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    DRUG:

    efavirenz

    i
    Other names: DMP 266, L 741211, L 743725, L 743726
    Company:
    Generic mfg.
    Drug class:
    Non-nucleoside reverse transcriptase inhibitor
    11d
    Physiologically-Based Pharmacokinetics of Ribociclib Drug-Drug Interactions and Organ Impairment Pharmacokinetics in Early Breast Cancer. (PubMed, Pharmaceuticals (Basel))
    PBPK modeling predicted that ritonavir or erythromycin (strong and moderate CYP3A4 inhibitors) would increase ribociclib steady-state area under the concentration-time curve (AUC) by 1.84-fold or show no meaningful impact, respectively. Steady-state ribociclib AUC was estimated to decrease by 83% and 74% with rifampicin and efavirenz, strong and moderate CYP3A4 inducers, respectively. Ribociclib was estimated to increase CYP3A4 substrate midazolam exposure by 280%. Mild HI or mild/moderate RI did not show an apparent impact on ribociclib PK. Using relevant data and methodology for EBC patients, this analysis informed the approved ribociclib label of no dose adjustment for EBC patients with concomitant use of a moderate CYP3A inhibitor, any degree of HI, or mild/moderate RI, and a reduced 200 mg dose for patients with concomitant use of a strong CYP3A inhibitor or severe RI.
    PK/PD data • Journal
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    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
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    Kisqali (ribociclib) • efavirenz • midazolam hydrochloride • rifampicin • ritonavir
    20d
    Efavirenz for the Treatment of Creutzfeldt-Jakob Disease (clinicaltrials.gov)
    P3, N=246, Not yet recruiting, Xuanwu Hospital, Beijing
    New P3 trial
    |
    efavirenz
    22d
    "TACKITON: The T Cell Activator of Cell Killing ("TACK") IT ON" STUDY (clinicaltrials.gov)
    P=N/A, N=26, Recruiting, University of Toronto | Trial completion date: Sep 2026 --> Nov 2028 | Trial primary completion date: Jan 2026 --> Nov 2027
    Trial completion date • Trial primary completion date
    |
    efavirenz
    2ms
    Study on the Effect of Antiretroviral Therapy Centered on Enovirine on PD-1 Expression of CD8+ T Cells Induced by Cholesterol (ChiCTR2500113428)
    P4, N=150, Completed, Xixi Hospital of Hangzhou; Xixi Hospital of Hangzhou
    New P4 trial
    |
    efavirenz
    3ms
    A Single-center, Randomized, Open-label, Parallel-design Clinical Study to Evaluate the Pharmacokinetic Effects of Itraconazole, Fluconazole or Efavirenz on a Single Dose of Clifutinib in Healthy Participants (clinicaltrials.gov)
    P1, N=80, Not yet recruiting, Sunshine Lake Pharma Co., Ltd.
    New P1 trial
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    clifutinib (HEC73543) • itraconazole • efavirenz
    5ms
    REPURPOSE: Phase II study of Efavirenz in platinum resistant or heavily pretreated high-grade serous ovarian cancer (ACTRN12625001259437)
    P2, N=48, Not yet recruiting, The University of Newcastle
    New P2 trial • Platinum resistant
    |
    MUC16 (Mucin 16, Cell Surface Associated)
    |
    efavirenz
    5ms
    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
    |
    CYP2B6 (Cytochrome P450 Family 2 Subfamily B Member 6)
    |
    cyclophosphamide • efavirenz
    6ms
    Efavirenz (EFV) Intensification (clinicaltrials.gov)
    P4, N=7, Completed, Washington University School of Medicine
    New P4 trial
    |
    efavirenz
    8ms
    A Study of the Effect Efavirenz on the Plasma Levels of MK-7602 in Healthy Participants (MK-7602-005) (clinicaltrials.gov)
    P1, N=34, Completed, Merck Sharp & Dohme LLC | Active, not recruiting --> Completed
    Trial completion
    |
    efavirenz
    8ms
    Renaissance: Reverse Triple Negative Immune Resistant Breast Cancer (clinicaltrials.gov)
    P2, N=70, Recruiting, Fudan University | N=30 --> 70 | Trial completion date: Mar 2023 --> Mar 2027 | Trial primary completion date: Dec 2022 --> Dec 2026
    Enrollment change • Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 expression
    |
    AiRuiKa (camrelizumab) • trastuzumab rezetecan (SHR-A1811) • SHR-A2102 • efavirenz • AiRuiLi (adebrelimab) • HHPG-19K (mecapegfilgrastim)
    9ms
    Signature-based repurposed drugs resemble the inhibition of TGFβ-induced NDRG1 as potential therapeutics for triple-negative breast cancer. (PubMed, Int J Biol Sci)
    In conclusion, these findings demonstrate the potential of efavirenz, ouabain, and vinburnine as repurposed agents capable of inhibiting TNBC cell proliferation, stemness, and migration. Their synergistic effects with docetaxel in organoid cultures further underscore their translational relevance and highlight a promising strategy for combination therapies to improve TNBC treatment.
    Journal
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    TGFB1 (Transforming Growth Factor Beta 1) • NDRG1 (N-Myc Downstream Regulated 1)
    |
    docetaxel • efavirenz
    9ms
    Drug-Drug Interaction Potential of Mavorixafor (clinicaltrials.gov)
    P1, N=38, Completed, X4 Pharmaceuticals | Recruiting --> Completed
    Trial completion
    |
    Xolremdi (mavorixafor) • efavirenz