- |||||||||| Edurant (rilpivirine) / J&J, Tivicay (dolutegravir) / ViiV Healthcare, Vitekta (elvitegravir) / Japan Tobacco, Gilead
Journal: Reduction of CD8 T cell functionality but not inhibitory capacity by integrase inhibitors. (Pubmed Central) - Apr 29, 2022 In summary, our study provides first evidence on a significant, negative impact on CD8 T cell effector functions in the presence of two INSTIs, dolutegravir and elvitegravir, which may contribute to the limited success of eradicating HIV-infected cells through "shock-and-kill" strategies. Although our findings are coherent with recent studies highlighting a possible role of dolutegravir in weight gain, further investigations are necessary to fully understand the impact of INSTI-based regimens on the health of the individual during antiretroviral therapy.
- |||||||||| Edurant (rilpivirine) / J&J
Journal: Implication of autophagy in the antifibrogenic effect of Rilpivirine: when more is less. (Pubmed Central) - Apr 28, 2022 Finally, we also provide evidence that RPV compromises the viability of TGF-β-induced HSC independently of its antifibrogenic effect, observed as reduced collagen 1A1 synthesis, and that this effect does not include RPV´s modulation of autophagy. In summary, as a contributor to the mechanisms involved in the hepatoprotective action of RPV, autophagy may be a good candidate to explore when developing novel therapeutics for LF.
- |||||||||| Edurant (rilpivirine) / J&J
Trial completion date, Trial primary completion date, HEOR, Real-world evidence: 'COMBINE-2': Real-world Evidence for Effectiveness of Two Drug Regimen, Antiretroviral Therapy With Integrase Inhibitors Plus a Reverse Transcriptase Inhibitor (clinicaltrials.gov) - Apr 11, 2022 P=N/A, N=1, Recruiting, In the real world, the risks of discontinuation due to TF and VF were more than two times higher in patients switching to DTG-based 2DR than INSTI-based 3DR, with no difference in discontinuation due to AEs. Trial completion date: Dec 2021 --> Jan 2023 | Trial primary completion date: Dec 2021 --> Jan 2023
- |||||||||| Edurant (rilpivirine) / J&J, Prezcobix (darunavir/cobicistat) / Gilead, J&J, Tivicay (dolutegravir) / ViiV Healthcare
Trial completion, Trial completion date: Effect on HIV Medications on EPC Cells (clinicaltrials.gov) - Mar 22, 2022 P=N/A, N=22, Completed, The presented method could be used for the development of new pharmaceutical products based on cabotegravir. Recruiting --> Completed | Trial completion date: Dec 2020 --> Dec 2021
- |||||||||| Vocabria (cabotegravir oral) / ViiV Healthcare, Edurant (rilpivirine) / J&J
Journal: Virus-Mimicking Polymer Nanoparticles Targeting CD169 Macrophages as Long-Acting Nanocarriers for Combination Antiretrovirals. (Pubmed Central) - Mar 19, 2022 Intracellular localization of GM3-presenting PLA NPs in VCCs correlated with retention of intracellular ARV concentrations and sustained inhibition of HIV-1 infection. This work elucidates the design criteria of lipid-coated polymer NPs to utilize CD169 macrophages as cellular drug depots for eradicating the viral reservoir sites or to achieve long-acting prophylaxis against HIV-1 infection.
- |||||||||| Comtan (entacapone) / Novartis, Orion Corp, Edurant (rilpivirine) / J&J
Review, Journal: Insights into the chemistry and therapeutic potential of acrylonitrile derivatives. (Pubmed Central) - Mar 17, 2022 In this review, diverse synthetic strategies for constructing desired acrylonitriles are discussed, and the different biological activities and medicinal significance of various acrylonitrile derivatives are critically evaluated. The information gathered is expected to provide rational guidance for the development of clinically useful agents from acrylonitriles.
- |||||||||| Edurant (rilpivirine) / J&J
Clinical, Journal: Short-cycle therapy in HIV-infected adults: rilpivirine combination 4 days on/3 days off therapy. (Pubmed Central) - Mar 5, 2022 A higher discontinuation rate was observed with DTG-STR compared to RPV-STR in particular within 3 months from the switch. SCT with rilpivirine-containing regimens could be an effective alternative to continuous therapy in selected HIV-infected patients with previous long-term virological suppression.
- |||||||||| Preclinical, Journal: Evaluation of the Potency of Anti-HIV and Anti-HCV Drugs to Inhibit P-Glycoprotein Mediated Efflux of Digoxin in Caco-2 Cell Line and Human Precision-Cut Intestinal Slices. (Pubmed Central) - Feb 27, 2022
However, abacavir, dolutegravir, maraviroc, sofosbuvir, tenofovir disoproxil fumarate, and zidovudine had no inhibitory effect...More inhibitors were identified when using digoxin as the ABCB1 probe substrate than when using rhodamine123. However, both approaches had limitations, indicating that inhibitory potency should be tested with at least these two ABCB1 probes.
- |||||||||| Vocabria (cabotegravir oral) / ViiV Healthcare, Apretude (cabotegravir extended-release injectable suspension) / ViiV Healthcare
Journal: Cabotegravir (Apretude) for HIV-1 pre-exposure prophylaxis. (Pubmed Central) - Feb 23, 2022 However, both approaches had limitations, indicating that inhibitory potency should be tested with at least these two ABCB1 probes. No abstract available
- |||||||||| Edurant (rilpivirine) / J&J, Descovy (emtricitabine/tenofovir alafenamide) / Gilead, Isentress (raltegravir) / Merck (MSD)
PREDICTED IMPACT OF ART SWITCH ON BODY MASS INDEX AMONG WOMEN WITH HIV ([VIRTUAL]) - Feb 7, 2022 - Abstract #CROI2022CROI_660; Exposure time to zidovudine, efavirenz (EFV) and raltegravir, depressive symptoms and recent recreational drug use were associated with lower BMI; tenofovir alafenamide (TAF), rilpivirine and higher CD4 counts were associated with higher BMI...Of the 353 WWH predicted to achieve ?5% BMI decrease following switch, two regimens accounted for 97.5% of the optimal predicted ART regimens – TAF/emtricitabine(FTC)/EFV (51%) and TAF/FTC/atazanavir/ritonavir (46%) although other factors may preclude their use...However, only 25% of the women were predicted to achieve ?5% decrease in BMI following ART switch. Optimization of other clinical factors may need to be implemented to achieve reductions in BMI among WWH.
- |||||||||| bictegravir (GS-9883) / Gilead
REVERSIBILITY OF CENTRAL NERVOUS SYSTEM ADVERSE EVENTS IN COURSE OF ART ([VIRTUAL]) - Feb 7, 2022 - Abstract #CROI2022CROI_613; Central nervous system (CNS) adverse events (AE) can occur during various antiretroviral therapies (ART), as well as being a major cause of treatment discontinuation during dolutegravir-containing ART (DTG)...Sixty SNC-AE leading to ART discontinuation were reported, 26/3613 (0.7%) in non DTG-cohorts (2/731 lopinavir, 1/616 atazanavir, 2/721 darunavir, 8/421 rilpivirine, 5/514 raltegravir, 3/339 elvitegravir and 5/211 bictegravir), and 34/1138 (3.1%) in DTG-cohort...AE leading to ART discontinuation were more frequent in DTG than non-DTG treated PLWH. However, most AE resolved after ART switch, with similar frequency in DTG and non-DTG cohorts.
- |||||||||| efavirenz / Generic mfg.
EFAVIRENZ PLASMA LEVELS, COGNITION, AND CENTRAL NERVOUS SYSTEM SIDE EFFECTS ([VIRTUAL]) - Feb 7, 2022 - Abstract #CROI2022CROI_612; Such marker can be useful to identify Pt who can benefit the most from EFV discontinuation. EFV-but not 8-OH-EFV- Cp were marginally associated with NC performances, suggesting possible different pathways in determining detrimental effects on cognitive function.
- |||||||||| Edurant (rilpivirine) / J&J
CARD8 ACTIVATION BY HIV-1 PR TRIGGERS GSDMD-DEPENDENT AND -INDEPENDENT CELL DEATH ([VIRTUAL]) - Feb 7, 2022 - Abstract #CROI2022CROI_513; This work reveals that HIV-1-infected cells can undergo CASP1-induced lytic cell death after CARD8 inflammasome activation in GSDMD-dependent and -independent manners. This study broadens our understanding of CARD8 inflammasome-induced cell death and has implications for the clearance of HIV-1 reservoir cells in patients.
- |||||||||| zidovudine / Generic mfg.
PK/PD data, Review, Journal: A Review on Pharmacokinetics properties of antiretroviral drugs to treat HIV-1 infections. (Pubmed Central) - Jan 18, 2022 These drugs are Fuzeon, Selzentry, Complera, Epivir, Retrovir, Emtriva, Ziagen, Edurant, Intelence, Pifeltro, Sustiva, Viramune, Isentress, Genvoya, Tivicay, Reyataz, Prezista, Lexiva, Invirase, Aptivus etc. classified into five major classes: fusion inhibitors, Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs), Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs), Integrase Strand transfer inhibitors (INSTIs) and Protease inhibitors (PIs). This review may be helpful for the future development of potent antiretroviral drugs with improved pharmacokinetic properties.
- |||||||||| Rescriptor (delavirdine mesylate) / ViiV Healthcare, Edurant (rilpivirine) / J&J, Intelence (etravirine) / J&J
Journal: Application of Molecular Docking for the Development of Improved HIV-1 Reverse Transcriptase Inhibitors. (Pubmed Central) - Jan 14, 2022 This review may be helpful for the future development of potent antiretroviral drugs with improved pharmacokinetic properties. In this study, we have identified and proposed some novel molecules with improved binding capacity for HIV RT using a fragment-based approach.
- |||||||||| Edurant (rilpivirine) / J&J, Cabenuva (cabotegravir long acting/rilpivirine long acting) / J&J, GSK, ViiV Healthcare, Pfizer, Shionogi
Review, Journal: Therapeutic review of cabotegravir/rilpivirine long-acting antiretroviral injectable and implementation considerations at an HIV specialty clinic. (Pubmed Central) - Jan 7, 2022 Clinics will need to address barriers related to management of clinic workflow, procurement, reimbursement, and nonadherence. The aim of this review is to summarize the available safety, efficacy and pharmacokinetic/pharmacodynamic (PK/PD) data of this long-acting (LA) injectable regimen as well as discuss some potential considerations for prescribing and operationalization.
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