efavirenz / Generic mfg. - LARVOL DELTA

The Effect of Rifampicin on the Plasma and Intracellular Pharmacokinetics of Tenofovir Alafenamide Fumarate in Participants with HIV-associated Tuberculosis. (PubMed, J Acquir Immune Defic Syndr) - "When combined with rifampicin, ART containing standard-dose TAF resulted in higher TFV-DP concentrations than TDF-based ART in participants with HIV-associated tuberculosis, supporting its use with rifampicin-containing tuberculosis therapy."

Journal • PK/PD data • Human Immunodeficiency Virus • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis

Drug Resistance Among Newly Diagnosed People Living with HIV-1 in Sichuan, China: A Large-Scale Population-Based Cross-Sectional Study. (PubMed, Infect Drug Resist) - "Within NNRTIs, efavirenz (EFV) and nevirapine (NVP) resistance rates were 6.26% and 6.50%, respectively. The prevalence of TDR in Sichuan had reached moderate epidemic levels, with certain cities already experiencing high epidemic rates. It is urgent that we urgently expand targeted genotypic drug resistance detection and implement interventions to improve medication adherence."

Journal • Observational data • Human Immunodeficiency Virus • Infectious Disease

Magnitude of Hyperuricemia and Its Associated Factors Among People Living with Human Immunodeficiency Virus Who Enrolled in First-Line Antiretroviral Therapy in Amhara Region, Ethiopia. (PubMed, J Int Assoc Provid AIDS Care) - "Significant associated factors included male sex, older age, obesity, and longer ART duration. Therefore, early screening, particularly in males, older adults, those with obesity, and long-term ART users, is essential to prevent complications."

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

Impact of Dihydrocapsaicin on the Metabolism of Efavirenz In Vitro and In Vivo. (PubMed, Pharmacol Res Perspect) - "Drug-drug interactions were observed between DHC and EFV, altering the pharmacokinetics of EFV both in vivo and in vitro. The dosage of capsaicin should be monitored and adjusted in patients receiving EFV maintenance therapy."

Journal • Preclinical • Human Immunodeficiency Virus

CYP46A1 Activation Improves Retinal Neovascularization in a Mouse Model of Retinopathy of Prematurity. (PubMed, bioRxiv) - "Seven-day-old (P7) C57BL/6J mice maintained in room air (controls) or subjected to oxygen-induced retinopathy (OIR) were treated with/without 20 mg/kg efavirenz (EFV), a CYP46A1 activator administered intraperitoneally from P7 to P17...The current study demonstrates the developmental regulation of CYP46A1 and the dysregulated expression and levels of the downstream metabolite 24-Hydroxycholesterol (24HC) in OIR mice. The study further suggests that pharmacological CYP46A1 activation may improve key pathological features associated with pathological neovascularization in OIR mice."

Journal • Preclinical • Age-related Macular Degeneration • Retinal Disorders • Retinopathy of Prematurity • CYP46A1

Development of an UPLC-MS/MS method for quantification of donafenib and its metabolite in rat plasma: application to drug-drug interaction. (PubMed, Biochem Pharmacol) - "In vivo, the AUC(0-t), AUC(0-∞) and Cmax of donafenib and donafenib N-oxide were significantly increased in the presence of efavirenz, which indicated that efavirenz increased the exposure of donafenib in rats. In short, this UPLC-MS/MS method was reliable for quantifying donafenib and its metabolite, and the findings suggested that efavirenz had an inhibitory effect on the metabolism of donafenib in vitro and in vivo."

Journal • Preclinical • Hepatocellular Cancer • Human Immunodeficiency Virus • Infectious Disease • Oncology • Solid Tumor

In-silico identification of phytochemical compounds from various medicinal plants as potent HIV-1 non-nucleoside reverse transcriptase inhibitors utilizing molecular docking and molecular dynamics simulations. (PubMed, Biol Methods Protoc) - "The ADMET profile of Arctigenin was similar to that of Efavirenz, and better than that of other top compounds...Out of the top five compounds identified in this study, Rosmarinic acid, a current inhibitor of HIV-1 RT in vitro, showed the most promising prediction. However, further in vivo studies and human clinical trials are required to provide more concrete information regarding its efficacy as potent HIV-1 RT inhibitors."

Journal • Human Immunodeficiency Virus • Infectious Disease

Development, Verification, and Application of a Chinese Pediatric Physiologically Based Pharmacokinetic Model: Emphasis on CYP Metabolism and Renal Elimination. (PubMed, AAPS J) - "The model was tested using two drugs predominately metabolized by CYP3A4 (fentanyl and midazolam), one dual CYP3A4/CYP2C9 substrate (ruxolitinib), two by other CYPs (efavirenz and theophylline), and two by renal elimination (ceftazidime and vancomycin). Given the increased regulatory use of pediatric PBPK models in drug development, expanding these models to other ethnic groups is important. There is a need to further develop the current model across a wider range of drugs with different elimination pathways, to increase model confidence, this should involve academia, industry, model providers, and regulatory agencies."

Journal • PK/PD data • Pediatrics • CYP2C9 • CYP3A4

REPURPOSE: Phase II study of Efavirenz in platinum resistant or heavily pretreated high-grade serous ovarian cancer (ANZCTR) - P2 | N=48 | Not yet recruiting | Sponsor: The University of Newcastle

New P2 trial • Platinum resistant • Fallopian Tube Cancer • High Grade Serous Ovarian Cancer • Oncology • Ovarian Cancer • Peritoneal Cancer • Solid Tumor • MUC16

HIV Comorbid Infection and Liver-Directed AAV-Based Gene Therapy in Adults with Severe and Moderately Severe Hemophilia B: Efficacy and Safety Results from Phase 2b and the Pivotal Phase 3 HOPE-B Trials 3 Years after Administration of a Single Dose of Etranacogene Dezaparvovec (ASH 2023) - P2, P3 | "Concerns about increased hepatotoxicity of liver-directed adeno-associated viral (AAV) vectors in patients receiving potentially hepatotoxic HIV medications (eg, efavirenz) have excluded this population from participating in many of gene therapy hemophilia trials. Etranacogene dezaparvovec were observed to be safe and effective in a subset of study participants living with HIV. These results support the use of etranacogene dezaparvovec, the first approved liver-directed AAV-based gene therapy product for the treatment of patients with severe or moderately severe hemophilia B in the US and Europe, for eligible patients with controlled comorbid HIV infection. Owing to the small number of patients with HIV being enrolled in trials, long-term collection of data and special attention in the real-world setting is recommended."

Clinical • Gene therapy • P2b data • P3 data • Gene Therapies • Hematological Disorders • Hemophilia • Hemophilia B • Hepatitis C • Hepatology • Human Immunodeficiency Virus • Infectious Disease • Inflammation • Rare Diseases • CD4

Pharmacogenetics in Tuberculosis-HIV Coinfected Populations: A Systematic Review of Genetic Variants Influencing Antiretroviral and Anti-Tuberculosis Drug Response. (PubMed, J Multidiscip Healthc) - "An analysis of 39 included studies indicated that efavirenz and CYP2B6*6 are the most extensively researched antiretroviral therapy (ART) and gene, respectively...Arylacetamide deacetylase (AADAC) polymorphisms that increased rifapentine plasma levels could also reduce dolutegravir plasma concentrations...Consequently, a holistic approach to pharmacogenetics in TB-HIV populations is essential, considering all drug-gene-disease interactions. High-quality research, including randomized controlled trials (RCTs), is necessary for the implementation of pharmacogenetic testing in TB-HIV populations before it can be widely adopted in clinical practice, which is currently lacking."

Biomarker • Journal • Review • Human Immunodeficiency Virus • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis • NAT2

Efficacy of dolutegravir-based regimen in HIV-infected children in a treatment center in a regional health facility in Cameroon. (PubMed, Infect Dis Now) - "Children on dolutegravir had good viral load suppression compared with children on efavirenz."

Journal • Human Immunodeficiency Virus • Infectious Disease • Pediatrics

CYP2B6 downregulation by cell-penetrating dominant-negative activating transcription factor 5 peptide in glioblastoma cells. (PubMed, Drug Metab Dispos) - "Among the cytochrome P450 enzyme superfamily, CYP2B6 metabolizes drugs such as cyclophosphamide, efavirenz, methadone, and ecstasy. SIGNIFICANCE STATEMENT: The study found that the transcription factor activating transcription factor 5 regulates CYP2B6 expression in glioblastoma cell lines. Introducing a transactivator of transcription-fused cell-penetrating dominant-negative activating transcription factor 5 peptide downregulates CYP2B6 protein expression, suggesting its potential for personalized dosing strategies by targeting CYP2B6."

Journal • Brain Cancer • Glioblastoma • Glioma • Human Immunodeficiency Virus • Infectious Disease • Oncology • Solid Tumor • ATF5 • CYP2B6

Breast Milk Transfer and Infant Exposures to Dolutegravir, Tenofovir, and Tenofovir Alafenamide: Results from IMPAACT 2010/VESTED. (PubMed, J Acquir Immune Defic Syndr) - "Breastmilk transfer of DTG, TAF, and TFV is low and results in minimal systemic exposure in breastfed infants. The clinical relevance of infant exposure to low concentrations of these antiretrovirals - particularly DTG - is unknown but should be considered in the context of the risk of drug resistance in infants who acquire HIV."

Journal • Human Immunodeficiency Virus • Infectious Disease

Human immunodeficiency virus and antiretroviral therapies exert distinct influences across diverse gut microbiomes. (PubMed, Nat Microbiol) - "Efavirenz-associated Prevotella depletion may occur through cross-inhibition of prokaryotic reverse transcriptases involved in antiphage defences, as shown by computational and in vitro experiments. These observations could inform future geography-specific and microbiome-guided therapy."

Journal • Atherosclerosis • Cardiovascular • Human Immunodeficiency Virus • Infectious Disease • Inflammation

Allosteric modulation of the solute carrier transporter SLC39A8 potentiates manganese and cadmium uptake. (PubMed, J Clin Invest) - "We conducted a drug repurposing screen, identifying efavirenz as a potentiator of manganese and cadmium uptake by SLC39A8 and subsequently generated structure-activity relationships to guide design of analogs...This integrated approach allowed for iterative feedback where insights from experiments informed the model refinements and computational predictions guided future experimental designs. Furthermore, our data established that SLC39A8 transporter activity can be increased pharmacologically, potentially opening avenues for SLC transporter drug discovery."

Journal • Cardiovascular • CNS Disorders • Gastroenterology • Gastrointestinal Disorder • Genetic Disorders • Immunology • Inflammation • Inflammatory Bowel Disease • Metabolic Disorders • Psychiatry • Schizophrenia

Insights from systematic reviews (2019-2024) and drug interaction database analysis in people with HIV and comorbidities. (PubMed, Int J STD AIDS) - "Severe adverse drug reactions associated with ARTs, including efavirenz, darunavir, nevirapine, and atazanavir-ritonavir, especially when combined with treatments for TB and malaria. Key interactions included reduced drug levels from rifampicin and QT prolongation from artemether-lumefantrine...Database discrepancies were noted, especially for riociguat interactions and ritonavir through inhibition of P-gp or OATP1B1 functions.ConclusionsDDIs in PWH receiving ART with comorbidities have highlighted the crucial need for personalized treatment. Incorporating pharmacokinetic, pharmacodynamic, and pharmacogenomic factors is essential for optimizing therapy outcomes."

Journal • Cardiovascular • Human Immunodeficiency Virus • Hypertension • Infectious Disease • Malaria • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases • Tuberculosis

Doravirine Resistance Patterns Identified through Week 192 in the DRIVE-FORWARD and DRIVE-AHEAD Phase 3 Clinical Trials. (PubMed, J Acquir Immune Defic Syndr) - P3 | "In DRIVE-FORWARD and DRIVE-AHEAD, the development of resistance to doravirine was uncommon (genotypic 1.3%; phenotypic 1.0%) and occurred mainly during the first 48 weeks of treatment. Overall, the RAMs observed with doravirine were distinct from those of other NNRTIs."

Journal • P3 data • Human Immunodeficiency Virus • Infectious Disease

Pharmacogenomics in Orofacial Clefts Care: Insights from Whole-Genome Sequencing of Case-Parents Trios. (PubMed, J Pers Med) - "The identified variations were linked to the metabolism of frequently used pharmaceuticals in Africa, such as caffeine, ketoconazole, efavirenz, carbamazepine, and artemether. These findings highlight the need for pharmacogenetic screening to inform personalized medicine, diminish ADRs, and enhance the clinical care of OFCs in Sub-Saharan Africa."

Biomarker • Journal • ABCC3 • CYP1A2 • CYP27A1

Efficacy and safety of switching from lopinavir/ritonavir-based regimens to bictegravir/emtricitabine/tenofovir alafenamide in people living with HIV: A multicenter retrospective study. (PubMed, Virol Sin) - "These PLWH typically have a history of either treatment failure or intolerance to first-line efavirenz-based regimens. The median triglyceride level decreased from 2.4 mmol/L to 1.8 mmol/L (P < 0.001), while no difference in CD4 counts was observed. These findings demonstrate that BIC/FTC/TAF is an effective and metabolically favorable treatment option for PLWH switching from LPV/r based regimens, regardless of whether they have a prior history of virological failure."

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

HIV-1 genetic diversity and pretreatment drug resistance survey prior to dolutegravir introduction in Senegal. (PubMed, IJID Reg) - "Among NRTIs, the most frequent mutation was M184V (3/6), conferring high-level resistance to lamivudine and emtricitabine, and K103N (11/12) among NNRTIs, conferring resistance to efavirenz and nevirapine. Through a quasi-national survey, an intermediate level of NNRTI resistance was observed, with regional disparities in Senegal. These findings highlight the limitations of NNRTI-based first-line regimens in Senegal and support the transition to other antiretroviral therapy regimens, such as dolutegravir-based therapy in newly infected individuals as well as in treated patients."

Journal • Human Immunodeficiency Virus • Infectious Disease • Inflammation

Real-World 5-Year Virological Outcomes of People Living with HIV Initiated on Efavirenz or Dolutegravir or Switched to Dolutegravir Containing Regimens in Botswana, 2012-2025 (EACS 2025) - "The significantly higher rates of LTFU found in iDBR likely reflect less robust adherence in PLHIV in the Era of Test & Treat and same-day ART initiation. Higher rates of deaths in sDBR, likely reflect more complicated virological and clinical histories observed in treatment-experienced PLHIV."

Clinical • Late-breaking abstract • Real-world • Real-world evidence • Human Immunodeficiency Virus • Infectious Disease

Advanced coronary artery disease in a low-risk HIV patient – a case for early statin intervention (EACS 2025) - "His antiretroviral regimen initially was Kivexa and Efavirenz, which was then switched to Atripla in 2020 and switched to Descovy and Efavirenz in 2022. This case reinforces the inadequacy of relying solely on traditional risk scores for cardiovascular risk assessment in People Living With HIV(PLWH). Chronic inflammation and endothelial dysfunction associated with HIV infection may drive atherosclerosis independently of classical risk factors. In alignment with the REPRIEVE study outcomes, the BHIVA now recommends initiating statins in PLWH based on Q-Risk, advocating for early, primary preventive cardiovascular management in this population."

Clinical • Metastases • Human Immunodeficiency Virus • Infectious Disease • CD4

Changes in Metabolic Parameters after Switching from Efavirenz to Dolutegravir-based Regimen: A Cohort Study in Thai People Living with HIV (EACS 2025) - "Multivariate analysis revealed that higher baseline HDL-C levels significantly reduced the likelihood of SWG (OR 0.11 per 10 mg/dL increase, 95% CI 0.02–0.80, p = 0.030). Conclusions : Regular monitoring of BW and renal function should be incorporated into routine follow-up care, particularly for those who are already at risk for metabolic disorders."

Human Immunodeficiency Virus • Infectious Disease

Antiretroviral therapy in people with HIV and TB in France: a nationwide retrospective study between 2010 and 2023 (EACS 2025) - "Purpose : Since 2014, following EACS guidelines, raltegravir (RAL) and then dolutegravir (DTG) are proposed as alternatives to efavirenz (EFV)-based ART in people with HIV (PWH) treated for TB...First ART following the TB index date was used to classify ART as 2 NRTIs plus a boosted protease inhibitor (PI/r), an INSTI (RAL, DTG, or bictegravir [BIC]), EFV, or other combinations...​ Conclusions : In this French nationwide cohort, TB and HIV were diagnosed concomitantly in 40% of cases. DTG-based regimens have replaced EFV- and PI/r-based regimens over the past decade, representing half of ART prescriptions in PWH treated for TB in 2023."

Retrospective data • Human Immunodeficiency Virus • Infectious Disease • Tuberculosis