raltegravir / Generic mfg. 
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 104 Diseases   23 Trials   23 Trials   2308 News 


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  • ||||||||||  Tivicay (dolutegravir) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD), Vitekta (elvitegravir) / Japan Tobacco, Gilead
    Journal, Real-world evidence, Real-world:  Effectiveness and safety of integrase strand transfer inhibitors in Spain: a prospective real-world study. (Pubmed Central) -  Jul 16, 2023   
    Safety and tolerability were consistent with expected safety profiles. Whereas second-generation INSTIs are preferred treatment options worldwide, and DTG is one of the treatment of choices in resource-limited settings, first-generation INSTIs may still provide high virological and immunological effectiveness when DTG is not available.
  • ||||||||||  Edurant (rilpivirine) / J&J, Tivicay (dolutegravir) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD)
    Journal:  Identification of integrase inhibitor-related drug resistance mutations in newly diagnosed ART-na (Pubmed Central) -  Jul 10, 2023   
    At the same time, the seven compounds showed good binding free energy after binding to the target proteins, providing potential drug candidates for the treatment and prevention of SARS-CoV-2 and SARS-CoV-2 variants. In summary, this study is the first to have surveyed the prevalence of integrase inhibitor resistance-related mutations and other drug resistance-related mutations among newly diagnosed ART-na
  • ||||||||||  Isentress (raltegravir) / Merck (MSD)
    Preclinical, Journal:  Novel Perspectives on the Design and Development of a Long-Acting Subcutaneous Raltegravir Injection for Treatment of HIV-In Vitro and In Vivo Evaluation. (Pubmed Central) -  May 27, 2023   
    This compound showed an excellent in vitro release profile, with a half-life (t) of 19.3 d and 82% of RAL released over 45 d. In mice, 25 extended the half-life of unmodified RAL by 4.2-fold (t = 3.18 h), providing initial proof of concept of the ability of amino-AOCOM prodrugs to extend drug lifetimes in vivo. Although this effect was not as pronounced as seen in vitro-presumably due to enzymatic degradation and rapid clearance of the prodrug in vivo-the present results nevertheless pave the way for development of more metabolically stable prodrugs, to facilitate long-acting delivery of ARVs.
  • ||||||||||  Pifeltro (doravirine) / Merck (MSD), Isentress (raltegravir) / Merck (MSD)
    Trial completion date, Trial primary completion date:  DORAL: HIV-1 Infected Patients, Phase II Trial, Dual Combination Doravirine/Raltegravir Open Label (clinicaltrials.gov) -  May 12, 2023   
    P2,  N=150, Recruiting, 
    Virological failure in a patient treated with raltegravir forces to a rapid change in ARV therapy because its continued use may favor new mutations and resistance to second-generation INSTIs. Trial completion date: Oct 2022 --> Oct 2024 | Trial primary completion date: Oct 2021 --> Oct 2023
  • ||||||||||  Isentress (raltegravir) / Merck (MSD)
    Journal, PARP Biomarker, IO biomarker:  HIV-1 integrase inhibitor raltegravir promotes DNA damage-induced apoptosis in multiple myeloma. (Pubmed Central) -  May 7, 2023   
    We report for the first time that treatment with raltegravir is associated with decreased cell viability, apoptosis induction, DNA damage accumulation, and alteration of mRNA expression of genes involved in V(D)J recombination and DNA repair in MM cell lines, all of which show its potential for anti-myeloma effects. Hence, raltegravir may significantly impact the treatment of MM, and further studies are required to confirm its efficacy and mechanism of action in more detail in patient-derived myeloma cells and in-vivo models.
  • ||||||||||  Tivicay (dolutegravir) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD)
    Journal:  Obesity Modifies the Relationship Between Raltegravir and Dolutegravir Hair Concentrations and Body Weight Gain in Women Living with HIV. (Pubmed Central) -  May 4, 2023   
    Over ~1y, women experienced median increases in body weight: 1.71% (-1.78, 5.00) with RAL; 2.40% (-2.82, 6.50) with EVG; 2.48% (-3.60, 7.88) with DTG.??Baseline obesity status modified the relationship between hair concentrations and percent weight change for DTG and RAL (p's<0.05): higher DTG, yet lower RAL concentrations were associated with greater weight gain among non-obese women. Additional pharmacologic assessments are needed to understand the role of drug exposure in INSTI-associated weight gain.
  • ||||||||||  Tivicay (dolutegravir) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD), Vitekta (elvitegravir) / Japan Tobacco, Gilead
    Journal:  Development of Potential Inhibitors for Human T-lymphotropic virus type I Integrase enzyme: A molecular modeling approach. (Pubmed Central) -  Apr 28, 2023   
    Additional pharmacologic assessments are needed to understand the role of drug exposure in INSTI-associated weight gain. Combing structure-based design and virtual screening resulted in identifying three drug-like molecules (PubChem CID_138739497, _70381610, and _140084032) that are suggested as lead compounds for developing effective drugs targeting HTLV-1 integrase enzyme.
  • ||||||||||  Tivicay (dolutegravir) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD), Vitekta (elvitegravir) / Japan Tobacco, Gilead
    INTEGRASE INHIBITORS IN CHILDREN AND ADOLESCENTS: CLINICAL USE AND RESISTANCE (STATION 5) -  Apr 21, 2023 - Abstract #ESPID2023ESPID_722;    
    Combing structure-based design and virtual screening resulted in identifying three drug-like molecules (PubChem CID_138739497, _70381610, and _140084032) that are suggested as lead compounds for developing effective drugs targeting HTLV-1 integrase enzyme. Overall, 318 INI-based regimens were implemented in 288 patients [53.8% female; median age at start of 14.3 years (IQR 12.0
  • ||||||||||  Isentress (raltegravir) / Merck (MSD)
    Type I interferons and TGF-? cooperate to induce liver fibrosis during HIV-1 infection under antiretroviral therapy (P621) (Exhibit Hall; Poster Board No. P621) -  Apr 11, 2023 - Abstract #IMMUNOLOGY2023IMMUNOLOGY_1139;    
    Consistently, we detected elevated markers of liver injury, M2LMs, and of IFN signaling in blood specimens and liver biopsies from PLWH compared with those of healthy individuals. These findings identify the IFN-I/M2LM/HepSC axis in HIV/ART-induced liver diseases and suggest that inhibiting IFN-I signaling or M2LM may provide a novel therapeutic strategy for treating HIV/ART-associated liver diseases in PLWH treated with ART.
  • ||||||||||  Pifeltro (doravirine) / Merck (MSD), Biktarvy (bictegravir/emtricitabine/tenofovir alafenamide) / Gilead, Isentress (raltegravir) / Merck (MSD)
    Enrollment open:  PANNA-B PK: Study on PhArmacokinetics of First liNe Antiretrovirals in Healthy Breastfeeding Volunteers (clinicaltrials.gov) -  Apr 10, 2023   
    P4,  N=36, Recruiting, 
    These findings identify the IFN-I/M2LM/HepSC axis in HIV/ART-induced liver diseases and suggest that inhibiting IFN-I signaling or M2LM may provide a novel therapeutic strategy for treating HIV/ART-associated liver diseases in PLWH treated with ART. Not yet recruiting --> Recruiting
  • ||||||||||  Isentress (raltegravir) / Merck (MSD)
    Enrollment closed, Enrollment change, Trial completion date, Trial primary completion date:  Combination Antiretroviral Therapy (cART) for PBC (clinicaltrials.gov) -  Mar 27, 2023   
    P2,  N=37, Active, not recruiting, 
    Not yet recruiting --> Recruiting Recruiting --> Active, not recruiting | N=60 --> 37 | Trial completion date: Oct 2026 --> Jan 2024 | Trial primary completion date: Oct 2024 --> Oct 2022
  • ||||||||||  Isentress (raltegravir) / Merck (MSD)
    Trial completion, Enrollment change:  Protease Inhibitor vs. Raltegravir-based ART and Inflammation in HIV Infection (clinicaltrials.gov) -  Mar 21, 2023   
    P4,  N=6, Completed, 
    Recruiting --> Active, not recruiting | N=60 --> 37 | Trial completion date: Oct 2026 --> Jan 2024 | Trial primary completion date: Oct 2024 --> Oct 2022 Unknown status --> Completed | N=44 --> 6
  • ||||||||||  Vemlidy (tenofovir alafenamide) / Gilead
    Preclinical, Journal:  Adipocyte differentiation of 3T3-L1 cells under TAF, TDF and INSTIs selective challenge: an in vitro model. (Pubmed Central) -  Feb 27, 2023   
    The calculated results showed that raltegravir and hesperidin had high binding affinities and stabilities to Omicron with ?G of?-?75.7304? Our data support the evidence that in-vitro challenge of 3T3-L1 cells with INSTIs is able to increase adipocytic differentiation and to drive a number of these cells toward the expression of fibroblastic features, with a different degree according to the various drugs used whereas TAF and TDF have an antagonistic role on this phenomenon.
  • ||||||||||  Edurant (rilpivirine) / J&J, Tivicay (dolutegravir) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD)
    Trial completion, Enrollment change:  POPARV: Population Pharmacokinetics of Antiretroviral in Children (clinicaltrials.gov) -  Feb 21, 2023   
    P=N/A,  N=65, Completed, 
    No abstract available Recruiting --> Completed | N=700 --> 65
  • ||||||||||  Prezista (darunavir) / J&J, Isentress (raltegravir) / Merck (MSD)
    Journal:  Antiretroviral Levels in the Cerebrospinal Fluid: The Effect of Inflammation and Genetic Variants. (Pubmed Central) -  Jan 22, 2023   
    At bi-variate analysis, several associations, including the effect of BBBi (emtricitabine, raltegravir), age (zidovudine and darunavir), and high CSF neopterin (NRTIs and border-line for PIs) were suggested...At multivariate analysis age, gender, BMI, and altered BBB were independent predictors of nucleoside reverse transcriptase CSF concentrations; age (for protease inhibitors) and body mass index and altered BBB (integrase strand transfer inhibitors) were also associated with ARV CSF exposure. We describe factors associated with CSF concentrations, showing that demographic, BBB integrity and, partially, genetic factors may be predictors of drug passage in the central nervous system.
  • ||||||||||  Journal:  Primary resistance to integrase inhibitors in Shenzhen. (Pubmed Central) -  Jan 1, 2023   
    ​Continued surveillance for resistance to INSTIs is recommended and treatment regimens should be adopted based on the pattern of resistance to INSTIs. ​Dolutegravir or bictegravir is first recommended when considering INSTIs as treatment regimens.
  • ||||||||||  Review, Journal:  Different Pathways Conferring Integrase Strand-Transfer Inhibitors Resistance. (Pubmed Central) -  Dec 24, 2022   
    To counteract these resistant mutants, second-generation INSTI drugs have been developed: Dolutegravir (DTG), Cabotegravir (CAB), and Bictegravir (BIC)...The role of unintegrated viral DNA is also discussed as a new pathway involved in conferring resistance to INSTIs. This allows us to have a more detailed understanding of HIV resistance to these inhibitors, which may contribute to the development of new INSTIs in the future.
  • ||||||||||  Isentress (raltegravir) / Merck (MSD)
    Journal, Adherence:  Determinants of Antiretroviral Treatment Success and Adherence in People With Human Immunodeficiency Virus Treated for Tuberculosis. (Pubmed Central) -  Dec 22, 2022   
    Antiretroviral pill burden was the only factor associated with pill count adherence ratio ≥95% (OR, 0.81; 95% CI, .71-.92; P = .0018). In PWH with tuberculosis receiving raltegravir or efavirenz-based regimens, female sex, optimal adherence, and baseline HIV-1 RNA <100 000 copies/mL were associated with virologic success, and the number of antiretroviral tablets taken daily was a strong predictor of adherence.
  • ||||||||||  Isentress (raltegravir) / Merck (MSD)
    Journal:  Recent Advancement in Synthesis and Bioactivities of 1,3,4-Oxadiazole. (Pubmed Central) -  Dec 2, 2022   
    Stable isomeric oxadiazole forms of pleconaril, raltegravir, butalamine, fasiplon, oxolamine, and several other drugs are among the numerous potent and effective pharmaceuticals that are now on the market...The use of biological and in-silico models has enabled scientists to identify more synthetic analogues of cancer prevention, antifungal, and anti-HIV medications. This article provides recent information regarding procedures synthesizing 1,3,4-oxadiazoles and their biological actions on the body.
  • ||||||||||  Selzentry (maraviroc) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD)
    PK/PD data, Preclinical, Journal, IO biomarker:  Pharmacokinetics, the immunological impact and the effect on HIV ex-vivo infectivity of maraviroc, raltegravir and lopinavir in MSM using Post-exposure Prophylaxis. (Pubmed Central) -  Nov 24, 2022   
    Merging together changes in MMC in all arms, we found a positive correlation in the CD8 T-cell lineage between the infectivity at day 7 and activation (CD38+ r=0.43, p=0.025, DR+ r=0.547, p=0.003 and 38+DR+ r=0.526, p=0.05), senescence (CD57+CD28- r=0.479, p=0.012), naïve cells (RA+CCR7+ r=0.484, p=0.01) and CCR5 expression (r=0.593, p=0.001). We conclude that maraviroc in combination with tenofovir/emtricitabine was associated with viral suppression in rectal explants and that overall ex-vivo HIV infectivity correlated with activation and senescence in CD8 mucosal mononuclear cells.