bictegravir (GS-9883) / Gilead - LARVOL DELTA

Baseline and week 48 resistance analysis in participants receiving bictegravir + lenacapavir in the phase 2 ARTISTRY-1 study. (PubMed, AIDS) - "Despite high frequencies of baseline resistance, substantial rates of viral suppression were maintained through Week 48 and no on-treatment resistance to study drugs was detected. These findings support the development of once-daily BIC + LEN STR to improve and optimize treatment options in individuals on complex ART."

Journal • P2 data • Human Immunodeficiency Virus • Infectious Disease

Bictegravir's effect on persistent low-level viraemia and immunological response: BELAIR study: a pilot prospective observational study (ESCMID Global 2026) - No abstract available

Clinical • Observational data • Gene Therapies • Human Immunodeficiency Virus • Infectious Disease

A 48-week, Randomized Controlled Trial of Doravirine for Individuals with HIV and Obesity on Integrase Inhibitors and Tenofovir Alafenamide: The Do IT Study (ACTG A5391). (PubMed, Clin Infect Dis) - P4 | "In people with HIV and obesity, switching from an INSTI+TAF/FTC regimen to DOR/FTC with either TAF or TDF did not produce clinically meaningful differences in weight change or metabolic health after 48 weeks."

Journal • Genetic Disorders • Human Immunodeficiency Virus • Infectious Disease • Obesity

Two cases of possible transmitted HIV drug resistance to all currently available integrase inhibitors, the Netherlands, 2025. (PubMed, Euro Surveill) - "The cases are not phylogenetically linked, representing two independent introductions of integrase inhibitor resistant HIV into the Dutch population. These observations highlight the need for strengthened surveillance and prevention efforts in Europe and globally."

Journal • Human Immunodeficiency Virus • Infectious Disease

Virological Failure on Long-Acting Injectable Cabotegravir and Rilpivirine: An Analysis of Subtypes, Drug Levels, Resistance, and Therapeutic Implications. (PubMed, Clin Infect Dis) - "Emergent resistance in VF cases often resulted in cross-resistance to other nonnucleoside reverse transcriptase inhibitors and integrase strand transfer inhibitors. Although most cases did not meet the high-risk profile as defined by registration trials, subtype A lineages were overrepresented. Low drug levels were not elevated versus treatment successes. These data suggest that subtype-specific factors beyond A6 may influence VF risk and merit further study."

Journal

Prioritization of adverse events related to integrase inhibitors and NNRTIs: a disproportionality analysis using data from the FAERS database. (PubMed, J Antimicrob Chemother) - "This study provides a systematic framework for evaluating post-marketing AEs of INSTIs and NNRTIs using a semi-quantitative scoring system. Our findings identified five high-priority AEs that require clinical validation and further investigation."

Adverse events • Journal • Eosinophilia • Hematological Disorders • Hepatology • Human Immunodeficiency Virus • Infectious Disease • Liver Failure

Switch to single-tablet bictegravir-lenacapavir from a complex HIV regimen (ARTISTRY-1): a randomised, open-label, phase 3 clinical trial. (PubMed, Lancet) - P2/3 | "Bictegravir-lenacapavir STR demonstrated non-inferior efficacy to complex regimens, with a similar safety profile and increased treatment satisfaction. Bictegravir-lenacapavir offers new opportunities for HIV-1 treatment optimisation for people taking complex regimens."

Journal • P3 data • Human Immunodeficiency Virus • Infectious Disease

Pharmacovigilance study of INSTIs associated with weight gain and glucose/lipid metabolism adverse events based on the FDA adverse event reporting system. (PubMed, HIV Med) - "This study identified metabolic AEs associated with INSTIs, with agent-specific differences in risk and timing, highlighting the need for regular monitoring and individualized management during INSTI-based ART."

Adverse events • Journal • Dyslipidemia • Human Immunodeficiency Virus • Infectious Disease • Metabolic Disorders

Metabolic dysfunction-associated steatotic liver disease linked to antiretroviral exposure in cohort of people with HIV. (PubMed, AIDS) - "Our findings suggest that commonly used antiretrovirals may contribute to the development of MASLD. Prospective studies examining the possible causal effects of these therapies on MASLD development and progression are warranted."

Journal • Diabetes • Hepatology • Human Immunodeficiency Virus • Infectious Disease • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease

Sex and gender differences in weight gain associated with second-generation integrase strand transfer inhibitors: A scoping review. (PubMed, HIV Med) - "Second-generation INSTIs, especially dolutegravir, appear to be associated with greater average and excessive weight gain among cis women, although this effect varies by setting, regimen and clinical context. Further research, especially in diverse populations, is needed to explore underlying mechanisms, determine risk factors and evaluate these trends in newer antiretroviral medications."

Journal • Review • Human Immunodeficiency Virus • Infectious Disease

Exploring the impact of Cabotegravir-Rilpivirine long-acting on weight gain, body composition and quality of life in adults living with HIV. (PubMed, HIV Med) - "CAB + RPV LA was not associated with significant weight gain, clinically relevant changes in body composition or adverse metabolic effects over 48 weeks. Virologic suppression was maintained, renal laboratory parameters improved in prior INSTI users and treatment was well tolerated with increasing satisfaction. These findings support CAB + RPV LA as a safe, effective and metabolically neutral alternative to daily oral ART."

HEOR • Journal • Dyslipidemia • Fibrosis • Human Immunodeficiency Virus • Immunology • Infectious Disease

Reversible Severe Hyperglycemia Without Ketoacidosis After Initiation of Bictegravir-containing Antiretroviral Therapy. (PubMed, AACE Endocrinol Diabetes) - "Incorporating metabolic monitoring (glycemia, weight, and lipid profile) and patient education for BIC into clinical practice, and utilizing a multidisciplinary team, can reduce the risk of acute hyperglycemia and glycemia-related hospitalization. Patients starting a BIC-containing ART who have a history of obesity and/or dysglycemia should be educated and monitored for risk of developing acute hyperglycemia, which can be reversed upon BIC discontinuation."

Journal • Diabetes • Genetic Disorders • Human Immunodeficiency Virus • Infectious Disease • Metabolic Disorders • Obesity • CD4

Bictegravir concentrations in breastmilk of healthy, lactating women without HIV. (PubMed, J Antimicrob Chemother) - "Exposure to bictegravir through breastmilk is very low, with a relative infant dose below 1%. Even though metabolizing capacity in newborns is not yet fully developed, it is not expected to cause infant toxicity."

Journal • Human Immunodeficiency Virus • Infectious Disease

Resistance to second-generation integrase inhibitors in people with HIV following treatment failure on dolutegravir- or bictegravir-based ART in Taiwan. (PubMed, J Antimicrob Chemother) - "Although RAMs to second-generation INSTIs may be detected during treatment failure, the overall prevalence remains low for both dolutegravir- and bictegravir-based ART. Viral resuppression can be achieved through salvage therapy or continued use of second-generation INSTI-based regimens."

Journal • Retrospective data • Human Immunodeficiency Virus • Infectious Disease • CD4

An ultra-long-acting dimeric bictegravir prodrug defined by a short pharmacokinetic tail. (PubMed, Nat Commun) - "NMXBIC's physicochemical properties and high BIC loading/unit mass of the prodrug contribute to its unique ULA PK profile. These results support its development as a ULA formulation for HIV-1 treatment and prevention."

Journal • PK/PD data • Human Immunodeficiency Virus • Infectious Disease

Prediction of interactions between the SARS-CoV-2 ORF3a protein and small-molecule ligands using the ANDSystem cognitive platform, graph neural networks, and molecular modeling. (PubMed, Vavilovskii Zhurnal Genet Selektsii) - "Localization analysis showed that the binding sites of bictegravir and 4-(benzoylamino)benzoic acid lie in a cytosolic surface pocket of the protein that is solvent-exposed; L-threonine binds within the intersubunit cleft of the dimer; and austocystin D and N-acetyl-D-glucosamine are positioned at the boundary between the cytosolic surface and the transmembrane region. The accessibility of these binding sites may be reduced by the influence of the lipid bilayer. The binding energetics for bictegravirum were more favorable than for 4-(benzoylamino)benzoic acid (docking score -7.37 kcal/mol; MM/GBSA ΔG -14.71 ± 3.12 kcal/mol), making bictegravirum a promising candidate for repurposing as an ORF3a inhibitor."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Longitudinal analysis of metabolic changes in people with HIV on integrase inhibitor-based versus efavirenz-based therapy: a prospective real-world cohort study in China. (PubMed, BMC Infect Dis) - "INSTI-based ART was associated with sustained weight gain but did not worsen long-term dyslipidemia compared to an EFV-based regimen in a real-world setting. Hepatic steatosis correlated with metabolic parameters rather than INSTI exposure."

Journal • Real-world evidence • Dyslipidemia • Human Immunodeficiency Virus • Infectious Disease • Metabolic Disorders

Switch to BIC/TAF/FTC or DTG + TDF/FTC in virologically suppressed PWH: outcomes in real-world setting with and without tenofovir resistance. (PubMed, Clin Infect Dis) - P | "in a real-world setting, switching to BIC/TAF/FTC or DTG + TDF/FTC in PWH with virological success was associated with a non-significant risk of VF, but M184V or M184I mutations and tenofovir resistance had no effect on VF. Most VF were blips or related to unmeasured adherence issues."

Journal • Real-world evidence • Human Immunodeficiency Virus • Infectious Disease

Real-Life Long-Term Weight Trends After Switching to INSTI-Based Therapy in People Living with HIV: A 12-Year Retrospective Cohort Study. (PubMed, New Microbiol) - "Switching from PI- to INSTI-based cART in virologically suppressed PLWH is associated with modest but sustained increases in body weight and BMI over time, without evident deterioration in metabolic health. These results support the favourable safety profile of INSTIbased regimens while underscoring the need for routine anthropometric monitoring and preventive lifestyle interventions during long-term therapy."

Journal • Retrospective data • Human Immunodeficiency Virus • Infectious Disease

Localized inflammasome inhibition mitigates foreign body response to subcutaneous long-acting antiretroviral therapy for HIV. (PubMed, J Control Release) - "In this study, we incorporated MCC950, a selective NLRP3 (NOD-, LRR-, and pyrin domain-containing protein 3) inhibitor, into a subcutaneous nanofluidic implant co-delivering TAF and bictegravir (BIC)...Sustained plasma levels of both drugs were maintained for up to 45 days, and imaging mass cytometry and histological analyses confirmed localized immunomodulation. These findings establish inflammasome inhibition as a viable strategy to improve the safety and tolerability of subcutaneous LA-ART and lay the groundwork for future immunomodulatory-enhanced drug delivery systems."

Journal • Fibrosis • Human Immunodeficiency Virus • Immunology • Infectious Disease • Inflammation • NLRP3

Despite increasing use of integrase inhibitors to treat HIV infection, resistance to this class remains stable. (PubMed, J Antimicrob Chemother) - "Although the use of INSTIs has increased over time with differences in the duration of use, we did not observe a corresponding increase in the proportion of ARV-treated PLWHIV who experienced virological failure with INSTI-resistant viruses during the study period."

Journal • Human Immunodeficiency Virus • Infectious Disease

Bictegravir's effect on persistent low-level viremia and immunological response. BELAIR study: A pilot prospective observational study. (PubMed, Int J STD AIDS) - "A significant gradual elevation of CD4/CD8 ratio was also observed (0.51 ± 0.30 before switch vs 0.69 ± 0.35 at 12 months, p < 0.001).ConclusionThe results of the present study indicate that BIC/TAF/FTC may improve the immunological response and reduce the proportion of PWHIV experiencing persistent LLV. Further studies in larger patient series are needed to determine the full beneficial role of bictegravir."

Journal • Observational data • Human Immunodeficiency Virus • Infectious Disease • CD4 • CD8

AI-driven discovery of antiretroviral drug bictegravir and etravirine as inhibitors against monkeypox and related poxviruses. (PubMed, Commun Biol) - "These findings support the repurposing of bictegravir and etravirine for treating mpox, especially for patients co-infected with HIV, warranting follow-up clinical investigation. The established AI pipeline and our antiviral drug discovery strategies bear major implications for responding to the ongoing mpox emergency and preparing for future poxvirus epidemics."

Journal • Human Immunodeficiency Virus • Infectious Disease

Canadian guideline on HIV pre- and postexposure prophylaxis: 2025 update. (PubMed, CMAJ) - "Multiple safe, effective PrEP and PEP regimens are now available in Canada, making it increasingly possible to find suitable options for all who could benefit. Implementation of this guideline should expand access to biomedical HIV prevention interventions for those at risk and decrease the incidence of HIV in Canada."

Clinical guideline • Journal • Human Immunodeficiency Virus • Infectious Disease

Differential adipose tissue remodeling and metabolic effects of dolutegravir and bictegravir: implications for HIV therapy. (PubMed, Biomed Pharmacother) - "Collectively, these findings demonstrate that DTG and BIC exert distinct yet overlapping influences on adipogenesis and WAT biology that might contribute to metabolic alterations in PWH. Understanding these mechanisms is essential for optimizing long-term HIV treatment strategies and mitigating the cardiometabolic risk associated with modern antiretroviral regimens."

Journal • Human Immunodeficiency Virus • Infectious Disease • Metabolic Disorders