Twenty-eight day safety, antiviral activity, and pharmacokinetics of tenofovir alafenamide for treatment of chronic hepatitis B infection

Journal of Hepatology

Volumn 62, Issue 3, 2015, Pages 533-540

  Agarwal, Kosh ^a   Fung, Scott K ^b   Nguyen, Tuan T ^c   Cheng, Wendy ^d   Sicard, Eric ^e   Ryder, Stephen D ^f   Flaherty, John F ^g   Lawson, Eileen ^g   Zhao, Sally ^g   Subramanian, G Mani ^g   McHutchison, John G ^g   Gane, Edward J ^h   Foster, Graham R ⁱ  

^a KING S COLLEGE HOSPITAL   (United Kingdom)

^b TORONTO GENERAL HOSPITAL   (Canada)

^c T Nguyen Research and Education   (United States)

^d ROYAL PERTH HOSPITAL   (Australia)

^e Algorithme Pharma ^*  (Canada)

^f NOTTINGHAM UNIVERSITY HOSPITALS NHS TRUST   (United Kingdom)

^g GILEAD SCIENCES   (United States)

^h Auckland Clinical Studies   (New Zealand)

ⁱ QUEEN MARY UNIVERSITY OF LONDON   (United Kingdom)

Author keywords

Antiviral; Clinical Trial; Treatment; Viral hepatitis

Indexed keywords

ALANINE AMINOTRANSFERASE; ALKALINE PHOSPHATASE; AMYLASE; ASPARTATE AMINOTRANSFERASE; CREATINE KINASE; CREATININE; HEPATITIS B(E) ANTIGEN; PHOSPHATE; TENOFOVIR ALAFENAMIDE; TENOFOVIR DISOPROXIL; VIRUS DNA; ADENINE; ANTIVIRUS AGENT; GS-7340; TENOFOVIR;

ABDOMINAL DISTENSION; ADULT; ALANINE AMINOTRANSFERASE BLOOD LEVEL; ALKALINE PHOSPHATASE BLOOD LEVEL; AMYLASE BLOOD LEVEL; ANTIVIRAL ACTIVITY; ANTIVIRAL THERAPY; AREA UNDER THE CURVE; ARTHRALGIA; ARTICLE; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; CHRONIC HEPATITIS; CLINICAL ARTICLE; CONSTIPATION; CONTROLLED STUDY; COUGHING; CREATINE KINASE BLOOD LEVEL; CREATININE BLOOD LEVEL; CREATININE CLEARANCE; DIZZINESS; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG EXPOSURE; DRUG INDUCED HEADACHE; DRUG SAFETY; DRUG TOLERABILITY; ELIMINATION HALF-LIFE; FATIGUE; FEMALE; FLATULENCE; FOLLICULITIS; FOLLOW UP; GLOMERULUS FILTRATION RATE; GLUCOSURIA; HEMATURIA; HEPATITIS B; HEPATITIS B VIRUS; HUMAN; HYPERGLYCEMIA; INFLUENZA; KIDNEY FUNCTION; LETHARGY; LIMIT OF QUANTITATION; MALE; MAXIMUM PLASMA CONCENTRATION; MEDICAL DICTIONARY FOR REGULATORY ACTIVITIES; MIDDLE AGED; MYALGIA; NAUSEA; OPEN STUDY; OROPHARYNX PAIN; PHASE 1 CLINICAL TRIAL; PHOSPHATE BLOOD LEVEL; PLASMA CONCENTRATION-TIME CURVE; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; RHINORRHEA; SIDE EFFECT; TIME TO MAXIMUM PLASMA CONCENTRATION; TREATMENT DURATION; TREATMENT OUTCOME; TREATMENT RESPONSE; VOMITING; YOUNG ADULT; ANALOGS AND DERIVATIVES; BLOOD; CLINICAL TRIAL; HEPATITIS B, CHRONIC; METABOLISM; TIME; VIROLOGY;

ADENINE; ADULT; ANTIVIRAL AGENTS; DNA, VIRAL; FEMALE; HEPATITIS B, CHRONIC; HUMANS; MALE; MIDDLE AGED; TENOFOVIR; TIME FACTORS; TREATMENT OUTCOME; YOUNG ADULT;

EID: 84922840729     PISSN: 01688278     EISSN: 16000641     Source Type: Journal    
DOI: 10.1016/j.jhep.2014.10.035     Document Type: Article

References (30)

1. B. Custer, S.D. Sullivan, T.K. Hazlet, U. Iloeje, D.L. Veenstra, and K.V. Kowdley Global epidemiology of hepatitis B virus J Clin Gastroenterol 38 2004 S158 S168
2. J.J. Ott, G.A. Stevens, J. Groeger, and S.T. Wiersma Global epidemiology of hepatitis B virus infection: new estimates of age-specific HBsAg seroprevalence and endemicity Vaccine 30 2012 2212 2219
3. C.-J. Chen, H.-I. Yang, J. Su, C.-L. Jen, S.-L. You, and S.-N. Lu Risk of hepatocellular carcinoma across a biological gradient of serum hepatitis B virus DNA level JAMA 295 2006 65 73
4. U.H. Iloeje, H.-I. Yang, C.-L. Jen, J. Su, L.-Y. Wang, and S.-L. You Risk and predictors of mortality associated with chronic hepatitis B infection Clin Gastroenterol Hepatol 5 2007 921 931
5. European Association for the Study of the Liver EASL clinical practice guidelines: management of chronic hepatitis B virus infection J Hepatol 57 2012 167 185
6. Y.F. Liaw, J.H. Kao, T. Piratvisuth, H.L.Y. Chan, R.-N. Chien, and C.-J. Liu Asian-Pacific consensus statement on the management of chronic hepatitis B: a 2012 update Hepatol Int 6 2012 531 561
7. S. Fung, P. Kwan, M. Fabri, A. Horban, M. Pelemis, and H.W. Hann Randomized comparison of tenofovir disoproxil fumarate vs. emtricitabine and tenofovir disoproxil fumarate in patients with lamivudine-resistant chronic hepatitis B Gastroenterology 146 2014 980 988
8. T. Berg, F. Zoulim, B. Moeller, H. Trinh, P. Marcellin, and S. Chan Long-term efficacy and safety of emtricitabine plus tenofovir DF vs. tenofovir DF monotherapy in adefovir-experienced chronic hepatitis B patients J Hepatol 60 2014 715 722
9. P. Marcellin, E. Gane, M. Buti, N. Afdahl, W. Sievert, and I.M. Jacobson Regression of cirrhosis during treatment with tenofovir disoproxil fumarate for chronic hepatitis B: a 5-year open-label follow-up study Lancet 381 2013 468 475
10. K.M. Kitrinos, A. Corsa, Y. Liu, J. Flaherty, A. Snow-Lampart, and P. Marcellin No detectable resistance to tenofovir disoproxil fumarate after 6 years of therapy in patients with chronic hepatitis B Hepatology 59 2014 434 442
11. N. Gara, X. Zhao, M.T. Collins, W.H. Chong, D.E. Kleiner, and J. Liang Renal tubular dysfunction during long-term adefovir and tenofovir therapy in chronic hepatitis B Aliment Pharmacol Ther 35 2012 1317 1325
12. D.M. Gracey, P. Snelling, P. McKenzie, and S.I. Strasser Tenofovir-associated Fanconi syndrome in patients with chronic hepatitis B monoinfection Antiviral Ther 18 2013 945 948
13. A.M. Hall Update on tenofovir toxicity in the kidney Pediatr Nephrol 28 2013 1011 1023
14. C.L.N. Woodward, A.M. Hall, I.G. Williams, S. Madge, A. Copas, and D. Nair Tenofovir-associated renal and bone toxicity HIV Med 10 2009 482 487
15. VIREAD (Tenofovir Disoproxil Fumarate) Tablets and Powder. US Prescribing Information. In. Edited by Foster City CGSI; 2013.
16. Murakami E, Babusis D, Wang T, Park Y, Lepist E-I, Hao J, et al. Efficient hepatic delivery of tenofovir by prodrug tenofovir alafenamide in nonclinical studies supports low-dose treatment of hepatitis B virus. HepDart 2013. Dec 8-12, 2013, Hawaii, Hawaii. Abstract 104.
17. Birkus G, Bam RA, Frey CR, Tsai L, Stray KM, Yant SR, et al. Intracellular activation pathways for GS 7340 and the effect of antiviral protease inhibitors. In: 19th Conference on Retroviruses and Opportunistic Infections. Mar 5 8, 2012, Seattle, WA. Abstract 577.
18. P.J. Ruane, E. DeJesus, D. Berger, M. Markowitz, U.F. Bredeek, and C. Callebaut Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1-positive adults J Acquir Immune Defic Syndr 63 2013 449 455
19. M. Markowitz, A. Zolopa, K. Squires, P. Ruane, D. Coakley, and B. Kearney Phase I/II study of the pharmacokinetics, safety and antiretroviral activity of tenofovir alafenamide, a new prodrug of the HIV reverse transcriptase inhibitor tenofovir, in HIV-infected adults J Antimicrob Chemother 69 2014 1362 1369
20. P. Sax, A. Zolopa, I. Brar, R. Elion, R. Ortiz, and F. Post Tenofovir alafenamide vs. tenofovir disoproxil fumarate in a single tablet regimens for initial HIV-1 therapy: a randomized phase 2 study J Acquir Immune Defic Syndr 67 2014 52 58
21. D. Babusis, T.K. Phan, W.A. Lee, W.J. Watkins, and A.S. Ray Mechanism for effective lymphoid cell and tissue loading following oral administration of nucleotide prodrug GS-7340 Mol Pharm 10 2013 459 466
22. D.W. Cockcroft, and M.H. Gault Prediction of creatinine clearance from serum creatinine Nephron 16 1976 31 41
23. A.S. Levey, L.A. Stevens, C.H. Schmid, Y.L. Zhang, A.F. Castro 3rd, and H.I. Feldman A new equation to estimate glomerular filtration rate Ann Intern Med 150 2009 604 612
24. A.R. Zolopa, D.S. Berger, H. Lampiris, L. Zhong, S.L. Chuck, and J.V. Enejosa Activity of elvitegravir, a once-daily integrase inhibitor, against resistant HIV type 1: results of a phase 2, randomized, controlled, dose-ranging clinical trial J Infect Dis 201 2010 814 822
25. P. Marcellin, E.J. Heathcoate, M. Buti, E. Gane, R.A. de Man, and Z. Krastev Tenofovir disoproxil fumarate versus adefovir dipivoxil for chronic hepatitis B N Engl J Med 359 2008 2442 2455
26. Ramanathan S, Wei X, Custodio J, Wang H, Dave A, Cheng A, et al. Pharmacokinetics of a novel EVG/COBI/FTC/GS-7340 single tablet regimen. In: 13th International Workshop on Clinical Pharmacology of HIV Therapy. Barcelona, Spain, Apr 16-18, 2012.
27. Jin F, Fordyce M, Garner W, Ray A, Tanamly S, Lindow J, et al. Pharmacokinetics, metabolism and excretion of tenofovir alafenamide. In: 14th International Workshop on Clinical Pharmacology of HIV Therapy. Amsterdam, Netherlands, Apr 22-24, 2013.
28. S. Rodriquez-Novoa, P. Labarga, A. D'Avolio, P. Barreiro, M. Albalate, and E. Vispo Impairment in kidney tubular function in patients receiving tenofovir is associated with higher tenofovir plasma concentrations AIDS 24 2010 1064 1066
29. I. Poizot-Martin, C. Solas, J. Allemand, V. Obry-Roguet, V. Pradel, and S. Bregigeon Renal impairment in patients receiving a tenofovir-cART regimen: impact of tenofovir trough concentration J Acquir Immune Defic Syndr 62 2013 375 380
30. K.K.A. Van Rompay, L. Durand-Gasselin, L.L. Brignolo, A.S. Ray, K. Abel, and T. Cihlar Chronic administration of tenofovir to rhesus macaques from infancy through adulthood and pregnancy: summary of pharmacokinetics and biological and virological effects Antimicrob Agents Chemother 52 2008 3144 3160