raltegravir / Generic mfg. - LARVOL DELTA

From immune signatures to vaccine mimetics: A systems pharmacology–driven medicinal chemistry framework for host-directed antiviral discovery | Poster Board #D05 (ACS-Fall 2026) - "Prioritized candidates included epigenetic modulators, kinase pathway activators, and antivirals such as raltegravir and lopinavir...Using BCG-induced trained immunity as a representative host-response paradigm, this study demonstrates the translation of protective immune signatures into candidate antiviral small molecules. These findings establish a generalizable AI-ready framework for host-directed antiviral drug discovery, enabling the rational design and prioritization of broad-spectrum small molecule therapeutics with the potential to mitigate viral resistance."

Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Incidence of neonatal sepsis among HIV exposed neonates of mothers on integrase strand transfer inhibitors in sub-Saharan Africa: a systematic review and meta-analysis. (PubMed, BMC Infect Dis) - "INSTI-based ART was not associated with a significant difference in neonatal sepsis risk compared with non-INSTI regimens. However, the low number of events limited the precision of the estimates, highlighting the need for further research."

Clinical • Journal • Retrospective data • Review • Diabetes • Human Immunodeficiency Virus • Infectious Disease • Novel Coronavirus Disease • Septic Shock

National cross-sectional survey on acquired HIV drug resistance in Haiti in 2023: warnings resistance to dolutegravir (AIDS 2026) - "3.77% of HIVs were resistant to dolutegravir and bictegravir, 4.4% to cabotegravir, 4.72% to raltegravir, and 5.03% to elvitegravir. Additionally, 15.19% of the viral strains were resistant to abacavir, 13.92% to lamivudine and emtricitabine, 6.65% to zidovudine, 8.23% to stavudine and didanosine, and 4.13% to tenofovir...Furthermore, some HIVs strains developed resistance against efavirenz (49.37%), nevirapine (50%), Rilpivirine (20.25%), Etravirine (12.66%), and doravirine (3.61%). Finally, HIV genome resistance was 0.63% against atazanavir/ritonavir and indinavir/ritonavir, 0.95% against lopinavir/ritonavir and 0.32% against darunavir/ritonavir. HIV acquired pharmacoresistance is moderate in Haiti and requires innovating adapted strategy for preventing its development, its transmission, and for protecting PLHIV health, while emphasizing on children and male individuals."

Human Immunodeficiency Virus • Infectious Disease • Respiratory Diseases

Sustained HIV-1 remission following CCR5 delta32/delta32 allogeneic hematopoietic stem cell transplantation: the Kansas City patient (AIDS 2026) - "The gray shaded area indicates time on ART (raltegravir, emtricitabine/tenofovir, darunavir/cobicistat; then bictegravir, emtricitabine, tenofovir)...AlloHSCT, which occurred in October 2020 following myeloablative conditioning (busulfan/cyclophosphamide), led to full donor chimerism and remission... We report HIV-1 remission sustained for 14 months following ATI in our patient post alloHSCT from a CCR5 delta32/delta32 donor. Ongoing monitoring will further determine HIV reservoir eradication."

Clinical • Late-breaking abstract • Acute Graft versus Host Disease • Acute Myelogenous Leukemia • Bone Marrow Transplantation • Gastrointestinal Disorder • Graft versus Host Disease • Hematological Malignancies • Human Immunodeficiency Virus • Immunology • Infectious Disease • Leukemia • Transplantation • CCR5 • CD34

Cross-resistance to second-generation INSTI after raltegravir-based regimen failure in children living with HIV under 14 years of age (AIDS 2026) - "Pediatric formulations of protease inhibitors are not available, the supply of nevirapine oral solution is intermittent, and raltegravir is the only INSTI available in a pediatric formulation for children weighing <20 kg. In this group of children who experienced failure on a raltegravir-based regimen, cross-resistance to second-generation integrase inhibitors was high, reaching approximately 77%, with 44% of cases showing high-level or intermediate-level resistance. Raltegravir is the drug of choice for the management of children living with HIV under 12 years of age in Colombia; however, it is not recommended in international pediatric treatment guidelines, except for use in infants younger than 30 days, with a recommendation to switch to dolutegravir after this age. In Colombia, the lack of access to second-generation INSTIs for children weighing less than 20 kg has negatively affected the achievement of virologic control, allowed the development of resistance at..."

Clinical • Human Immunodeficiency Virus • Infectious Disease

High frequency of raltegravir resistance mutations in children living with HIV with virological failure in Northeast Brazil (AIDS 2026) - "A high prevalence of RAL resistance mutations was observed among individuals with virological failure, indicating substantial compromise of this first-generation INSTI. These findings highlight the need for systematic resistance surveillance and reinforce the importance of resistance testing to guide ART optimisation in children, particularly in settings with early and widespread INSTI use."

Clinical • Human Immunodeficiency Virus • Infectious Disease

National-level prospective longitudinal study on the dynamics of HIV-1 drug resistance in Taiwan, 2017–2024 (AIDS 2026) - "NNRTI-associated mutations remained the most frequent. The INSTI-associated mutations might be affected by the selection and development of INSTIs. Prevalence increased from 2018 to 2021; raltegravir use might be the key factor."

Clinical • Longitudinal study • Observational data • Human Immunodeficiency Virus • Infectious Disease

Deep sequencing unveils underestimated burden of integrase inhibitor resistance: a global individual participant data meta-analysis (AIDS 2026) - "BACKGROUND: Integrase strand transfer inhibitors (INSTIs), particularly second-generation agents like dolutegravir (DTG), are the cornerstone of global antiretroviral therapy (ART)...IPD analysis revealed that treated PLWH exhibited significantly elevated intermediate- to high-level resistance to first-generation agents (raltegravir/elvitegravir)... Conventional surveillance significantly underestimates the global burden of INSTI resistance by failing to detect low-frequency variants. This "hidden reservoir" of resistance (3.61% PDRMs and 2.46% ADRMs missed) poses a threat to the long-term success of INSTI-based programs, potentially facilitating the silent transmission of resistant strains and compromising long-acting regimens. Standardized deep sequencing surveillance is essential to accurately monitor evolving resistance patterns and guide clinical decision-making worldwide."

Retrospective data • Human Immunodeficiency Virus • Infectious Disease

HIV resistance to integrase strand-transfer inhibitors: a disproportionality analysis using the WHO global safety database (AIDS 2026) - " We carried out a disproportionality analysis to assess resistance to bictegravir, cabotegravir, dolutegravir, elvitegravir and raltegravir using the WHO global database of individual case safety reports (ICSRs), VigiBase®, as a data source. HIV resistance was differentially reported for the first- and second-generation INSTIs. The findings corroborate the WHO recommendations for continuous monitoring of HIV resistance to INSTIs, aiming to detect, control, and prevent this outcome, while expanding the use of this class of drugs."

Clinical • Human Immunodeficiency Virus • Infectious Disease

Unveiling the Black Box: explainable deep learning reveals novel accessory mutations driving raltegravir resistance in HIV-1 integrase (AIDS 2026) - "This study validates Explainable AI for predicting HIV-1 resistance, uncovering critical accessory mutations (T97, L74, M50) that drive treatment failure. These markers warrant elevated weight in clinical scoring. Our interpretable framework bridges the gap between computational power and clinical trust, enabling precise, AI-driven salvage therapies."

Human Immunodeficiency Virus • Infectious Disease

Outcomes for persons with triple-class resistant HIV and a history of virologic failure. (PubMed, Int J Antimicrob Agents) - "Although the most common outcome after TRIO was switch to another ≥3 drug regimen, almost one third of virologically suppressed PWH under TRIO (with a history of multi-drug resistance) switched to a drug-reducing regimen, the majority of whom maintained suppression."

Journal • Human Immunodeficiency Virus • Infectious Disease

Selection of Mutations in HIV-1 Nucleocapsid and Integrase in Individuals Living with HIV Experiencing Virologic Failure After Initiating or Switching to Tenofovir-Lamivudine-Dolutegravir. (PubMed, medRxiv) - "Site-directed NC and IN mutants were tested for susceptibility to DTG, raltegravir and cabotegravir in the TZM-bl HIV-1 indicator cell line and evaluated for infectivity and replication in multi-round assays. This work provides the first clinical evidence of NC mutation selection in individuals on failing TLD ART and shows that NC mutations, combined with IN mutations, can further decrease susceptibility to DTG. Our findings support additional investigations of the contributions of mutations outside of IN to virologic failure of integrase inhibitor-containing ART regimens."

Journal • Human Immunodeficiency Virus • Infectious Disease

Antiproliferative effects of HIV integrase strand transfer inhibitors in experimental models for cancer research: A narrative review. (PubMed, J Pharmacol Exp Ther) - "Preclinical studies describe as INSTIs, including dolutegravir, raltegravir, cabotegravir, and elvitegravir and some 1,2,3-triazole derivatives, can inhibit the growth of various cancer cell lines and some of them seem to also have direct inhibitory effects on human endogenous retrovirus reactivation. SIGNIFICANCE STATEMENT: Currently, the effects of using integrase strand transfer inhibitors (INSTIs) on cancer development in people living with HIV are difficult to determine because of the multifactorial cause of cancer in these patients and the long period in which cancer manifests. This review examines the antiproliferative properties of INSTIs, describing the proposed mechanisms through which they may exert this effect in preclinical studies."

Journal • Review • Human Immunodeficiency Virus • Infectious Disease • Oncology

Generation and evaluation of an EcoHIV mouse model to study HIV-1 integration and expression. (PubMed, Virology) - "The immunofluorescence staining indicated EcoHIV can be efficiently transmitted from infected CD4 + T cells to macrophages in vitro and EcoHIV expression was effectively inhibited by Abacavir and Raltegravir. Importantly, BLI data demonstrate that EcoHIV establishes latent reservoirs -like state in mice which can be reactivated by LRA treatment. Altogether, our model provides a valuable platform for the controlled study of HIV entry, integration, transmission, latency within tissue-resident compartments under ART and for the preclinical evaluation of latency-reversing and curative strategies."

Journal • Preclinical • Hematological Malignancies • Human Immunodeficiency Virus • Infectious Disease • Leukemia • Oncology • CD4

Impact of Raltegravir on the Viral Reservoirs (clinicaltrials.gov) - P=N/A | N=0 | Withdrawn | Sponsor: Centre Hospitalier Universitaire de Nice | N=20 ➔ 0 | Unknown status ➔ Withdrawn

Enrollment change • Trial withdrawal • Human Immunodeficiency Virus • Infectious Disease • CD4

Chemoinformatic Approaches to Identify Bioactive Inhibitors Against Type I Dehydroquinase (DHQ1) Enzyme of Typhoidal Salmonella. (PubMed, Bioinform Biol Insights) - "A total of 10 ligands were selected with the highest binding affinities ranging from -9.8 to -9.1 (kcal/mol), ie, Cabotegravir, Imatinib, Prulifloxacin, Limonin, Silibinin, Atovaquone, Betamethasone Valerate, GSK1324726A, Isavuconazole, and Raltegravir. Molecular dynamic simulations were used to verify the stability of the protein "DHQ1" docked with 3 hit ligands Cabotegravir, Limonin, and Silibinin by calculating root mean square fluctuation (RMSF), root mean square deviation (RMSD), radius of gyration (Rg), H-bond interaction, and molecular mechanics/generalized Born surface area (MM/GBSA) scores. Based on molecular dynamic (MD) simulations, it is reported that Cabotegravir and Limonin showed the optimal binding features with bacterial DHQ1 enzyme and can be deemed as a repurposed drug candidate as compared to Silibinin, which did not show favorable interactions with DHQ1 and needs to be explored further against typhoidal Salmonella."

Journal • Infectious Disease

HIV resistance to integrase strand-transfer inhibitors: disproportionality analysis of individual case safety reports from the WHO global safety database (VigiBase). (PubMed, Curr Med Res Opin) - "Disproportionality signals for drug resistance were observed for all first-generation (ROR= 52.5; CI 95% = 47.6-57.9; IC = 5.56; 95% CI = 5.4-5.7 - raltegravir) and second-generation INSTIs (ROR = 55.9; CI 95% = 50.8-61.5; IC = 5.65; 95% CI = 5.5-5.8 - dolutegravir). These findings should be interpreted with caution given the inherent limitations of spontaneous reporting. Resistance monitoring in clinical settings is relevant."

Journal • Human Immunodeficiency Virus • Infectious Disease

Weight Gain on Contemporary Integrase Strand Transfer Inhibitors and Tenofovir Alafenamide in Persons with HIV Starting Antiretroviral Therapy in the United States and Canada. (PubMed, J Infect Dis) - "Weight gain with non-EFV NNRTIs was lower than with PIs and INSTIs, with the greatest increases observed among Black females starting TAF with contemporary INSTIs."

Journal • Human Immunodeficiency Virus • Infectious Disease

Use of Integrase Strand Transfer Inhibitors Among Children Living With HIV in Latin America and the Caribbean. (PubMed, Pediatr Infect Dis J) - "INSTI use among children has increased in parts of Latin American And Caribbean. As more children start INSTI regimens, further research is needed on their clinical impact."

Journal • Human Immunodeficiency Virus • Infectious Disease

Pharmacogenomics of current antiretroviral drugs. (PubMed, Pharmacogenomics) - "We searched Pharmacogenomics Knowledgebase (PharmGKB®) for abacavir, tenofovir disoproxil fumarate, tenofovir alafenamide, lamivudine, emtricitabine, dolutegravir, elvitegravir, raltegravir, bictegravir, cabotegravir, atazanavir/ritonavir, darunavir/ritonavir, lopinavir/ritonavir, lenacapavir, rilpivirine and doravirine. Actionable pharmacogenetic associations with antiretroviral drugs remain limited to abacavir. Future research should prioritize replicating pharmacogenetic associations across diverse populations and establishing clinical relevance."

Biomarker • Journal • Review • Human Immunodeficiency Virus • Infectious Disease • HLA-B • UGT1A1

Myalgic Encephalomyelitis/Chronic Fatigue Syndrome: Successful Therapeutic Plasma Exchange Treatment After SARS-CoV-2 Infection-A Case Report. (PubMed, Clin Case Rep) - "More recently, in the context of SARS-CoV-2 infection, potential pathophysiological overlaps and disease modulation have been hypothesized. Our successful case highlights the need to investigate novel therapeutic approaches, including plasma exchange."

Journal • CNS Disorders • Fatigue • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

EXPRESS: Clinical and virological effects of the integrase inhibitor raltegravir in cats with naturally progressive feline leukaemia virus infection. (PubMed, J Feline Med Surg) - "A definitive virological or survival benefit, however, could not be demonstrated. Longer-term, controlled studies-potentially within multimodal antiviral strategies-are warranted to further define its therapeutic role."

Journal • Hematological Malignancies • Infectious Disease • Leukemia • Lymphoma • Oncology

Raltegravir Plasma Exposure: A Machine Learning-Based Model for its Prediction Using Limited Sampling Strategy. (PubMed, AAPS J) - "A machine learning model using only three sampling timepoints has been developed and validated in different datasets, enabling accurate estimation of RAL AUC₀-₁₂. This approach provides a tool for pharmacokinetic and PK/PD studies and reduces intensive sampling need in clinical settings."

Journal

Downregulation of claudin-2 expression and chemoresistance by saquinavir in human lung adenocarcinoma cells. (PubMed, Eur J Pharmacol) - "In contrast, ritonavir, another HIV protease inhibitor, or raltegravir, an HIV integrase inhibitor, has no significant effect, indicating that inhibition of viral enzymes is not directly involved in the regulation of CLDN2 expression. Notably, SQV enhanced the cytotoxic effects of multiple anticancer agents, including doxorubicin, cisplatin, and SN-38, in lung adenocarcinoma cell line-derived spheroids and patient-derived organoids. We suggest that SQV improves chemoresistance by reducing CLDN2 expression and oxidative stress in lung adenocarcinoma."

Journal • Human Immunodeficiency Virus • Infectious Disease • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • CLDN2 • NFE2L2

The Monitoring of Vertical Transmission of HIV in the Northeastern Romania Cohort-A Continuing Challenge. (PubMed, Medicina (Kaunas)) - "All women delivered by elective cesarean section, and all infants received neonatal antiretroviral prophylaxis, with Raltegravir added in selected higher-risk situations...In northeastern Romania, PVT programs remain highly effective when maternal viral suppression is achieved. Residual transmission was confined to situations of maternal viremia driven by ART non-adherence, highlighting the continued importance of adherence support during pregnancy."

Journal • Observational data • Retrospective data • Human Immunodeficiency Virus • Infectious Disease • Obstetrics • Pediatrics