中文English
ISSN 1001-5256 (Print)
ISSN 2097-3497 (Online)
CN 22-1108/R
Volume 35 Issue 8
Aug.  2019
Turn off MathJax
Article Contents

Research advances in the clinical effect of tenofovir alafenamide in treatment of chronic hepatitis B

DOI: 10.3969/j.issn.1001-5256.2019.08.040
Research funding:

 

  • Received Date: 2019-04-04
  • Published Date: 2019-08-20
  • Tenofovir alafenamide (TAF) is a novel nucleoside reverse transcriptase inhibitor used in the treatment of human immunodeficiency virus (HIV) infection and chronic hepatitis B virus (HBV) infection. Compared with tenofovir disoproxil fumarate, TAF has better plasma stability and stronger liver-targeting ability and can significantly reduce the adverse events of renal injury and reduced bone mineral density. This article summarizes the research advances in the pharmacological characteristics, metabolic pathways, drug interactions, drug resistance, and renal safety of TAF and its role in patients with chronic HBV infection.

     

  • loading
  • [1] Chinese Society of Hepatology and Chinese Society of Infectious Diseases, Chinese Medical Association. The guideline of prevention and treatment for chronic hepatitis B:A 2015 update[J]. J Clin Hepatol, 2015, 31 (12) :1941-1960. (in Chinese) 中华医学会肝病学分会, 中华医学会感染病学分会.慢性乙型肝炎防治指南 (2015年更新版) [J].临床肝胆病杂志, 2015, 31 (12) :1941-1960.
    [2] TERRAULT NA, LOK ASF, McMAHON BJ, et al. Update on prevention, diagnosis, and treatment of chronic hepatitis B:AASLD 2018 hepatitis B guidance[J]. Hepatol, 2018, 67 (4) :1560-1599.
    [3] SARIN SK, KUMAR M, LAU GK, et al. Asian-Pacific clinical practice guidelines on the management of hepatitis B:A 2015update[J]. Hepatol Int, 2016, 10 (1) :1-98.
    [4] European Association for the Study of the Liver. EASL 2017clinical practice guidelines on the management of hepatitis B virus infection[J]. J Hepatol, 67 (2) :370-398.
    [5] HEATHCOTE EJ, MARCELLIN P, BUTI M, et al. Three year efficacy and safety of tenofovir disoproxil fumarate treatment for chronic hepatitis B[J]. Gastroenterology, 2011, 140 (1) :132-143.
    [6] MARCELLIN P, GANE E, BUTI M, et al. Regression of cirrhosis during treatment with tenofovir disoproxil fumarate for chronic hepatitis B:A 5-year open-label follow up study[J].Lancet, 2013, 381 (9865) :468-475.
    [7] PETERSEN J, HEYNE R, MAUSS S, et al. Effectiveness and safety of tenofovir disoproxil fumarate in chronic hepatitis B:A3-year prospective field practice study in Germany[J]. Dig Dis Sci, 2016, 61 (10) :3061-3071.
    [8] CHEN YH, CAO QF, HONG QY, et al. Effect of tenofovir disoproxil fumarate on serum FGF-23, β2-MG, Cys-C and RBP level in patients with chronic hepatitis B[J]. Chin J Clin Pharmacol Ther, 2017, 22 (7) :799-804. (in Chinese) 陈勇华, 曹群奋, 洪琼怿, 等.替诺福韦酯治疗对慢性乙型肝炎患者血清FGF-23、β2-MG、Cys-C及RBP水平的影响[J].中国临床药理学与治疗学, 2017, 22 (7) :799-804.
    [9] CHAN HL, FUNG S, SETO WK, et al. Tenofovir alafenamide versus tenofovir disoproxil fumarate for the treatment of HBe Ag-positive chronic hepatitis B virus infection:A randomized, double-blind, phase 3, non-inferiority trial[J]. Lancet Gastroenterol Hepatol, 2016, 1 (3) :185-195.
    [10] TONG MJ, PAN CQ, HAN SH, et al. An expert consensus for the management of chronic hepatitis B in Asian Americans[J]. Aliment Pharmacol Ther, 2018, 47 (8) :1181-1200.
    [11] MURAKAMI E, WANG T, PARK Y, et al. Implications of efficient hepatic delivery by tenofovir alafenamide (GS-7340) for hepatitis B virus therapy[J]. Antimicrob Agents Chemother, 2015, 59 (6) :3563-3569.
    [12] BABUSIS D, PHAN TK, LEE WA, et al. Mechanism for effective lymphoid cell and tissue loading following oral administration of nucleotide prodrug GS-7340[J]. Mol Pharm, 2013, 10 (2) :459-466.
    [13] AGARWAL K, FUNG SK, NGUYEN TT, et al. Twenty-eight day safety, antiviral activity and pharmacokinetics of tenofovir alafenamide for treatment of chronic hepatitis B infection[J]. J Hepatol, 2015, 62 (3) :533-540.
    [14] RUANE PJ, DEJESUS E, BERGER D, et al. Antiviral activity, safety and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1 positive adults[J]. J Acquir Immune Defic, 2013, 63 (4) :449-455.
    [15] Center for Drug Evaluation and Research. Clinical pharmacology and biopharmaceutics review (s) [Z/OL].[2018-06-14]. https://www. accessdata. fda. gov/drugsatfda_docs/nda/2016/208464Orig1s000ClinPharmR. pdf
    [16] GONZALES ZAMORA JA. Adverse effects of direct acting antivirals in HIV/HCV coinfected patients:A 4-year experience in Miami, Florida[J]. Diseases, 2018, 6 (2) :51.
    [17] BONORA S, CALCAGNO A, TRENTALANGE A, et al. Elvitegravir, cobicistat, emtricitabine and tenofovir alafenamide for the treatment of HIV in adults[J]. Expert Opin Pharmacother, 2016, 17 (3) :409-419.
    [18] BAM RA, BIRKUS G, BABUSIS D, et al. Metabolism and antiretroviral activity of tenofovir alafenamide in CD4+T-cells and macrophages from demographically diverse donors[J].Antivir Ther, 2014, 19 (7) :669-677.
    [19] BUTI M, GANE E, SETO WK, et al. Tenofovir alafenamide versus tenofovir disoproxil fumarate for the treatment of patients with HBe Ag-negative chronic hepatitis B virus infection:A randomised, double-blind, phase 3, non-inferiority trial[J]. Lancet Gastroenterol Hepatol, 2016, 1 (3) :196-206.
    [20] AGARWAL K, BRUNETTO M, SETO WK, et al. 96 weeks treatment of tenofovir alafenamide vs. tenofovir disoproxil fumarate for hepatitis B virus infection[J]. J Hepatol, 2018, 68 (4) :672-681.
    [21] LAU GK, PIRATVISUTH T, LUO KX, et al. Peginterferon alfa-2a, lamivudine, and the combination for HBe Ag-positive chronic hepatitis B[J]. N Engl J Med, 2005, 352 (26) :2682-2695.
    [22] JAFRI SM, LOK AS. Antiviral therapy for chronic hepatitis B[J]. Clin Liver Dis, 2010, 14 (3) :425-438.
    [23] CHEN CH, LIN CL, KAO CH. Association between chronic hepatitis B virus infection and risk of osteoporosis:A nationwide population-based and study[J]. Medicine (Baltimore) , 2015, 94 (50) :e2276.
    [24] SETO WK, ASAHINA Y, BROWN TT, et al. Improved bone safety of tenofovir alafenamide compared to tenofovir disoproxil fumarate over 2 years in patients with chronic HBV infection[J]. Clin Gastroenterol Hepatol, 2018.[Epub ahead of print]
    [25] FONG TL, LEE BT, TIEN A, et al. Improvement of bone mineral density and markers of proximal renal tubular function in chronic hepatitis B patients switched from tenofovir disoproxil fumarate to tenofovir alafenamide[J]. J Viral Hepat, 2019, 26 (5) :561-567.
    [26] LIU Y, MILLER MD, KITRINOS KM. Tenofovir alafenamide demonstrates broad cross-genotype activity against wild-type HBV clinical isolates and maintains susceptibility to drug-resistant HBV isolates in vitro[J]. Antiviral Res, 2017, 139 (3) :25-31.
    [27] CATHCART AL, CHAN HL, BHARDWAJ N, et al. No resistance to tenofovir alafenamide detected through 96 weeks of treatment in patients with chronic hepatitis B[J]. Antimicrob Agents Chemother, 2018, 62 (10) :e01064-18.
    [28] PARK ES, LEE AR, KIM DH, et al. Identification of a quadruple mutation that confers tenofovir resistance in chronic hepatitis B patients[J]. J Hepatol, 2019, 70 (6) :1093-1102.
    [29] LIU Y, CHEN RJ, LI XD. The rt S106C+H126Y+D134E triple variant of hepatitis B virus has no direct association with tenofovir resistance in Chinese patients[C]. APASL, Feb20-24, 2019, Manila, Poster ID589.
    [30] BAM RA, YANT SR, CIHLAR T. Tenofovir alafenamide is not a substrate for renal organic anion transporters (OATs) and does not exhibit OAT-dependent cytotoxicity[J]. Antivir Ther, 2014, 19 (7) :687-692.
    [31] CUSTODIO JM, FORDYCE M, GARNER W, et al. Pharmacokinetics and safety of tenofovir alafenamide in HIV-uninfected subjects with severe renal impairment[J]. Antimicrob Agents Chemother, 2016, 60 (9) :5135-5140.
    [32] KARRIS MY. Short communication:Resolution of tenofovir disoproxil fumarate induced Fanconi syndrome with switch to tenofovir alafenamide fumarate in a HIV-1 and hepatitis B coinfected patient[J]. AIDS Res Hum Retroviruses, 2017, 33 (7) :718-722.
    [33] CUSTODIO JM, MA G, CUVIN J, et al. Pharmacokinetics and safety of tenofovir alafenamide in subjects with severe hepatic impairment[J]. J Hepatol, 2016, 64 (1 Suppl) :s594-s595.
    [34] WONG GL, CHAN HL, MAK CW, et al. Entecavir treatment reduces hepatic events and deaths in chronic hepatitis B patients with liver cirrhosis[J]. Hepatol, 2013, 58 (5) :1537-1547.
    [35] WU CY, LIN JT, HO HJ, et al. Association of nucleos (t) ide analogue therapy with reduced risk of hepatocellular carcinoma in patients with chronic hepatitis B:A nationwide cohort study[J]. Gastroenterology, 2014, 147 (1) :143-151.
    [36] LIM YS, HAN SB, HEO NY, et al. Mortality, liver transplantation, and hepatocellular carcinoma among patients with chronic hepatitis B treated with entecavir vs lamivudine[J]. Gastroenterology, 2014, 147 (1) :152-161.
    [37] CHOI J, KIM HJ, LEE J, et al. Risk of hepatocellular carcinoma in patients treated with entecavir vs tenofovir for chronic hepatitis B:A Korean nationwide cohort study[J]. JAMA Oncol, 2018, 5 (1) :30-36.
    [38] MURATA K, ASANO M, MATSUMOTO A, etal. Induction of IFN-λ3 as an additional effect of nucleotide, not nucleoside, analogues:A new potential target for HBV infection[J]. Gut, 2018, 67 (2) :362-371.
    [39] ABUSHAHBA W, BALAN M, CASTANEDA I, et al. Antitumor activity of type I and type III interferons in BNL hepatoma model[J]. Cancer Immunol Immunother, 2010, 59 (7) :1059-1071.
    [40] SATO A, OHTSUKI M, HATA M, et al. Antitumor activity of IFN-lambda in murine tumor models[J]. J Immunol, 2006, 176 (12) :7686-7694.
    [41] GORDON SC, ZHOU YR, LI J, et al. Effect of treatment of hepatitis B patients with tenofovir disoproxil or entecavir on risk of hepatocellular cancer death in a U. S. Cohort[J]. J Hepatol, 2019, 70 (1 Suppl) :e147.
    [42] KIM SU, SEO YS, LEE HA, et al. A multi-center study of entecavir vs. tenofovir on prognosis of treatment-nave chronic hepatitis B in the Republic of Korea[J]. J Hepatol, 2019.[Epub ahead of print]
    [43] WONG GL, CHAN HL, TSE YK, et al. Normal on-treatment ALT during antiviral treatment is associated with a lower risk of hepatic events in patients with chronic hepatitis B[J]. J Hepatol, 2018, 69 (4) :793-802.
    [44] SETO WK, LO YR, PAWLOTSKY JM. Chronic hepatitis B virus infection[J]. Lancet, 2018, 392 (10161) :2313-2324.
    [45] YUEN MF, AGARWAL K, GANE E, et al. Assembly biosciences presents interim data from two phase 2a studies of ABI-H0731 in HBV-infected subjects in a late-breaker oral session at EASL 2019[J]. J Hepatol, 2019, 70 (1 Suppl) :e81-e132.
    [46] YUEN MF, LOCARNINI S, LIM TH, et al. PS-080-Short term RNA interference therapy in chronic hepatitis B using JNJ-3989 brings majority of patients to HBs Ag <100 IU/ml threshold[J]. J Hepatol, 2019, 70 (1 Suppl) :e51-e52.
  • 加载中

Catalog

    通讯作者: 陈斌, bchen63@163.com
    • 1. 

      沈阳化工大学材料科学与工程学院 沈阳 110142

    1. 本站搜索
    2. 百度学术搜索
    3. 万方数据库搜索
    4. CNKI搜索

    Article Metrics

    Article views (3026) PDF downloads(568) Cited by()
    Proportional views
    Related

    /

    DownLoad:  Full-Size Img  PowerPoint
    Return
    Return