Coadministration with lopinavir and ritonavir decreases exposure to BILR 355, a nonnucleoside reverse transcriptase inhibitor, in healthy volunteers

Journal of Clinical Pharmacology

Volumn 51, Issue 7, 2011, Pages 1061-1070

  Huang, Fenglei ^a   Scholl, Paul ^a   Huang, David B ^a   MacGregor, Thomas R ^a   Vinisko, Richard ^a   Castles, Mark A ^a   Berger, Frank ^a   Robinson, Patrick ^a  

^a BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

Author keywords

BILR 355; drug drug interaction; HIV; lopinavir; nonnucleoside reverse transcriptase inhibitor; P glycoprotein; protease inhibitor (PI); ritonavir

Indexed keywords

ASPARTATE AMINOTRANSFERASE; BILR 355; CREATINE KINASE; HEMOGLOBIN; LOPINAVIR; LOPINAVIR PLUS RITONAVIR; NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR; RITONAVIR; UNCLASSIFIED DRUG;

ADULT; AREA UNDER THE CURVE; ARTICLE; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; BLOOD SAMPLING; CONTROLLED STUDY; CREATINE KINASE BLOOD LEVEL; DIARRHEA; DISEASE SEVERITY; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG ERUPTION; DRUG EXPOSURE; DRUG FATALITY; DRUG HALF LIFE; DRUG SAFETY; DRUG SCREENING; DRUG TOLERABILITY; DRUG WITHDRAWAL; ECG ABNORMALITY; FATIGUE; FEMALE; GASTROINTESTINAL SYMPTOM; HEMOGLOBIN BLOOD LEVEL; HUMAN; HYPOGLYCEMIA; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; OPEN STUDY; PHASE 1 CLINICAL TRIAL; RANDOMIZED CONTROLLED TRIAL; SIDE EFFECT; STEADY STATE; TIME TO MAXIMUM PLASMA CONCENTRATION; TREATMENT DURATION; TRIACYLGLYCEROL BLOOD LEVEL; UNSPECIFIED SIDE EFFECT; VITAL SIGN;

EID: 79958788137     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1177/0091270010376971     Document Type: Article

References (33)

1. Palella FJ, Delaney KM, Moorman AC, et al. Declining morbidity and mortality among patients with advanced human immunodeficiency virus infection. N Engl J Med. 1998 ; 338: 853-860 (Pubitemid 28135961)
2. Hogg RS, Heath KV, Yip B, et al. Improved survival among HIV-infected individuals following initiation of antiretroviral therapy. JAMA. 1998 ; 279: 450-454 (Pubitemid 28082255)
3. Katzenstein DA, Holodniy M, Israelski DM, et al. Plasma viremia in human immunodeficiency virus infection: relationship to stage of disease and antiviral treatment. J Acquir Immune Defic Syndr. 1992 ; 5: 107-112
4. Clotet B. Strategies for overcoming resistance in HIV-1 infected patients receiving HAART. AIDS Rev. 2004 ; 6: 123-130 (Pubitemid 39599982)
5. Delaugerre C, Rohban R, Simon A, et al. Resistance profile and cross-resistance of HIV-1 among patients failing a non-nucleoside reverse transcriptase inhibitor-containing regimen. J Med Virol. 2001 ; 65: 445-448 (Pubitemid 32959067)
6. D'Aquila RT, Schapiro JM, Brun-Vezinet F, et al. Drug resistance mutations in HIV-1. Top HIV Med. 2003 ; 11: 92-96
7. Richman DD, Havlir D, Corbeil J, et al. Nevirapine resistance mutations of human immunodeficiency virus type 1 selected during therapy. J Virol. 1994 ; 68: 1660-1666 (Pubitemid 24065732)
8. Demeter LM, Shafer RW, Meehan PM, et al. Delavirdine susceptibilities and associated reverse transcriptase mutations in human immunodeficiency virus type 1 isolates from patients in a phase I/II trial of delavirdine monotherapy (ACTG 260). Antimicrob Agents Chemother. 2000 ; 44: 794-797 (Pubitemid 30117986)
9. Huang F, Koenen-Bergmann M, MacGregor TR, Ring A, Hattox S, Robinson P. Pharmacokinetic and safety evaluation of BILR 355, a second generation non-nucleoside reverse transcriptase inhibitor, in healthy volunteers. Antimicrob Agents Chemother. 2008 ; 52: 4300-4307
10. Bonneau P, Robinson PA, Duan J, et al. Antiviral characterization and human experience with BILR 355 BS, a novel next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with a broad antiHIV-1 profile. Abstract presented at: 12th Conference on Retroviruses and Opportunistic Infections ; Boston, Mass ;..
11. Boone LR. Next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors. Curr Opin Investig Drugs. 2006 ; 7: 128-135 (Pubitemid 43230908)
12. Huang F, Drda K, MacGregor TR, et al. Pharmacokinetics of BILR 355 after multiple oral dosing co-administered with low dose of ritonavir. Antimicrob Agents Chemother. 2009 ; 53: 95-103
13. Oldfield V, Plosker GL. Lopinavir/ritonavir: a review of its use in the management of HIV infection. Drugs. 2006 ; 66: 1275-1299 (Pubitemid 44055872)
14. Barragan P, Podzamczer D. Lopinavir/ritonavir: a protease inhibitor for HIV-1 treatment. Expert Opin Pharmacother. 2008 ; 9: 2363-2375
15. Kaplan SS, Hicks CB. Lopinavir/ritonavir in the treatment of human immunodeficiency virus infection. Expert Opin Pharmacother. 2005 ; 6: 1573-1585 (Pubitemid 41131696)
16. Kaplan SS, Hicks CB. Safety and antiviral activity of lopinavir/ritonavir-based therapy in human immunodeficiency virus type 1 (HIV-1) infection. J Antimicrob Chemother. 2005 ; 56: 273-276 (Pubitemid 41158512)
17. Benson CA, Deeks SG, Brun SC, et al. Safety and antiviral activity at 48 weeks of lopinavir/ritonavir plus nevirapine and 2 nucleoside reverse-transcriptase inhibitors in human immunodeficiency virus type 1-infected protease inhibitor-experienced patients. J Infect Dis. 2002 ; 185: 599-607 (Pubitemid 34171464)
18. Cohen C, Nieto-Cisneros L, Zala C, et al. Comparison of atazanavir with lopinavir/ritonavir in patients with prior protease inhibitor failure: a randomized multinational trial. Curr Med Res Opin. 2005 ; 21: 1683-1692 (Pubitemid 41505034)
19. Johnson M, Grinsztejn B, Rodriguez C, et al. 96-week comparison of once-daily atazanavir/ritonavir and twice-daily lopinavir/ritonavir in patients with multiple virologic failures. AIDS. 2006 ; 20: 711-718 (Pubitemid 43884298)
20. Huang F, Allen L, MacGregor TR, et al. Pharmacokinetic interaction of BILR 355/r and Combivir in healthy volunteers. Paper presented at: 2009 American Association of pharmaceutical Scientists (AAPS) Annual Meeting and Exposition ; Los Angeles, Calif ;..
21. Huang F, Scholl P, Vinisko R, et al. Pharmacokinetic interaction of BILR355 and TRUVADA in healthy volunteers. Paper presented at: 48th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) ; Washington, DC ;..
22. Diletti E, Hauschke D, Steinijans VW. Sample size determination for bioequivalence assessment by means of confidence intervals. Int J Clin Pharmacol Ther Toxicol. 1992 ; 30 (suppl 1). S51 - S58
23. North Chicago, Ill: Abbott Laboratories ;
24. Robertson SM, Penzak SR, Pau A. Drug interactions in the management of HIV infection: an update. Expert Opin Pharmacother. 2007 ; 8: 2947-2963 (Pubitemid 350300966)
25. Yeh RF, Gaver VE, Patterson KB, et al. Lopinavir/ritonavir induces the hepatic activity of cytochrome P450 enzymes CYP2C9, CYP2C19, and CYP1A2 but inhibits the hepatic and intestinal activity of CYP3A as measured by a phenotyping drug cocktail in healthy volunteers. J Acquir Immune Defic Syndr. 2006 ; 42: 52-60 (Pubitemid 43947946)
26. Wyen C, Fuhr U, Frank D, et al. Effect of an antiretroviral regimen containing ritonavir boosted lopinavir on intestinal and hepatic CYP3A, CYP2D6 and P-glycoprotein in HIV-infected patients. Clin Pharmacol Ther. 2008 ; 84: 75-82 (Pubitemid 351861487)
27. van Heeswijk RP, Bourbeau M, Campbell P, et al. Time-dependent interaction between lopinavir/ritonavir and fexofenadine. J Clin Pharmacol. 2006 ; 46: 758-767 (Pubitemid 43882799)
28. la Porte CJL, Martin P, Seguin I, Cameron DW, van Heeswijk RP, Owen A. The effect of multiple dose lopinavir/ritonavir on intestinal mRNA expression of ABCB1, ABCC1, ABCC2, CYP2B6, CYP3A4, SLCO1B1, CAR, FXR, PXR and RXR in healthy volunteers. Abstract presented at: 10th International Workshop on Clinical Pharmacology of HIV Therapy ; Amsterdam, The Netherlands ;..
29. Marzolini C, Tirona RG, Lee W, et al. Unexpected complexity in nuclear receptors activation by HIV protease inhibitors and induction of CYP enzymes and transporters. Abstract presented at: 11th Conference on Retroviruses and Opportunistic Infections ; San Francisco, Calif ;..
30. Callaghan R, Crowley E, Potter S, Kerr ID. P-glycoprotein: so many ways to turn it on. J Clin Pharmacol. 2008 ; 48: 365-378
31. Mathias AA, West S, Hui J, Kearney BP. Dose-response of ritonavir on hepatic CYP3A activity and elvitegravir oral exposure. Clin Pharmacol Ther. 2009 ; 85: 64-70
32. Mathias AA, Hinkle J, Shen G, et al. Effect of ritonavir-boosted tipranavir or darunavir on the steady-state pharmacokinetics of elvitegravir. J Acquir Immune Defic Syndr. 2008 ; 49: 156-162
33. van Heeswijk RP, Veldkamp A, Mulder JW, et al. Combination of protease inhibitors for the treatment of HIV-1-infected patients: a review of pharmacokinetics and clinical experience. Antivir Ther. 2001 ; 6: 201-229 (Pubitemid 34174760)