The Pharmacokinetic Interaction Between an Oral Contraceptive Containing Ethinyl Estradiol and Norethindrone and the HCV Protease Inhibitor Telaprevir

2012 ◽  
Vol 52 (10) ◽  
pp. 1574-1583 ◽  
Author(s):  
Varun Garg ◽  
Rolf van Heeswijk ◽  
Yijun Yang ◽  
Robert Kauffman ◽  
Frances Smith ◽  
...  
Keyword(s):  
Oral Contraceptive ◽  
Protease Inhibitor ◽  
Ethinyl Estradiol ◽  
Pharmacokinetic Interaction ◽  
Hcv Protease ◽  
Protease Inhibitor Telaprevir

1244 THE PHARMACOKINETIC INTERACTION BETWEEN METHADONE AND THE INVESTIGATIONAL HCV PROTEASE INHIBITOR TELAPREVIR

2011 ◽  
Vol 54 ◽  
pp. S491-S492 ◽  
Author(s):  
R. van Heeswijk ◽  
A. Vandevoorde ◽  
P. Verboven ◽  
G. Boogaerts ◽  
E. De Paepe ◽  
...  
Keyword(s):  
Protease Inhibitor ◽  
Pharmacokinetic Interaction ◽  
Hcv Protease ◽  
Protease Inhibitor Telaprevir

Stereoselective Lithiation and Carboxylation of Boc-Protected Bicyclopyrrolidine: Synthesis of a Key Building Block for HCV Protease Inhibitor Telaprevir

2014 ◽  
Vol 18 (10) ◽  
pp. 1234-1244 ◽  
Author(s):  
Gerald J. Tanoury ◽  
Minzhang Chen ◽  
Yong Dong ◽  
Raymond Forslund ◽  
Valdas Jurkauskas ◽  
...  
Keyword(s):  
Protease Inhibitor ◽  
Building Block ◽  
Hcv Protease ◽  
Protease Inhibitor Telaprevir

scholarly journals Pharmacokinetic Interaction between Telaprevir and Methadone

2013 ◽  
Vol 57 (5) ◽  
pp. 2304-2309 ◽  
Author(s):  
Rolf van Heeswijk ◽  
Peter Verboven ◽  
Ann Vandevoorde ◽  
Petra Vinck ◽  
Jan Snoeys ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Methadone Maintenance ◽  
Pharmacokinetic Interaction ◽  
Opioid Withdrawal ◽  
Maximum Plasma ◽  
Time Curve ◽  
Hcv Antibody ◽  
Hcv Protease ◽  
Protease Inhibitor Telaprevir ◽  
Time Of Administration

ABSTRACTHepatitis C virus (HCV) antibody is present in most patients enrolled in methadone maintenance programs. Therefore, interactions between the HCV protease inhibitor telaprevir and methadone were investigated. The pharmacokinetics ofR-andS-methadone were measured after administration of methadone alone and after 7 days of telaprevir (750 mg every 8 h [q8h]) coadministration in HCV-negative subjects on stable, individualized methadone therapy. UnboundR-methadone was measured in predose plasma samples before and during telaprevir coadministration. Safety and symptoms of opioid withdrawal were evaluated throughout the study. In total, 18 subjects were enrolled; 2 discontinued prior to receiving telaprevir. The minimum plasma concentration in the dosing interval (Cmin), the maximum plasma concentration (Cmax), and the area under the plasma concentration-time curve from h 0 (time of administration) to 24 h postdose (AUC0–24) forR-methadone were reduced by 31%, 29%, and 29%, respectively, in the presence of telaprevir. The AUC0–24ratio ofS-methadone/R-methadone was not altered. The median unbound percentage ofR-methadone increased by 26% in the presence of telaprevir. TheR-methadone median (absolute) unboundCminvalues in the absence (10.63 ng/ml) and presence (10.45 ng/ml) of telaprevir were similar. There were no symptoms of opioid withdrawal and no discontinuations due to adverse events. In summary, exposure to totalR-methadone was reduced by approximately 30% in the presence of telaprevir, while the exposure to unboundR-methadone was unchanged. No symptoms of opioid withdrawal were observed. These results suggest that dose adjustment of methadone is not required when initiating telaprevir treatment. (This study has been registered at ClinicalTrials.gov under registration no. NCT00933283.)

Determination of the HCV Protease Inhibitor Telaprevir in Plasma and Dried Blood Spot by Liquid Chromatography–Tandem Mass Spectrometry

2015 ◽  
Vol 37 (5) ◽  
pp. 626-633 ◽  
Author(s):  
Corrien P. W. G. M. Verweij-van Wissen ◽  
Marga J. A. de Graaff-Teulen ◽  
Clara T. M. M. de Kanter ◽  
Rob E. Aarnoutse ◽  
David M. Burger
Keyword(s):  
Mass Spectrometry ◽  
Liquid Chromatography ◽  
Protease Inhibitor ◽  
Tandem Mass ◽  
Chromatography Tandem Mass Spectrometry ◽  
Liquid Chromatography Tandem Mass ◽  
Hcv Protease ◽  
Protease Inhibitor Telaprevir ◽  
Blood Spot

1245 THE EFFECT OF SEVERE RENAL IMPAIRMENT ON THE PHARMACOKINETICS OF THE INVESTIGATIONAL HCV PROTEASE INHIBITOR TELAPREVIR

2011 ◽  
Vol 54 ◽  
pp. S492 ◽  
Author(s):  
R. van Heeswijk ◽  
A. Vandevoorde ◽  
G. Boogaerts ◽  
E. De Paepe ◽  
R. van Solingen-Ristea ◽  
...  
Keyword(s):  
Renal Impairment ◽  
Protease Inhibitor ◽  
Severe Renal Impairment ◽  
Hcv Protease ◽  
Protease Inhibitor Telaprevir
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