Results 151 to 160 of about 5,420 (200)

An Improved Synthesis of Elvitegravir

Journal of Heterocyclic Chemistry, 2015
An improved process for the active pharmaceutical ingredient of a new HIV integrase inhibitor elvitegravir (1) has been developed. It starts from commercially available 2,4‐dimethoxyacetophenone, which is selectively halogenated into the position 5. The 5‐halo acetophenones are condensed with dialkyl carbonates to give the corresponding benzoylacetates.
Stanislav Rádl, Jan Stach, Ondřej Píša, Josef Cinibulk, Jaroslav Havlíček, Markéta Zajícová, Tomáš Pekárek   +6 more
openaire   +1 more source

Comprehensive Review on Different Analytical Techniques for HIV 1- Integrase Inhibitors: Raltegravir, Dolutegravir, Elvitegravir and Bictegravir

Critical reviews in analytical chemistry, 2022
The advent of HIV-Integrase inhibitors (IN) has marked a significant impact on the lives of HIV patients. Since the launch of the first anti retro-viral drug “Azidothymidine” to the recent advances of IN inhibitors, about 27.4 million people benefit by ...
P. Jain, Anusha Thota, P. Saini, R. Raghuvanshi   +3 more
semanticscholar   +1 more source

In vitro resistance selections using elvitegravir, raltegravir, and two metabolites of elvitegravir M1 and M4

Antiviral Research, 2012
Elvitegravir is a strand transfer inhibitor of HIV-1 integrase that is currently undergoing phase 3 clinical testing. The two predominant metabolites of elvitegravir, M1 and M4 (elvitegravir hydroxide and elvitegravir glucuronide), have been shown to inhibit HIV-1 integrase in vitro.
Nicolas A, Margot, Rebecca M, Hluhanich, Gregg S, Jones, Kristen N, Andreatta, Manuel, Tsiang, Damian J, McColl, Kirsten L, White, Michael D, Miller   +7 more
openaire   +2 more sources

Pegylated solid lipid nanoparticles for the intranasal delivery of combination antiretroviral therapy composed of Atazanavir and Elvitegravir to treat NeuroAIDS.

International journal of pharmaceutics
Intranasal drug administration offers a promising strategy for delivering combination antiretroviral therapy (cART) directly to the central nervous system to treat NeuroAIDS, leveraging the nose-to-brain route to bypass the blood-brain barrier.
Arya Bazargani, Mohammad Hejazi, M. Fernandez, A. Cordeiro, Johanna Tsala Ebode, Nastassja Lewinski, Sandro R.P. da Rocha, Laleh Golshahi   +7 more
semanticscholar   +1 more source

Switch to fixed-dose ainuovirine, lamivudine, and tenofovir DF versus elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide in virologically suppressed people living with HIV-1: the 48-week results of the SPRINT trial, a multi-centre, randomised, double-blind, active-controlled, phase 3

The Lancet Regional Health - Western Pacific
Summary Background We compared the efficacy and safety profiles of ainuovirine (ANV), a new-generation non-nucleoside reverse transcriptase inhibitor (NNRTI), with boosted elvitegravir (EVG), both coformulated with two nucleoside reverse transcriptase ...
Fujie Zhang, Hao Wu, Weiping Cai, Ping Ma, Qingxia Zhao, Hongxia Wei, Hongzhou Lu, Hui Wang, Shenghua He, Zhu Chen, Yaokai Chen, Min Wang, Wan Wan, Heliang Fu, Hong Qin   +14 more
semanticscholar   +1 more source

A Phase 1 Clinical Trial to Assess the Safety and Pharmacokinetics of a Tenofovir Alafenamide/Elvitegravir Insert Administered Rectally for HIV Prevention.

Journal of Infectious Diseases
BACKGROUND On-demand topical products could be an important tool for HIV prevention. We evaluated the safety, pharmacokinetics, and ex vivo pharmacodynamics of a tenofovir alafenamide/elvitegravir (TAF/EVG; 16 mg/20 mg) insert administered rectally ...
Sharon A Riddler, Clifton W Kelly, C. Hoesley, Ken S Ho, Jeanna M. Piper, S. Edick, Faye Heard, Gustavo F. Doncel, Sherri Johnson, Peter L Anderson, Rhonda M Brand, R. P. Kunjara Na Ayudhya, J. Bauermeister, Sharon L. Hillier, Craig W. Hendrix   +14 more
semanticscholar   +1 more source

Elvitegravir for the treatment of HIV infection

Drugs of Today, 2014
Advances in antiretroviral treatment have transformed HIV-1 infection from a deadly disease to a chronic one. Novel antiretroviral drugs have been approved for clinical use. In order to achieve long-term suppression of viremia, patients have to commit and take these drugs, or others approved in the future, for the rest of their lives.
openaire   +2 more sources

Pharmacokinetic Interaction of Ritonavir-Boosted Elvitegravir and Maraviroc

JAIDS Journal of Acquired Immune Deficiency Syndromes, 2010
The pharmacokinetic (PK) interaction between ritonavir-boosted elvitegravir (elvitegravir/r) and maraviroc was evaluated.Healthy subjects were randomized to receive elvitegravir/r (150/100 mg once daily) before or after elvitegravir/r plus maraviroc (150 mg twice daily) (group 1; n = 20) or receive maraviroc before or after maraviroc plus elvitegravir ...
Srinivasan, Ramanathan, Samantha, Abel, Sarah, Tweedy, Steve, West, James, Hui, Brian P, Kearney   +5 more
openaire   +2 more sources

Elvitegravir: An Emerging HIV Integrase Inhibitor

Future HIV Therapy, 2008
Integration of the reverse transcribed HIV dsDNA into the host cell chromosome is critical for the subsequent production of progeny virions. In October 2007, the US FDA approved the first HIV-1 integrase inhibitor, raltegravir, as a therapeutic agent for treatment-experienced HIV-1-infected patients.
Kazuya Shimura, Eiichi Kodama
openaire   +1 more source

Population Pharmacokinetics of Boosted‐Elvitegravir in HIV‐Infected Patients

The Journal of Clinical Pharmacology, 2015
AbstractElvitegravir (EVG) is an HIV strand transfer integrase inhibitor approved for the treatment of HIV infection as a part of antiretroviral regimens containing cobicistat (COBI) or ritonavir (RTV) as a booster. The population pharmacokinetics of EVG in treatment‐naive and ‐experienced HIV patients was determined, and the effects of demographic ...
Joseph M, Custodio, Toufigh, Gordi, Lijie, Zhong, Kah Hiing J, Ling, Srini, Ramanathan   +4 more
openaire   +2 more sources