Pharmacokinetic interaction between etravirine or rilpivirine and telaprevir in healthy volunteers: A randomized, two-way crossover trial

Journal of Clinical Pharmacology

Volumn 54, Issue 5, 2014, Pages 563-573

  Kakuda, Thomas N ^a   Leopold, Lorant ^a   Nijs, Steven ^b   Vandevoorde, Ann ^b   Crauwels, Herta M ^b   Bertelsen, Kirk M ^a   Stevens, Marita ^b   Witek, James ^a   Van Delft, Yvon ^c   Tomaka, Frank ^a   Hoetelmans, Richard M W ^b  

^a JANSSEN RESEARCH AND DEVELOPMENT   (United States)

^b JANSSEN RESEARCH FOUNDATION   (Belgium)

^c Janssen   (Netherlands)

Author keywords

drug drug interaction; etravirine; non nucleoside reverse transcriptase inhibitor; pharmacokinetics; rilpivirine; telaprevir

Indexed keywords

ETRAVIRINE; HEMOGLOBIN; RILPIVIRINE; TELAPREVIR; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; NITRILE; OLIGOPEPTIDE; PYRIDAZINE DERIVATIVE; PYRIMIDINE DERIVATIVE; RNA DIRECTED DNA POLYMERASE INHIBITOR;

ABDOMINAL DISCOMFORT; ACNE; ADULT; AREA UNDER THE CURVE; ARTICLE; CONSTIPATION; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG BLOOD LEVEL; DRUG SAFETY; DRUG TOLERABILITY; FEMALE; HEADACHE; HEART MUSCLE ISCHEMIA; HEMOGLOBIN BLOOD LEVEL; HUMAN; HUMAN TISSUE; LYMPHOCYTE COUNT; MALE; MAXIMUM PLASMA CONCENTRATION; MORNING DOSAGE; OPEN STUDY; PHASE 1 CLINICAL TRIAL; PRURITUS; RANDOMIZED CONTROLLED TRIAL; SIDE EFFECT; SINGLE DRUG DOSE; XEROSTOMIA; ADOLESCENT; BLOOD; CLINICAL TRIAL; DRUG INTERACTION; MIDDLE AGED; NORMAL HUMAN; YOUNG ADULT;

ADOLESCENT; ADULT; ANTI-HIV AGENTS; CROSS-OVER STUDIES; DRUG INTERACTIONS; FEMALE; HEALTHY VOLUNTEERS; HUMANS; MALE; MIDDLE AGED; NITRILES; OLIGOPEPTIDES; PYRIDAZINES; PYRIMIDINES; REVERSE TRANSCRIPTASE INHIBITORS; YOUNG ADULT;

EID: 84898606422     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1002/jcph.245     Document Type: Article

References (34)

1. Alter MJ., Epidemiology of viral hepatitis and HIV co-infection. J Hepatol 2006; 44: S6-S9. (Pubitemid 43053865)
2. Martin-Carbonero L, Benhamou Y, Puoti M, Berenguer J, Mallolas J, Quereda C, Arizcorreta A, Gonzalez A, Rockstroh J, Asensi V, Miralles P, Laguno M, Moreno L, Girõn JA, Vogel M, García-Samaniego J, Nuñez M, Romero M, Moreno S, de la Cruz JJ, Soriano V., Incidence and predictors of severe liver fibrosis in human immunodeficiency virus-infected patients with chronic hepatitis C: a European collaborative study. Clin Infect Dis 2004; 38: 128-133. (Pubitemid 38045883)
3. Martinez-Sierra C, Arizcorreta A, Díaz F, Roldán R, Martín-Herrera L, Pérez-Guzmán E, Girõn- González JA., Progression of chronic hepatitis C to liver fibrosis and cirrhosis in patients coinfected with hepatitis C virus and human immunodeficiency virus. Clin Infect Dis 2003; 36: 491-498. (Pubitemid 36241318)
4. Molina JM, Cahn P, Grinsztejn B, Lazzarin A, Mills A, Saag M, Supparatpinyo K, Walmsley S, Crauwels H, Rimsky LT, Vanveggel S, Boven K;, ECHO study group. Rilpivirine versus efavirenz with tenofovir and emtricitabine in treatment-naïve adults infected with HIV-1 (ECHO): a phase 3 randomised double-blind active-controlled trial. Lancet 2011; 378: 238-246.
5. Cohen CJ, Andrade-Villanueva J, Clotet B, Fourie J, Johnson MA, Ruxrungtham K, Wu H, Zorrilla C, Crauwels H, Rimsky LT, Vanveggel S, Boven K;, THRIVE Study Group. Rilpivirine versus efavirenz with two background nucleoside or nucleotide reverse transcriptase inhibitors in treatment-naïve adults infected with HIV-1 (THRIVE): a phase 3, randomised, non-inferiority trial. Lancet 2011; 378: 229-237.
6. Cohen C, Molina JM, Cahn P, Clotet B, Fourie J, Grinsztejn B, Wu H, Johnson MA, Saag M, Supparatpinyo K, Crauwels H, Lefebvre E, Rimsky LT, Vanveggel S, Williams P, Boven K;, ECHO Study Group; THRIVE Study Group. Efficacy and safety of rilpivirine (TMC278) versus efavirenz at 48 weeks in treatment-naïve, HIV-1-infected patients: pooled results from the phase 3 double-blind, randomized ECHO and THRIVE trials. J Acquir Immune Defic Syndr 2012; 60: 33-42.
7. Cohen C, Molina JM, Cassetti I, Chetchotisakd P, Lazzarin A, Orkin C, Rhame F, Stellbrink HJ, Li T, Crauwels H, Rimsky L, Vanveggel S, Williams P, Boven K;, ECHO, THRIVE study groups. Week 96 efficacy and safety of rilpivirine in treatment-naïve, HIV-1 patients in two Phase III randomised trials. AIDS 2013; 27: 939-950.
8. Katlama C, Haubrich R, Lalezari J, Lazzarin A, Madruga JV, Molina JM, Schechter M, Peeters M, Picchio G, Vingerhoets J, Woodfall B, De Smedt G;, DUET-1, DUET-2 study groups. Efficacy and safety of etravirine in treatment-experienced, HIV-1 patients: pooled 48 week analysis of two randomized, controlled trials. AIDS 2009; 23: 2289-2300.
9. Katlama C, Clotet B, Mills A, Trottier B, Molina JM, Grinsztejn B, Towner W, Haubrich R, Nijs S, Vingerhoets J, Woodfall B, Witek J., Efficacy and safety of etravirine at week 96 in treatment-experienced HIV type-1-infected patients in the DUET-1 and DUET-2 trials. Antivir Ther 2010; 15: 1045-1052.
10. Jacobson IM, McHutchison JG, Dusheiko G, DiBisceglie AM, Reddy KR, Bzowej NH, Marcellin P, Muir AJ, Ferenci P, Flisiak R, George J, Rizzetto M, Shouval D, Sola R, Terg RA, Yoshida EM, Adda N, Bengtsson L, Sankoh AJ, Kieffer TL, George S, Kauffman RS, Zeuzem S;, ADVANCE Study Team. Telaprevir for previously untreated chronic hepatitis C virus infection. N Engl J Med 2011; 364: 2405-2416.
11. Sherman KE, Flamm SL, Afdhal NH, Nelson DR, Sulkowski MS, Everson GT, Fried MW, Adler M, Reesink HW, Martin M, Sankoh AJ, Adda N, Kauffman RS, George S, Wright CI, Poordad F;, ILLUMINATE Study Team. Response-guided telaprevir combination treatment for hepatitis C virus infection. N Engl J Med 2011; 365: 1014-1024.
12. Zeuzem S, Andreone P, Pol S, Lawitz E, Diago M, Roberts S, Focaccia R, Younossi Z, Foster GR, Horban A, Ferenci P, Nevens F, Müllhaupt B, Pockros P, Terg R, Shouval D, van Hoek B, Weiland O, Van Heeswijk R, De Meyer S, Luo D, Boogaerts G, Polo R, Picchio G, Beumont M;, REALIZE Study Team. Telaprevir for retreatment of HCV infection. N Engl J Med 2011; 364: 2417-2428.
13. Sulkowski MS, Sherman KE, Dieterich DT, Bsharat M, Mahnke L, Rockstroh JK, Gharakhanian S, McCallister S, Henshaw J, Girard PM, Adiwijaya B, Garg V, Rubin RA, Adda N, Soriano V., Combination therapy with telaprevir for chronic hepatitis C virus genotype 1 infection in patients with HIV: a randomized trial. Ann Intern Med 2013; 159: 86-96.
14. Schöller-Gyüre M, Kakuda TN, Raoof A, De Smedt G, Hoetelmans RM., Clinical pharmacokinetics and pharmacodynamics of etravirine. Clin Pharmacokinet 2009; 48: 561-574.
15. van Heeswijk R, Hoetelmans R, Kestens D, Stevens M, Peeters M, Boven K, Williams P, Woodfall B., The effects of CYP3A4 modulation on the pharmacokinetics of TMC278, an investigational non-nucleoside reverse transcriptase inhibitor (NNRTI). Presentation at: 7th International Workshop on Clinical Pharmacology of HIV Therapy; April 20-22, 2006; Lisbon, Portugal. Abstract 74.
16. Crauwels HM, van Heeswijk RPG, Stevens T, Stevens M, Buelens A, K Boven K, Hoetelmans RMW., The effect of TMC278, a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI), on CYP3A activity in vivo. Presentation at: 10th International Workshop on Clinical Pharmacology of HIV Therapy; April 15-17, 2009; Amsterdam, The Netherlands. Abstract P28.
17. Crauwels HM, Deckx H, Stevens M, Hoetelmans RM., Absence of a pharmacokinetic interaction of rilpivirine with the P-glycoprotein substrate digoxin in healthy volunteers. Presentation at: 11th International Congress on Drug Therapy in HIV Infection; November 11-15, 2012; Glasgow, UK. Abstract P071.
18. Garg V, Chandorkar G, Farmer HF, Smith F, Alves K, van Heeswijk RP., Effect of telaprevir on the pharmacokinetics of midazolam and digoxin. J Clin Pharmacol 2012; 52: 1566-1573.
19. Moss DM, Liptrott NJ, Curley P, Siccardi M, Back DJ, Owen A., Rilpivirine inhibits drug transporters ABCB1, SLC22A1, and SLC22A2 in vitro. Antimicrob Agents Chemother 2013. 57: 5612-5618.
20. Zembruski NC, Haefeli WE, Weiss J., Interaction potential of etravirine with drug transporters assessed in vitro. Antimicrob Agents Chemother 2011; 55: 1282-1284.
21. Crauwels HM, Deckx H, Stevens M, Kirsila T, Houtmeyers E, Lachau-Durand S, Hoetelmans RMW., Absence of a pharmacokinetic interaction between rilpivirine, an NNRTI, and metformin. Presentation at: 14th European AIDS Conference; October 16-19, 2013; Brussels, Belgium. Abstract PE10/4.
22. Williams EJ., Experimental designs balanced for the estimation of residual effects of treatments. Aust J Sci Res 1949; 2: 149-168.
23. Lee JE, van Heeswijk R, Alves K, Smith F, Garg V., Effect of the hepatitis C virus protease inhibitor telaprevir on the pharmacokinetics of amlodipine and atorvastatin. Antimicrob Agents Chemother 2011; 55: 4569-4574.
24. Schöller-Gyüre M, Kakuda TN, Sekar V, Woodfall B, DeSmedt G, Lefebvre E, Peeters M, Hoetelmans RM., Pharmacokinetics of darunavir/ritonavir and TMC125 alone and coadministered in HIV-negative volunteers. Antivir Ther 2007; 12: 789-796. (Pubitemid 47235493)
25. Crauwels HM, van Heeswijk RPG, Buelens A, Stevens M, Boven K, Hoetelmans RM., Impact of food and different meal types on the pharmacokinetics of rilpivirine. J Clin Pharmacol 2013; 53: 834-840.
26. Fridericia LS., Die Systolendauer im Elektrokardiogramm bei normalen Menschen und bei Herzkranken. Acta Med Scand 1920; 15: 469-486.
27. Kakuda TN, Schöller-Gyüre M, Hoetelmans RM., Pharmacokinetic interactions between etravirine and non-antiretroviral drugs. Clin Pharmacokinet 2011; 50: 25-39.
28. van Heeswijk RP, Beumont M, Kauffman RS, Garg V., Review of drug interactions with telaprevir and antiretrovirals. Antivir Ther 2012; 17: 1211-1221.
29. Schöller-Gyüre M, Kakuda TN, De Smedt G, Woodfall B, Lachaert R, Beets G, Peeters M, Hoetelmans RM., Pharmacokinetics of TMC125 in once- and twice-daily regimens in HIV-1 negative volunteers. Presentation at: 47th Interscience Conference Agents and Chemotherapy; September 17-20, 2007; Chicago, USA. Abstract A-1427.
30. Hammond KP, Wolfe P, Burton JR, Jr., Predhomme JA, Ellis CM, Ray ML, Bushman LR, Kiser JJ., Pharmacokinetic interaction between boceprevir and etravirine in HIV/HCV seronegative volunteers. J Acquir Immune Defic Syndr 2013; 62: 67-73.
31. Crauwels HM, Stevens M, De la Rosa G, Boven K., Absence of pharmacokinetic interaction between the NNRTI rilpivirine (RPV, TMC278) and the integrase inhibitor raltegravir (RAL). 19th Conference on Retroviruses and Opportunistic Infections; March 5-8, 2012; Washington DC, USA. Abstract 617.
32. Crauwels H, Vingerhoets J, Ryan R, Witek J, Anderson D., Pharmacokinetic parameters of once-daily rilpivirine following administration of efavirenz in healthy subjects. Antivir Ther 2012; 17: 439-446.
33. Rhee EG, Feng H, Xuan F, Lin W, Smith C, Zhu Y, Butterton J., Absence of a significant pharmacokinetic interaction between the HCV protease inhibitor boceprevir and HIV-1 NNRTI rilpivirine. 20th Conference on Retroviruses and Opportunistic Infections; March 3-6, 2013; Atlanta, GA, USA. Abstract 537.
34. Vanveggel S, Buelens A, Crauwels HM, van Heeswijk R, Leopold L, Stevens M, Boven K., TMC278 25mg qd has no effect on corrected QT interval in a study in HIV-negative volunteers. Presentation at: 47th Annual Meeting of the Infectious Diseases Society of America; Oct 29-Nov 1, 2009; Philadelphia, USA. Abstract 1620.