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    DRUG:

    itraconazole

    Company:
    Generic mfg.
    Drug class:
    CYP51A1 inhibitor
    Related drugs:
    4d
    A Study to Evaluate the Effect of Itraconazole on the Concentration of GSK3923868 in the Blood in Healthy Participants (clinicaltrials.gov)
    P1, N=20, Completed, GlaxoSmithKline | Not yet recruiting --> Completed
    Trial completion
    |
    itraconazole
    4d
    A Study to Learn if the Study Medicine Called Itraconazole and if Food Changes How the Body Processes the Other Study Medicine Called PF 07258669 in Older Adults or Healthy Adults (clinicaltrials.gov)
    P1, N=26, Completed, Pfizer | Recruiting --> Completed
    Trial completion
    |
    itraconazole
    5d
    A Study to Investigate the Pharmacokinetics of AZD2389 When Administered Alone and in Combination With Itraconazole in Healthy Participants (clinicaltrials.gov)
    P1, N=24, Recruiting, AstraZeneca | Not yet recruiting --> Recruiting
    Enrollment open
    |
    itraconazole
    11d
    D7960C00011: An Open-label Study in Healthy Participants to Evaluate AZD0780 as an Object or Precipitant of CYP3A4-mediated Drug-drug Interactions (clinicaltrials.gov)
    P1, N=78, Recruiting, AstraZeneca | N=42 --> 78
    Enrollment change
    |
    itraconazole • midazolam hydrochloride
    12d
    A Study to Investigate the Pharmacokinetics of AZD2389 When Administered Alone and in Combination With Itraconazole in Healthy Participants (clinicaltrials.gov)
    P1, N=24, Not yet recruiting, AstraZeneca
    New P1 trial
    |
    itraconazole
    12d
    A Drug-Drug Interaction Study to Evaluate the Effects of Itraconazole, Carbamazepine, Quinidine and Fluconazole on the Pharmacokinetics and Safety of EDP-323. (clinicaltrials.gov)
    P1, N=48, Recruiting, Enanta Pharmaceuticals, Inc
    New P1 trial
    |
    itraconazole
    12d
    A Phase 1 Study to Examine the Effects of Itraconazole After Single Dose Administration of Varegacestat (AL102) to Healthy Participants (clinicaltrials.gov)
    P1, N=22, Active, not recruiting, Immunome, Inc. | Trial completion date: Jan 2025 --> Apr 2025
    Trial completion date
    |
    itraconazole • varegacestat (AL102)
    19d
    A Drug-drug Interaction Study with TS-172 in Healthy Adult Male Subjects (clinicaltrials.gov)
    P1, N=30, Not yet recruiting, Taisho Pharmaceutical Co., Ltd.
    New P1 trial
    |
    itraconazole
    26d
    WX081-DDI: Drug-Drug Interaction and Food Effect of Sudapyridine(WX-081) With Itraconazole and Rifampin in Healthy Chinese Adults (clinicaltrials.gov)
    P1, N=16, Not yet recruiting, Shanghai Jiatan Pharmatech Co., Ltd | Initiation date: Dec 2024 --> May 2025 | Trial primary completion date: Feb 2025 --> Oct 2025
    Trial initiation date • Trial primary completion date
    |
    itraconazole • rifampicin
    26d
    Phase 1/1b Study of TLC-6740 in Healthy Subjects and Subjects with Obesity, with or Without Diabetes (clinicaltrials.gov)
    P1, N=506, Recruiting, OrsoBio, Inc | N=341 --> 506 | Trial completion date: Mar 2025 --> Aug 2025 | Trial primary completion date: Jan 2025 --> Jun 2025
    Enrollment change • Trial completion date • Trial primary completion date
    |
    itraconazole
    1m
    Clinical Assessment of the Drug-Drug Interaction Potential of Omaveloxolone in Healthy Adult Participants. (PubMed, J Clin Pharmacol)
    Coadministration of the strong CYP3A4 inhibitor itraconazole significantly increased omaveloxolone maximum plasma concentration (Cmax) and area under the plasma concentration-time curve from time 0 extrapolated to infinity (AUC0-∞) by approximately 3- and 4-fold, respectively. Conversely, coadministration with the moderate CYP3A4 inducer efavirenz decreased Cmax and AUC0-∞ of omaveloxolone by 38.0% and 48.5%, respectively. Omaveloxolone exposure was also increased following coadministration with verapamil, a moderate CYP3A4 and P-glycoprotein (P-gp) inhibitor, but it was unaffected by the strong CYP2C8 inhibitor gemfibrozil...Omaveloxolone was well tolerated when administered alone and in combination with the DME and DT modulators or substrates. These findings support concomitant medication precautions and dosing recommendations for omaveloxolone when coadministered with a moderate or strong CYP3A4 inhibitor or inducer, as well as the substrates of certain CYP450 enzymes or transporters.
    Journal
    |
    SLC22A1 (Solute Carrier Family 22 Member 1)
    |
    itraconazole • efavirenz • Skyclarys (omaveloxolone)
    1m
    Itraconazole promotes melanoma cells apoptosis via inhibiting hedgehog signaling pathway-mediated autophagy. (PubMed, Front Pharmacol)
    In vivo, itraconazole significantly reduced tumor growth in A375 and A2058 xenograft models. Itraconazole induces autophagy-mediated apoptosis in melanoma cells by inhibiting Hedgehog signaling, underscoring its potential as a therapeutic option for melanoma treatment.
    Journal
    |
    SQSTM1 (Sequestosome 1)
    |
    itraconazole
    1m
    A Study in People With Advanced Cancer to Test Whether the Amount of BI 907828 in the Blood is Influenced by Taking an OATP Inhibitor or a CYP3 Inhibitor (clinicaltrials.gov)
    P1, N=34, Active, not recruiting, Boehringer Ingelheim | Trial completion date: Feb 2025 --> Jun 2025
    Trial completion date
    |
    TP53 (Tumor protein P53)
    |
    TP53 wild-type
    |
    brigimadlin (BI 907828) • itraconazole • rifampicin
    1m
    A Study Investigating the Effect of Different Approved Medications on How the Body Processes the Study Compound RO7795081 (clinicaltrials.gov)
    P1, N=50, Recruiting, Hoffmann-La Roche
    New P1 trial
    |
    itraconazole • cyclosporine
    1m
    A Multi-part Study of ALG-000184 to Evaluate Safety, Tolerability, Pharmacokinetics and Drug-drug Interaction Potential After Single and Multiple Doses in Healthy Volunteers (clinicaltrials.gov)
    P1, N=24, Active, not recruiting, Aligos Therapeutics | Not yet recruiting --> Active, not recruiting
    Enrollment closed
    |
    itraconazole
    1m
    The O-glycosyltransferase C1GALT1 promotes EWSR1::FLI1 expression and is a therapeutic target for Ewing sarcoma. (PubMed, Nat Commun)
    Itraconazole, an FDA-approved anti-fungal agent that is known to inhibit C1GALT1, reduces EWSR1::FLI1 levels in ES cell lines and suppresses growth of ES xenografts in mice. Our study reveals a therapeutically targetable mechanism that promotes EWSR1::FLI1 expression and ES tumor growth.
    Journal
    |
    EWSR1 (EWS RNA Binding Protein 1) • FLI1 (Fli-1 Proto-Oncogene ETS Transcription Factor)
    |
    itraconazole
    1m
    529 DDI ITZ: A Study to Assess Change in How Oral Icalcaprant With Itraconazole Moves Through the Body in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=12, Completed, AbbVie | Active, not recruiting --> Completed
    Trial completion
    |
    itraconazole
    1m
    A Study to Determine the Effect of Itraconazole on the Pharmacokinetics of Divarasib in Healthy Participants (clinicaltrials.gov)
    P1, N=18, Active, not recruiting, Genentech, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    divarasib (RG6330) • itraconazole
    2ms
    A Study to Learn if the Study Medicines Called Itraconazole and Cyclosporine Change How the Body Processes the Other Study Medicine Called Danuglipron in Healthy Adults. (clinicaltrials.gov)
    P1, N=12, Active, not recruiting, Pfizer | Not yet recruiting --> Active, not recruiting
    Enrollment closed
    |
    itraconazole • cyclosporine
    2ms
    C1GALT1 expression predicts poor survival in osteosarcoma and is crucial for ABCC1 transporter-mediated doxorubicin resistance. (PubMed, J Pathol)
    Pharmacological inhibition of C1GALT1 using itraconazole replicated these effects, suggesting a potential therapeutic strategy to overcome chemoresistance.
    Journal
    |
    ABCC1 (ATP Binding Cassette Subfamily C Member 1)
    |
    doxorubicin hydrochloride • itraconazole
    2ms
    Clinical Study Aiming to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of a Single Administration of ZE50-0134 at 5 Dose Levels in Healthy Volunteers (clinicaltrials.gov)
    P1, N=88, Recruiting, Eilean Therapeutics
    New P1 trial
    |
    itraconazole
    2ms
    Evaluation of VX-828 in Healthy Participants and in Participants With Cystic Fibrosis (clinicaltrials.gov)
    P1, N=225, Recruiting, Vertex Pharmaceuticals Incorporated | N=159 --> 225 | Trial completion date: Apr 2025 --> Dec 2025
    Enrollment change • Trial completion date
    |
    itraconazole • midazolam hydrochloride
    2ms
    A Study to Learn if the Study Medicine Called Itraconazole and if Food Changes How the Body Processes the Other Study Medicine Called PF 07258669 in Older Adults or Healthy Adults (clinicaltrials.gov)
    P1, N=26, Recruiting, Pfizer | Not yet recruiting --> Recruiting | N=14 --> 26
    Enrollment open • Enrollment change
    |
    itraconazole
    2ms
    A Drug-Drug Interaction (DDI) Study of ADC189 With Itraconazole in Healthy, Adult Subjects (clinicaltrials.gov)
    P1, N=16, Completed, Jiaxing AnDiCon Biotech Co.,Ltd | Recruiting --> Completed | Trial completion date: Dec 2024 --> Sep 2024
    Trial completion • Trial completion date
    |
    itraconazole
    2ms
    Сlinical Study Aiming to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single and Multiple Ascending Doses of ZE63-0302 in Healthy Volunteers (clinicaltrials.gov)
    P1, N=88, Recruiting, Eilean Therapeutics
    New P1 trial
    |
    itraconazole
    2ms
    A Phase 1 Study to Examine the Effects of Itraconazole After Single Dose Administration of Varegacestat (AL102) to Healthy Participants (clinicaltrials.gov)
    P1, N=22, Active, not recruiting, Immunome, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    itraconazole • varegacestat (AL102)
    2ms
    Studies Evaluating the Effects of Itraconazole or Rifampicin on the Pharmacokinetics of TY-9591 Tablets in Healthy Subjects (clinicaltrials.gov)
    P1, N=48, Completed, TYK Medicines, Inc | Recruiting --> Completed | Trial completion date: Aug 2024 --> Dec 2024
    Trial completion • Trial completion date
    |
    itraconazole • Kardorisso (asandeutertinib) • rifampicin
    2ms
    Studies Evaluating the Effects of Itraconazole or Rifampicin on the Pharmacokinetics of TY-9591 Tablets in Healthy Subjects (clinicaltrials.gov)
    P1, N=48, Completed, TYK Medicines, Inc | Recruiting --> Completed | Trial completion date: Aug 2024 --> Dec 2024
    Trial completion • Trial completion date
    |
    itraconazole • Kardorisso (asandeutertinib) • rifampicin
    2ms
    529 DDI ITZ: A Study to Assess Change in How Oral Icalcaprant With Itraconazole Moves Through the Body in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=12, Active, not recruiting, AbbVie | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    itraconazole
    3ms
    Itraconazole Reversing Acquired Resistance to Osimertinib in NSCLC by Inhibiting the SHH/DUSP13B/p-STAT3 Axis. (PubMed, Adv Sci (Weinh))
    In lung adenocarcinoma, p-STAT3 is positively correlated with SHH but negatively correlated with DUSP13B. Together, these results highlight the crucial role of itraconazole in reversing the acquired resistance to osimertinib and provide a scientific rationale for the therapeutic strategy of combining osimertinib with itraconazole.
    Preclinical • Journal
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • GLI1 (GLI Family Zinc Finger 1) • DUSP1 (Dual Specificity Phosphatase 1) • SHH (Sonic Hedgehog Signaling Molecule)
    |
    EGFR mutation
    |
    Tagrisso (osimertinib) • itraconazole
    3ms
    To assess the safety, tolerability and pharmacokinetics of INCB86550 in healthy adult population. (ACTRN12621000103864)
    P1, N=75, Completed, Incyte Corporation | Not yet recruiting --> Completed
    Trial completion
    |
    itraconazole • INCB86550
    3ms
    Drug-Drug Interaction of ASN51 With Fluvoxamine, Itraconazole and Paroxetine in Healthy Subjects (clinicaltrials.gov)
    P1, N=50, Completed, Asceneuron S.A. | Recruiting --> Completed
    Trial completion
    |
    itraconazole
    3ms
    MK-1708-008: A Study to Evaluate the Effects of Itraconazole on MK-1708 in Healthy Participants (MK-1708-003) (clinicaltrials.gov)
    P1, N=12, Completed, Merck Sharp & Dohme LLC | Active, not recruiting --> Completed
    Trial completion
    |
    itraconazole
    3ms
    A Study to Determine the Effect of Itraconazole on the Pharmacokinetics of Divarasib in Healthy Participants (clinicaltrials.gov)
    P1, N=18, Recruiting, Genentech, Inc. | Not yet recruiting --> Recruiting | Trial completion date: Jan 2025 --> Jul 2025 | Trial primary completion date: Jan 2025 --> Jul 2025
    Enrollment open • Trial completion date • Trial primary completion date
    |
    divarasib (RG6330) • itraconazole
    3ms
    A Clinical Trial to Evaluate the Effects of Itraconazole or Rifampicin on the Pharmacokinetics of VC004 Capsules in Healthy Adult Subjects (clinicaltrials.gov)
    P1, N=56, Completed, Jiangsu vcare pharmaceutical technology co., LTD | Not yet recruiting --> Completed
    Trial completion
    |
    itraconazole • VC004 • rifampicin
    3ms
    529 DDI ITZ: A Study to Assess Change in How Oral Icalcaprant With Itraconazole Moves Through the Body in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=12, Recruiting, AbbVie
    New P1 trial
    |
    itraconazole
    3ms
    A Study of the Effect of Itraconazole and Phenytoin on MK-1084 in Healthy Adults (MK-1084-008) (clinicaltrials.gov)
    P1, N=28, Completed, Merck Sharp & Dohme LLC
    New P1 trial
    |
    MK-1084 • itraconazole
    3ms
    Investigation of Drug-drug Interaction of Ritonavir and Itraconazole on the Pharmacokinetics of SHR-A1811 in Subjects With HER2-expressing Advanced Breast Cancer (clinicaltrials.gov)
    P1, N=32, Not yet recruiting, Jiangsu HengRui Medicine Co., Ltd.
    New P1 trial • Metastases
    |
    trastuzumab rezetecan (SHR-A1811) • itraconazole • ritonavir
    3ms
    BGB-11417-107: A Study to Evaluate the Effects of Phenytoin and Itraconazole on Sonrotoclax (BGB-11417) in Healthy Volunteers (clinicaltrials.gov)
    P1, N=30, Completed, BeiGene | Recruiting --> Completed
    Trial completion
    |
    itraconazole • sonrotoclax (BGB-11417)
    3ms
    A Study to Learn if the Study Medicine Called Itraconazole Changes How the Body Processes the Other Study Medicine Called PF-07258669 In Older Adults (clinicaltrials.gov)
    P1, N=14, Not yet recruiting, Pfizer
    New P1 trial
    |
    itraconazole
    3ms
    Clinical and Physiologically Based Pharmacokinetic Model Evaluations of Adagrasib Drug-Drug Interactions. (PubMed, Clin Pharmacol Ther)
    The PBPK model well-described the single and multiple-dose adagrasib PK data as well as DDI data with itraconazole, rifampin, midazolam, warfarin, dextromethorphan, and digoxin, with model predictions within 1.5-fold of the observed clinical data. is predicted to be a strong inhibitor of CYP3A4, a moderate inhibitor of CYP2C9 and CYP2D6, and an inhibitor of P-glycoprotein (P-gp). These results successfully supported regulatory interactions with the United States Food and Drug Administration regarding dosing recommendations for when adagrasib is used concomitantly with other medications, supporting a range of label claims in lieu of clinical trials.
    PK/PD data • Journal
    |
    KRAS (KRAS proto-oncogene GTPase) • CYP2C9 (Cytochrome P450 Family 2 Subfamily C Member 9) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Krazati (adagrasib) • itraconazole • midazolam hydrochloride • rifampicin
    4ms
    A Double-Blind, Placebo-Controlled, First-in-Human Study of the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ZE50 0134 in Healthy Volunteers (ACTRN12624000093583)
    P1, N=88, Recruiting, Eilean Therapeutics AU Pty Ltd (A subsidiary of Eilean Therapeutics LLC) | N=40 --> 88
    Enrollment change • Trial initiation date
    |
    itraconazole