{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,29]],"date-time":"2026-04-29T08:37:18Z","timestamp":1777451838878,"version":"3.51.4"},"reference-count":22,"publisher":"SAGE Publications","issue":"5","license":[{"start":{"date-parts":[[2010,7,1]],"date-time":"2010-07-01T00:00:00Z","timestamp":1277942400000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.sagepub.com\/page\/policies\/text-and-data-mining-license"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Antiviral Therapy"],"published-print":{"date-parts":[[2010,7]]},"abstract":"<jats:sec>\n                    <jats:title>Background<\/jats:title>\n                    <jats:p>A pharmacokinetic trial was conducted to evaluate the potential for once-daily etravirine in anti-retroviral regimens without and with darunavir\/ritonavir.<\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Methods<\/jats:title>\n                    <jats:p>During this multicentre, open-label, Phase IIa trial, treatment-naive patients aged \u226518 years with HIV type-1 (HIV-1) received etravirine 400 mg once daily with tenofovir disoproxil fumarate\/emtricitabine 300\/200 mg once daily from days 1\u201314; on days 15\u201328, darunavir\/ritonavir 800\/100 mg once daily was added. On day 29, etravirine was discontinued and patients continued with the other medications to day 42. Serial blood sampling for etravirine pharmacokinetics was performed over 24 h on day 14 and 28; patients fasted for \u226510 h prior to these visits.<\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Results<\/jats:title>\n                    <jats:p>\n                      Of 23 enrolled patients (male 87%, Caucasian 39%), pharmacokinetic profiles for etravirine were available for 21 and 20 patients on day 14 and 28, respectively. The plasma concentration\u2013time profile and pharmacokinetics for etravirine were unchanged with or without darunavir\/ritonavir. The mean maximum plasma concentration (C\n                      <jats:sub>max<\/jats:sub>\n                      ) was reached 4 h after administration and was 790 and 801 ng\/ml on day 14 and 28, respectively; mean area under the plasma concentration\u2013time curve (AUC) from before administration to 24 h after administration was 10,410 ng\u2022h\/ml on day 14 and 10,720 ng\u2022h\/ml on day 28. In a post-hoc analysis, etravirine C\n                      <jats:sub>max<\/jats:sub>\n                      was higher, minimum plasma concentration was lower and AUC was similar when compared with etravirine 200 mg twice daily.\n                    <\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Conclusions<\/jats:title>\n                    <jats:p>Addition of darunavir\/ritonavir to etravirine, all dosed once daily, did not have a clinically significant effect on the pharmacokinetics of etravirine. Findings support further investigation of etravirine 400 mg once daily in HIV-1-infected patients. (Trial registration number NCT00534352.)<\/jats:p>\n                  <\/jats:sec>","DOI":"10.3851\/imp1562","type":"journal-article","created":{"date-parts":[[2010,6,4]],"date-time":"2010-06-04T15:31:08Z","timestamp":1275665468000},"page":"711-720","source":"Crossref","is-referenced-by-count":36,"title":["Pharmacokinetics of once-daily Etravirine without and with Once-daily Darunavir\/ritonavir in Antiretroviral-Naive HIV type-1-Infected Adults"],"prefix":"10.1177","volume":"15","author":[{"given":"Edwin","family":"DeJesus","sequence":"first","affiliation":[{"name":"Orlando Immunology Center, Orlando, FL, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jacob P","family":"Lalezari","sequence":"additional","affiliation":[{"name":"Quest Clinical Research, San Francisco, CA, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Olayemi O","family":"Osiyemi","sequence":"additional","affiliation":[{"name":"Triple O Medical Services, Inc., West Palm Beach, FL, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Peter J","family":"Ruane","sequence":"additional","affiliation":[{"name":"Lightsource Medical, Los Angeles, CA, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Robert","family":"Ryan","sequence":"additional","affiliation":[{"name":"Tibotec, Inc., Titusville, NJ, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Thomas N","family":"Kakuda","sequence":"additional","affiliation":[{"name":"Tibotec, Inc., Titusville, NJ, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"James","family":"Witek","sequence":"additional","affiliation":[{"name":"Tibotec Therapeutics, Titusville, NJ, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"179","published-online":{"date-parts":[[2010,7,1]]},"reference":[{"key":"bibr1-IMP1562","doi-asserted-by":"publisher","DOI":"10.1128\/JVI.79.20.12773-12782.2005"},{"key":"bibr2-IMP1562","doi-asserted-by":"publisher","DOI":"10.1007\/s10865-007-9147-y"},{"key":"bibr3-IMP1562","doi-asserted-by":"crossref","first-page":"655","DOI":"10.1177\/135965350801300505","volume":"13","author":"Kakuda T.N.","year":"2008","journal-title":"Antivir Ther"},{"key":"bibr4-IMP1562","unstructured":"Scholler M., Hoetelmans R., Beets G. Substantial improvement of oral bioavailability of TMC125 using new tablet formulations in healthy volunteers.\n                      International AIDS Society Conference.\n                      24\u201327 July 2005, Rio de Janeiro, Brazil. Abstract TuPe3.1B11."},{"key":"bibr5-IMP1562","doi-asserted-by":"publisher","DOI":"10.1592\/phco.28.10.1215"},{"key":"bibr6-IMP1562","doi-asserted-by":"publisher","DOI":"10.1345\/aph.1K681"},{"key":"bibr7-IMP1562","doi-asserted-by":"publisher","DOI":"10.1016\/S0140-6736(07)60497-8"},{"key":"bibr8-IMP1562","unstructured":"DeJesus E., Ortiz R., Khanlou H. Efficacy and safety of darunavir\/ritonavir versus lopinavir\/ritonavir in ARV treatment-na\u00efve HIV-1-infected patients at Week 48: ARTEMIS.\n                      Interscience Conference on Antimicrobial Agents and Chemotherapy\n                      . 17\u201320 September 2007, Chicago, IL, USA. Abstract H-718b. Available from: http:\/\/www.tibotec.com\/content\/congresses\/www.tibotec.com\/DeJesus_TMC114_Artemis.pdf(accessed 15 July 2009)."},{"key":"bibr9-IMP1562","doi-asserted-by":"publisher","DOI":"10.1016\/S0140-6736(07)61049-6"},{"key":"bibr10-IMP1562","doi-asserted-by":"crossref","first-page":"789","DOI":"10.1177\/135965350701200511","volume":"12","author":"Scholler-Gyure M.","year":"2007","journal-title":"Antivir Ther"},{"key":"bibr11-IMP1562","doi-asserted-by":"publisher","DOI":"10.1016\/S0140-6736(07)61048-4"},{"key":"bibr12-IMP1562","doi-asserted-by":"publisher","DOI":"10.1016\/S0140-6736(07)61047-2"},{"key":"bibr13-IMP1562","unstructured":"Mills A., Cahn P., Molina J-M, Nijs S., Vingerhoets J., Witek J. Etravirine demonstrates durable efficacy in treatment-experienced patients in the DUET trials: pooled 96-week results.\n                      5th IAS Conference on HIV Pathogenesis, Treatment and Prevention\n                      . 19\u201322 July 2009, Cape Town, South Africa. Available from: http:\/\/www.ias2009.org\/pag\/PDF\/2344.pdf (accessed 11 January 2010)."},{"key":"bibr14-IMP1562","unstructured":"Kakuda T.N., Wade J.R., Snoeck E. Pharmacokinetics and pharmacodynamics of the NNRTI etravirine (ETR; TMC125) in treatment-experienced HIV-1-infected patients: pooled 24-week results of DUET-1 and DUET-2.\n                      15th Conference on Retroviruses and Opportunistic Infections\n                      . 3\u20136 February 2008, Boston, MA, USA. Poster 762."},{"key":"bibr15-IMP1562","doi-asserted-by":"crossref","unstructured":"Lalezari J., DeJesus E., Osiyemi O. Pharmacokinetics (PK) of once-daily etravirine (ETR) without and with once-daily darunavir\/ritonavir (DRV\/r) in antiretroviral-naive HIV-1 infected adults.\n                      Ninth International Congress on Drug Therapy in HIV Infection\n                      . 9\u201313 November 2008, Glasgow, UK. Poster 53.","DOI":"10.1186\/1758-2652-11-S1-O40"},{"key":"bibr16-IMP1562","first-page":"S34","volume":"12","author":"Vingerhoets J.","year":"2007","journal-title":"Antivir Ther"},{"key":"bibr17-IMP1562","unstructured":"Kakuda T., Sch\u00f6ller-Gy\u00fcre M., Peeters M. Pharmacokinetics of etravirine (ETR; TMC125) are not affected by sex, age, race, use of enfuvirtide (ENF) or treatment duration in HIV-1-infected subjects.\n                      9th International Workshop on Clinical Pharmacology of HIV Therapy\n                      . 7\u20139 April 2008, New Orleans, LA, USA. Available from: http:\/\/www.tibotec.com\/content\/congresses\/www.tibotec.com\/Kakuda_TMC125_PK_ENF_treat_dur.pdf (accessed 26 May 2009)."},{"key":"bibr18-IMP1562","doi-asserted-by":"publisher","DOI":"10.1345\/aph.1K615"},{"key":"bibr19-IMP1562","doi-asserted-by":"publisher","DOI":"10.1097\/QAD.0b013e3282170ab1"},{"key":"bibr20-IMP1562","first-page":"119","volume":"15","author":"Johnson V.A.","year":"2007","journal-title":"Top HIV Med"},{"key":"bibr21-IMP1562","doi-asserted-by":"publisher","DOI":"10.1097\/QAD.0b013e32833677ac"},{"key":"bibr22-IMP1562","unstructured":"De Meyer S., Dierynck I., Lathouwers E. Identification of mutations predictive of a diminished response to darunavir ritonavir: analysis of data from treatment-experienced patients in POWER1, 2, and 3 and DUET-1 and DUET-2.\n                      6th European HIV Drug Resistance Workshop\n                      . 26\u201328 March 2008, Budapest, Hungary. Abstract 54."}],"container-title":["Antiviral Therapy"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/journals.sagepub.com\/doi\/pdf\/10.3851\/IMP1562","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/journals.sagepub.com\/doi\/pdf\/10.3851\/IMP1562","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2026,4,28]],"date-time":"2026-04-28T12:49:31Z","timestamp":1777380571000},"score":1,"resource":{"primary":{"URL":"https:\/\/journals.sagepub.com\/doi\/10.3851\/IMP1562"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2010,7]]},"references-count":22,"journal-issue":{"issue":"5","published-print":{"date-parts":[[2010,7]]}},"alternative-id":["10.3851\/IMP1562"],"URL":"https:\/\/doi.org\/10.3851\/imp1562","relation":{},"ISSN":["1359-6535","2040-2058"],"issn-type":[{"value":"1359-6535","type":"print"},{"value":"2040-2058","type":"electronic"}],"subject":[],"published":{"date-parts":[[2010,7]]}}}