Evaluation of Drug-Drug Interactions Between Direct-Acting Anti-Hepatitis C Virus Combination Regimens and the HIV-1 Antiretroviral Agents Raltegravir, Tenofovir, Emtricitabine, Efavirenz, and Rilpivirine.
CONCLUSIONS: No dose adjustment is required during coadministration of raltegravir, tenofovir DF, or emtricitabine with the 3D regimen. Rilpivirine is not recommended and efavirenz is contraindicated for coadministration with the 3D regimen. PMID: 26953200 [PubMed - as supplied by publisher] (Source: Antimicrobial Agents and Chemotherapy)
Source: Antimicrobial Agents and Chemotherapy - March 7, 2016 Category: Microbiology Authors: Khatri A, Dutta S, Dunbar M, Podsadecki T, Trinh R, Awni W, Menon R Tags: Antimicrob Agents Chemother Source Type: research

Efavirenz / Emtricitabine / Tenofovir disoproxil fumarate
Atripla is a fixed-dose combination tablet containing efavirenz, emtricitabine, and tenofovir disoproxil fumarate (tenofovir DF). Each Atripla tablet contains 600 mg of efavirenz, 200 mg of emtricitabine, and 300 mg of tenofovir DF (which is equivalent to 245 mg of tenofovir disoproxil) as active ingredients. [#] Sustiva is the brand name for efavirenz, a non-nucleoside reverse transcriptase inhibitor. Emtriva is the brand name for emtricitabine, a synthetic nucleoside analog of cytidine. Viread is the brand name for tenofovir DF, which is converted in vivo to tenofovir, an acyclic nucleoside phosphonate (nucleotide) analo...
Source: Aids Info Drugs - February 16, 2016 Category: Drugs & Pharmacology Source Type: research

Elvitegravir, cobicistat, emtricitabine and tenofovir alafenamide for the treatment of HIV in adults.
Authors: Bonora S, Calcagno A, Trentalange A, Di Perri G Abstract INTRODUCTION: Tenofovir alafenamide (TAF) is is a novel tenofovir prodrug with a 90% reduction in plasma tenofovir concentrations as compared to tenofovir disoproxil fumarate (TDF) and such property suggests that TAF-containing regimens can improve renal and bone safety compared with TDF-containing regimens. Single tablet regimen elvitegravir/cobicistat/emtricitabine/TAF (E/C/F/TAF) is the first coformulation that includes TAF in place of TDF. This review aims to provide an overview of its role in the treatment of HIV infection. AREA...
Source: Expert Opinion on Pharmacotherapy - February 14, 2016 Category: Drugs & Pharmacology Tags: Expert Opin Pharmacother Source Type: research

Rilpivirine vs. efavirenz-based single-tablet regimens in treatment-naive adults: week 96 efficacy and safety from a randomized phase 3b study
Objectives: To compare efficacy, safety, tolerability, and patient-reported outcomes between two single-tablet regimens, rilpivirine/emtricitabine/tenofovir disoproxil fumarate (RPV/FTC/TDF) and efavirenz/emtricitabine/tenofovir disoproxil fumarate (EFV/FTC/TDF), in HIV-1-infected, treatment-naive adults. Design: This was a phase 3b, 96-week, randomized, open-label, international, noninferiority trial. Methods: A total of 799 participants were randomized (1 : 1) to receive RPV/FTC/TDF or EFV/FTC/TDF. The primary efficacy endpoint evaluated proportions of participants with HIV-1 RNA less than 50 copies/ml using the Snap...
Source: AIDS - December 23, 2015 Category: Infectious Diseases Tags: Clinical Science Source Type: research

Greater change in bone turnover markers for efavirenz/emtricitabine/tenofovir disoproxil fumarate versus dolutegravir + abacavir/lamivudine in antiretroviral therapy-naive adults over 144 weeks
Conclusion: DTG + ABC/3TC in antiretroviral therapy-naive patients resulted in significantly lower increases in BTMs (CTx, osteocalcin, BSAP, P1NP) compared with EFV/FTC/TDF over 144 weeks. The observed changes are consistent with results from other smaller, randomized trials. These differences in BTMs likely correlate with changes in bone mineral density over time. (Source: AIDS)
Source: AIDS - November 13, 2015 Category: Infectious Diseases Tags: Clinical Science Source Type: research

Stribild: a review of component characteristics and combination drug efficacy.
CONCLUSIONS: Stribild provides viral suppression, comparable to other combination HIV drugs through review of non-inferiority and regimen simplification studies, with minimal adverse effects. Although the breadth of Stribild effectiveness has begun to unfold, studies are lacking in older patients as well as adolescents. PMID: 25807445 [PubMed - indexed for MEDLINE] (Source: Pharmacological Reviews)
Source: Pharmacological Reviews - October 26, 2015 Category: Drugs & Pharmacology Authors: Murrell DE, Moorman JP, Harirforoosh S Tags: Eur Rev Med Pharmacol Sci Source Type: research

Antiretroviral drugs do not interfere with bryostatin-mediated hiv-1 latency reversal
Publication date: Available online 30 September 2015 Source:Antiviral Research Author(s): Marta Martínez-Bonet, Maria Isabel Clemente, Susana Álvarez, Laura Díaz, Dolores García-Alonso, Eduardo Muñoz, Santiago Moreno, Maria Ángeles Muñoz-Fernández Although an effective combination of antiretroviral therapy (cART) controls HIV-1 viraemia in infected patients, viral latency established soon after infection hinders HIV-1 eradication. It has been shown that bryostatin-1 (BRY) inhibits HIV-infection in vitro and reactivates the latent virus through the protein kinase C-NF-κB pathway. We determined t...
Source: Antiviral Therapy - October 2, 2015 Category: Virology Source Type: research

Antiretroviral drugs do not interfere with bryostatin-mediated HIV-1 latency reversal.
Abstract Although an effective combination of antiretroviral therapy (cART) controls HIV-1 viraemia in infected patients, viral latency established soon after infection hinders HIV-1 eradication. It has been shown that bryostatin-1 (BRY) inhibits HIV-infection in vitro and reactivates the latent virus through the protein kinase C-NF-κB pathway. We determined the in vitro potential effect of BRY in combination with currently used antiretroviral drugs. BRY alone or in combination with maraviroc (MVC)/Atripla (ATP) was tested for its capacity to reactivate latent virus and inhibit new infections. JLTRG-R5 ce...
Source: Antiviral Research - September 29, 2015 Category: Virology Authors: Martínez-Bonet M, Clemente MI, Álvarez S, Díaz L, García-Alonso D, Muñoz E, Moreno S, Muñoz-Fernández MÁ Tags: Antiviral Res Source Type: research

Genomewide association study of tenofovir pharmacokinetics and creatinine clearance in AIDS Clinical Trials Group protocol A5202
Conclusion: Among patients randomized to receive TDF/emtricitabine in A5202, there were no significant genomewide associations with change in CrCl. This study did not replicate polymorphisms previously implicated in tenofovir-associated renal injury. (Source: Pharmacogenetics and Genomics)
Source: Pharmacogenetics and Genomics - August 3, 2015 Category: Genetics & Stem Cells Tags: Original Articles Source Type: research

Differential Reduction in Monocyte Activation and Vascular Inflammation With Integrase Inhibitor-Based Initial Antiretroviral Therapy Among HIV-Infected Individuals
Conclusions. EVG/c/FTC/TDF led to greater decreases in sCD14, hsCRP, and Lp-PLA2 levels, compared with EFV/FTC/TDF. Randomization group independently predicted the change in sCD14 level, and changes in monocyte activation independently predicted the change in Lp-PLA2 level. There appears to be a more favorable effect of the integrase inhibitor EVG over efavirenz on immune activation, which may affect vascular inflammation. (Source: The Journal of Infectious Diseases)
Source: The Journal of Infectious Diseases - July 10, 2015 Category: Infectious Diseases Authors: Hileman, C. O., Kinley, B., Scharen-Guivel, V., Melbourne, K., Szwarcberg, J., Robinson, J., Lederman, M. M., Mccomsey, G. A. Tags: HIV/AIDS Source Type: research

Emtricitabine/rilpivirine/tenofovir disoproxil fumarate single-tablet regimen in HIV-1 infection: a guide to its use in the EU
Abstract Emtricitabine/rilpivirine/tenofovir disoproxil fumarate (tenofovir DF) [Eviplera® (EU); Complera® (USA)] is a convenient and effective addition to the other single-tablet regimens currently available for the treatment of HIV-1 infection. Once-daily emtricitabine/rilpivirine/tenofovir DF was noninferior to once-daily emtricitabine/efavirenz/tenofovir DF in establishing virological suppression in treatment-naïve adults. Switching to the once-daily single tablet maintained virological suppression and was noninferior to remaining on a more complex multiple-tablet regimen in treatment-experienced p...
Source: Drugs and Therapy Perspectives - June 27, 2015 Category: Drugs & Pharmacology Source Type: research

Tenofovir plasma concentrations related to estimated glomerular filtration rate changes in first-line regimens in African HIV-infected patients: ANRS 12115 DAYANA substudy
Conclusions In this population of mostly female HIV-1-infected African patients, tenofovir plasma overexposure was associated with PI/ritonavir and a time-dependent decrease in eGFR, probably via an inhibition of MRP2/MRP4 efflux transporters. The close monitoring over time of the eGFR using MDRD or CKD-EPI calculations and by using other biomarkers of renal disorder should be proposed as an alternative to therapeutic drug monitoring in resource-limited countries. (Source: Journal of Antimicrobial Chemotherapy)
Source: Journal of Antimicrobial Chemotherapy - April 13, 2015 Category: Microbiology Authors: Le, M. P., Landman, R., Koulla-Shiro, S., Charpentier, C., Sow, P.-S., Diallo, M.-B., Ngom Gueye, N. F., Ngolle, M., Le Moing, V., Eymard-Duvernay, S., Benalycherif, A., Delaporte, E., Girard, P.-M., Peytavin, G., on behalf of the DAYANA Study Group, on b Tags: Original research Source Type: research

Steady-state pharmacokinetics of rilpivirine under different meal conditions in HIV-1-infected Ugandan adults
Conclusions A food effect was observed for steady-state pharmacokinetic parameters of rilpivirine (AUC0–24 and C24) when TDF/FTC/RPV was administered in the fasted state compared with the moderate-fat meal. The TDF/FTC/RPV formulation can be administered with either a low-fat or moderate-fat meal. (Source: Journal of Antimicrobial Chemotherapy)
Source: Journal of Antimicrobial Chemotherapy - April 13, 2015 Category: Microbiology Authors: Lamorde, M., Walimbwa, S., Byakika-Kibwika, P., Katwere, M., Mukisa, L., Sempa, J. B., Else, L., Back, D. J., Khoo, S. H., Merry, C. Tags: Original research Source Type: research

Abacavir/Dolutegravir/Lamivudine Single-Tablet Regimen: A Review of Its Use in HIV-1 Infection
Abstract A fixed-dose, single-tablet regimen comprising the integrase strand transfer inhibitor (INSTI) dolutegravir and the nucleos(t)ide reverse transcriptase inhibitors (NRTIs) abacavir and lamivudine (abacavir/dolutegravir/lamivudine; Triumeq®) is now available for the treatment of HIV-1 infection. In a randomized, double-blind, phase III trial in antiretroviral therapy (ART)-naive adults (SINGLE), once-daily dolutegravir plus abacavir/lamivudine had noninferior efficacy to once-daily efavirenz/tenofovir disoproxil fumarate (tenofovir DF)/emtricitabine with regard to establishing and sustaining virol...
Source: Drugs - February 20, 2015 Category: Drugs & Pharmacology Source Type: research

Renal and Metabolic Toxicities Following Initiation of HIV-1 Treatment Regimen in a Diverse, Multinational Setting: A Focused Safety Analysis of ACTG PEARLS (A5175)
Conclusions: TDF is associated with lower serious metabolic toxicities but not higher risk of RAs, serious renal events, or worsening CrCl over time compared to ZDV in this randomized multinational study. Content Type Journal ArticleCategory Original ArticlePages 246-260DOI 10.1310/hct1506-246Authors F. Touzard Romo, The Miriam Hospital, Providence, Rhode Island, USAL. M. Smeaton, Harvard School of Public Health, Boston, Massachusetts, USAT. B. Campbell, University of Colorado Denver, Aurora, Colorado, USAC. Riviere, Institut Nacional de Laboratoire et Recherches, Port-au-Prince, HaitiR. Mngqibisa, University of KwaZulu...
Source: HIV Clinical Trials - November 29, 2014 Category: Infectious Diseases Tags: HIV Clinical Trials Source Type: research