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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
    22d
    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
    30d
    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
    2ms
    Efavirenz (EFV) Intensification (clinicaltrials.gov)
    P4, N=7, Completed, Washington University School of Medicine
    New P4 trial
    |
    efavirenz
    4ms
    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
    4ms
    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)
    5ms
    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
    |
    TGFB1 (Transforming Growth Factor Beta 1) • NDRG1 (N-Myc Downstream Regulated 1)
    |
    docetaxel • efavirenz
    5ms
    Drug-Drug Interaction Potential of Mavorixafor (clinicaltrials.gov)
    P1, N=38, Completed, X4 Pharmaceuticals | Recruiting --> Completed
    Trial completion
    |
    Xolremdi (mavorixafor) • efavirenz
    6ms
    Approaches to repurposing reverse transcriptase antivirals in cancer. (PubMed, Br J Clin Pharmacol)
    There is a need to examine the relationship between PARP1, PARP2 and mutated BRCA proteins in normal and abnormal LINE-1 retrotransposition. This review explores how efavirenz and related RT inhibitors suppress endogenous reverse transcriptase, providing a basis for preclinical evaluation of RT inhibitors as potential repurposed drugs for cancer treatment.
    Review • Journal • BRCA Biomarker • PARP Biomarker
    |
    BRCA (Breast cancer early onset) • PARP1 (Poly(ADP-Ribose) Polymerase 1) • STING (stimulator of interferon response cGAMP interactor 1) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • CGAS (Cyclic GMP-AMP Synthase) • PARP2 (Poly(ADP-Ribose) Polymerase 2)
    |
    BRCA mutation
    |
    efavirenz
    7ms
    A Study of the Effect Efavirenz on the Plasma Levels of MK-7602 in Healthy Participants (MK-7602-005) (clinicaltrials.gov)
    P1, N=34, Active, not recruiting, Merck Sharp & Dohme LLC | N=16 --> 34
    Enrollment change
    |
    efavirenz
    8ms
    Drug-Drug Interaction Potential of Mavorixafor (clinicaltrials.gov)
    P1, N=36, Recruiting, X4 Pharmaceuticals
    New P1 trial
    |
    Xolremdi (mavorixafor) • efavirenz
    9ms
    A Study of the Effect Efavirenz on the Plasma Levels of MK-7602 in Healthy Participants (MK-7602-005) (clinicaltrials.gov)
    P1, N=16, Active, not recruiting, Merck Sharp & Dohme LLC | Recruiting --> Active, not recruiting | Trial completion date: Apr 2025 --> Jul 2025 | Trial primary completion date: Apr 2025 --> Jul 2025
    Enrollment closed • Trial completion date • Trial primary completion date
    |
    efavirenz
    9ms
    A Study of the Effect Efavirenz on the Plasma Levels of MK-7602 in Healthy Participants (MK-7602-005) (clinicaltrials.gov)
    P1, N=16, Recruiting, Merck Sharp & Dohme LLC | Not yet recruiting --> Recruiting
    Enrollment open
    |
    efavirenz