- |||||||||| Vocabria (cabotegravir oral) / ViiV Healthcare, Edurant (rilpivirine) / J&J
PK/PD data, Journal: Cabotegravir pharmacokinetics in Asian population with and without HIV. (Pubmed Central) - Jul 2, 2025 No dose adjustment is recommended for Asian populations with and without HIV. Cabotegravir pharmacokinetic data from any Asian country/region may guide pharmacokinetic evaluation and regulatory considerations across Asian regions.
- |||||||||| Edurant (rilpivirine) / J&J
Journal: Rilpivirine Ionic Liquid Nanoemulsion Augments the Oral Bioavailability of Rilpivirine and Its Delivery to the HIV Sanctuary Sites. (Pubmed Central) - May 20, 2025 Furthermore, compared to the RPV suspension, both SNES formulations containing RPV-Doc resulted in significantly higher and sustained RPV levels in the HIV sanctuary sites such as mesenteric lymph nodes and the brain. Taken together, our innovative approach can be used to improve the oral bioavailability and tissue penetration of RPV, which can eventually result in a reduction in the pharmacokinetic variability and therapeutic dose of RPV leading to optimal drug utilization.
- |||||||||| Edurant (rilpivirine) / J&J, Rekambys (rilpivirine LA) / J&J, Cabenuva (cabotegravir long acting/rilpivirine long acting) / J&J, GSK, ViiV Healthcare, Pfizer, Shionogi
Clinical data, Journal, Real-world evidence: Clinical Outcomes and Perspectives of People With Human Immunodeficiency Virus Type 1 Twelve Months After Initiation of Long-acting Cabotegravir and Rilpivirine in an Observational Real-world US Study (BEYOND). (Pubmed Central) - Apr 30, 2025 Proportions of participants reporting "always" or "often" experiencing challenges related to HIV-1 treatment (fear of disclosure, adherence anxiety, reminder of HIV-1 status, and feeling stigmatized) decreased from baseline to month 12. Month 12 results from the real-world BEYOND study support the effectiveness of CAB + RPV LA for maintenance of virologic suppression and as a preferred treatment option for people with HIV-1.
- |||||||||| Edurant (rilpivirine) / J&J, Tivicay (dolutegravir) / ViiV Healthcare
New challenges and molecular approaches to adipose damage associated with obesogenic medications () - Apr 21, 2025 - Abstract #ECO2025ECO_739; Our studies show that DTG strongly alters adipocyte functionality, acting mainly at the mitochondrial level as well as on lipid and glucose metabolism. Finally, TSP1 serum levels in DTG-treated patients infected with HIV could represent a potential biomarker of adipose tissue dysfunction.
- |||||||||| Edurant (rilpivirine) / J&J, Cabenuva (cabotegravir long acting/rilpivirine long acting) / J&J, GSK, ViiV Healthcare, Pfizer, Shionogi
Clinical, Journal: Early Experience and Effectiveness of Long-Acting Injectable Cabotegravir and Rilpivirine in a South Side Chicago HIV Clinic. (Pubmed Central) - Mar 12, 2025 In a pharmacy-led model, 118 (18%) people with HIV were referred and 78 (12%) initiated long-acting injectable cabotegravir/rilpivirine from 1 January 2021 to 31 May 2023. Implementation, especially for people with HIV who were not virally suppressed, requires further support for patients, providers, and clinic systems.
- |||||||||| Observational data, Journal: Change in weight and BMI associated with switching to bictegravir/emtricitabine/tenofovir alafenamide versus a dolutegravir-based regimen among virologically suppressed adults living with HIV through 144 weeks. (Pubmed Central) - Mar 12, 2025
This observational study collected demographics, clinical characteristics, weight, and BMI from virologically suppressed adults switched to BIC/emtricitabine/tenofovir alafenamide (TAF), emtricitabine/TAF plus DTG, DTG/abacavir/lamivudine, DTG/rilpivirine (RPV), and DTG/lamivudine 2 years prior to switch through 144 weeks post-switch...DTG plus emtricitabine/TAF switches had the highest annualized weight gain (0.68?kg/year, 95% confidence interval: -0.32, 1.65) whereas, DTG/RPV switches had the lowest annualized weight gain (-2.22?kg/year, 95% confidence interval: -3.69, -0.62) post-switch...Baseline BMI?<?18.5?kg/m2 was associated with the highest annualized weight gain post-switch, whereas switching from protease inhibitors and self-report of dieting were associated with the lowest annualized weight gain post-switch. At week 144, switching to a BIC versus DBR were both associated with lower annualized weight gain post-switch among a large and diverse cohort of treatment-experienced people living with HIV.
- |||||||||| In Vitro Modulation of Adipocyte Differentiation by TAF/TDF After Challenge With New ARV Regimens (Poster Hall) - Mar 3, 2025 - Abstract #CROI2025CROI_1371;
Background We previously demonstrated in a 3T3L1cells in vitro model of adipogenesis, that Integrase Strand Transfer Inhibitors (INSTI) increase adipogenesis, while, tenofovir alafenamide fumarate (TAF) and tenofovir disoproxil fumarate (TDF), displayed an inhibitory effect, counteracting increased adipogenesis caused by INSTIs [dolutegravir (DTG), bictegravir (BIC)]...Methods We used a 3T3-L1 cells in vitro model of adipogenesis to study the effects on adipocyte differentiation of the NNRTIs doravirine (DOR) and rilpivirine (RPV), alone or in combination with the previously evaluated DTG and the newer INSTI cabotegravir (CAB), or TDF or TAF...Furthermore, NNRTIs and CAB enhanced the expression levels of ER-TR7 compared to control, being the combination DTG+DOR less effective in this activity. Conclusions Our data support the evidence that in-vitro challenge of 3T3-L1 cells with INSTIs and NNRTIs is able to increase adipocytic differentiation and to drive a number of these cells toward the expression of fibroblastic features, whereas TAF and TDF when combined to different ARV have an antagonistic role on this phenomenon confirming our previous report.
- |||||||||| Edurant (rilpivirine) / J&J, Isentress (raltegravir) / Merck (MSD)
Molecular Epidemiology of HIV-1 Transmitted Drug Resistance Among Subtypes Circulating in Italy (Poster Hall) - Mar 3, 2025 - Abstract #CROI2025CROI_914; However, the impact of the detected TDR on the susceptibility to currently recommended first-line regimens is negligible. NGS genotyping can improve the characterization of transmission networks of resistance, allowing the detection of TC harbouring minority-resistant species not detectable with Sanger.
- |||||||||| Edurant (rilpivirine) / J&J
Rilpivirine Drug-Resistant Mutations in Experienced Patients in Mexico: Impact on Long-Acting ART (Poster Hall) - Mar 3, 2025 - Abstract #CROI2025CROI_912; Conclusions This retrospective analysis indicates that rilpivirine DRMs are common in a setting wherein NNRTI-based treatment was widely implemented, and has implications for operational implementation of CAB/RPV LA. Screening for existing DRMs is logistically and technically challenging in Mexico and could be a barrier to use of CAB/RPV LA.
- |||||||||| Vocabria (cabotegravir oral) / ViiV Healthcare, Edurant (rilpivirine) / J&J, Pifeltro (doravirine) / Merck (MSD)
HIV-1 Drug Resistance Trends in the Era of Modern Antiretrovirals: 2018-2024 (Poster Hall) - Mar 3, 2025 - Abstract #CROI2025CROI_911; Doravirine and rilpivirine DRMs remained low, with respective 2024 prevalences of 2% (RNA) and 2.9% (DNA) and 6.3% (RNA) and 10.1% (DNA)...Cabotegravir DRM prevalence in 2024 was 3.8% (RNA) and 2.5% (DNA)...Conclusions Prevalence of NRTI and NNRTI resistance declined which is consistent with increased use of regimens with higher resistance barriers, improved tolerability, and more convenient dosing, resulting in better adherence. Prevalence of INSTI DRMs was low, supporting US guidelines for limiting INSTI resistance testing to cases of treatment failure, suspected transmitted resistance, or infection during INSTI-based PrEP.
- |||||||||| ART Exposure and Accelerated Aging in PLHIV: Insights From Proteomic and Methylation Clocks (Poster Hall) - Mar 3, 2025 - Abstract #CROI2025CROI_605;
P In contrast, longer exposure to tenofovir disoproxil fumarate (TDF), emtricitabine (FTC), darunavir (DRV), atazanavir (ATV), and dideoxynucleoside analogues (d-drugs) was related to higher age advancement scores (Figure 1; P<0.05, adjusted for chronological age)...Conclusions Cumulative ART exposure influences age acceleration in PLHIV, with distinct effects across regimens and drug classes. Innate immune pathways appear to be key drivers of these effects and are promising therapeutic targets to mitigate accelerated aging.
- |||||||||| Edurant (rilpivirine) / J&J, Pifeltro (doravirine) / Merck (MSD), Tivicay (dolutegravir) / ViiV Healthcare
Dolutegravir With Either Doravirine or Rilpivirine: Two-Drug Antiretroviral Therapy Outcomes (Poster Hall) - Mar 3, 2025 - Abstract #CROI2025CROI_526; Conclusions Observed differences in VS following switch to DRG+RPV and DTG+DOR may be due to differences in participant characteristics, adherence, viral resistance patterns, and the dual regimens. Further studies are needed to evaluate efficacy of dual NRTI-free regimens in real-world settings.
- |||||||||| Juluca (dolutegravir/rilpivirine) / ViiV Healthcare, J&J, Edurant (rilpivirine) / J&J, Tivicay (dolutegravir) / ViiV Healthcare
PK/PD data, Journal: The steady-state pharmacokinetics of fixed-dose combination dolutegravir+rilpivirine in hemodialysis. (Pubmed Central) - Feb 26, 2025 Exposures throughout the dosing interval were greater than the reported protein-binding-adjusted IC90 efficacy values for DTG (64?ng/ml) and RPV (12?ng/ml) in all participants. These data suggest no dosing modifications are needed for the FDC DTG+RPV regimen in hemodialysis.
- |||||||||| Apretude (cabotegravir extended-release injectable suspension) / ViiV Healthcare, Edurant (rilpivirine) / J&J, Cabenuva (cabotegravir long acting/rilpivirine long acting) / J&J, GSK, ViiV Healthcare, Pfizer, Shionogi
Journal: Willingness to Switch to Long-Acting Injectable Cabotegravir and Rilpivirine Every 2 Months for People Living with HIV in Nanjing, China. (Pubmed Central) - Feb 10, 2025 Our survey demonstrated that the majority of PLWH were willing to switch to CAB+RPV therapy, mainly due to its improved convenience and reduced risk of disease exposure. However, their concerns regarding price, efficacy, and safety could be the key challenges for the clinical implementation of the CAB+RPV LA regimen in the future.
- |||||||||| Cabenuva (cabotegravir long acting/rilpivirine long acting) / J&J, GSK, ViiV Healthcare, Pfizer, Shionogi
P3 data, Journal, Patient reported outcomes: Improvements in Patient-Reported Outcomes After 12 Months of Maintenance Therapy With Cabotegravir?+?Rilpivirine Long-Acting Compared With Bictegravir/Emtricitabine/Tenofovir Alafenamide in the Phase 3b SOLAR Study. (Pubmed Central) - Jan 17, 2025 P3 Most (90%, 382/425) questionnaire respondents preferred CAB?+?RPV LA vs. BIC/FTC/TAF (5%, 21/425). Switching to CAB?+?RPV LA was associated with significantly improved treatment satisfaction and relief from the fear of disclosure, anxiety surrounding adherence and reminder of HIV status.
- |||||||||| Preclinical, Journal: Repurposing Non-Nucleosidic Reverse Transcriptase Inhibitors (NNRTIs) to Overcome EGFR T790M-Mediated Acquired Resistance in Non-Small Cell Lung Cancer. (Pubmed Central) - Jan 14, 2025
Using in silico molecular docking, Rilpivirine demonstrated a docking score of -7.534?kcal/mol, comparable to established epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) like Osimertinib and WZ4002...Enzymatic assays revealed that Rilpivirine inhibited the double mutant epidermal growth factor receptor tyrosine kinase (EGFR TK) with an IC50 value of 54.22?nM and spared the wild-type EGFR TK with an IC50 of 22.52?nM. These findings suggest Rilpivirine's potential as a therapeutic agent for NSCLC with EGFR L858R/T790M mutations.
- |||||||||| Apretude (cabotegravir extended-release injectable suspension) / ViiV Healthcare, Edurant (rilpivirine) / J&J, Cabenuva (cabotegravir long acting/rilpivirine long acting) / J&J, GSK, ViiV Healthcare, Pfizer, Shionogi
Journal: Cabotegravir and rilpivirine long acting injectables in a pregnant woman living with HIV. (Pubmed Central) - Dec 17, 2024 Despite placental transfer, no congenital malformations were noted. Bimonthly CAB/RPV LAI may not be suitable for pregnant women and monitoring of exposed infants is warranted.
- |||||||||| Edurant (rilpivirine) / J&J, Intelence (etravirine) / J&J
Review, Journal: Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors (2019-2023). (Pubmed Central) - Nov 23, 2024 Moreover, developing new DAPY analogues with broad-spectrum antiviral activity has become a key research priority. This review provides a comprehensive overview of the evolution of DAPYs from 2019 to 2023, including scaffold hopping and structural modifications of the right wing, left wing, central pyrimidine core, and linker, affording valuable insights for the future development of effective HIV-1 inhibitors.
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