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- Tivicay (dolutegravir) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD)
Efficacy and safety of efavirenz, raltegravir and dolutegravir in HIV/TB co-infection. A retrospective cohort study (eLibrary) - Sep 18, 2021 - Abstract #EACS2021EACS_204;
We included all patients co-infected with HIV and tuberculosis starting a rifampicin-based regimen, with a plasma viral load (VL)>1000 copies/mL. In this retrospective study, raltegravir and dolutegravir yielded similar efficacy and safety results to efavirenz for the treatment of patients co-infected with HIV and TB.
- Edurant (rilpivirine) / J&J, Isentress (raltegravir) / Merck (MSD)
Incidence of diabetes mellitus in PLWHIV: impact of antiretroviral therapy (eLibrary) - Sep 18, 2021 - Abstract #EACS2021EACS_182;
This fact will require an important effort to diagnose and treat DM2 early. Some antiretroviral therapy drugs could play a differential role in the development of DM2, RPV being a potentially beneficial drug.
- Isentress (raltegravir) / Merck (MSD)
Factors associated with high adherence in HIV-1 infected adults with tuberculosis receiving raltegravir or efavirenz-based antiretroviral therapy in the ANRS 12300 Reflate TB2 trial (eLibrary) - Sep 18, 2021 - Abstract #EACS2021EACS_130;
Higher treatment adherence measured by PCAR was driven mainly by ART pill burden. Virologic efficacy of the raltegravir based regimen might have been hampered by a high pill burden.
- Dovato (dolutegravir/lamivudine) / ViiV Healthcare
DOLAMA STUDY 200: effectiveness, safety and economic evaluation of a dual therapy with dolutegravir plus lamivudine in treatment-experienced HIV patients (eLibrary) - Sep 18, 2021 - Abstract #EACS2021EACS_109;
The 5 patients with VF:3 didn't have resistance studies, 1 didn't amplify and one had K103R and S147G mutations (Which don't limit the activity of INIs). All of them were virologically resupressed after a change in their ART.
- bictegravir (GS-9883) / Gilead
Weight gain after switching to integrase inhibitor-based ART is not associated with hepatic steatosis in HIV-infected patients (eLibrary) - Sep 18, 2021 - Abstract #EACS2021EACS_91;
Purpose: Weight gain is associated with integrase inhibitors (INSTI)-based regimens, particularly when combined with tenofovir alafenamide (TAF)...However, switching from efavirenz to raltegravir was not associated with HS, despite weight gain after the switch...Of them, 67 (43%) switched to dolutegravir, 47 (31%) to raltegravir, 22 (14%) to bictegravir and 18 (12%) to elvitegravir-cobicistat... Weight gain in HIV-infected patients after switching to INSTI-based regimens is not paralleled by changes in HS one year after the switch.Weight gain associated after switching to INSTI-based regimens does not parallel to an increase in HS in HIV-infected patients one year after the switch.
- bictegravir (GS-9883) / Gilead
Increasing trend of pretreatment integrase inhibitors resistance in a cohort of antiretroviral therapy-naïve people living with HIV (eLibrary) - Sep 18, 2021 - Abstract #EACS2021EACS_54;
The only factor associated with InSTI resistance was HIV-1 subtype non-B. Prevalence of at least low-level InSTI DR was anecdotal between 2009–2013 and then gradually raised from 1.3% in 2014 to 3.9% in 2019 (p-for-trend<0.001); prevalence of at least intermediate InSTI DR increased from 0% in 2009 to 2% in 2019 (p-for-trend=0.188, ).
- || Isentress (raltegravir) / Merck (MSD)
PK/PD data, Journal: Characterization of Seasonal Pharmacokinetic Variability in Woodchucks. (Pubmed Central) - Sep 15, 2021
These compounds were selected to study changes in oxidative metabolism [antipyrine (AP)], glucuronidation [raltegravir (RTG)], renal clearance [lamivudine (3TC)], and hepatic function [indocyanine green (ICG)]...Investigation of seasonal PK changes is perhaps of greater interest to pharmaceutical industry scientists using the woodchuck model to optimize the scheduling of woodchuck studies to avoid seasonally-driven variation in drug PK and/or toxicity. This information is also valuable to drug metabolism and veterinary scientists in understanding woodchuck's seasonal metabolism and behavior under the pseudo-hibernation condition.
- || Tivicay (dolutegravir) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD), Vitekta (elvitegravir) / Japan Tobacco, Gilead
Clinical, Journal: Structural effects of HIV-1 subtype C integrase mutations on the activity of integrase strand transfer inhibitors in South African patients. (Pubmed Central) - Sep 8, 2021
Molecular modeling and docking showed that RAMs and polymorphisms associated with INSTI-based therapy affect protein stability and this is supported by their weakened hydrogen-bond interactions compared to the wild-type. To the best of our knowledge, this is the first study to identify a double mutant in the 140's loop region from South African HIV-1C isolates and study its effects on Raltegravir, Elvitegravir, and Dolutegravir binding.Communicated by Ramaswamy H. Sarma.
- || Tivicay (dolutegravir) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD)
Clinical, Journal: First case of Dolutegravir and Darunavir/r multi drug-resistant HIV-1 in Cameroon following exposure to Raltegravir: lessons and implications in the era of transition to Dolutegravir-based regimens. (Pubmed Central) - Sep 4, 2021
To the best of our knowledge, this is the first study to identify a double mutant in the 140's loop region from South African HIV-1C isolates and study its effects on Raltegravir, Elvitegravir, and Dolutegravir binding.Communicated by Ramaswamy H. Sarma. As African countries transition to dolutegravir-based regimens, prior raltegravir-exposure may prompt selection (and potential transmission) of dolutegravir-resistance, supporting case surveillance.
- | bictegravir (GS-9883) / Gilead
Journal: Structural basis for the inhibition of HTLV-1 integration inferred from cryo-EM deltaretroviral intasome structures. (Pubmed Central) - Sep 1, 2021
The structures reveal subtle differences in the coordination environment of the Mg ion pair involved in the interaction with the INSTIs. Our results elucidate the binding of INSTIs to the HTLV-1 intasome and support their use for pre-exposure prophylaxis and possibly future treatment of HTLV-1 infection.
- | Tivicay (dolutegravir) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD)
Journal: Limited HIV-1 Subtype C nef 3'PPT Variation in Combination Antiretroviral Therapy Naïve and Experienced People Living with HIV in Botswana. (Pubmed Central) - Aug 29, 2021
Dolutegravir (DTG) is a potent anti-HIV drug that is used to treat HIV globally...In addition, we generated separate integrase and nef gene sequences by Sanger sequencing of plasma samples from individuals with virologic failure (VF) while on a DTG/raltegravir (RAL)-based cART...Our study confirms the high conservation of the HIV-1 nef gene 3'PPT motif in 'real-world' patients and showed no differences in the motif according to VL suppression or INSTI-based cART failure. Future studies should explore other HIV-1 regions outside of the pol gene for associations with DTG failure.
- || bictegravir (GS-9883) / Gilead
Clinical, Review, Journal: Do All Integrase Strand Transfer Inhibitors Have the Same Lipid Profile? Review of Randomised Controlled Trials in Naïve and Switch Scenarios in HIV-Infected Patients. (Pubmed Central) - Aug 28, 2021
In naïve patients, RAL, DTG, and bictegravir (BIC) produce a similar, slight increase in lipids...No changes were observed in lipids by switching trials between INSTIs. In summary, RAL, DTG, and BIC have superior lipid profiles compared with boosted-PI, efavirenz, and EVG/c, in studies conducted in naïve participants, and they are associated with a clinically significant decrease in lipoproteins by switching studies.
- | Prezista (darunavir) / J&J, Isentress (raltegravir) / Merck (MSD)
Journal: Changes in lipidomic profile by anti-retroviral treatment regimen: An ACTG 5257 ancillary study. (Pubmed Central) - Aug 26, 2021
The INSTI-based regimen had an opposite response of ceramide species ((d38:1), (d42:2)), PCs((35:2), (38:4)), phosphatidylethanolamines (PEs(38:4), (38:6)), and sphingomyelin(SMd38:1) species compared with the PI-based regimens. There were no differences observed between 2 PI-based regimens.We observed differences in response of small molecule lipid species by ART regimens in treatment-naive people living with HIV.
- || Isentress (raltegravir) / Merck (MSD)
Clinical, PK/PD data, Journal: Pharmacokinetics and Safety of a Raltegravir-Containing Regimen in Children Aged 4 Weeks to 2 Years Living With Human Immunodeficiency Virus and Receiving Rifampin for Tuberculosis. (Pubmed Central) - Aug 20, 2021
P1/2
We found that 12 mg/kg twice daily raltegravir chewable tablets (administered after crushing) safely achieved pharmacokinetic targets in children living with HIV aged 4 weeks to <2 years receiving concurrent rifampin to treat TB. NCT01751568.
- | Journal: Changes in functional connectivity in people with HIV switching antiretroviral therapy. (Pubmed Central) - Aug 20, 2021
Changes in fMRI are evident in PWH without perceived neuropsychiatric complaints switching cART. fMRI may be a useful tool in assisting to elucidate the underlying pathogenic mechanisms of cART-related neuropsychiatric effects.
- | Isentress (raltegravir) / Merck (MSD), Vitekta (elvitegravir) / Japan Tobacco, Gilead
Biomarker, Journal: HIV-1 drug resistance mutation analyses of Cameroon derived Integrase sequences. (Pubmed Central) - Aug 20, 2021
HIV-1 CRF02_AG was the predominant subtype (44.7.%) in this study analyses. The occurrence of INSTI RAMs among the sequences at baseline needs to be monitored carefully.
- || Isentress (raltegravir) / Merck (MSD)
Clinical, Journal: Raltegravir-associated Drug-Reaction With Eosinophilia and Systemic Symptoms Syndrome in a Pediatric Patient Without Characteristic Human Leukocyte Antigen B*57:01 or B*53:01 alleles. (Pubmed Central) - Aug 20, 2021
We present the first published case of raltegravir-associated drug-reaction with eosinophilia and systemic symptoms (DRESS) syndrome in a child without characteristic human leukocyte antigen haplotypes HLA-B*57:01 or HLA-B*53:01. A 4-year-old African American female with perinatally acquired human immunodeficiency virus infection was hospitalized for DRESS after starting a raltegravir-based antiretroviral regimen.
- || Isentress (raltegravir) / Merck (MSD)
Clinical, Journal: NO SIGNIFICANT INCREASE IN BODY FAT MASS IN NAIVE HIV-INFECTED PATIENTS STARTING RALTEGRAVIR PLUS TENOFOVIR DISOPROXIL FUMARATE/EMTRICITABINE. (Pubmed Central) - Aug 20, 2021
The median increase in body fat mass (IQR) was +1.27 Kg (+1.09, +1.43; p=0.278) in raltegravir group, and +1.04 Kg (+0.89, +1.22; p=0.781) in darunavir/ritonavir group. In conclusion, in our study, an initial regimen including raltegravir plus tenofovir/emtricitabine after 12 months led to a small and not significant increase in weight and body fat mass, and changes were comparable to a darunavir/ritonavir-based initial regimen.
- || Tivicay (dolutegravir) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD), Vitekta (elvitegravir) / Japan Tobacco, Gilead
Clinical, Journal: Overall tolerability of Integrase Inhibitors in clinical practice: results from a multicenter Italian cohort. (Pubmed Central) - Aug 20, 2021
Our data confirm the good tolerability of INIs in clinical practice. Differences emerge between the three drugs in reasons for discontinuation.
- | Journal: The Use of Integrase Strand Transfer Inhibitors to Treat HIV in Pregnancy. (Pubmed Central) - Aug 20, 2021
Here, we present the case of a pregnant woman with well-controlled HIV on a well-tolerated prepregnancy regimen of bictegravir, emtricitabine, and tenofovir alafenamide...In the second trimester, because of adverse effects from the new ART regimen and after a risk-benefit discussion, the patient restarted the original regimen. She was able to maintain viral suppression until giving birth.
- | Prezista (darunavir) / J&J, Isentress (raltegravir) / Merck (MSD)
Journal: Evaluation of Platelet Activation by HIV Protease Inhibitors - The HIV-PLA II Study. (Pubmed Central) - Aug 17, 2021
In the past, protease inhibitors (PIs) and the reverse transcriptase inhibitor abacavir were identified increasing the risk for thromboembolic complications and cardiovascular events (CVE) of HIV infected patients taking a combination antiretroviral therapy (cART)...The open label, monocentric HIV-PLA II-study investigated HIV-1-infected, therapy-naïve adults (n=45) starting with cART, consisting either of boosted PI (atazanavir, n= 6, darunavir, n=11), NNRTI (efavirenz, n=14) or integrase inhibitor (raltegravir, n=14), each plus tenofovir/emtricitabine co-medication...The findings of this study revealed a yet unknown pathway of platelet activation, possibly contributing to the increased risk for CVE under HIV protease inhibitor containing cART. DRKS00000288.
- || Tivicay (dolutegravir) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD)
Clinical, Journal: HIV-1 Subtype C Drug Resistance Mutations in Heavily Treated Patients Failing Integrase Strand Transfer Inhibitor-Based Regimens in Botswana. (Pubmed Central) - Aug 15, 2021
Individuals with 4-class DRMs plus integrase T97 and E157Q mutations appear to have worse outcomes. There is a need for frequent VL monitoring and GRT amongst treatment-experienced HIV-1C diagnosed individuals.
- | Journal: Virologic Outcomes Among People Living With Human Immunodeficiency Virus With High Pretherapy Viral Load Burden Initiating on Common Core Agents. (Pubmed Central) - Aug 13, 2021
ART-naive PLWH with high VLs initiating on DTG were significantly less likely to experience virologic failure compared to EVG, RAL, and DRV initiators.Antiretroviral therapy-naïve people living with HIV (PLWH) initiating therapy with viral loads ≥100,000 copies/mL varied markedly at baseline. In adjusted models, PLWH initiating dolutegravir-based regimens were less likely to experience virologic failure as compared to elvitegravir, raltegravir and darunavir initiators.
- | Isentress (raltegravir) / Merck (MSD)
Trial completion, Trial completion date: Hepatic Safety of Raltegravir Versus Efavirenz as HIV Therapy for Patients With HIV and HCV Coinfection (clinicaltrials.gov) - Aug 13, 2021
P4, N=80, Completed, Sponsor: University of Hawaii
In adjusted models, PLWH initiating dolutegravir-based regimens were less likely to experience virologic failure as compared to elvitegravir, raltegravir and darunavir initiators. Active, not recruiting --> Completed | Trial completion date: Jun 2017 --> Jun 2021
- || Isentress (raltegravir) / Merck (MSD)
PK/PD data, Journal: Pharmacokinetic/pharmacodynamic investigation of raltegravir with or without lamivudine in the context of HIV-1 pre-exposure prophylaxis (PrEP). (Pubmed Central) - Aug 12, 2021
P4
Active, not recruiting --> Completed | Trial completion date: Jun 2017 --> Jun 2021 Raltegravir 400 mg+lamivudine 150 mg showed high levels of ex vivo HIV protection, associated with high drug concentrations persisting after discontinuation in vaginal and rectal compartments, supporting further investigation of these agents for PrEP.
- | Isentress (raltegravir) / Merck (MSD), Vitekta (elvitegravir) / Japan Tobacco, Gilead
Journal: Hepatic steatosis associated with exposure to elvitegravir and raltegravir. (Pubmed Central) - Aug 11, 2021
P=N/A
Moderate-to-severe hepatic steatosis in people living with HIV without viral hepatitis or excessive alcohol intake was associated with cumulative exposure to stavudine, elvitegravir and raltegravir. Prospective trials are required to establish a causal association.
- || Selzentry (maraviroc) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD)
Clinical, Journal, IO biomarker: Altered subcutaneous adipose tissue parameters after switching ART-controlled HIV+ patients to raltegravir/maraviroc. (Pubmed Central) - Aug 8, 2021
However, immune activation/inflammation profile was globally lowered. We propose that raltegravir/maraviroc might favor SCAT gain but reduce inflammation/immune activation.
- | Prezista (darunavir) / J&J, Isentress (raltegravir) / Merck (MSD)
Journal: Effects of atazanavir, darunavir, and raltegravir on fat and muscle among persons living with HIV. (Pubmed Central) - Aug 7, 2021
DRV/r was associated with greater fat area and lower density of both fat and muscle, and RAL with less intermuscular psoas fat. Higher density psoas and paraspinal musculature were associated with better physical function, suggesting potential clinical relevance of these findings.
- | Selzentry (maraviroc) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD)
Journal: Targeting SARS-COV-2 non-structural protein 16: a virtual drug repurposing study. (Pubmed Central) - Aug 5, 2021
Also, the MD simulation results suggested that the Maraviroc and Raltegravir are more effective drug candidates than Sinefungin for inhibiting the enzyme. It is concluded that Raltegravir and Maraviroc which may be used in the treatment of COVID-19 after Invitro and invivo studies and clinical trial for final confirmation of drug effectiveness.Communicated by Ramaswamy H. Sarma.
- || imatinib / Generic mfg.
FDA event, Review, Journal: Identification of FDA approved drugs against SARS-CoV-2 RNA dependent RNA polymerase (RdRp) and 3-chymotrypsin-like protease (3CLpro), drug repurposing approach. (Pubmed Central) - Aug 5, 2021
Six drugs based on binding energy and number of hydrogen bonds were chosen for the next step of molecular dynamics (MD) simulations to investigate drug-protein interactions (including Nilotinib, Imatinib and dihydroergotamine for 3clpro and Lapatinib, Dexasone and Relategravir for RdRp)...Raltegravir, an anti-HIV drug, was observed to be the best compound against RdRp based on docking binding energy (-9.5 kcal/mole) and MD results...We hope that they can be beneficial for patients with certain specific symptoms of SARS-CoV-2 infection, but they can also probably inhibit viral enzymes. We recommend further experimental evaluations in vitro and in vivo on these FDA-approved drugs to assess their potential antiviral effect on SARS-CoV-2.
- | bezafibrate / Generic mfg.
Journal: Combination antiretroviral therapy improves recurrent primary biliary cholangitis following liver transplantation. (Pubmed Central) - Aug 4, 2021
Herein, we describe the utility of combination antiretroviral therapy to manage rPBC in two patients treated with open label tenofovir/emtricitabine based regimens in combination with either lopinavir or raltegravir. Both patients experienced sustained biochemical and histological improvement with treatment but the antiretroviral therapy was associated with side effects.
- || Isentress (raltegravir) / Merck (MSD)
Clinical, PK/PD data, Journal: Raltegravir pharmacokinetics before and during treatment with ombitasvir, paritaprevir/ritonavir plus dasabuvir in adults with HIV-1 and hepatitis C virus co-infection: AIDS Clinical Trials Group Sub-Study A5334s. (Pubmed Central) - Jul 28, 2021
Both patients experienced sustained biochemical and histological improvement with treatment but the antiretroviral therapy was associated with side effects. The majority of participants' plasma raltegravir exposures were lower after initiation of HCV therapy in co-infected adults; however, confidence intervals were wide.
- || bictegravir (GS-9883) / Gilead
Clinical, Review, Journal: HIV-1 Integrase Inhibitors: A Comparative Review of Efficacy and Safety. (Pubmed Central) - Jul 28, 2021
The newest INSTI, cabotegravir, represents an alternative to oral administration of life-long antiretroviral therapy with the availability of a long-acting injectable formulation. This review summarizes the current use of INSTIs in adults living with HIV, highlighting the similarities and differences within the class related to pharmacodynamics, pharmacokinetics, safety, dosing, and administration that contribute to their role in modern antiretroviral therapy.
- || Triumeq (dolutegravir/abacavir/lamivudine) / ViiV Healthcare, Genvoya (elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide) / Gilead, Isentress (raltegravir) / Merck (MSD)
Clinical, Journal: Evaluation of Kidney Function Tests in HIV-Positive Patients Receiving Combined Antiretroviral Therapy. (Pubmed Central) - Jul 28, 2021
The use of TDF-containing regimens causes renal dysfunction. Therefore, we recommend close monitoring of renal function, especially in patients treated with TDF.
- || Tivicay (dolutegravir) / ViiV Healthcare
Clinical, Journal: Forgiveness of Dolutegravir-Based Triple Therapy Compared With Older Antiretroviral Regimens: A Prospective Multicenter Cohort of Adherence Patterns and HIV-RNA Replication. (Pubmed Central) - Jul 27, 2021
Among PWH with >95% Av-Adh, there were no significant differences in the risk of VR among the different ARVs. These findings support the concept that dolutegravir in combination with 2 other active ARVs achieves greater virological suppression than older ARVs, including raltegravir, NNRTI, and bPI, among PWH with lower adherence.
- | imatinib / Generic mfg., risperidone / Generic mfg., irinotecan / Generic mfg.
Journal: Computational studies on phylogeny and drug designing using molecular simulations for COVID-19. (Pubmed Central) - Jul 20, 2021
Further we performed molecular dynamics simulations to understand the evolution in protein upon interaction with drug. Also, we have performed a phylogenetic analysis of 43 different coronavirus strains infecting 12 different mammalian species.Communicated by Ramaswamy H. Sarma.
- | midazolam hydrochloride / Generic mfg.
Journal: Human variability in isoform-specific UDP-glucuronosyltransferases: markers of acute and chronic exposure, polymorphisms and uncertainty factors. (Pubmed Central) - Jul 14, 2021
The data show that UGT-related uncertainty factors were mostly below the default toxicokinetic uncertainty factor of 3.16, with the exception of five probe substrates (1-OH-midazolam, ezetimibe, raltegravir, SN38 and trifluoperazine), with three of these substrates being metabolised by the polymorphic isoform 1A1. Data gaps and future work to integrate UGT-related variability distributions with in vitro data to develop quantitative in vitro-in vivo extrapolations in chemical risk assessment are discussed.
- || Isentress (raltegravir) / Merck (MSD)
Review, Journal: Not only in silico drug discovery: Molecular modeling towards in silico drug delivery formulations. (Pubmed Central) - Jul 9, 2021
One of the most famous examples is raltegravir, a HIV integrase inhibitor, which was developed after the discovery of a previously unknown transient binding area thanks to molecular dynamics simulations...Such knowledge is a fundamental pillar to perform device engineering and to achieve efficient and safe formulations. After a brief theoretical background, this review aims at discussing the potential of molecular simulations for the rational design of drug delivery systems.
- Tivicay (dolutegravir) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD)
[VIRTUAL] A randomised comparison of DTG-based ART vs standard of care in infants and young children living with HIV weighing 3 to 14kg: results from the ODYSSEY trial () - Jul 8, 2021 - Abstract #IASHIV2021IAS_HIV_1789;
NRTI-backbones in both groups were predominantly ABC/3TC for first-line and ZDV/3TC for second-line... ODYSSEY will provide the first randomised evidence for DTG in infants and young children <14kg; these results are keenly anticipated to support World Health Organization guidelines recommending DTG-based regimens down to 4 weeks of age and 3kg.
- | Isentress (raltegravir) / Merck (MSD)
Trial completion, Enrollment change: RALNOVO: Testing the Effect of Raltegravir on Persistent de Novo HIV Infection in Virologic Responders to Antiretroviral Therapy (clinicaltrials.gov) - Jul 7, 2021
P=N/A, N=120, Completed, Sponsor: University Hospital, Montpellier
ODYSSEY will provide the first randomised evidence for DTG in infants and young children <14kg; these results are keenly anticipated to support World Health Organization guidelines recommending DTG-based regimens down to 4 weeks of age and 3kg. Recruiting --> Completed | N=60 --> 120
- | Isentress (raltegravir) / Merck (MSD)
Preclinical, Journal: Cellular Immune Response Induced by DNA Immunization of Mice with Drug Resistant Integrases of HIV-1 Clade A Offers Partial Protection against Growth and Metastatic Activity of Integrase-Expressing Adenocarcinoma Cells. (Pubmed Central) - Jul 4, 2021
We designed DNA-vaccines against drug-resistant HIV-1 based on consensus clade A integrase (IN) resistant to raltegravir: IN_in_r1 (L74M/E92Q/V151I/N155H/G163R) or IN_in_r2 (E138K/G140S/Q148K) carrying D64V abrogating IN activity...IN-expressing tumors displayed compromised metastatic activity restricted to lungs with reduced metastases size. Protective potential of IN immunogens relied on their immunogenicity for CD8+ T-cells, dependent on proteasomal processing and low level of oxidative stress.
- || Intelence (etravirine) / J&J, Isentress (raltegravir) / Merck (MSD)
Clinical, Journal: Once-daily etravirine/raltegravir (400/800 mg q24h) dual therapy maintains viral suppression over 48 weeks in HIV-infected patients switching from a twice-daily etravirine/raltegravir (200/400 mg q12h) regimen. (Pubmed Central) - Jul 2, 2021
Protective potential of IN immunogens relied on their immunogenicity for CD8+ T-cells, dependent on proteasomal processing and low level of oxidative stress. Switching patients virally suppressed on etravirine/raltegravir q12h to the same regimen but given q24h was highly effective in maintaining virological suppression in HIV-infected patients.
- || Tivicay (dolutegravir) / ViiV Healthcare, Isentress (raltegravir) / Merck (MSD), Vitekta (elvitegravir) / Japan Tobacco, Gilead
Clinical, Journal: The impact of integrase inhibitor-based regimens on markers of inflammation among HIV naïve patients. (Pubmed Central) - Jul 1, 2021
In conclusion, our results provide further data on changes of inflammatory marker levels, especially for the new INSTIs. Our data show that among INSTIs, EVG seems to have a worse impact on inflammation.
- ||| Isentress (raltegravir) / Merck (MSD)
Clinical, P3 data, Journal, Head-to-Head: Standard dose raltegravir or efavirenz-based antiretroviral treatment for patients co-infected with HIV and tuberculosis (ANRS 12 300 Reflate TB 2): an open-label, non-inferiority, randomised, phase 3 trial. (Pubmed Central) - Jun 30, 2021
P3
In patients with HIV given tuberculosis treatment, non-inferiority of raltegravir compared with efavirenz was not shown. Raltegravir was well tolerated and could be considered as an option, but only in selected patients.
- || Prezista (darunavir) / J&J, Isentress (raltegravir) / Merck (MSD)
Biomarker, Clinical, PK/PD data, Journal: Population pharmacokinetics and pharmacogenetics of ritonavir-boosted darunavir in the presence of raltegravir or tenofovir disoproxil fumarate/emtricitabine in HIV-infected adults and the relationship with virological response: a sub-study of the NEAT001/ANRS143 randomized trial. (Pubmed Central) - Jun 28, 2021
Polymorphisms investigated had little impact on study-drug pharmacokinetics. Darunavir/ritonavir + raltegravir may be an appropriate option for patients experiencing NRTI-associated toxicity.
- || Tivicay (dolutegravir) / ViiV Healthcare
PK/PD data, Journal: Prediction of dolutegravir pharmacokinetics and dose optimization in neonates via physiologically based pharmacokinetic (PBPK) modelling. (Pubmed Central) - Jun 26, 2021
Dolutegravir pharmacokinetics were successfully simulated in the neonatal PBPK model. The predictions suggest that during the first 3 weeks of life a 5 mg dose administered every 48 h may achieve plasma exposures needed for therapy and prophylaxis.
- || Isentress (raltegravir) / Merck (MSD)
Clinical, Journal: Impact of genotypic diversity on selection of subtype-specific drug resistance profiles during raltegravir-based therapy in individuals infected with B and BF recombinant HIV-1 strains. (Pubmed Central) - Jun 26, 2021
Alternative resistance pathways to raltegravir develop in subtypes B and F IN genomes, with implications for clinical practice. Evaluating the role of HIV-1 subtype in development and persistence of mutations that confer resistance to INIs will be important to improve algorithms for resistance testing and optimize the use of INIs.
- || Prezista (darunavir) / J&J, Isentress (raltegravir) / Merck (MSD)
Clinical, Journal: Five-year follow-up of patients enrolled in the NEAT 001/ANRS 143 randomized clinical trial: NEAT 001/ANRS 143 LONG TERM study. (Pubmed Central) - Jun 26, 2021
After a median of 5.6 years, subjects initiating ritonavir-boosted darunavir + raltegravir or ritonavir-boosted darunavir + tenofovir disoproxil fumarate/emtricitabine experienced few serious clinical adverse events. Most discontinuations were for reasons unrelated to adverse events or virological failure.
- || Intelence (etravirine) / J&J, Isentress (raltegravir) / Merck (MSD)
Clinical, Journal: Characterization of viral rebounds on dual etravirine/raltegravir maintenance therapy (ANRS-163 ETRAL trial). (Pubmed Central) - Jun 26, 2021
The dual etravirine/raltegravir regimen as maintenance therapy was effective and the emergence of mutations in cases of VF was similar to that seen in other dual-regimen studies. No HIV-DNA level modification was evidenced by Week 96.
- || Tivicay (dolutegravir) / ViiV Healthcare
Retrospective data, Review, Journal: HIV-1 integrase resistance associated mutations and the use of dolutegravir in Sub-Saharan Africa: a systematic review and meta-analysis protocol. (Pubmed Central) - Jun 26, 2021
Results will therefore help in setting-up baseline data for an optimal management of people living with HIV as Sub-Saharan African countries are transitioning to dolutegravir-based regimens. Evidence will also support HIV/AIDS programs in identifying gaps and actions to be undertaken for improved long-term care and treatment of people living with HIV in Sub-Saharan Africa.