Clinical pharmacokinetics and pharmacodynamics of dolutegravir used as a single tablet regimen for the treatment of HIV-1 infection

被引:13
作者
Bollen, Pauline [1 ,2 ,3 ]
Reiss, Peter [4 ,5 ]
Schapiro, Jonathan [6 ]
Burger, David [1 ,2 ]
机构
[1] Radboud Univ Nijmegen, Med Ctr, Dept Pharm, NL-6525 GA Nijmegen, Netherlands
[2] RIHS, Nijmegen, Netherlands
[3] Hosp Pharm Midden Brabant, Elisabeth TweeSteden Hosp, Tilburg, Netherlands
[4] Univ Amsterdam, Acad Med Ctr, Div Infect Dis, NL-1105 AZ Amsterdam, Netherlands
[5] Dept Global Hlth, Amsterdam, Netherlands
[6] Chaim Sheba Med Ctr, Natl Hemophilia Ctr, Ramat Gan, Israel
关键词
abacavir; dolutegravir; fixed-dose combination; HIV; integrase inhibitor; lamivudine; nucleoside reverse transcriptase inhibitor; ANTIRETROVIRAL-NAIVE ADULTS; ONCE-DAILY DOLUTEGRAVIR; INTEGRASE INHIBITOR DOLUTEGRAVIR; STEADY-STATE PHARMACOKINETICS; STRAND TRANSFER INHIBITORS; DOUBLE-BLIND; MYOCARDIAL-INFARCTION; SERONEGATIVE SUBJECTS; ABACAVIR-LAMIVUDINE; ANTIVIRAL ACTIVITY;
D O I
10.1517/14740338.2015.1059818
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Introduction: With the introduction of the coformulated dolutegravir, abacavir and lamivudine, a new single tablet regimen (STR) is made available for the use in treatment-naive and treatment-experienced HIV-infected patients. This drug combination is the fourth STR that will be positioned next to the STRs with efavirenz, rilpivirine or elvitegravir as third agents, respectively. Areas covered: The objective of this review is to provide an overview of the efficacy and safety of the combined dolutegravidabacavir/lannivudine coformulation. The review will focus on dolutegravir and includes both published data as well as data presented at recent major international HIV/AIDS conferences. Expert opinion: The dolutegravir/abacavir/lamivudine regimen is highly effective in achieving sustained suppression of HIV-1 RNA plasma concentrations. The SIR has a favorable safety profile and a low potential for drug interactions, which will contribute to a prominent role in therapy. As this STR contains abacavir as backbone component, the use requires patients to be HLA-B*5701 negative, with good hepatic function. Other first-line treatment combinations are preferred for patients with hepatitis B co-infection or with a high cardiovascular risk.
引用
收藏
页码:1457 / 1472
页数:16
相关论文
共 91 条
[1]  
Akil B, 2014, ANTIVIR THER
[2]  
[Anonymous], 39 INT C ANT AG CHEM
[3]  
[Anonymous], 20 INT AIDS C MELB A
[4]  
[Anonymous], 20 C RETR OPP INF AT
[5]   Long-term incidence of hepatitis B virus resistance to lamivudine in human immunodeficiency virus-infected patients [J].
Benhamou, Y ;
Bochet, M ;
Thibault, V ;
Di Martino, V ;
Caumes, E ;
Bricaire, F ;
Opolon, P ;
Katlama, C ;
Poynard, T .
HEPATOLOGY, 1999, 30 (05) :1302-1306
[6]   Dolutegravir versus raltegravir in antiretroviral-experienced, integrase-inhibitor-naive adults with HIV: week 48 results from the randomised, double-blind, non-inferiority SAILING study [J].
Cahn, Pedro ;
Pozniak, Anton L. ;
Mingrone, Horacio ;
Shuldyakov, Andrey ;
Brites, Carlos ;
Andrade-Villanueva, Jaime F. ;
Richmond, Gary ;
Beltran Buendia, Carlos ;
Fourie, Jan ;
Ramgopal, Moti ;
Hagins, Debbie ;
Felizarta, Franco ;
Madruga, Jose ;
Reuter, Tania ;
Newman, Tamara ;
Small, Catherine B. ;
Lombaard, John ;
Grinsztejn, Beatriz ;
Dorey, David ;
Underwood, Mark ;
Griffith, Sandy ;
Min, Sherene .
LANCET, 2013, 382 (9893) :700-708
[7]   In vitro phenotypes to elvitegravir and dolutegravir in primary macrophages and lymphocytes of clonal recombinant viral variants selected in patients failing raltegravir [J].
Canducci, Filippo ;
Ceresola, Elisa Rita ;
Saita, Diego ;
Castagna, Antonella ;
Gianotti, Nicola ;
Underwood, Mark ;
Burioni, Roberto ;
Lazzarin, Adriano ;
Clementi, Massimo .
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 2013, 68 (11) :2525-2532
[8]   Dolutegravir in Antiretroviral-Experienced Patients With Raltegravir- and/or Elvitegravir-Resistant HIV-1: 24-Week Results of the Phase III VIKING-3 Study [J].
Castagna, Antonella ;
Maggiolo, Franco ;
Penco, Giovanni ;
Wright, David ;
Mills, Anthony ;
Grossberg, Robert ;
Molina, Jean-Michel ;
Chas, Julie ;
Durant, Jacques ;
Moreno, Santiago ;
Doroana, Manuela ;
Ait-Khaled, Mounir ;
Huang, Jenny ;
Min, Sherene ;
Song, Ivy ;
Vavro, Cindy ;
Nichols, Garrett ;
Yeo, Jane M. .
JOURNAL OF INFECTIOUS DISEASES, 2014, 210 (03) :354-362
[9]   Metabolism, Excretion, and Mass Balance of the HIV-1 Integrase Inhibitor Dolutegravir in Humans [J].
Castellino, Stephen ;
Moss, Lee ;
Wagner, David ;
Borland, Julie ;
Song, Ivy ;
Chen, Shuguang ;
Lou, Yu ;
Min, Sherene S. ;
Goljer, Igor ;
Culp, Amanda ;
Piscitelli, Stephen C. ;
Savina, Paul M. .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2013, 57 (08) :3536-3546
[10]   Evaluation of the effect of UGT1A1 polymorphisms on dolutegravir pharmacokinetics [J].
Chen, Shuguang ;
St Jean, Pamela ;
Borland, Julie ;
Song, Ivy ;
Yeo, Astrid J. ;
Piscitelli, Stephen ;
Rubio, Justin P. .
PHARMACOGENOMICS, 2014, 15 (01) :9-16