Ester prodrugs are commonly used to increase the intestinal absorption of drugs with permeabilitylimited absorption. The high functional activity of este rases in blood and liver allows a rapid bio acti va tion of the prodrug after reaching the sys temic circu lation. However, the increased efficiency of prodrugs to pass the intestinal barrier may be decreased by its rapid esterase-mediated hyd...

Developing a single analytical method for estimation of individual drug from a multidrug composition is a very challenging task. A complexation, derivatization, extraction, evaporation, and sensitive-free direct UV spectrophotometric method is developed and validated for the simultaneous estimation of some antiviral drugs such as emtricitabine (EMT), tenofovir disoproxil fumarate (TDF), and ril...

This open-label, multinational, pilot study randomized (1:2 ratio) adults with HIV-1 RNA <40 copies per milliliter and nucleos(t)ide-related safety/tolerability issues to switch to ritonavir-boosted atazanavir (ATV/r) plus tenofovir disoproxil fumarate/emtricitabine (n = 37) or the nucleos(t)ide reverse transcriptase inhibitor-sparing regimen of ATV/r plus raltegravir (RAL) (n = 72). At 24 week...

Human immunodeficiency virus (HIV) therapy has evolved over the last 20 years from mono-drug therapy given five times daily to regimens consisting of three or four drugs combined in a single-tablet dosed once daily. To allow once-daily administration, several drugs require pharmacokinetic boosting by a concomitantly administered P-glycoprotein and cytochrome P450 inhibitor such as ritonavir. Th...

Tenofovir is an acyclic nucleotide analog with activity against human immunodeficiency virus (HIV) and hepatitis B virus (HBV). Tenofovir disoproxil fumarate (tenofovir DF), a bis-alkoxyester prodrug of tenofovir, is approved for the treatment of HIV and is currently being developed to treat chronic hepatitis B. In this report, we further characterize the in vitro activity of tenofovir against ...

OBJECTIVES A safe and effective topical prevention strategy will likely require sustained delivery of potent antiviral drugs and a delivery system that simultaneously maximizes drug distribution and overcomes the behavioural challenges related to adherence. Activity against HIV and herpes simplex virus (HSV) would be advantageous, given the epidemiological link between the two pathogens. We hyp...

We have entered a new era in which antiretroviral agents have been demonstrated to be highly effective in preventing HIV-1 infection, especially in serodiscordant couples. The HPTN-052 randomized, controlled trial (RCT) of early versus delayed antiretroviral therapy (ART) for the HIV-1-infected persons in sexual partnerships with HIV-negative persons demonstrated at least a 96% reduction in HIV...

INTRODUCTION Data on renal impairment in sub-Saharan Africa (SSA) remains scarce, determination of renal function is not part of routine assessments. We evaluated renal function and blood pressure in a cohort of people living with HIV (PLWH) on antiretroviral treatment (ART) in the Renal Care Zambia project (ReCaZa). METHODS Using routine data from an HIV outpatient clinic from 2011-2013, we ...