The Fungal Cyp51 Inhibitor VT-1129 Is Efficacious in an Experimental Model of Cryptococcal Meningitis
Open accessAbstract
Cryptococcal meningitis is a significant cause of morbidity and mortality in immunocompromised patients. VT-1129 is a novel fungus-specific Cyp51 inhibitor with potent in vitro activity against Cryptococcus species.
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VT-1129 is an oral tetrazole with robust in vitro and in vivo efficacy against C. neoformans and C. gattii, maintaining activity (mean MIC 0.027 μg/mL) against fluconazole-resistant or dose-dependent C. neoformans isolates.
“Preclinical studies have demonstrated robust in vitro and in vivo efficacy against C. neoformans and C. gattii, notably maintaining activity (mean MIC 0.027 μg/mL) against fluconazole-resistant or dose-dependent C. neoformans isolates (Fig. 1) [92–94].”
From Investigational Agents for the Treatment of Resistant Yeasts and Molds (2021) · cites this paper as [94]
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Shafiei, M., Peyton, L., Hashemzadeh, M., & Foroumadi, A. (2020) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2020.104240 · Cited by 295 · see citing works
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- Authors
- Wiederhold, N. P., Najvar, L. K., Garvey, E. P., Brand, S. R., Xu, X., Ottinger, E. A., Alimardanov, A., Cradock, J., Behnke, M., Hoekstra, W. J., Schotzinger, R. J., Jaramillo, R., Olivo, M., Kirkpatrick, W. R., & Patterson, T. F.
- Affiliations
- The University of Texas at San Antonio Health Science Center (US)
- Viamet Pharmaceuticals (United States) (US)
- National Institutes of Health (US)
- Venue
- Antimicrobial Agents and Chemotherapy
- Publisher
- American Society for Microbiology
- Published
- 2018-09
- Volume
- 62
- Issue
- 9
- ISSN
- 0066-4804 (ISSN-L)
- 1098-6596
- PMC
- PMC6125545
- OpenAlex
- W2881489398
- Cited by
- 27
- References
- 20
- Citations by year
- 2026: 2 · 2025: 2 · 2024: 1 · 2023: 3 · 2022: 5 · 2021: 5 · 2020: 4 · 2019: 4 · 2018: 1
- FWCI
- 2.73
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Antimicrobial Agents and Chemotherapy (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Funders
- HHS | NIH | National Cancer Institute (HHSN261200800001E)
- Topics
- Health Sciences › Medicine › Epidemiology › Fungal Infections and Studies
- Health Sciences › Medicine › Infectious Diseases › Antifungal resistance and susceptibility
- Life Sciences › Immunology and Microbiology › Microbiology › Bacterial Infections and Vaccines
- Keywords
- CYP51 inhibitors, cryptococcal meningitis, Cryptococcus neoformans, fluconazole, oral antifungal therapy, survival, pharmacokinetics, mouse model
- MeSH terms
- Animals, Antifungal Agents, Cryptococcosis, Cryptococcus neoformans, Microbial Sensitivity Tests, Models, Theoretical, Pyridines, Tetrazoles, Fluconazole, Meningitis, Cryptococcal, Mice, Sterol 14-Demethylase, 14-alpha Demethylase Inhibitors
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