Base de dados : MEDLINE
Pesquisa : D02.626.809 [Categoria DeCS]
Referências encontradas : 244 [refinar]
Mostrando: 1 .. 10   no formato [Detalhado]

página 1 de 25 ir para página                         

  1 / 244 MEDLINE  
              next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29246084
[Au] Autor:Capetti AF; Cossu MV; Paladini L; Rizzardini G
[Ad] Endereço:a First Division of Infectious Diseases , ASST Fatebenefratelli-Sacco , Milano , Italy.
[Ti] Título:Dolutegravir plus rilpivirine dual therapy in treating HIV-1 infection.
[So] Source:Expert Opin Pharmacother;19(1):65-77, 2018 Jan.
[Is] ISSN:1744-7666
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: The HIV-infected population is aging and comorbidities and polypharmacological regimens are increasing. To reduce toxicity and drug burden researchers are evaluating the efficacy, safety and durability of dual therapies as a switch option in subjects who have achieved stable virologic suppression. Initially effective dual combinations relied on protease inhibitors but when dolutegravir, the first integrase inhibitor to display a high genetic barrier, became commercially available, many physicians began to use it in a variety of dual regimens, generating several observational cohorts. Areas covered: This review covers the most recent data from observational cohorts and randomized clinical trials concerning the switch to the dual combination of dolutegravir plus rilpivirine and the reasons that lead to consider this option. Also, viral failures, due to poor adherence or to other factors, and drug resistance are investigated. Articles which are searchable on MEDLINE/PubMed and from the main national/international congresses in the field of HIV therapy are reviewed. Expert opinion: The observation period for this regimen is getting longer and data showing its efficacy in maintaining HIV-1 RNA < 50 copies/mL are now consolidated. Metabolic data suggest some benefit in the lipid profile, improvement in bone mineral density and reduced bone reabsorption.
[Mh] Termos MeSH primário: Infecções por HIV/tratamento farmacológico
Compostos Heterocíclicos com 3 Anéis/administração & dosagem
Rilpivirina/administração & dosagem
[Mh] Termos MeSH secundário: Fármacos Anti-HIV/administração & dosagem
Fármacos Anti-HIV/uso terapêutico
Quimioterapia Combinada
HIV-1/efeitos dos fármacos
Seres Humanos
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anti-HIV Agents); 0 (Heterocyclic Compounds, 3-Ring); DKO1W9H7M1 (dolutegravir); FI96A8X663 (Rilpivirine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180306
[Lr] Data última revisão:
180306
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171217
[St] Status:MEDLINE
[do] DOI:10.1080/14656566.2017.1417984


  2 / 244 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29317618
[Au] Autor:Kirtane AR; Abouzid O; Minahan D; Bensel T; Hill AL; Selinger C; Bershteyn A; Craig M; Mo SS; Mazdiyasni H; Cleveland C; Rogner J; Lee YL; Booth L; Javid F; Wu SJ; Grant T; Bellinger AM; Nikolic B; Hayward A; Wood L; Eckhoff PA; Nowak MA; Langer R; Traverso G
[Ad] Endereço:Department of Chemical Engineering and David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA, 02139, USA.
[Ti] Título:Development of an oral once-weekly drug delivery system for HIV antiretroviral therapy.
[So] Source:Nat Commun;9(1):2, 2018 01 09.
[Is] ISSN:2041-1723
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The efficacy of antiretroviral therapy is significantly compromised by medication non-adherence. Long-acting enteral systems that can ease the burden of daily adherence have not yet been developed. Here we describe an oral dosage form composed of distinct drug-polymer matrices which achieved week-long systemic drug levels of the antiretrovirals dolutegravir, rilpivirine and cabotegravir in a pig. Simulations of viral dynamics and patient adherence patterns indicate that such systems would significantly reduce therapeutic failures and epidemiological modelling suggests that using such an intervention prophylactically could avert hundreds of thousands of new HIV cases. In sum, weekly administration of long-acting antiretrovirals via a novel oral dosage form is a promising intervention to help control the HIV epidemic worldwide.
[Mh] Termos MeSH primário: Fármacos Anti-HIV/administração & dosagem
Sistemas de Liberação de Medicamentos/métodos
Compostos Heterocíclicos com 3 Anéis/administração & dosagem
Piridonas/administração & dosagem
Rilpivirina/administração & dosagem
[Mh] Termos MeSH secundário: Administração Oral
Animais
Fármacos Anti-HIV/farmacocinética
Fármacos Anti-HIV/uso terapêutico
Avaliação Pré-Clínica de Medicamentos
Compostos Heterocíclicos com 3 Anéis/farmacocinética
Compostos Heterocíclicos com 3 Anéis/uso terapêutico
Seres Humanos
Modelos Teóricos
Cooperação do Paciente
Estudo de Prova de Conceito
Piridonas/farmacocinética
Piridonas/uso terapêutico
Rilpivirina/farmacocinética
Rilpivirina/uso terapêutico
Suínos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-HIV Agents); 0 (GSK1265744); 0 (Heterocyclic Compounds, 3-Ring); 0 (Pyridones); DKO1W9H7M1 (dolutegravir); FI96A8X663 (Rilpivirine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180111
[St] Status:MEDLINE
[do] DOI:10.1038/s41467-017-02294-6


  3 / 244 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29304154
[Au] Autor:Kerrigan D; Mantsios A; Gorgolas M; Montes ML; Pulido F; Brinson C; deVente J; Richmond GJ; Beckham SW; Hammond P; Margolis D; Murray M
[Ad] Endereço:Department of Health, Behavior & Society, Johns Hopkins University Bloomberg School of Public Health, Baltimore, Maryland, United States of America.
[Ti] Título:Experiences with long acting injectable ART: A qualitative study among PLHIV participating in a Phase II study of cabotegravir + rilpivirine (LATTE-2) in the United States and Spain.
[So] Source:PLoS One;13(1):e0190487, 2018.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Challenges with adherence to daily oral antiretroviral therapy (ART) among people living with HIV (PLHIV) have stimulated development of injectable long-acting (LA) regimens. We conducted 39 in-depth interviews with participants and providers in a Phase IIb study (LATTE-2) evaluating an injectable LA regimen in the U.S. and Spain. Interviews exploring participant and provider attitudes and experiences with LA versus oral ART were audiotaped, transcribed and analyzed using thematic content analysis. Participants described the convenience of LA injections versus daily pills and emotional benefits such as minimized potential for HIV disclosure and eliminating the "daily reminder of living with HIV." Providers recognized benefits but cautioned that LA candidates still need to adhere to clinic visits for injections and raised questions around ongoing clinical management. LA was seen as preferable to daily oral ART among PLHIV. Further research is needed regarding appropriate candidates, including with women and "non-adherent" populations across settings.
[Mh] Termos MeSH primário: Fármacos Anti-HIV/administração & dosagem
Infecções por HIV/tratamento farmacológico
Piridonas/uso terapêutico
Rilpivirina/uso terapêutico
[Mh] Termos MeSH secundário: Seres Humanos
Piridonas/administração & dosagem
Pesquisa Qualitativa
Rilpivirina/administração & dosagem
Espanha
Estados Unidos
[Pt] Tipo de publicação:CLINICAL TRIAL, PHASE II; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-HIV Agents); 0 (GSK1265744); 0 (Pyridones); FI96A8X663 (Rilpivirine)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180221
[Lr] Data última revisão:
180221
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180106
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0190487


  4 / 244 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28465101
[Au] Autor:Wei L; Wang HL; Huang L; Chen CH; Morris-Natschke SL; Lee KH; Xie L
[Ad] Endereço:Beijing Institute of Pharmacology & Toxicology, 27 Tai-Ping Road, Beijing 100850, China.
[Ti] Título:Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
[So] Source:Bioorg Med Chem Lett;27(12):2788-2792, 2017 06 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:On the basis of our prior structure-activity relationship (SAR) results, our current lead optimization of 1,5-diarylanilines (DAANs) focused on the 4-substituent (R ) on the central phenyl ring as a modifiable position related simultaneously to improved drug resistance profiles and drug-like properties. Newly synthesized p-cyanovinyl-DAANs (8a-8g) with different R side chains plus prior active p-cyanoethyl-DAANs (4a-4c) were evaluated not only for anti-HIV potency against both wild-type HIV virus and rilpivirine-resistant (E138K, E138K+M184I) viral replication, but also for multiple drug-like properties, including aqueous solubility, lipophilicity, and metabolic stability in human liver microsomes and human plasma. This study revealed that both ester and amide R substituents led to low nanomolar anti-HIV potency against wild-type and rilpivirine-resistant viral strains (E138K-resistance fold changes<3). The N-substituted amide-R side chains were superior to ester-R likely due to improved aqueous solubility, lipophilicity, and higher metabolic stability in vitro. Thus, three amide-DAANs 8e, 4a, and 4b were identified with high potency against wild-type and rilpivirine-resistant viral strains and multiple desirable drug-like properties.
[Mh] Termos MeSH primário: Compostos de Anilina/farmacologia
Fármacos Anti-HIV/farmacologia
Transcriptase Reversa do HIV/antagonistas & inibidores
HIV-1/efeitos dos fármacos
Inibidores da Transcriptase Reversa/farmacologia
Rilpivirina/farmacologia
[Mh] Termos MeSH secundário: Compostos de Anilina/síntese química
Compostos de Anilina/química
Fármacos Anti-HIV/química
Relação Dose-Resposta a Droga
Farmacorresistência Viral/efeitos dos fármacos
Transcriptase Reversa do HIV/metabolismo
HIV-1/genética
Testes de Sensibilidade Microbiana
Estrutura Molecular
Mutação
Inibidores da Transcriptase Reversa/síntese química
Inibidores da Transcriptase Reversa/química
Rilpivirina/química
Relação Estrutura-Atividade
Replicação Viral/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Aniline Compounds); 0 (Anti-HIV Agents); 0 (Reverse Transcriptase Inhibitors); EC 2.7.7.49 (HIV Reverse Transcriptase); FI96A8X663 (Rilpivirine)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:171124
[Lr] Data última revisão:
171124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170504
[St] Status:MEDLINE


  5 / 244 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28854832
[Au] Autor:Capetti AF; Astuti N; Cattaneo D; Rizzardini G
[Ad] Endereço:a 1st Division of Infectious Diseases , ASST Fatebenefratelli-Sacco , Milano , Italy.
[Ti] Título:Pharmacokinetic drug evaluation of dolutegravir plus rilpivirine for the treatment of HIV.
[So] Source:Expert Opin Drug Metab Toxicol;13(11):1183-1192, 2017 Nov.
[Is] ISSN:1744-7607
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: The search for simple, potent, metabolic-friendly and nucleoside/nucleotide sparing antiretroviral regimens has led clinical investigators to move steps towards dual therapies. Among these the association of rilpivirine and dolutegravir is emerging as a twin randomized clinical trial (SWORD1&2) and at least three observational cohort describe it as a safe and highly effective regimen for switch from other therapies Areas covered: We review the evidence supporting the use of dolutegravir plus rilpivirine for the treatment of HIV in virologically suppressed patients taking other antiretroviral regimens. The reasons for the switch in clinical practice may range from simplification to tolerability/toxicity issues, to the prevention of future metabolic damage, to predicted drug-drug interactions when treatment of HCV co-infection is planned. Articles searchable on MEDLINE/PubMed and from the main international congresses in the field of HIV therapy were reviewed to provide context for use of dolutegravir plus rilpivirine Expert opinion: This treatment is highly effective in maintaining HIV-1 RNA <50 copies/mL. Although the studies up to date requested patient to switch to drugs they had no experience of, a predictable 'radical change' effect did not impact negatively on the results. Further data from these studies may help elucidate the possible advantage in terms of safety and metabolic effect in the next few months.
[Mh] Termos MeSH primário: Fármacos Anti-HIV/administração & dosagem
Infecções por HIV/tratamento farmacológico
Compostos Heterocíclicos com 3 Anéis/administração & dosagem
Rilpivirina/administração & dosagem
[Mh] Termos MeSH secundário: Animais
Fármacos Anti-HIV/efeitos adversos
Fármacos Anti-HIV/farmacocinética
Interações Medicamentosas
Quimioterapia Combinada
HIV-1/efeitos dos fármacos
Compostos Heterocíclicos com 3 Anéis/efeitos adversos
Compostos Heterocíclicos com 3 Anéis/farmacocinética
Seres Humanos
Ensaios Clínicos Controlados Aleatórios como Assunto
Rilpivirina/efeitos adversos
Rilpivirina/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anti-HIV Agents); 0 (Heterocyclic Compounds, 3-Ring); DKO1W9H7M1 (dolutegravir); FI96A8X663 (Rilpivirine)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171108
[Lr] Data última revisão:
171108
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170901
[St] Status:MEDLINE
[do] DOI:10.1080/17425255.2017.1361929


  6 / 244 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28845699
[Au] Autor:Zainuddin R; Zaheer Z; Sangshetti JN; Momin M
[Ad] Endereço:a Depatment of Quality Assurance, Y.B. Chavan College of Pharmacy , Dr. Rafiq Zakaria Campus , Aurangabad , India.
[Ti] Título:Enhancement of oral bioavailability of anti-HIV drug rilpivirine HCl through nanosponge formulation .
[So] Source:Drug Dev Ind Pharm;43(12):2076-2084, 2017 Dec.
[Is] ISSN:1520-5762
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: To synthesize ß cyclodextrin nanosponges using a novel and efficient microwave mediated method for enhancing bioavailability of Rilpivirine HCl (RLP). SIGNIFICANCE: Belonging to BCS class II RLP has pH dependent solubility and poor oral bioavailability. However, a fatty meal enhances its absorption hence the therapy indicates that the dosage form be consumed with a meal. But then it becomes tedious and inconvenient to continue the therapy for years with having to face the associated gastric side effects such as nausea. METHOD: Microwave synthesizer was used to mediate the poly-condensation reaction between ß-cyclodextrin and cross-linker diphenylcarbonate. Critical parameters selected were polymer to cross-linker ratio, Watt power, reaction time and solvent volume. Characterization studies were performed using FTIR, DSC, SEM, H-NMR and PXRD. Molecular modeling was applied to confirm the possibility of drug entrapment. In vitro drug dissolution followed by oral bioavailability studies was performed in Sprawley rats. Samples were analyzed using HPLC. RESULTS: Microwave synthesis yields para-crystalline, porous nanosponges (∼205 nm). Drug entrapment led to enhancement of solubility and a two-fold increase in drug dissolution (P < 0.001) following Higuchi release model. Enhanced oral bioavailability was observed in fasted Sprawley rats where C and AUC increases significantly (C of NS∼ 586 ± 5.91 ng/mL; plain RLP ∼310 ± 5. 74 ng/mL). CONCLUSION: The approach offers a comfortable dosing zone for AIDs patients, negating the requirement of consuming the formulation in a fed state due to enhancement in drugs' oral bioavailability.
[Mh] Termos MeSH primário: Fármacos Anti-HIV/administração & dosagem
Fármacos Anti-HIV/farmacologia
Polímeros/química
Rilpivirina/administração & dosagem
Rilpivirina/farmacologia
beta-Ciclodextrinas/química
[Mh] Termos MeSH secundário: Animais
Fármacos Anti-HIV/metabolismo
Disponibilidade Biológica
Varredura Diferencial de Calorimetria
Química Farmacêutica
Ratos
Rilpivirina/química
Solubilidade
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-HIV Agents); 0 (Polymers); 0 (beta-Cyclodextrins); FI96A8X663 (Rilpivirine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171018
[Lr] Data última revisão:
171018
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170829
[St] Status:MEDLINE
[do] DOI:10.1080/03639045.2017.1371732


  7 / 244 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28683720
[Au] Autor:Sculier D; Gayet-Ageron A; Battegay M; Cavassini M; Fehr J; Hirzel C; Schmid P; Bernasconi E; Calmy A; Swiss HIV Cohort Study
[Ad] Endereço:Division of Infectious Diseases, University Hospital Geneva, Geneva, Switzerland. delphine.sculier@hcuge.ch.
[Ti] Título:Rilpivirine use in the Swiss HIV cohort study: a prospective cohort study.
[So] Source:BMC Infect Dis;17(1):476, 2017 Jul 06.
[Is] ISSN:1471-2334
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Rilpivirine is safe and effective in HIV-naïve patients with low baseline HIV-RNA or in switch strategy. It offers the advantages of few drug-drug interactions and a favourable toxicity profile. We aimed to determine the reasons for prescribing the rilpivirine (RPV)/tenofovir disoproxil (TDF)/emtricitabine (FTC) co-formulation within the Swiss HIV Cohort Study and to assess its effectiveness and safety over a 24 months period. METHODS: All individuals enrolled in the Swiss HIV Cohort Study who initiated a RPV/TDF/FTC co-formulation between April 2013 and March 2014 were included. Primary outcomes were the HIV-RNA viral load (copies/mL) and CD4 cell count (cells/mm ) at 6, 12 and 24 months. Reasons for a switch to RPV/TDF/FTC were evaluated through a standardized questionnaire. We also assessed discontinuation and reasons for discontinuation of RPV/TDF/FTC until October 30, 2015. RESULTS: Of 644 individuals who started the RPV/TDF/FTC co-formulation, only 7.5% were treatment-naïve. At 24 months, viral suppression (HIV-RNA <50 copies/mL) was achieved in 100% and 96.7% of cART-naïve and cART-experienced patients respectively. The switch to RPV was mainly done for simplification (44.6%) and to overcome central nervous system toxicity symptoms due to efavirenz (24%). Six months after switch, 74.8% of patients reported an improvement of psycho-neurological symptoms with continued improvement at 12 months for almost 80%. However, one quarter of patients reported a discontinuation of RPV/TDF/FTC on October 30, 2015 after a median time of 18.4 months. Reasons for discontinuation included physician decision (5.3%) and side-effects (3.9%) mainly related to the central nervous system and to renal toxicity. CONCLUSION: The RPV/TDF/FTC co-formulation was safe and effective throughout 24 months of follow-up but barely prescribed for HIV-naïve patients. Despite excellent virological suppression among both treatment-naïve and -experienced patients, we observed a high rate of treatment discontinuation.
[Mh] Termos MeSH primário: Fármacos Anti-HIV/uso terapêutico
Emtricitabina/uso terapêutico
Infecções por HIV/tratamento farmacológico
Rilpivirina/uso terapêutico
Tenofovir/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Terapia Antirretroviral de Alta Atividade/métodos
Benzoxazinas/efeitos adversos
Contagem de Linfócito CD4
Combinação de Medicamentos
Feminino
HIV-1/genética
Seres Humanos
Masculino
Meia-Idade
Estudos Prospectivos
Resultado do Tratamento
Carga Viral
[Pt] Tipo de publicação:CLINICAL TRIAL; JOURNAL ARTICLE; MULTICENTER STUDY
[Nm] Nome de substância:
0 (Anti-HIV Agents); 0 (Benzoxazines); 0 (Drug Combinations); 99YXE507IL (Tenofovir); FI96A8X663 (Rilpivirine); G70B4ETF4S (Emtricitabine); JE6H2O27P8 (efavirenz)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171010
[Lr] Data última revisão:
171010
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170708
[St] Status:MEDLINE
[do] DOI:10.1186/s12879-017-2579-2


  8 / 244 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28408657
[Au] Autor:Sharma D; Turkistani AA; Chang W; Hu C; Xu Z; Chang TKH
[Ad] Endereço:Faculty of Pharmaceutical Sciences, (D.S., A.A.T., C.H., T.K.H.C.), and Food, Nutrition, and Health Program, Faculty of Land and Food Systems (W.C., Z.X.), The University of British Columbia, Vancouver, British Columbia, Canada.
[Ti] Título:Negative Regulation of Human Pregnane X Receptor by MicroRNA-18a-5p: Evidence for Suppression of MicroRNA-18a-5p Expression by Rifampin and Rilpivirine.
[So] Source:Mol Pharmacol;92(1):48-56, 2017 Jul.
[Is] ISSN:1521-0111
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Small noncoding microRNAs act as post-transcriptional regulators of gene expression involved in diverse biologic functions. Pregnane X receptor (PXR, NR1I2), a member of the superfamily of nuclear receptors, is a transcription factor governing the transport and biotransformation of various drugs and other chemicals. In the present study, we identified a specific microRNA (miR) involved in regulating the expression and functionality of human PXR (hPXR). According to bioinformatics analysis employing three commonly used algorithms (TargetScan, miRanda, and DIANA-microT-CDS), miR-18a-5p was predicted to be the top candidate microRNA regulator of hPXR. Consequently, this microRNA was selected for detailed experimental investigation. As shown in cell-based dual-luciferase reporter gene assays, functional interaction occurred between miR-18a-5p and the microRNA recognition element of miR-18a-5p in the 3'-untranslated region of hPXR mRNA. Transfection of LS180 human colorectal adenocarcinoma cells with an miR-18a-5p mimic decreased hPXR mRNA and protein expression, whereas transfection of LS180 cells with an miR-18a-5p inhibitor increased hPXR mRNA and protein expression. The decrease in hPXR expression by the miR-18a-5p mimic was associated with a reduction in the extent of hPXR target gene ( ) induction by rifampin and rilpivirine. Treatment of untransfected LS180 cells with either of these hPXR agonists decreased endogenous expression of miR-18a-5p, and this preceded the onset of induction. In conclusion, miR-18a-5p is a negative regulator of hPXR expression and the hPXR agonists rifampin and rilpivirine are chemical suppressors of miR-18a-5p expression.
[Mh] Termos MeSH primário: MicroRNAs/antagonistas & inibidores
MicroRNAs/biossíntese
Receptores de Esteroides/antagonistas & inibidores
Receptores de Esteroides/biossíntese
Rifampina/farmacologia
Rilpivirina/farmacologia
[Mh] Termos MeSH secundário: Linhagem Celular Tumoral
Relação Dose-Resposta a Droga
Expressão Gênica
Seres Humanos
Luciferases de Renilla
MicroRNAs/genética
Receptores de Esteroides/agonistas
Inibidores da Transcriptase Reversa/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (MIRN18A microRNA, human); 0 (MicroRNAs); 0 (Receptors, Steroid); 0 (Reverse Transcriptase Inhibitors); 0 (pregnane X receptor); EC 1.13.12.5 (Luciferases, Renilla); FI96A8X663 (Rilpivirine); VJT6J7R4TR (Rifampin)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170614
[Lr] Data última revisão:
170614
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170415
[St] Status:MEDLINE
[do] DOI:10.1124/mol.116.107003


  9 / 244 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28303548
[Au] Autor:Nyaku AN; Kelly SG; Taiwo BO
[Ad] Endereço:Division of Infectious Diseases, Department of Medicine, Rutgers-New Jersey Medical School, Newark, NJ, USA.
[Ti] Título:Long-Acting Antiretrovirals: Where Are We now?
[So] Source:Curr HIV/AIDS Rep;14(2):63-71, 2017 Apr.
[Is] ISSN:1548-3576
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PURPOSE OF REVIEW: Current HIV treatment options require daily use of combination antiretroviral drugs. Many persons living with HIV experience treatment fatigue and suboptimal adherence as a result. Long-acting antiretroviral drugs are being developed to expand options for HIV treatment. Here, we review the agents in development, and evaluate data from recent clinical trials. In addition, we anticipate challenges to successful widespread use of long-acting antiretrovirals. RECENT FINDINGS: Parenteral nanosuspensions of cabotegravir and rilpivirine, and dapivirine vaginal ring are the farthest in clinical development. Long-acting modalities in earlier development stages employ drug-loaded implants, microparticles, or targeted mutagenesis, among other innovations. Long-acting antiretroviral drugs promise new options for HIV prevention and treatment, and ways to address poor adherence and treatment fatigue. Further studies will identify the long-acting agents or combinations that are suitable for routine use. Creative solutions will be needed for anticipated implementation challenges.
[Mh] Termos MeSH primário: Fármacos Anti-HIV/administração & dosagem
Antirretrovirais/uso terapêutico
Preparações de Ação Retardada/administração & dosagem
Infecções por HIV/tratamento farmacológico
[Mh] Termos MeSH secundário: Descoberta de Drogas/tendências
Feminino
Seres Humanos
Rilpivirina/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anti-HIV Agents); 0 (Anti-Retroviral Agents); 0 (Delayed-Action Preparations); FI96A8X663 (Rilpivirine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171107
[Lr] Data última revisão:
171107
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170318
[St] Status:MEDLINE
[do] DOI:10.1007/s11904-017-0353-0


  10 / 244 MEDLINE  
              first record previous record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28219799
[Au] Autor:Simiele M; Ariaudo A; De Nicolò A; Favata F; Ferrante M; Carcieri C; Bonora S; Di Perri G; De Avolio A
[Ad] Endereço:University of Turin, Department of Medical Sciences,(2) Laboratory of Clinical Pharmacology and Pharmacogenetics,(3) Amedeo di Savoia Hospital, CorsoSvizzera 164, 10149, Turin, Italy; "CoQuaLab", Academic Apin-off of University of Turin, Italy.
[Ti] Título:UPLC-MS/MS method for the simultaneous quantification of three new antiretroviral drugs, dolutegravir, elvitegravir and rilpivirine, and other thirteen antiretroviral agents plus cobicistat and ritonavir boosters in human plasma.
[So] Source:J Pharm Biomed Anal;138:223-230, 2017 May 10.
[Is] ISSN:1873-264X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Rilpivirine (RPV), dolutegravir (DTG) and elvitegravir (EVG) are the latest antiretroviral drugs approved for treatment of HIV infection. Currently, poor information is currently available concerning their pharmacokinetic and pharmacodynamic properties, thus making the use of therapeutic drug monitoring for these drugs not useful. This lack of information is partially due to the absence of an high-throughput method for their simultaneous quantification together with other antiretroviral drugs. In this work, we describe the development and validation of a new UPLC-MS/MS method to quantify these drugs, together with other fourteen antiretroviral agents, in human plasma. One hundred microliters of plasma samples were added with internal standard (6,7-Dimethyl- 2,3-di(2-pyridyl) quinoxaline), underwent a simple protein precipitation with methanol:acetonitrile (50:50v/v) followed by sample dilution with water. Chromatographic separation was performed on a Acquity UPLC HSS T3 column (150mm x 2.1mm I.D) with a particle size of 1.8µm and compounds were detected with a tandem mass detector, monitoring two ion transitions for each drugs. The mean recovery of RPV, DTG and EVG were 101%, 87% and 112.3% respectively. Accuracy and precision inter/intra-day were below 15% for all drugs, in accordance to Food and Drug Administration guidelines requirements. The UPLC-MS/MS method reported here could be used routinely to monitor plasma concentrations of antiviral drugs, including RPV, DTG and EVG.
[Mh] Termos MeSH primário: Antirretrovirais/sangue
Antirretrovirais/química
Cromatografia Líquida de Alta Pressão/métodos
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Fármacos Anti-HIV/sangue
Fármacos Anti-HIV/química
Cobicistat/sangue
Cobicistat/química
Compostos Heterocíclicos com 3 Anéis/sangue
Compostos Heterocíclicos com 3 Anéis/química
Seres Humanos
Limite de Detecção
Quinolonas/sangue
Quinolonas/química
Reprodutibilidade dos Testes
Rilpivirina/sangue
Rilpivirina/química
Ritonavir/sangue
Ritonavir/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-HIV Agents); 0 (Anti-Retroviral Agents); 0 (Heterocyclic Compounds, 3-Ring); 0 (JTK 303); 0 (Quinolones); DKO1W9H7M1 (dolutegravir); FI96A8X663 (Rilpivirine); LW2E03M5PG (Cobicistat); O3J8G9O825 (Ritonavir)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170628
[Lr] Data última revisão:
170628
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170222
[St] Status:MEDLINE



página 1 de 25 ir para página                         
   


Refinar a pesquisa
  Base de dados : MEDLINE Formulário avançado   

    Pesquisar no campo  
1  
2
3
 
           



Search engine: iAH v2.6 powered by WWWISIS

BIREME/OPAS/OMS - Centro Latino-Americano e do Caribe de Informação em Ciências da Saúde