showed excellent both studies. No effect seen on serum creatinphosphokinase (CK, the isoenzyme...