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DRUG CLASS:

CYP51A1 inhibitor

16d
Ectopic ACTH-Dependent Cushing's Syndrome Emerging at a Late Stage of a Mixed Histology Neuroendocrine Neoplasm: A Case Report. (PubMed, Case Rep Oncol)
Urinary free cortisol measurement was 21-fold the upper limit of the reference range (3,614.0 nmol/24 h), and cortisol concentration did not decrease after 1mg-dexamethasone suppression test (1,812 nmol/L for an expected value <50 nmol/L), confirming the ACTH-dependent CS...Hypercortisolism symptoms were effectively managed with an adrenal enzyme inhibitor (ketoconazole) in combination with somatostatin analogs...This redifferentiation phenomenon in neuroendocrine tumors should be further investigated as patients might be, under certain conditions, eligible for PRRT. Therefore, we suggest that newly occurring paraneoplastic syndromes in patients with NEC should always be evaluated using 68Ga-DOTATATE PET/CT.
Journal
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SSTR (Somatostatin Receptor)
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SSTR Expression
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dexamethasone
17d
Testing the Role of Anti-fungal Therapy in Improving the Response to Therapies for Crohn's Disease (clinicaltrials.gov)
P3, N=120, Recruiting, Weill Medical College of Cornell University | Not yet recruiting --> Recruiting
Enrollment open • Combination therapy
28d
Intravitreal Fluconazole Injection for Fungal Endophthalmitis as Treatment Option in a Patient With End-Stage Liver and Kidney Diseases. (PubMed, J Med Cases)
In the meantime, the retinal infiltrate became inactive and vitreous opacity resolved. Intravitreal fluconazole injection is a treatment option for fungal endophthalmitis in the case that a patient cannot undergo vitrectomy and cannot take a maximum dose of fluconazole because of poor renal function.
Journal
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CRP (C-reactive protein)
1m
Itraconazole to Prevent Recurrent Barrett's Esophagus (clinicaltrials.gov)
P1, N=10, Active, not recruiting, University of Kansas Medical Center | Recruiting --> Active, not recruiting | Trial completion date: Dec 2023 --> Jun 2025 | Trial primary completion date: Sep 2023 --> Feb 2024
Enrollment closed • Trial completion date • Trial primary completion date
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itraconazole
2ms
Research on Precise Differentiation and Treatment Response Markers and Prediction Model of VVC Spleen Deficiency Dampness Syndrome Based on PBMC (ChiCTR2400087052)
P=N/A, N=200, Not yet recruiting, Guangdong Provincial Hospital of Chinese Medicine (Guangdong Provincial Academic of Chinese Medicine Science; Second Clinical Medical College, Guangzh
New trial
2ms
Knockouts of CYP51A1, DHCR24, or SC5D from cholesterol synthesis reveal pathways modulated by sterol intermediates. (PubMed, iScience)
In contrast, SC5D and DHCR24 KO cells with elevated lathosterol or desmosterol proliferated slowly, with downregulated E2F, mitosis, and enriched HNF1A. These findings demonstrate that increase of lanosterol and 24,25-dihydrolanosterol, but not other sterols, promotes cell proliferation in hepatocytes.
Journal
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HNF1A (HNF1 Homeobox A)
3ms
Plasma TNF-α Elevation in Biologic Naive Rheumatoid Arthritis Patients Belonging to a Population with New Mutations in TLR4 and CYP51A1 genes without Association with Disease-Related Antibodies Levels. (PubMed, Int J Mol Cell Med)
The data of this study showed that both TLR4 rs141534085 and CYP51A1 rs6 related DNA regions should be considered as hotspot areas in RA pathogenicity. Moreover, these data indicated that, TNF- α did not alter the production of anti-CCP and RF pathogenic antibodies in patients with long-term RA.
Journal • IO biomarker
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TNFA (Tumor Necrosis Factor-Alpha) • TLR4 (Toll Like Receptor 4) • IL6R (Interleukin 6 receptor)
3ms
New trial
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TREM2 (Triggering Receptor Expressed On Myeloid Cells 2)
4ms
HNF4α improves hepatocyte regeneration by upregulating PXR. (PubMed, FASEB J)
Meanwhile, when the upward trend of PXR gene expression was inhibited by ketoconazole, the proliferation rate decreased. By inhibiting HNF4α and creating a partial hepatectomy (PHx), we demonstrated that HNF4α can upregulate PXR to promote liver regeneration in vivo. Therefore, HNF4α is shown to improve hepatocyte regeneration by upregulating PXR, which provides a reference for future research on the combined application of drugs for the treatment of liver injury.
Journal
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HNF1A (HNF1 Homeobox A)
4ms
Ocimum basilicum and Lagenaria siceraria Loaded Lignin Nanoparticles as Versatile Antioxidant, Immune Modulatory, Anti-Efflux, and Antimicrobial Agents for Combating Multidrug-Resistant Bacteria and Fungi. (PubMed, Antioxidants (Basel))
OB-LNPs and LS-LNPs were further tested for their anti-efflux activity against ciprofloxacin-resistant Salmonella enterica strains and for treating Salmonella infection in a rat model. Treatment of T. rubrum-infected guinea pigs with OB-LNPs and LS-LNPs topically in combination with itraconazole resulted in a reduction in lesion scores, microscopy, and culture results. In conclusion, OB-LNPs and LS-LNPs possess immunomodulatory and antioxidant potential and can be used as naturally derived nanoparticles for drug delivery and treatment of Salmonellosis and dermatophytosis infections.
Journal
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IFNG (Interferon, gamma) • TNFA (Tumor Necrosis Factor-Alpha)
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itraconazole
4ms
Endothelial Derived Hyperpolarization Factor and Vascular Control (clinicaltrials.gov)
P4, N=30, Recruiting, University of Oklahoma | Trial completion date: Jun 2024 --> May 2025 | Trial primary completion date: Jun 2024 --> Dec 2024
Trial completion date • Trial primary completion date
4ms
New P1 trial
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itraconazole
5ms
Impact of Cerebrospinal Fluid Leukocyte Infiltration and Neuroimmmune Mediators on Survival with HIV-Associated Cryptococcal Meningitis. (PubMed, medRxiv)
We enrolled 401 adults with HIV-associated cryptococcal meningitis in Uganda who received amphotericin and fluconazole induction therapy...18-week survival after diagnosis of cryptococcal meningitis was associated with higher CSF leukocytes at baseline with greater T helper 1 (IFN-γ, IL-2 and TNF-α cytokines), T helper 17 (IL-17A cytokine) and CXCR3 + T cell (CXCL10 chemokine) responses. These results highlight the interdependent contribution of soluble and cellular immune responses in predicting survival with HIV-associated cryptococcal meningitis.
Journal
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CD8 (cluster of differentiation 8) • IFNG (Interferon, gamma) • TNFA (Tumor Necrosis Factor-Alpha) • CXCL10 (Chemokine (C-X-C motif) ligand 10) • CD4 (CD4 Molecule) • IL2 (Interleukin 2) • IL17A (Interleukin 17A) • CXCR3 (C-X-C Motif Chemokine Receptor 3)
5ms
Trial completion
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itraconazole
5ms
New P3 trial
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itraconazole
6ms
CD-IT: Evaluation of the Response of Itraconazole and Terbinafine Therapy in Subjects With Crohn's Disease (clinicaltrials.gov)
P2, N=16, Terminated, Montreal Heart Institute | N=68 --> 16 | Trial completion date: Dec 2024 --> Feb 2024 | Recruiting --> Terminated | Trial primary completion date: Dec 2024 --> Feb 2024; Insufficient patient enrollment
Enrollment change • Trial completion date • Trial termination • Trial primary completion date
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itraconazole
6ms
Enrollment closed
6ms
Drug-Cannabinoid Interactions in Selected Therapeutics for Symptoms Associated with Epilepsy, Autism Spectrum Disorder, Cancer, Multiple Sclerosis, and Pain. (PubMed, Pharmaceuticals (Basel))
For example, the combination of cannabis-derived compounds and the antifungal drug ketoconazole, a CYP3A4 inhibitor, increases the plasma concentration of Δ-9-tetrahydrocannabinol (THC) and cannabidiol (CBD). In contrast, rifampicin, a CYP3A4 inducer, stands out for reducing plasma THC levels by approximately 20-40% and 50% to 60% for CBD...Although further studies are still pending, there is currently clinical evidence supporting drug interactions with cannabinoids, requiring doctors to evaluate the risk of drug combinations with cannabinoids and vice versa. The tables provided here were designed to facilitate the identification of biorelevant interactions that may compromise therapeutic efficacy and toxicity.
Review • Journal
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CYP2C9 (Cytochrome P450 Family 2 Subfamily C Member 9)
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rifampicin
6ms
Machine learning-assisted SERS approach enables the biochemical discrimination in Bcl-2 and Mcl-1 expressing yeast cells treated with ketoconazole and fluconazole antifungals. (PubMed, Talanta)
Also, cell viability assay, Annexin V-FITC/PI double staining, and total oxidant and antioxidant status analyses were performed to support Raman measurements. We strongly believe that the proposed approach paves the way for the evaluation of various biochemical structures/changes in various cells.
Journal • IO biomarker • Machine learning
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BCL2 (B-cell CLL/lymphoma 2) • MCL1 (Myeloid cell leukemia 1) • ANXA5 (Annexin A5)
6ms
Search for new biologically active compounds: in vitro studies of antitumor and antimicrobial activity of dirhodium(II,II) paddlewheel complexes. (PubMed, Dalton Trans)
Antimicrobial tests showed that the Rh2-Rh4 complexes exerted a strong inhibitory effect on G+ bacteria B. cereus and G- bacteria V. parahaemolyticus as well as on the yeast C. tropicalis, which showed a higher sensitivity compared to fluconazole. The cytotoxic activity of Rh1-Rh4 complexes tested on three cancer cell lines (HeLa, HCT116 and MDA-MB-231) and on healthy MRC-5 cells showed that all investigated complexes elicited more efficient cytotoxicity on all tested tumor cells than on control cells. Investigation of the mechanism of action revealed that the Rh1-Rh4 complexes inhibit cell proliferation via different mechanisms of action, namely apoptosis (increase in expression of the pro-apoptotic Bax protein and caspase-3 protein in HeLa and HCT116 cells; changes in mitochondrial potential and mitochondrial damage; release of cytochrome c from the mitochondria; cell cycle arrest in G2/M phase in both HeLa and HCT116 cells together with a decrease in the expression of cyclin A and cyclin B) and autophagy (reduction in the expression of the protein p62 in HeLa and HCT116 cells).
Preclinical • Journal
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BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • CCNA2 (Cyclin A2)
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BAX expression
6ms
Neuro-pharmacological Properties of Repurposed Ketoconazole in Glioblastomas (clinicaltrials.gov)
P1, N=5, Recruiting, Milton S. Hershey Medical Center | Trial completion date: May 2024 --> Jan 2025 | Trial primary completion date: May 2024 --> Dec 2024
Trial completion date • Trial primary completion date
6ms
MYCDERM: Mycosis Culture Collection From Dermatological Isolated (clinicaltrials.gov)
P=N/A, N=200, Active, not recruiting, University of Rome Tor Vergata | Recruiting --> Active, not recruiting
Enrollment closed
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itraconazole
6ms
Enrollment open
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itraconazole
7ms
Blue Light Emitting Diode Therapy on Vulvovaginal Candidiasis (clinicaltrials.gov)
P=N/A, N=60, Completed, Cairo University | Enrolling by invitation --> Completed
Trial completion
8ms
Study to Evaluate Itraconazole Administered as Inhaled Dry Powder in Adults With Asthma and ABPA (clinicaltrials.gov)
P2, N=8, Terminated, Pulmatrix Inc. | Active, not recruiting --> Terminated; Low enrollment
Trial termination
8ms
The activation of the adaptor protein STING depends on its interactions with the phospholipid PI4P. (PubMed, Sci Signal)
In contrast, STING activation was enhanced when the lipid-shuttling protein OSBP, which removes PI4P from the Golgi apparatus, was inhibited by the US Food and Drug Administration-approved antifungal itraconazole...Furthermore, a mutant STING that could not bind to PI4P failed to traffic from the ER to the Golgi apparatus in response to a STING agonist, whereas forced relocalization of STING to PI4P-enriched areas elicited STING activation in the absence of stimulation with a STING agonist. Thus, PI4P is critical for STING activation, and manipulating PI4P abundance may therapeutically modulate STING-dependent immune responses.
Journal
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STING (stimulator of interferon response cGAMP interactor 1) • IFNB1 (Interferon Beta 1)
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STING mutation
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itraconazole
8ms
Village Integrated Eye Workers Trial (clinicaltrials.gov)
P=N/A, N=223671, Active, not recruiting, University of California, San Francisco | Trial completion date: Dec 2023 --> Jan 2025 | Trial primary completion date: Dec 2023 --> Jan 2025
Trial completion date • Trial primary completion date
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itraconazole
8ms
New trial
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itraconazole
9ms
Endothelial Derived Hyperpolarization Factor and Vascular Control (clinicaltrials.gov)
P4, N=30, Recruiting, University of Oklahoma | Trial primary completion date: Jan 2024 --> Jun 2024
Trial primary completion date
9ms
CD-IT: Evaluation of the Response of Itraconazole and Terbinafine Therapy in Subjects With Crohn's Disease (clinicaltrials.gov)
P2, N=68, Recruiting, Montreal Heart Institute | Trial completion date: Mar 2024 --> Dec 2024 | Trial primary completion date: Mar 2024 --> Dec 2024
Trial completion date • Trial primary completion date
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itraconazole
9ms
New P3 trial • Combination therapy
9ms
GLITZ: Oral Itraconazole Versus Combination of Systemic Glucorticoids and Oral Itraconazole in CPA-ABPA Overlap Syndrome (clinicaltrials.gov)
P=N/A, N=104, Recruiting, Postgraduate Institute of Medical Education and Research | Trial primary completion date: Dec 2023 --> Dec 2024
Trial primary completion date
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prednisone • itraconazole • prednisolone
9ms
THRIVE-yeast: Vulvovaginal Candidiasis in Canadian Females (clinicaltrials.gov)
P1, N=105, Recruiting, University of Manitoba | Trial completion date: Apr 2025 --> Apr 2026 | Trial primary completion date: Apr 2024 --> Apr 2025
Trial completion date • Trial primary completion date
9ms
A Randomized Controlled Trial to Compare the Clinical Outcomes With Six Months of Therapy With Oral Itraconazole Versus Oral Voriconazole for Management of Treatment naïve Subjects With Chronic Pulmonary Aspergillosis (clinicaltrials.gov)
P3, N=100, Active, not recruiting, Postgraduate Institute of Medical Education and Research | Recruiting --> Active, not recruiting | Trial completion date: Dec 2023 --> Mar 2024 | Trial primary completion date: Dec 2023 --> Mar 2024
Enrollment closed • Trial completion date • Trial primary completion date
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itraconazole
9ms
Enrollment open
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itraconazole
10ms
Itraconazole inhibits tumor growth via CEBPB-mediated glycolysis in colorectal cancer. (PubMed, Cancer Sci)
Itraconazole inhibited cell glycolysis and tumor growth via the CEBPB-ENO1 axis. In this study, we illustrate a new energy metabolism mechanism for itraconazole on tumor growth in CRC that will provide a theoretical basis for CRC targeting/combination therapy.
Journal
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ENO1 (Enolase 1)
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itraconazole
10ms
Efficacy and Safety Study of Miconazole Oil Versus Vehicle on Fungal Infection of the Ear Canal (Otomycosis) (clinicaltrials.gov)
P2/3, N=382, Completed, Hill Dermaceuticals, Inc. | Phase classification: P3 --> P2/3
Phase classification
10ms
Phase III Efficacy and Safety Study of Miconazole Oil for Otomycosis (clinicaltrials.gov)
P3, N=100, Recruiting, Hill Dermaceuticals, Inc. | Not yet recruiting --> Recruiting | Trial completion date: Nov 2023 --> Nov 2024 | Trial primary completion date: Sep 2023 --> Sep 2024
Enrollment open • Trial completion date • Trial primary completion date
10ms
Study to Evaluate Itraconazole Administered as Inhaled Dry Powder in Adults With Asthma and ABPA (clinicaltrials.gov)
P2, N=8, Active, not recruiting, Pulmatrix Inc. | Recruiting --> Active, not recruiting | N=30 --> 8 | Trial completion date: Jul 2024 --> Feb 2024 | Trial primary completion date: Jul 2024 --> Feb 2024
Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
11ms
Itraconazole halts hepatocellular carcinoma progression by modulating sonic hedgehog signaling in rats: A novel therapeutic approach. (PubMed, Pathol Res Pract)
Moreover, itraconazole exhibited a promise to impede the transformation of epithelial cells into a more mesenchymal-like phenotype. Overall, this study emphasizes the significance of targeting the hedgehog pathway with itraconazole as a promising avenue for further exploration in clinical studies related to HCC treatment.
Preclinical • Journal
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NOTCH1 (Notch 1) • GLI1 (GLI Family Zinc Finger 1) • GLI2 (GLI Family Zinc Finger 2)
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itraconazole