Intelence (etravirine) / J&J - LARVOL DELTA

Characteristics and Outcomes of Patients Who Received Etravirine and/or Darunavir (clinicaltrials.gov) - P=N/A | N=871 | Completed | Sponsor: Elizabeth Glaser Pediatric AIDS Foundation | Active, not recruiting ➔ Completed

Trial completion • Human Immunodeficiency Virus • Infectious Disease

Cryo-EM structure-based discovery of etravirine as a specific inhibitor of PRMT5/pICln protein-protein interaction for prostate cancer treatment. (PubMed, J Enzyme Inhib Med Chem) - "Functionally, etravirine reduced prostate cancer cell proliferation, inhibited tumour growth, and downregulated AR and AR-V7 expression in cells and in mouse models. These results demonstrate that the unique P4I interface is a promising therapeutic target and that etravirine serves as a proof-of-concept lead compound for exploring the potential of P4I-targeted strategies in prostate cancer."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • PRMT5

Switching from etravirine to doravirine in people with HIV harbouring NNRTI resistance-associated mutations: the DorSwitch pilot study. (PubMed, J Antimicrob Chemother) - "In this small, highly selected pilot cohort, switching from etravirine to doravirine as part of an otherwise suppressive regimen was associated with maintenance of virological suppression through Week 48 and a more favourable predicted NNRTI resistance profile in most participants. The favourable resistance profile, safety, metabolic effects and PK findings consistent with expected exposure-particularly in combination with darunavir/cobicistat- support further evaluation of doravirine as a switch option in carefully selected individuals with prior NNRTI failure."

Journal • Human Immunodeficiency Virus • Infectious Disease

Deep learning-based prediction of drug-target interactions between antiviral drugs and SARS-CoV-2 proteins using an image-based representation approach. (PubMed, Comput Biol Chem) - "Results consistently identified five antivirals - MK-5172 (Grazoprevir), Simeprevir, Lopinavir, Etravirine, and Atazanavir - as top-ranked candidates across all targets. Comparative analysis with the MT-DTI model demonstrated competitive and, in several cases, superior ranking performance despite a simpler architecture. Importantly, these predictions are supported by independent experimental and clinical evidence, highlighting the potential of image-based representations as a computationally efficient and biologically meaningful approach for drug-target interaction prediction and drug repurposing."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

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

Resistance to etravirine and doravine in experienced PLHIV in Mexico. Impact on salvage treatment (AIDS 2026) - "BACKGROUND: Doravirine (DOR) and Etravirine (ETV) are the only NNRTIs indicated in people living with HIV (PLHIV) after virologic failure (VF) to first-generation NNRTIs as Efavirenz and Nevirapine. In our study, resistance to ETR in adult PLHIV who experienced at least two treatment failures in Mexico, was lower than to DOR. HLR was uncommon specially with respect to total sample, but higher (almost double) to DOR. Resistance prevalence could be higher, as most of the genotypes were performed without the NNRTI drug pressure."

Human Immunodeficiency Virus • Infectious Disease

Budget impact analysis of medication reviews by junior pharmacists in polypharmacy patients: a hospital perspective. (PubMed, Int J Clin Pharm) - "Junior pharmacist-led medication reviews provide a modest cost-saving intervention from the hospital perspective, demonstrating savings across clinical populations with polypharmacy."

HEOR • Journal

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

Repurposing Antiretroviral Drugs for Urological Cancers: Differential Effects of Protease Inhibitors and NNRTIs on Prostate and Bladder Cancer Cells. (PubMed, Cells) - "This study evaluated the anticancer potential of three antiretroviral drugs, namely ritonavir (RIT), saquinavir (SAQ), and rilpivirine (RPV), in PC-3 and UM-UC-5 cancer cell lines, using MTT, clonogenic, wound healing, toxicity assessment with fibroblast cells, and DCFDA assays; this last method included efavirenz (EFV) and etravirine (ETV) for intracellular reactive oxygen species (ROS) production. Generally, all drugs showed minimal toxicity in non-malignant cells, with SAQ exhibiting some toxicity but only for concentrations higher than those required for anticancer activity. Overall, these findings suggest that antiretroviral, especially protease inhibitors, may cause anticancer effects, although these are concentration- and context-dependent, and further investigation is needed to understand the mechanisms involved."

Journal • Bladder Cancer • Genito-urinary Cancer • Oncology • Solid Tumor • Urethral Cancer

The TMC125-C214 Study Provides Early Access to TMC125 for HIV-1 Infected Patients Who Have Failed Multiple Antiretroviral Regimens and Will Also Gather Information on the Long-term Safety and Tolerability of TMC125 Combined With Other Antiretroviral Drugs (clinicaltrials.gov) - P=N/A | N=0 | Approved for marketing | Sponsor: Tibotec Pharmaceuticals, Ireland | N=5178 ➔ 0

Enrollment change • Human Immunodeficiency Virus • Infectious Disease

TMC125-TiDP35-C239 - Continued Access to Etravirine (ETR) in Treatment Experienced HIV-1 Infected Participants (clinicaltrials.gov) - P3 | N=180 | Completed | Sponsor: Janssen Sciences Ireland UC | Active, not recruiting ➔ Completed

Trial completion • Human Immunodeficiency Virus • Infectious Disease

FAERS DATABASE ANALYSIS REVEALS ANENCEPHALY ASSOCIATED WITH ANTIRETROVIRAL DRUG EXPOSURE (ISPOR 2026) - "Emtricitabine had the highest number of reports (n=51), followed by Ritonavir (n=32) and Tenofovir (n=28)...Tipranavir showed the strongest signal (551.688; 343.42-886.26), followed by Etravirine (97.723; 50.453-189.28) and Enfuvirtide (97.684; 48.489-196.789). Among FDCs, Lamivudine and Zidovudine (87.799; 50.529-152.56) had the highest signal... This study highlights a potential safety concern regarding the association between antiretroviral agents and anencephaly. Continued pharmacovigilance and targeted epidemiological studies are warranted to further investigate and mitigate these risks in vulnerable populations."

CNS Disorders

Physiologically Based Pharmacokinetic Modeling to Assess Antiretroviral-BTK Inhibitor Interactions and Provide Recommendations for Co-Administration Regimens. (PubMed, Pharmaceutics) - "Model performance was verified by comparing simulated pharmacokinetic parameters and DDI magnitudes with probe drugs (midazolam or maraviroc) with reported clinical data. The PBPK models accurately predicted the in vivo pharmacokinetics of ibrutinib, zanubrutinib, acalabrutinib, and those of the antiretrovirals darunavir/ritonavir, efavirenz, and etravirine, and the DDIs between them. The dose adjustment strategies provided information valuable to the optimization of antineoplastic therapy in HIV-related lymphoma (HRL) patients."

Journal • PK/PD data • Hematological Malignancies • Human Immunodeficiency Virus • Infectious Disease • Lymphoma • Oncology

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

Drug Resistance in HIV Following First-line ART Failure: Insights from a Cross-sectional Study in India. (PubMed, J Assoc Physicians India) - "Ensuring adequate drug exposure history in patients can prevent poor outcomes in PLH being treated with ART due to resistance. Resistance profiling is especially relevant following first-line ART failure."

Journal • Observational data • Human Immunodeficiency Virus • Infectious Disease

Drug resistance characteristics of rilpivirine in HIV-1-infected patients before starting antiretroviral therapy in nine provinces of China (PubMed, Zhonghua Liu Xing Bing Xue Za Zhi) - "The cross-resistance rate between RPV and efaviren/nevirapine (EFV/NVP) in total HIV-1-infected patients before ART was 57.5% (92/160), which was significantly higher than that between RPV and doravirine (DOR) (25.0%, 40/160) and that between RPV and etravirine (ETR) (34.4%, 55/160) (all P<0.001). The RPV resistance rate of HIV-1-infected patients with a history of antiretroviral drug exposure was relatively higher. It is recommended to conduct HIV-1 resistance testing for them before starting ART and formulate individualized treatment plans."

Journal • Human Immunodeficiency Virus • Infectious Disease

TMC125-TiDP35-C239 - Continued Access to Etravirine (ETR) in Treatment Experienced HIV-1 Infected Participants (clinicaltrials.gov) - P3 | N=180 | Active, not recruiting | Sponsor: Janssen Sciences Ireland UC | Trial completion date: Jan 2032 ➔ Apr 2026

Trial completion date • Human Immunodeficiency Virus • Infectious Disease

Cyclization-Inspired Structural Optimization: Designing Potent Non-nucleoside Reverse Transcriptase Inhibitors with Enhanced Safety and Selectivity. (PubMed, J Med Chem) - "To improve the safety and selectivity of etravirine (ETR), cyclization strategy was employed by replacing the pyrimidine ring with a dihydropteridin-6(5H)-one scaffold affording a series of novel bicyclic tetrahydropteridine derivatives...Notably, 16a showed negligible cytotoxicity (CC50 = 196.46 μM) and high selectivity index (SI = 65,789), greatly surpassing ETR (CC50 > 4.6 μM, SI > 1436) and rilpivirine (RPV) (CC50 > 4.0 μM, SI > 3989)...Additionally, 16a displayed minimal sensitivity to CYP enzymes, no inhibition of the hERG potassium channel, and no detectable acute toxicity at an in vivo dose of 2 g/kg. Collectively, these results highlight 16a as a highly promising on-nucleoside reverse transcriptase inhibitor candidate."

Journal • Human Immunodeficiency Virus • Infectious Disease

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

Switching from etravirine to doravirine in virologically suppressed people with HIV: results from the French multicentre SWEED observational study. (PubMed, J Antimicrob Chemother) - "Doravirine-based ART maintained virological suppression in PWH switching from etravirine-based ART, even in presence of prior NNRTI resistance. Its once-daily dosing, favourable safety profile, and minimal drug interactions support its use in long-term ART strategies."

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

Potential treatment options following virological failure with long-acting injectable cabotegravir and rilpivirine: an analysis based on reported cases (EACS 2025) - "Purpose : Virological failure (VF) with long-acting injectable cabotegravir and rilpivirine (LAI-CAB/RPV) is rare but may lead to selection of resistance-associated mutations (RAMs) that limit future treatment options. Resistance to CAB/RPV was common, being more prevalent among people with A compared to non-A subtypes. Reduced susceptibility to alternative treatment options was more pronounced for INI (dolutegravir/bictegravir) than for NNRTI (doravirine/etravirine)."

Clinical • Human Immunodeficiency Virus • Infectious Disease

IMPACT OF PREEXISTING K103N ON THE EFFECTIVINES OF LA-CAB+RPV: REAL-LIFE RELATIVITY COHORT (EACS 2025) - "Purpose : K103N is a nonpolymorphic NNRTI resistance-associated mutation (RAM) selected in people with HIV (PWH) treated with nevirapine (NVP) or efavirenz (EFV). It reduces susceptibility to NVP and EFV by approximately 50-fold and 20-fold, respectively, but does not affect susceptibility to rilpivirine (RPV), etravirine (ETR), or doravirine (DOR)...BASELINE CHARACTERISTICS REGARDING THE PRESENCE OF K103N Conclusions : The presence of the K103N mutation was not associated with an increased risk of virological failure in PWH treated with LA-CAB+RPV. These findings suggest that a history of K103N should not preclude the use of this regimen."

Clinical • Human Immunodeficiency Virus • Infectious Disease

Exploring Potential for Repurposing Antiretroviral Drugs Etravirine and Efavirenz in Prostate and Bladder Cancer. (PubMed, Pharmaceuticals (Basel)) - " EFV and ETV exhibit selective anticancer activity in prostate and bladder cancer cells, with enhanced effects when combined. These findings support their potential as repurposed therapeutic agents and warrant further preclinical evaluation for prostate and bladder cancer therapy."

Journal • Bladder Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Bioisosterism-driven design of orally active, safe, and broad-spectrum biphenyl-DAPY derivatives as highly potent HIV-1 non-nucleoside reverse transcriptase inhibitors. (PubMed, Acta Pharm Sin B) - "Furthermore, this analog exhibited minimal adverse effects with significantly reduced cytotoxicity (CC50 = 195 μmol/L) and a high selectivity index (SI = 102,608), superior to those of etravirine (CC50 > 4.6 μmol/L, SI > 1436) and rilpivirine (CC50 = 3.98 μmol/L, SI = 3989). Additionally, A12 exhibited favorable oral bioavailability (F = 29.2%) and an extended elimination half-life (T 1/2 = 13.56 h), enabling convenient oral administration at minimal doses. These findings indicated that A12 could serve as a promising drug candidate for HIV treatment."

Journal • Human Immunodeficiency Virus • Infectious Disease