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Year Number of Results
2004 1
2005 2
2006 5
2007 14
2008 17
2009 22
2010 34
2011 104
2012 151
2013 193
2014 233
2015 172
2016 62
2017 25
2018 14
2019 6
2020 0
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923 results
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Page 1
Validating Enterovirus D68-2A(pro) as an Antiviral Drug Target and the Discovery of Telaprevir as a Potent D68-2A(pro) Inhibitor.
Musharrafieh R, et al. J Virol 2019. PMID 30674624 Free PMC article.
Telaprevir inhibits EV-D68 2A(pro) through a nearly irreversible, biphasic binding mechanism. In cell culture, telaprevir showed submicromolar-to-low-micromolar potency against several recently circulating neurotropic strains of EV-D68 in different human cell lines. ...The binding of telaprevir potently inhibits its enzymatic activity, and using drug resistance selection, we show that the potent antiviral activity of telaprevir was due to 2A(pro) inhibition. ...
Telaprevir inhibits EV-D68 2A(pro) through a nearly irreversible, biphasic binding mechanism. In cell culture, telaprevir show
[Telaprevir resistance].
Poveda E and García F. Enferm Infecc Microbiol Clin 2013 - Review. PMID 24063900 Spanish.
Like other HCV protease inhibitors, telaprevir has a low genetic barrier to resistance. Phase II/III clinical trials (ADVANCE, ILLUMINATE and REALIZE) have characterized resistance to telaprevir in combination with pegylated interferon and ribavirin both genotypically and phenotypically. ...The presence of polymorphisms or mutations associated with telaprevir resistance is very low (< 1%), especially for mutations with a higher impact on resistance. ...
Like other HCV protease inhibitors, telaprevir has a low genetic barrier to resistance. Phase II/III clinical trials (ADVANCE, ILLUMI …
Telaprevir-induced DRESS.
Kesar V, et al. J Drugs Dermatol 2014. PMID 24509972
Telaprevir, a protease inhibitor, was recently approved for management of Chronic Hepatits C (CHC) due to HCV genotype 1. Various RCTs have demonstarted increased incidence of cutaneous adverse effects with use of Telaprevir. Herein, we report two cases of drug rash with eosinophilia and systemic symptoms (DRESS) secondary to Telaprevir use....
Telaprevir, a protease inhibitor, was recently approved for management of Chronic Hepatits C (CHC) due to HCV genotype 1. Various RCT
Pharmacokinetic characteristics of telaprevir in healthy Korean male subjects and comparisons with Japanese.
Choi Y, et al. Drug Des Devel Ther 2018. PMID 29750017 Free PMC article.
In this study, the pharmacokinetic profile, safety, and tolerability of telaprevir and the effect of food on telaprevir exposure were evaluated in healthy Korean subjects, and compared with data from a previous study in Japanese male subjects. ...CONCLUSION: In conclusion, the telaprevir's pharmacokinetic characteristics were similar in Korean and Japanese subjects. Telaprevir was well tolerated in a single dose of up to 1,250 mg and in multiple doses of 750 mg....
In this study, the pharmacokinetic profile, safety, and tolerability of telaprevir and the effect of food on telaprevir exposu …
Twice-Daily Telaprevir for Posttransplant Genotype 1 Hepatitis C Virus: A Prospective Safety, Efficacy, and Pharmacokinetics Study.
Rubin RA, et al. Exp Clin Transplant 2018 - Clinical Trial. PMID 27855589 Free article.
During telaprevir treatment, median doses of tacrolimus and cyclosporine were 0.5 mg weekly and 25 mg daily. Target exposures were achieved for telaprevir with twice daily dosing and for ribavirin with reduced initial dosing. ...Calcineurin inhibitor dosing levels were substantially reduced with telaprevir....
During telaprevir treatment, median doses of tacrolimus and cyclosporine were 0.5 mg weekly and 25 mg daily. Target exposures were ac …
Effects of boceprevir and telaprevir on the pharmacokinetics of dolutegravir.
Johnson M, et al. Br J Clin Pharmacol 2014 - Clinical Trial. PMID 24838177 Free PMC article.
AIMS: The aim was to evaluate the effect of boceprevir and telaprevir on dolutegravir pharmacokinetics (PK); the effect of dolutegravir on boceprevir and telaprevir PK was assessed through comparison with historical data for each hepatitis C virus (HCV) drug's prescribing information alone. ...Coadministration of boceprevir or telaprevir with dolutegravir had no clinically significant effect on dolutegravir PK. Plasma boceprevir and telaprevir PK data for either combined treatment were similar to historical data, indicating no effect of dolutegravir on boceprevir or telaprevir exposure. ...
AIMS: The aim was to evaluate the effect of boceprevir and telaprevir on dolutegravir pharmacokinetics (PK); the effect of dolutegrav …
Intracellular and Plasma Trough Concentration and Pharmacogenetics of Telaprevir.
Cusato J, et al. J Pharm Pharm Sci 2015. PMID 26158282 Free article.
PURPOSE: Triple therapy for HCV-1 infection consists in boceprevir or telaprevir, ribavirin and PEG-interferon. Telaprevir is a P-glycoprotein substrate and it is metabolized by CYP3A4/5. ...Plasma ribavirin concentrations were directly correlated with plasma S-telaprevir concentrations. In linear regression analysis, only CYP24A1_rs2585428 SNP (p=0.003) and body mass index (p=0.038) were able to predict S-telaprevir PBMC concentrations. ...
PURPOSE: Triple therapy for HCV-1 infection consists in boceprevir or telaprevir, ribavirin and PEG-interferon. Telaprevir is …
Telaprevir drug monitoring during antiviral therapy of hepatitis C graft infection after liver transplantation.
Farnik H, et al. Liver Int 2015. PMID 24649882
Pharmacokinetic studies have shown significant drug-drug interactions between telaprevir and immunosuppression (IS), but telaprevir pharmacokinetics in OLT patients with IS are unknown. ...In one patient with tacrolimus-based IS, telaprevir dose had to be adjusted to achieve virological response. Telaprevir plasma concentrations were steady at treatment weeks 4, 8 and 12 in patients with and without IS. ...
Pharmacokinetic studies have shown significant drug-drug interactions between telaprevir and immunosuppression (IS), but telaprevi
Conformational study on telaprevir by HPLC-DAD-MS and theoretical calculation.
Sun X, et al. Biomed Chromatogr 2019. PMID 31276615
In the present work, the E-Z isomerization process of telaprevir in solution was revealed by online HPLC-DAD (diode array detector)-MS, variable-temperature and variable-gradient experiments. ...The investigation can provide more structure information about telaprevir in solution and in the binding process of HCV NS3•4A protease....
In the present work, the E-Z isomerization process of telaprevir in solution was revealed by online HPLC-DAD (diode array detector)-M …
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