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https://www.readbyqxmd.com/read/28648081/in-silico-and-in-vitro-screening-for-p-glycoprotein-interaction-with-tenofovir-darunavir-and-dapivirine-an-anti-retroviral-drug-combination-for-topical-prevention-of-colorectal-hiv-transmission
#1
Magda Swedrowska, Shirin Jamshidi, Abhinav Kumar, Charles Kelly, K Miraz Rahman, Ben Forbes
The aim of the study was to use in-silico and in vitro techniques to evaluate whether a triple formulation of antiretroviral drugs (tenofovir, darunavir and dapivirine) interacted with p-glycoprotein (P-gp) or exhibited any other permeability-altering drug-drug interactions in the colorectal mucosa. Potential drug interactions with P-gp were screened initially using molecular docking, followed by molecular dynamics simulations to analyse the identified drug-transporter interaction more mechanistically. The transport of tenofovir, darunavir and dapivirine was investigated in the Caco-2 cells models and colorectal tissue and their apparent permeability coefficient (Papp), efflux ratio (ER) and the effect of transporter inhibitors were evaluated...
June 25, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28627229/cobicistat-versus-ritonavir-similar-pharmacokinetic-enhancers-but-some-important-differences
#2
Alice Tseng, Christine A Hughes, Janet Wu, Jason Seet, Elizabeth J Phillips
OBJECTIVE: To describe properties of cobicistat and ritonavir; compare boosting data with atazanavir, darunavir, and elvitegravir; and summarize antiretroviral and comedication interaction studies, with a focus on similarities and differences between ritonavir and cobicistat. Considerations when switching from one booster to another are discussed. DATA SOURCES: A literature search of MEDLINE was performed (1985 to April 2017) using the following search terms: cobicistat, ritonavir, pharmacokinetic, drug interactions, booster, pharmacokinetic enhancer, HIV, antiretrovirals...
June 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28616684/influence-of-ethanol-on-darunavir-hepatic-clearance-and-intracellular-pk-pd-in-hiv-infected-monocytes-and-cyp3a4-darunavir-interactions-using-inhibition-and-in-silico-binding-studies
#3
Narasimha M Midde, Yuqing Gong, Theodore J Cory, Junhao Li, Bernd Meibohm, Weihua Li, Santosh Kumar
PURPOSE: Although the prevalence of alcohol consumption is higher in HIV+ people than general public, limited information is available on how alcohol affects the metabolism and bioavailability of darunavir (DRV). METHODS: DRV was quantified by using LC-MS/MS method. All in vitro experiments were performed using human liver microsomes and HIV-infected monocytic cells. CYP3A4 and DRV/Ritonavir (RTV) docking was performed using GOLD suite 5.8. RESULTS: Ethanol (20 mM) significantly decreased apparent half-life and increased degradation rate constant of RTV-boosted DRV but not for DRV alone...
June 14, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28605418/should-we-be-testing-for-baseline-integrase-resistance-in-patients-newly-diagnosed-with-hiv
#4
Yiannis Koullias, Paul E Sax, Naomi F Fields, Rochelle P Walensky, Emily P Hyle
Background: Current guidelines recommend genotype resistance testing at diagnosis to guide initial selection of antiretroviral therapy (ART). Many standard resistance genotypes exclude testing for resistance to integrase inhibitors ("IR-testing"), although this class of drugs is a component of most recommended first-line regimens. Methods: We compared the 96-week clinical outcomes and cost-effectiveness of two strategies: no IR-testing vs. IR-testing performed at HIV diagnosis...
June 9, 2017: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/28595364/antiretroviral-unbound-concentration-during-pregnancy-piece-of-interest-in-the-puzzle
#5
D Metsu, P L Toutain, E Chatelut, P Delobel, P Gandia
Atazanavir and darunavir total concentrations (drug bound to plasma proteins plus unbound drug) progressively decrease during pregnancy. This pharmacokinetic variation leads physicians to recommend increasing doses. Conversely, the unbound concentration (Cu), i.e. the pharmacologically active form of the drug, remains unchanged. The explanation of this desynchronization lies in the fact that the clearance of the unbound form, corresponding to the intrinsic metabolic capacity of the hepatocytes, is the only factor driving Cu, and is constant during pregnancy...
June 7, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28590329/antiretroviral-initiation-is-associated-with-increased-skeletal-muscle-area-and-fat-content
#6
Kristine M Erlandson, Suzanne Fiorillo, Fadzai Masawi, Ann Scherzinger, Grace A McComsey, Jordan E Lake, James H Stein, Judith S Currier, Todd T Brown
OBJECTIVE: A greater burden of physical function impairment occurs in HIV-infected adults; the impact of antiretroviral therapy (ART) initiation on muscle density (less dense = more fat), a measure of muscle quality, is unknown. DESIGN: AIDS Clinical Trials Group Study A5260 s, a cardiometabolic substudy of A5257, randomized HIV-infected, ART-naïve adults to ritonavir-boosted atazanavir, darunavir, or raltegravir with tenofovir/emtricitabine backbone. Single-slice abdominal computed tomography (CT) scans from baseline and week 96 were reanalyzed for lean muscle area and density...
June 5, 2017: AIDS
https://www.readbyqxmd.com/read/28579016/executive-summary-of-the-gesida-national-aids-plan-consensus-document-on-antiretroviral-therapy-in-adults-infected-by-the-human-immunodeficiency-virus-updated-january-2017
#7
(no author information available yet)
Antiretroviral therapy (ART) is recommended for all patients infected by HIV-1. The objective of ART is to achieve an undetectable plasma viral load (PVL). Initial ART should be based on a combination of 3 drugs, including 2 nucleoside reverse transcriptase inhibitors (tenofovir in either of its two formulations plus emtricitabine or abacavir plus lamivudine) and another drug from a different family. Four of the recommended regimens, all of which have an integrase inhibitor as the third drug (dolutegravir, elvitegravir boosted with cobicistat or raltegravir), are considered preferential, whereas a further 3 regimens (based on elvitegravir/cobicistat, rilpivirine, or darunavir boosted with cobicistat or ritonavir) are considered alternatives...
May 31, 2017: Enfermedades Infecciosas y Microbiología Clínica
https://www.readbyqxmd.com/read/28575323/darunavir-concentrations-in-csf-of-hiv-infected-individuals-when-boosted-with-cobicistat-versus-ritonavir
#8
Hanni Bartels, Laurent Decosterd, Manuel Battegay, Catia Marzolini
Objectives: Cobicistat and ritonavir have different inhibitory profiles for drug transporters that could impact the distribution of co-administered drugs. We compared darunavir concentrations in CSF when boosted by cobicistat versus ritonavir relative to plasma concentrations and with WT HIV-1 IC 50 and IC 90 . Methods: An open, single-arm, sequential clinical trial (NCT02503462) where paired CSF and blood samples were taken from seven HIV-infected patients presenting with HIV-associated neurocognitive disorders (HAND) and treated with a darunavir/ritonavir (800/100 mg) once-daily regimen...
June 1, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28569994/physiologically-based-pharmacokinetic-modeling-for-predicting-the-effect-of-intrinsic-and-extrinsic-factors-on-darunavir-or-lopinavir-exposure-coadministered-with-ritonavir
#9
Christian Wagner, Ping Zhao, Vikram Arya, Charu Mullick, Kimberly Struble, Stanley Au
Management of comorbidities and medications is complex in HIV-1-infected patients. The overall objective of this project was to develop separate physiologically based pharmacokinetic (PBPK) substrate models for the protease inhibitors darunavir and lopinavir. These protease inhibitors are used in the treatment of HIV infection. Both darunavir and lopinavir are coadministered with another medication that inhibits cytochrome (CYP) 3A. The current project focused on PBPK modeling for darunavir and lopinavir coadministered with ritonavir...
June 1, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28566227/boosted-protease-inhibitor-monotherapy-versus-boosted-protease-inhibitor-plus-lamivudine-dual-therapy-as-second-line-maintenance-treatment-for-hiv-1-infected-patients-in-sub-saharan-africa-anrs12-286-mobidip-a-multicentre-randomised-parallel-open-label-superiority
#10
Laura Ciaffi, Sinata Koulla-Shiro, Adrien Bruno Sawadogo, Cheik Tidiane Ndour, Sabrina Eymard-Duvernay, Pretty Rosereine Mbouyap, Liliane Ayangma, Jacques Zoungrana, Ndeye Fatou Ngom Gueye, Mohamadou Diallo, Suzanne Izard, Guillaume Bado, Coumba Toure Kane, Avelin Fobang Aghokeng, Martine Peeters, Pierre Marie Girard, Vincent Le Moing, Jacques Reynes, Eric Delaporte
BACKGROUND: Despite satisfactory efficacy of WHO-recommended second-line antiretroviral treatment for patients with HIV in low-income countries, the need for simplified, low-cost, and less-toxic maintenance strategies remains high. We compared boosted protease inhibitor monotherapy with dual therapy with boosted protease inhibitor plus lamivudine in patients on second-line antiretrovial therapy (ART). METHODS: We did a multicentre, randomised, parallel, open-label, superiority, trial in the HIV services of five hospitals in sub-Saharan Africa (Yaoundé, Cameroon; Dakar, Senegal; and Bobo Dioulasso, Burkina Faso)...
May 26, 2017: Lancet HIV
https://www.readbyqxmd.com/read/28562771/facial-botryomycosis-like-pyoderma-in-an-hiv-infected-patient-remission-after-initiation-of-darunavir-and-raltegravir
#11
Walter de Araujo Eyer-Silva, Guilherme Almeida Rosa da Silva, Fernando Raphael de Almeida Ferry, Jorge Francisco da Cunha Pinto
Botryomycosis is an uncommon, chronic, suppurative, bacterial infection that primarily affects the skin and subcutaneous tissues. It has long been associated with defects of cellular immunity. We report a 28-year-old woman who presented with a chronic, ulcerated lesion with draining sinuses in the right malar region. Predisposing factors were HIV infection with poor immunological control, alcoholism, and a previous trauma to the right cheek. Several courses of antimicrobial therapy provided only partial and temporary remission...
March 2017: Revista da Sociedade Brasileira de Medicina Tropical
https://www.readbyqxmd.com/read/28556627/a-mathematical-model-to-predict-hiv-virological-failure-and-elucidate-the-role-of-lymph-node-drug-penetration
#12
S Sanche, N Sheehan, T Mesplède, M A Wainberg, J Li, F Nekka
Preventing virological failure following HIV treatment remains a difficult task that is further complicated by the emergence of drug resistance. We have developed a mathematical model able to explain and predict HIV virological outcomes for various compounds and patients' drug intake patterns. Compared to current approaches, this model considers, altogether, drug penetration into lymph nodes, a refined adherence representation accounting for the propensity for long drug holidays, population pharmacokinetic and pharmacodynamic variability, drug interaction, and crossresistance...
May 27, 2017: CPT: Pharmacometrics & Systems Pharmacology
https://www.readbyqxmd.com/read/28553123/the-hiv-protease-inhibitor-nelfinavir-as-a-novel-therapeutic-approach-for-the-treatment-of-refractory-pediatric-leukemia
#13
Vanessa Meier-Stephenson, Justin Riemer, Aru Narendran
PURPOSE: Refractory pediatric leukemia remains one of the leading causes of death in children. Intensification of current chemotherapy regimens to improve the outcome in these children is often limited by the effects of drug resistance and cumulative toxicity. Hence, the search for newer agents and novel therapeutic approaches are urgently needed to formulate the next-generation early-phase clinical trials for these patients. MATERIALS AND METHODS: A comprehensive library of antimicrobials, including eight HIV protease inhibitors (nelfinavir [NFV], saquinavir, indinavir, ritonavir, amprenavir, atazanavir, lopinavir, and darunavir), was tested against a panel of pediatric leukemia cells by in vitro growth inhibition studies...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28539755/practical-synthesis-of-the-bicyclic-darunavir-side-chain-3r-3as-6ar-hexahydrofuro-2-3-b-furan-3-ol-from-monopotassium-isocitrate
#14
REVIEW
Gary L Moore, Rodger W Stringham, David S Teager, Tai-Yuen Yue
A practical synthesis of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol-a key intermediate in the synthesis of darunavir-from monopotassium isocitrate is described. The isocitric acid salt, obtained from a high-yielding fermentation fed by sunflower oil, was converted in several steps to a tertiary amide. This amide, along with the compound's ester functionalities, was reduced with lithium aluminum hydride to give, on acidic workup, a transient aminal-triol. This was converted in situ to the title compound, the bicyclic acetal furofuranol side chain of darunavir, a protease inhibitor used in treatment of HIV/AIDS...
January 20, 2017: Organic Process Research & Development
https://www.readbyqxmd.com/read/28525359/i36t%C3%A2-t-mutation-in-south-african-subtype-c-c-sa-hiv-1-protease-significantly-alters-protease-drug-interactions
#15
Sibusiso B Maseko, Eden Padayachee, Thavendran Govender, Yasien Sayed, Gert Kruger, Glenn E M Maguire, Johnson Lin
The efficacy of HIV-1 protease inhibition therapies is often compromised by the emergence of mutations in the protease molecule that reduces the binding affinity of inhibitors while maintaining viable catalytic activity and affinity for natural substrates. In the present study, we used a recombinant HIV-1 C-SA protease and a recently reported variant for inhibition (Ki, IC50) and thermodynamic studies against nine clinically used inhibitors. This is the first time that binding free energies for C-SA PR and the mutant are reported...
May 19, 2017: Biological Chemistry
https://www.readbyqxmd.com/read/28522147/cardiovascular-risk-in-advanced-na%C3%A3-ve-hiv-infected-patients-starting-antiretroviral-therapy-comparison-of-three-different-regimens-prevaleat-ii-cohort
#16
Paolo Maggi, Chiara Bellacosa, Armando Leone, Anna Volpe, Elena Delfina Ricci, Nicoletta Ladisa, Stefania Cicalini, Elisabetta Grilli, Rosaria Viglietti, Antonio Chirianni, Lara Ines Bellazzi, Renato Maserati, Canio Martinelli, Paola Corsi, Benedetto Maurizio Celesia, Federica Sozio, Gioacchino Angarano
BACKGROUND AND AIMS: PREVALEAT (PREmature VAscular LEsions and Antiretroviral Therapy) II is a multicenter, longitudinal cohort study aimed at the evaluation of cardiovascular risk among advanced HIV-positive, treatment-naïve patients starting their first therapy. We hypothesized that these patients, present a higher cardiovascular (CV) risk. METHODS: The study included all consecutive naïve patients with less than 200 CD4 cells/ml starting antiretroviral therapy...
May 5, 2017: Atherosclerosis
https://www.readbyqxmd.com/read/28520611/treatment-outcomes-of-third-line-antiretroviral-regimens-in-hiv-infected-thai-adolescents
#17
Wasana Prasitsuebsai, Jiratchaya Sophonphan, Kulkanya Chokephaibulkit, Jurai Wongsawat, Suparat Kanjanavanit, Pope Kosalaraksa, Chaiwat Ngampiyakul, Pakarat Sangkla, Rawiwan Hansudewechakul, Stephen J Kerr, Thanyawee Puthanakit, Jintanat Ananworanich
BACKGROUND: Efficacy and safety data of third-line antiretroviral (ARV) regimens in adolescents are limited. METHODOLOGY: This study enrolled HIV-infected Thais who were treated with third-line regimens consisting of darunavir/ritonavir (DRV/r), etravirine (ETR), tipranavir/ritonavir (TPV/r) or raltegravir (RAL). RESULTS: Fifty-four adolescents 2-17 years of age were enrolled from 8 sites and followed for 48 weeks. Reasons for switch were second-line failure (n=44) and toxicity to second-line regimens (n=10)...
May 16, 2017: Pediatric Infectious Disease Journal
https://www.readbyqxmd.com/read/28520610/candidates-for-inclusion-in-a-universal-antiretroviral-regimen-dolutegravir
#18
Pedro Cahn
PURPOSE OF REVIEW: The review addresses the role of dolutegravir (DTG) in first-line therapy. In the era of test and treat, where United Nations AIDS Program and WHO have set the ambitious targets of 90/90/90, new efficacious, well tolerated, and simple therapeutic options are needed. RECENT FINDINGS: DTG has been tested in large clinical trials in treatment-naïve patients, showing noninferiority to raltegravir and superiority compared with efavirenz and ritonavir-boosted darunavir, respectively...
July 2017: Current Opinion in HIV and AIDS
https://www.readbyqxmd.com/read/28484975/a-clinical-cassette-dosing-study-for-evaluating-the-contribution-of-hepatic-oatps-and-cyp3a-to-drug-drug-interactions
#19
Takashi Yoshikado, Kazuya Maeda, Sawako Furihata, Hanano Terashima, Takeshi Nakayama, Keiko Ishigame, Kazunobu Tsunemoto, Hiroyuki Kusuhara, Ken-Ichi Furihata, Yuichi Sugiyama
PURPOSE: To demonstrate the relative importance of organic anion-transporting polypeptides (OATPs) and cytochrome P450 3A (CYP3A) in the hepatic elimination of substrate drugs. METHODS: A cocktail of subtherapeutic doses of bosentan, repaglinide, clarithromycin, darunavir, simeprevir, and midazolam (CYP3A probe) was administered orally to eight healthy volunteers. Rifampicin (OATP inhibitor; 600 mg, p.o.) and itraconazole (CYP3A inhibitor; 200 mg, i.v.) were coadministered with the cocktail in the second and third phases, respectively...
May 8, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28482097/once-daily-atazanavir-cobicistat-and-darunavir-cobicistat-exposure-over-72%C3%A2-h-post-dose-in-plasma-urine-and-saliva-contribution-to-drug-pharmacokinetic-knowledge
#20
Emilie R Elliot, Alieu Amara, Nicole Pagani, Laura Else, Graeme Moyle, Alex Schoolmeesters, Chris Higgs, Saye Khoo, Marta Boffito
No abstract text is available yet for this article.
May 6, 2017: Journal of Antimicrobial Chemotherapy
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