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DRUG:

itraconazole

Company:
Generic mfg.
Drug class:
CYP51A1 inhibitor
Related drugs:
4d
Trial completion
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itraconazole
5d
Enrollment open
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itraconazole
11d
Enrollment change
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itraconazole • midazolam hydrochloride
12d
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
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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
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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
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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
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SLC22A1 (Solute Carrier Family 22 Member 1)
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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
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SQSTM1 (Sequestosome 1)
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itraconazole
1m
Trial completion date
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TP53 (Tumor protein P53)
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TP53 wild-type
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brigimadlin (BI 907828) • itraconazole • rifampicin
1m
New P1 trial
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itraconazole • cyclosporine
1m
Enrollment closed
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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
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EWSR1 (EWS RNA Binding Protein 1) • FLI1 (Fli-1 Proto-Oncogene ETS Transcription Factor)
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itraconazole
1m
Trial completion
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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
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divarasib (RG6330) • itraconazole
2ms
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
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ABCC1 (ATP Binding Cassette Subfamily C Member 1)
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doxorubicin hydrochloride • 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
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itraconazole • midazolam hydrochloride
2ms
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
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itraconazole
2ms
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
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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
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itraconazole • Kardorisso (asandeutertinib) • rifampicin
2ms
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
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • GLI1 (GLI Family Zinc Finger 1) • DUSP1 (Dual Specificity Phosphatase 1) • SHH (Sonic Hedgehog Signaling Molecule)
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EGFR mutation
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Tagrisso (osimertinib) • itraconazole
3ms
Trial completion
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itraconazole • INCB86550
3ms
Trial completion
|
itraconazole
3ms
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
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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
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itraconazole • VC004 • rifampicin
3ms
New P1 trial
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MK-1084 • itraconazole
3ms
New P1 trial • Metastases
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trastuzumab rezetecan (SHR-A1811) • itraconazole • ritonavir
3ms
Trial completion
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itraconazole • sonrotoclax (BGB-11417)
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
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KRAS (KRAS proto-oncogene GTPase) • CYP2C9 (Cytochrome P450 Family 2 Subfamily C Member 9) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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KRAS mutation • KRAS G12C • KRAS G12
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Krazati (adagrasib) • itraconazole • midazolam hydrochloride • rifampicin
4ms
Enrollment change • Trial initiation date
|
itraconazole