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https://www.readbyqxmd.com/read/27931507/hiv-non-nucleoside-reverse-transcriptase-inhibitor-efavirenz-reduces-neural-stem-cell-proliferation-in-vitro-and-in-vivo
#1
Jingji Jin, Bethany Grimmig, James Izzo, Lecia A M Brown, Charles Hudson, Adam J Smith, Jun Tan, Paula C Bickford, Brian Giunta
The prevalence of HIV-associated neurocognitive disorders (HAND) remains high despite combination antiretroviral therapy (cART). There is evidence that neural stem cells (NSCs) can migrate to sites of brain injury such as those caused by inflammation and oxidative stress, which are pathological features of HAND. Thus, reductions in NSCs may contribute to HAND pathogenesis. Since the HIV non-nucleoside reverse transcriptase inhibitor efavirenz (EFV) has previously been associated with cognitive deficits and promotion of oxidative stress pathways, we examined its effect on NSCs in vitro as well as in C57BL/6J mice...
November 2016: Cell Transplantation
https://www.readbyqxmd.com/read/27928647/triple-drug-combination-of-zidovudine-efavirenz-and-lamivudine-loaded-lactoferrin-nanoparticles-an-effective-nano-first-line-regimen-for-hiv-therapy
#2
Prashant Kumar, Yeruva Samrajya Lakshmi, Anand K Kondapi
PURPOSE: To enhance efficacy, bioavailability and reduce toxicity of first-line highly active anti-retroviral regimen, zidovudine + efavirenz + lamivudine loaded lactoferrin nanoparticles were prepared (FLART-NP) and characterized for physicochemical properties, bioactivity and pharmacokinetic profile. METHODS: Nanoparticles were prepared using sol-oil protocol and characterized using different sources such as FE-SEM, AFM, NanoSight, and FT-IR. In-vitro and in-vivo studies have been done to access the encapsulation-efficiency, cellular localization, release kinetics, safety analysis, biodistribution and pharmacokinetics...
December 7, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27928077/prevention-of-early-mortality-by-presumptive-tuberculosis-therapy-study-an-open-label-randomized-controlled-trial
#3
Yukari C Manabe, William Worodria, Frank van Leth, Harriet Mayanja-Kizza, Afsatou Ndama Traore, Josefo Ferro, Nadine Pakker, Matthias Frank, Martin P Grobusch, Robert Colebunders, Frank Cobelens
Early mortality after initiation of antiretroviral therapy (ART) occurs in 9-39% of patients in sub-Saharan Africa. A significant proportion of deaths are attributable to tuberculosis (TB). Low baseline CD4 T-cell count and low body mass index (BMI) are strongly associated with early mortality. We hypothesized that initiation of ART concurrent with presumptive anti-TB chemotherapy in high-risk patients would reduce mortality within the first 6 months by treating unrecognized TB. From October 2011 to December 2012, ART-naive, smear-negative participants with a CD4 T-cell count < 50 cells/μL and BMI < 18 kg/m(2) were randomly assigned to undergo either empiric four-drug anti-TB treatment followed 2 weeks later by efavirenz-based ART (N = 23) (ART + TB) or ART only (N = 20)...
December 7, 2016: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/27927852/frequency-of-viremic-episodes-in-hiv-infected-women-initiating-antiretroviral-therapy-during-pregnancy-a-cohort-study
#4
Landon Myer, Lorna Dunning, Maia Lesosky, Nei-Yuan Hsiao, Tamsin Phillips, Greg Petro, Allison Zerbe, James A McIntyre, Elaine J Abrams
BACKGROUND: The numbers of HIV-infected women initiating antiretroviral therapy (ART) in pregnancy are increasing rapidly with global policy changes. There are widespread concerns about ART adherence during pregnancy and postpartum but few data on viral suppression (VS) over time in these populations. METHODS: We followed a cohort of 523 women in Cape Town, South Africa initiating ART in pregnancy (once daily tenofovir 300mg, emtracitabine 200mg and efavirenz 600mg) and achieving VS (<50 copies/mL)...
December 7, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27926505/antitumor-effect-of-combination-of-the-inhibitors-of-two-new-oncotargets-proton-pumps-and-reverse-transcriptase
#5
Luana Lugini, Ilaria Sciamanna, Cristina Federici, Elisabetta Iessi, Enrico Pierluigi Spugnini, Stefano Fais
Tumor therapy needs new approaches in order to improve efficacy and reduce toxicity of the current treatments. The acidic microenvironment and the expression of high levels of endogenous non-telomerase reverse transcriptase (RT) are common features of malignant tumor cells. The anti-acidic proton pump inhibitor Lansoprazole (LAN) and the non-nucleoside RT inhibitor Efavirenz (EFV) have shown independent antitumor efficacy. LAN has shown to counteract drug tumor resistance. We tested the hypothesis that combination of LAN and EFV may improve the overall antitumor effects...
December 3, 2016: Oncotarget
https://www.readbyqxmd.com/read/27917125/comparison-of-liver-cell-models-using-the-basel-phenotyping-cocktail
#6
Benjamin Berger, Massimiliano Donzelli, Swarna Maseneni, Franziska Boess, Adrian Roth, Stephan Krähenbühl, Manuel Haschke
Currently used hepatocyte cell systems for in vitro assessment of drug metabolism include hepatoma cell lines and primary human hepatocyte (PHH) cultures. We investigated the suitability of the validated in vivo Basel phenotyping cocktail (caffeine [CYP1A2], efavirenz [CYP2B6], losartan [CYP2C9], omeprazole [CYP2C19], metoprolol [CYP2D6], midazolam [CYP3A4]) in vitro and characterized four hepatocyte cell systems (HepG2 cells, HepaRG cells, and primary cryopreserved human hepatocytes in 2-dimensional [2D] culture or in 3D-spheroid co-culture) regarding basal metabolism and CYP inducibility...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27914856/occult-hiv-1-drug-resistance-to-thymidine-analogues-following-failure-of-first-line-tenofovir-combined-with-a-cytosine-analogue-and-nevirapine-or-efavirenz-in-sub-saharan-africa-a-retrospective-multi-centre-cohort-study
#7
John Gregson, Pontiano Kaleebu, Vincent C Marconi, Cloete van Vuuren, Nicaise Ndembi, Raph L Hamers, Phyllis Kanki, Christopher J Hoffmann, Shahin Lockman, Deenan Pillay, Tulio de Oliveira, Nathan Clumeck, Gillian Hunt, Bernhard Kerschberger, Robert W Shafer, Chunfu Yang, Elliot Raizes, Rami Kantor, Ravindra K Gupta
BACKGROUND: HIV-1 drug resistance to older thymidine analogue nucleoside reverse transcriptase inhibitor drugs has been identified in sub-Saharan Africa in patients with virological failure of first-line combination antiretroviral therapy (ART) containing the modern nucleoside reverse transcriptase inhibitor tenofovir. We aimed to investigate the prevalence and correlates of thymidine analogue mutations (TAM) in patients with virological failure of first-line tenofovir-containing ART...
November 30, 2016: Lancet Infectious Diseases
https://www.readbyqxmd.com/read/27906030/cases-of-antiretroviral-associated-gynaecomastia-reported-to-the-national-hiv-tuberculosis-health-care-worker-hotline-in-south-africa
#8
Christine Njuguna, Annoesjka Swart, Marc Blockman, Gary Maartens, Briony Chisholm, Annemie Stewart, Anri Uys, Karen Cohen
BACKGROUND: Gynaecomastia is associated with exposure to antiretroviral therapy (ART), in particular efavirenz. There is limited data on clinical characteristics of patients with ART-associated gynaecomastia in resource-limited settings and little guidance on the optimal management of this adverse drug reaction (ADR). We describe the clinical characteristics, management and outcomes of gynaecomastia cases reported to the National HIV & Tuberculosis Health Care Worker Hotline in South Africa...
November 16, 2016: AIDS Research and Therapy
https://www.readbyqxmd.com/read/27906006/integrated-therapy-for-hiv-and-tuberculosis
#9
REVIEW
Weerawat Manosuthi, Surasak Wiboonchutikul, Somnuek Sungkanuparph
Tuberculosis (TB) has been the most common opportunistic infection and cause of mortality among HIV-infected patients, especially in resource-limited countries. Clinical manifestations of TB vary and depend on the degree of immunodeficiency. Sputum microscopy and culture with drug-susceptibility testing are recommended as a standard method for diagnosing active TB. TB-related mortality in HIV-infected patients is high especially during the first few months of treatment. Integrated therapy of both HIV and TB is feasible and efficient to control the diseases and yield better survival...
May 12, 2016: AIDS Research and Therapy
https://www.readbyqxmd.com/read/27905999/factors-associated-with-hiv-viral-load-blips-and-the-relationship-between-self-reported-adherence-and-efavirenz-blood-levels-on-blip-occurrence-a-case-control-study
#10
Aaron Farmer, Xun Wang, Anuradha Ganesan, Robert G Deiss, Brian K Agan, Thomas A O'Bryan, Kevin Akers, Jason F Okulicz
BACKGROUND: The uncertain etiology of HIV viral load (VL) blips may lead to increased use of clinical resources. We evaluated the association of self-reported adherence (SRA) and antiretroviral (ART) drug levels on blip occurrence in US Military HIV Natural History Study (NHS) participants who initiated the single-tablet regimen efavirenz/emtricitabine/tenofovir disoproxil fumarate (EFV/FTC/TDF). METHODS: ART-naïve NHS participants started on EFV/FTC/TDF between 2006 and 2013 who achieved VL suppression (<50 copies/mL) within 12 months and had available SRA and stored plasma samples were included...
March 22, 2016: AIDS Research and Therapy
https://www.readbyqxmd.com/read/27903949/possible-drug-herb-interaction-between-herbal-supplement-containing-horsetail-equisetum-arvense-and-antiretroviral-drugs-report-of-2-cases
#11
Ezequiel Cordova, Laura Morganti, Claudia Rodriguez
The use of alternative medicines, including herbs, is common among HIV-positive patients, even in those on antiretroviral treatment. Equisetum arvense, known as "horsetail," is mainly used for its diuretic properties. There are limited data about the pharmacological properties of this compound and the potential drug-herb interactions. The authors report 2 cases in which a possible drug-herb interaction may have led to virological breakthrough in patients who were maintained on the same regimen for many years, including lamivudine (3TC)/zidovudine (ZDV)/efavirenz (EFV) and emtricitabine (FTC)/tenofovir (TDF)/EFV, respectively...
November 30, 2016: Journal of the International Association of Providers of AIDS Care
https://www.readbyqxmd.com/read/27895013/frequent-cross-resistance-to-dapivirine-in-hiv-1-subtype-c-infected-individuals-on-failing-first-line-antiretroviral-therapy-in-south-africa
#12
Kerri J Penrose, Carole L Wallis, Chanson J Brumme, Kristen A Hamanishi, Kelley C Gordon, Raquel V Viana, P Richard Harrigan, John W Mellors, Urvi M Parikh
BACKGROUND: A vaginal ring containing dapivirine (DPV) has shown moderate protective efficacy against HIV-1 acquisition, but the activity of DPV against efavirenz (EFV)- and nevirapine (NVP)-resistant viruses that could be transmitted is not well-defined. We investigated DPV cross-resistance of subtype C HIV-1 from individuals on failing NVP- or EFV-containing antiretroviral therapy (ART) in South Africa (SA). METHODS: Plasma samples were obtained from individuals with >10,000 copies/mL HIV RNA and with HIV-1 containing at least one non-nucleoside reverse transcriptase (NNRTI) mutation...
November 28, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27891161/cases-of-antiretroviral-associated-gynaecomastia-reported-to-the-national-hiv-tuberculosis-health-care-worker-hotline-in-south-africa
#13
Christine Njuguna, Annoesjka Swart, Marc Blockman, Gary Maartens, Briony Chisholm, Annemie Stewart, Anri Uys, Karen Cohen
BACKGROUND: Gynaecomastia is associated with exposure to antiretroviral therapy (ART), in particular efavirenz. There is limited data on clinical characteristics of patients with ART-associated gynaecomastia in resource-limited settings and little guidance on the optimal management of this adverse drug reaction (ADR). We describe the clinical characteristics, management and outcomes of gynaecomastia cases reported to the National HIV & Tuberculosis Health Care Worker Hotline in South Africa...
2016: AIDS Research and Therapy
https://www.readbyqxmd.com/read/27879556/who-gets-severe-gynecomastia-among-hiv-infected-children-in-the-uk-and-ireland
#14
Julia Kenny, Katja Doerholt, Di M Gibb, Ali Judd
There are few data on gynecomastia in HIV-infected children. Within the UK/Ireland's national cohort, 56/1,873 (3%) HIV-infected children had gynecomastia, of which 10 (0.5%) were severe. All 10 had received antiretroviral therapy for a median of 27.5 [21,42] months; 4/10 had received efavirenz, 7/10 and 6/10 stavudine and/or didanosine respectively. Five were non-reversible, despite changing ART, and required breast reduction surgery.
November 22, 2016: Pediatric Infectious Disease Journal
https://www.readbyqxmd.com/read/27878300/induction-of-dna-damage-and-apoptosis-in-human-leukemia-cells-by-efavirenz
#15
Ansgar Brüning, Julia Jückstock, Bernd Kost, Panagiotis Tsikouras, Tobias Weissenbacher, Sven Mahner, Ioannis Mylonas
As part of the efforts to drug repurposing, some HIV drugs have recently been identified to exert anticancer effects. Selected nucleoside analogues of nucleosidic reverse-transcriptase inhibitors (NRTIs) have been shown to interfere with RNA transcription of HI viruses as well as with the replication of DNA in cancer cells. Non-nucleosidic reverse transcriptase inhibitors (NNRTIs) are believed to have less effects on human DNA replication and, thus, on cancer cell proliferation. Assessment of the effect of the NNRTI efavirenz in human cancer cells, however, revealed a high sensitivity of leukemia cells to this agent at pharmacologically relevant concentrations of less than 10 µg/ml...
November 15, 2016: Oncology Reports
https://www.readbyqxmd.com/read/27875362/relationship-between-hiv-infection-antiretroviral-therapy-inflammatory-markers-and-cerebrovascular-endothelial-function-among-adults-in-urban-china
#16
Felicia C Chow, Yanling Li, Yinghuan Hu, Joy Chan, Huanling Wang, Weihai Xu, Richard W Price, Farzaneh A Sorond, Taisheng Li
BACKGROUND: Cerebrovascular risk is increased in people living with HIV infection compared with age-matched uninfected individuals. Cerebrovascular endothelial dysfunction related to antiretroviral therapy and inflammation may contribute to higher stroke risk in HIV infection. METHODS: We compared cerebral vasoreactivity-a measure of cerebrovascular endothelial function assessed by the breath holding index (BHI) using transcranial Doppler ultrasound-between virologically suppressed Chinese HIV-infected individuals followed in an HIV clinic in Beijing, China and uninfected controls...
November 21, 2016: Journal of Acquired Immune Deficiency Syndromes: JAIDS
https://www.readbyqxmd.com/read/27872069/an-evaluation-of-doravirine-pharmacokinetics-when-switching-from-efavirenz-to-doravirine-in-healthy-subjects
#17
Ka Lai Yee, Rosa I Sanchez, Patrice Auger, Rachael Liu, Li Fan, Ilias Triantafyllou, Ming-Tain Lai, Mike Di Spirito, Marian Iwamoto, Sauzanne G Khalilieh
Doravirine is a novel, potent, human immunodeficiency virus-1 (HIV-1) non-nucleoside reverse transcriptase inhibitor (NNRTI) demonstrating a high genetic barrier to resistance and is well tolerated in studies to date. Doravirine is a candidate for patients switching from less-tolerated NNRTIs, such as efavirenz. While doravirine is a CYP3A4 substrate, efavirenz induces CYP3A4; therefore, the pharmacokinetics of both drugs following switching from efavirenz to doravirine were assessed.This was a 3-period, fixed-sequence, open-label study...
November 21, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27871359/focal-epithelial-hyperplasia-in-adult-patients-with-hiv-infection-clearance-with-topical-imiquimod
#18
Silvia Méndez-Flores, Lilly Esquivel-Pedraza, Amparo Hernández-Salazar, Yann Charli-Joseph, Marcela Saeb-Lima
Case 1 A 41-year-old man with human immunodeficiency virus (HIV) 1 diagnosed 16 years prior to his consultation was referred for an 8-month history of multiple painless lumps in his mouth. He had A2 status (CD4 cell count of 273 cells/mm(3) and viral load of 43,000 copies/L) and was taking treatment with lamivudine/zidovudine (combivir) and efavirenz. Physical examination showed multiple small mucosal-colored and lobulated papulonodules located in the palate and lower gingiva and a whitish verrucous plaque on the lower labial mucosa (Figure 1a)...
2016: Skinmed
https://www.readbyqxmd.com/read/27869478/etravirine-and-rilpivirine-drug-resistance-among-hiv-1-subtype-c-infected-children-failing-non-nucleoside-reverse-transcriptase-inhibitor-based-regimens-in-south-india
#19
Shanmugam Saravanan, Bagavathi Kausalya, Selvamurthi Gomathi, Sathasivam Sivamalar, Balakrishnan Pachamuthu, Selvamuthu Poongulali, Ambrose Pradeep, Solomon S Sunil, Sarvode N Mothi, Davey M Smith, Rami Kantor
We have analyzed reverse transcriptase (RT) region of HIV-1 pol gene from 97 HIV-infected children who were identified as failing first-line therapy that included a first generation non-nucleoside reverse transcriptase inhibitors (Nevirapine and Efavirenz) for at least 6 months. We found that 54% and 65% of the children had genotypically predicted resistance to second generation non-nucleoside reverse transcriptase inhibitors drugs Etravirine and Rilpivirine, respectively. These cross-resistance mutations may compromise future NNRTI based regimens, especially in resource-limited settings...
November 21, 2016: AIDS Research and Human Retroviruses
https://www.readbyqxmd.com/read/27860311/single-heteroatom-substitutions-in-the-efavirenz-oxazinone-ring-impact-metabolism-by-cyp2b6
#20
Philip M Cox, Namandjé N Bumpus
Previously, we observed that the oxazinone ring is important for cytochrome P450 2B6 (CYP2B6) activity toward efavirenz ((4S)-6-chloro-4-(2-cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one), a CYP2B6 substrate used to treat HIV. To further understand the structural characteristics of efavirenz that render it a CYP2B6 substrate, we tested the importance of each heteroatom of the oxazinone ring. We assembled a panel of five analogues: 6-chloro-4-(2-cyclopropylethynyl)-1,4-dihydro-2-methyl-4-(trifluoromethyl)-2H-3,1-benzoxazine (1), (4S)-6-chloro-4-[(1E)-2-cyclopropylethenyl]-3,4-dihydro-4-(trifluoromethyl)-2(1H)-quinazolinone (2), (4S)-6-chloro-4-(2-cyclopropylethynyl)-3,4-dihydro-4-(trifluoromethyl)-2(1H)-quinazolinone (3), 6-chloro-4-(cyclopropylethynyl)-3,4-dihydro-4-(trifluoromethyl)-2(1H)-quinolinone (4), and 6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-4H-benzo[d][1,3]dioxin-2-one (5)...
December 6, 2016: ChemMedChem
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