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).

P1, N=5, Recruiting, Milton S. Hershey Medical Center | Trial completion date: May 2024 --> Jan 2025 | Trial primary completion date: May 2024 --> Dec 2024

P=N/A, N=200, Active, not recruiting, University of Rome Tor Vergata | Recruiting --> Active, not recruiting

P1, N=32, Recruiting, Celgene | Not yet recruiting --> Recruiting

P=N/A, N=60, Completed, Cairo University | Enrolling by invitation --> Completed

P2, N=8, Terminated, Pulmatrix Inc. | Active, not recruiting --> Terminated; Low enrollment

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.

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

P1, N=430, Completed, Taro Pharmaceuticals USA

P=N/A, N=150, Not yet recruiting, First Hospital of China Medical University

P4, N=30, Recruiting, University of Oklahoma | Trial primary completion date: Jan 2024 --> Jun 2024

P2, N=68, Recruiting, Montreal Heart Institute | Trial completion date: Mar 2024 --> Dec 2024 | Trial primary completion date: Mar 2024 --> Dec 2024

P3, N=120, Not yet recruiting, Weill Medical College of Cornell University

P=N/A, N=104, Recruiting, Postgraduate Institute of Medical Education and Research | Trial primary completion date: Dec 2023 --> Dec 2024

P1, N=105, Recruiting, University of Manitoba | Trial completion date: Apr 2025 --> Apr 2026 | Trial primary completion date: Apr 2024 --> Apr 2025

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

P1, N=60, Recruiting, Alexion Pharmaceuticals, Inc. | Not yet recruiting --> Recruiting

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.

P2/3, N=382, Completed, Hill Dermaceuticals, Inc. | Phase classification: P3 --> P2/3

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

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

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.

[F]7b is a valuable radiometric tool to study TGase 2 in vitro under various conditions. However, its suitability for targeting tumor-associated TGase 2 is strongly limited due its unfavorable pharmacokinetic properties as demonstrated in rodents. Consequently, from a radiochemical perspective [F]7b requires appropriate structural modifications to overcome these limitations.

P2, N=68, Recruiting, Montreal Heart Institute

P1, N=157, Recruiting, Vertex Pharmaceuticals Incorporated | Not yet recruiting --> Recruiting

P3, N=123, Recruiting, Pulmocide Ltd | Trial completion date: Nov 2023 --> Apr 2025 | Trial primary completion date: Oct 2023 --> Mar 2025

P1, N=60, Not yet recruiting, Alexion Pharmaceuticals, Inc.

P1, N=32, Not yet recruiting, Celgene

P2, N=78, Not yet recruiting, VA Office of Research and Development | Trial completion date: Dec 2029 --> Feb 2029

P1, N=157, Not yet recruiting, Vertex Pharmaceuticals Incorporated

P4, N=30, Recruiting, University of Oklahoma | Trial completion date: Jan 2024 --> Jun 2024

In the present work, a series of N-terpenyl organoselenium compounds (CHB1-6) were evaluated for antimycotic activity by determining the minimum inhibitory concentration (MIC) for each compound in fluconazole (FLU)-sensitive (S1) and FLU-resistant (S2) strains of Candida albicans (C...Using a mouse model of vulvovaginal candidiasis (VVC), CHB4 and CHB6 both exhibited antimycotic efficacy by reducing yeast colonization of the vaginal tract, alleviating injury to the vaginal mucosa, and decreasing the abundance of myeloperoxidase (MPO) expression in the tissue, indicating a reduced inflammatory response. In conclusion, CHB4 and CHB6 demonstrate antifungal activity in vitro and in the mouse model of VVC and represent two new promising antifungal agents.

P2, N=102, Completed, Pulmocide Ltd | Active, not recruiting --> Completed

P1, N=14, Completed, Boehringer Ingelheim | Active, not recruiting --> Completed

P2, N=30, Recruiting, Pulmatrix Inc. | Trial completion date: Apr 2024 --> Jul 2024 | Trial primary completion date: Apr 2024 --> Jul 2024

P1, N=40, Completed, Lundquist Institute for Biomedical Innovation at Harbor-UCLA Medical Center | Active, not recruiting --> Completed

P1, N=14, Active, not recruiting, Boehringer Ingelheim | Recruiting --> Active, not recruiting

P1, N=14, Completed, Boehringer Ingelheim | Active, not recruiting --> Completed

We showed that ATO is an important inhibitor of HH pathway but ITRA can weaken the inhibitory effect of ATO. This study provides an experimental evidence for the clinical use of ATO and ITRA in the treatment of NB with HH pathway activation in cytology.

P4, N=17, Completed, University of Maryland, Baltimore | N=12 --> 17

P1, N=14, Active, not recruiting, Boehringer Ingelheim | Recruiting --> Active, not recruiting

After a 4-week amphotericin B and flucytosine treatment, his condition recovered well and then was followed by a 3-month oral fluconazole treatment. There was no evidence of recurrence within one year. Our case highlights that nucleic acids obtained from formalin-fixed tissue could be a feasible identification method, especially in those whose culture results are unavailable.