Results 21 to 30 of about 3,103 (173)

Quantum Mechanical-Based Stability Evaluation of Crystal Structures for HIV-Targeted Drug Cabotegravir

Molecules, 2021
The long-acting parenteral formulation of the HIV integrase inhibitor cabotegravir (GSK744) is currently being developed to prevent HIV infections, benefiting from infrequent dosing and high efficacy.
Yanqiang Han, Hongyuan Luo, Qianqian Lu, Zeying Liu, Jinyun Liu, Jiarui Zhang, Zhiyun Wei, Jinjin Li   +7 more
doaj   +1 more source

Synthesis and biological evaluation of novel 1,2,3-triazole hybrids of cabotegravir: identification of potent antitumor activity against lung cancer

Frontiers in Pharmacology, 2023
In pursuit of discovering novel anticancer agents, we designed and synthesized a series of novel 1,2,3-triazole hybrids based on cabotegravir analogues.
Yajie Guo, Dan Sang, Bin Guo, Dan Wang, Dan Wang, Xinyue Xu, Xinyue Xu, Huili Wang, Cuilan Hou, Longfei Mao, Longfei Mao, Fang Li, Sanqiang Li   +12 more
doaj   +1 more source

What will it take for an injectable ARV to change the face of the HIV epidemic in high‐prevalence countries? Considerations regarding drug costs and operations

Journal of the International AIDS Society, 2023
Introduction The proven effectiveness of injectable cabotegravir (CAB‐LA) is higher than that of any other HIV prevention intervention ever trialled or implemented, surpassing medical male circumcision, condoms and combination antiretroviral treatment ...
Gesine Meyer‐Rath, Lise Jamieson, Yogan Pillay   +2 more
doaj   +1 more source

Multitasking Pharmacophores Support Cabotegravir-Based Long-Acting HIV Pre-Exposure Prophylaxis (PrEP)

Molecules
Cabotegravir is an integrase strand transfer inhibitor (INSTI) for HIV treatment and prevention. Cabotegravir-based long-acting pre-exposure prophylaxis (PrEP) presents an emerging paradigm for infectious disease control. In this scheme, a combination of
Zheng Wan, Man Shi, Yanqing Gong, Massimo Lucci, Jinjin Li, Jiahai Zhou, Xiao-Liang Yang, Moreno Lelli, Xiao He, Jiafei Mao   +9 more
doaj   +1 more source

Cabotegravir, the Long-Acting Integrase Strand Transfer Inhibitor, Potently Inhibits Human T-Cell Lymphotropic Virus Type 1 Transmission in vitro

Frontiers in Medicine, 2022
Human T-cell lymphotropic virus type 1 (HTLV-1) is a deltaretrovirus most prevalent in southwestern Japan, sub-Saharan Africa, Australia, South America, and the Caribbean. Latest figures approximate 10 million people worldwide to be infected with HTLV-1.
Bethany S. Schneiderman, Michal S. Barski, Goedele N. Maertens   +2 more
doaj   +1 more source

A year-long extended release nanoformulated cabotegravir prodrug

Nature Materials, 2020
Long-acting cabotegravir (CAB) extends antiretroviral drug administration from daily to monthly. However, dosing volumes, injection site reactions and health-care oversight are obstacles towards a broad usage. The creation of poloxamer-coated hydrophobic and lipophilic CAB prodrugs with controlled hydrolysis and tissue penetrance can overcome these ...
Tanmay A. Kulkarni, Aditya N. Bade, Brady Sillman, Bhagya Laxmi Dyavar Shetty, Melinda S. Wojtkiewicz, Nagsen Gautam, James R. Hilaire, Sruthi Sravanam, Adam Szlachetka, Benjamin G. Lamberty, Brenda M. Morsey, Howard S. Fox, Yazen Alnouti, JoEllyn M. McMillan, R. Lee Mosley, Jane Meza, Paul L. Domanico, Tai-Yuen Yue, Gary Moore, Benson J. Edagwa, Howard E. Gendelman   +20 more
openaire   +3 more sources

Real-world trough concentrations and effectiveness of long-acting cabotegravir and rilpivirine: a multicenter prospective observational study in SwitzerlandResearch in context

The Lancet Regional Health. Europe
Summary: Background: The efficacy and tolerability of long-acting cabotegravir and rilpivirine were demonstrated in Phase III trials. However, low concentrations combined with other risk factors have been associated with an increased risk of virologic ...
Paul Thoueille, Susana Alves Saldanha, Fabian Schaller, Eva Choong, Aline Munting, Matthias Cavassini, Dominique Braun, Huldrych F. Günthard, Katharina Kusejko, Bernard Surial, Hansjakob Furrer, Andri Rauch, Mathieu Rougemont, Pilar Ustero, Alexandra Calmy, Marcel Stöckle, Catia Marzolini, Caroline Di Benedetto, Enos Bernasconi, Patrick Schmid, Rein Jan Piso, Pascal Andre, François R. Girardin, Monia Guidi, Thierry Buclin, Laurent A. Decosterd   +25 more
doaj   +1 more source

Mechanistic Basis of Cabotegravir–Glucuronide Disposition in Humans [PDF]

The Journal of Pharmacology and Experimental Therapeutics, 2019
Cabotegravir, a novel integrase inhibitor under development for treatment and prevention of HIV, is primarily metabolized by UDP-glucuronosyltransferase (UGT)1A1 and UGT1A9 to a direct ether glucuronide metabolite. The aim of these studies was to elucidate the mechanistic basis of cabotegravir-glucuronide disposition in humans.
Mitesh, Patel, H Christian, Eberl, Andrea, Wolf, Esaie, Pierre, Joseph W, Polli, Maciej J, Zamek-Gliszczynski   +5 more
openaire   +2 more sources

Perinatal and early infant outcomes after first‐versus second‐generation integrase strand transfer inhibitor use in pregnancy

HIV Medicine, EarlyView.
Abstract Introduction Integrase strand transfer inhibitors (INSTIs) are first‐line antiretroviral medications used in pregnancy. Pre‐clinical research suggests adverse effects in human stem cells associated with second‐ versus first‐generation INSTIs.
Rosa Balleny, Jeffrey Man Hay Wong, Terry Lee, Ari Bitnun, Isabelle Boucoiran, Jason Brophy, Jeannette Comeau, Fatima Kakkar, Athena McConnell, Laura Sauvé, Joel Singer, Alena Tse‐Chang, Deborah Money   +12 more
wiley   +1 more source

Efficacy of dolutegravir/lamivudine in adults with HIV‐1 and isolated reactive hepatitis B core antibody: Insights from Phase 3/3b study results

HIV Medicine, EarlyView.
Abstract Objectives As two‐drug HIV‐1 antiretroviral therapy (ART) regimens become standard, data gaps remain concerning their safety and efficacy among people with isolated reactive hepatitis B core antibodies (anti‐HBc). Here, we assessed the safety and efficacy of dolutegravir/lamivudine (DTG/3TC) versus three‐ or four‐drug regimens (3DRs/4DRs ...
D. Fox, J. Slim, E. T. Overton, A. Doblado‐Maldonado, P. Jeffery, R. A. Grove, S. D. Advani, R. Borsi, C. M. Parry, M. Underwood, B. Jones   +10 more
wiley   +1 more source