The development of an effective synthetic route of rilpivirine
Background Rilpivirine (RPV) was approved by the U.S. FDA (Food and Drug Administration) in 2011 to treat individuals infected with human immunodeficiency virus 1 (HIV-1). Significantly, rilpivirine is three fold more potent than etravirine.
Tao Zhang +7 more
doaj +1 more source
Background The recently approved anti-AIDS drug rilpivirine (TMC278, Edurant) is a nonnucleoside inhibitor (NNRTI) that binds to reverse transcriptase (RT) and allosterically blocks the chemical step of DNA synthesis.
Johnson Barry C +11 more
doaj +1 more source
Non-Nucleoside Reverse Transcriptase Inhibitors Join Forces with Integrase Inhibitors to Combat HIV
In the treatment of acquired immune deficiency syndrome (AIDS), the diarylpyrimidine (DAPY) analogs etravirine (ETR) and rilpivirine (RPV) have been widely effective against human immunodeficiency virus (HIV) variants that are resistant to other non ...
Daniel M. Himmel, Eddy Arnold
doaj +1 more source
Focus on chirality of HIV-1 non-nucleoside reverse transcriptase inhibitors [PDF]
Chiral HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are of great interest since one enantiomer is often more potent than the corresponding counterpart against the HIV-1 wild type (WT) and the HIV-1 drug resistant mutant strains.
Famiglini, Valeria, Silvestri, Romano
core +2 more sources
HIV-1 drug mutations in children from northern Tanzania [PDF]
Objectives: In resource-limited settings, it is a challenge to get quality clinical specimens due to poor infrastructure for their collection, transportation, processing and storage. Using dried blood spots (DBS) might be an alternative to plasma for HIV-
Shao, Elichilia R. +9 more
core +4 more sources
Potent inhibitors active against HIV reverse transcriptase with K101P, a mutation conferring rilpivirine resistance [PDF]
Catechol diether compounds have nanomolar antiviral and enzymatic activity against HIV with reverse transcriptase (RT) variants containing K101P, a mutation that confers high-level resistance to FDA-approved non-nucleoside inhibitors efavirenz and ...
Anderson, Karen S. +9 more
core +2 more sources
Computational development of rubromycin-based lead compounds for HIV-1 reverse transcriptase inhibition [PDF]
The binding of several rubromycin-based ligands to HIV1-reverse transcriptase was analyzed using molecular docking and molecular dynamics simulations. MM-PBSA analysis and examination of the trajectories allowed the identification of several promising ...
Bernardo, Carlos E. P., Silva, Pedro J.
core +3 more sources
Dolutegravir-based regimen maintains virological success in a patient with archived mutations to integrase inhibitors [PDF]
no abstract ...
Falasca, Francesca +3 more
core +1 more source
Effectiveness of dolutegravir-based regimens as either first-line or switch antiretroviral therapy: data from the Icona cohort [PDF]
Introduction: Concerns about dolutegravir (DTG) tolerability in the real-life setting have recently arisen. We aimed to estimate the risk of treatment discontinuation and virological failure of DTG-based regimens from a large cohort of HIV-infected ...
Abeli C. +155 more
core +4 more sources
Drug resistance in B and non-B subtypes amongst subjects recently diagnosed as primary/recent or chronic HIV-infected over the period 2013–2016: Impact on susceptibility to first-line strategies including integrase strand-transfer inhibitors [PDF]
Objectives To characterize the prevalence of transmitted drug resistance mutations (TDRMs) by plasma analysis of 750 patients at the time of HIV diagnosis from January 1, 2013 to November 16, 2016 in the Veneto region (Italy), where all drugs included in
Alvarez, M +18 more
core +1 more source

