The Investigational Fungal Cyp51 Inhibitor VT-1129 Demonstrates Potent In Vitro Activity against Cryptococcus neoformans and Cryptococcus gattii
Open accessAbstract
The in vitro activities of the novel fungal Cyp51 inhibitor VT-1129 were evaluated against a large panel of Cryptococcus neoformans and Cryptococcus gattii isolates. VT-1129 demonstrated potent activities against both Cryptococcus species as demonstrated by low MIC 50 and MIC 90 values. For C. gattii , the in vitro potency was maintained against all genotypes. In addition, significantly lower geometric mean MICs were observed for VT-1129 than for fluconazole against C. neoformans , including isolates with reduced fluconazole susceptibility.
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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 [92]
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- Authors
- Lockhart, S. R., Fothergill, A. W., Iqbal, N., Bolden, C. B., Grossman, N. T., Garvey, E. P., Brand, S. R., Hoekstra, W. J., Schotzinger, R. J., Ottinger, E., Patterson, T. F., & Wiederhold, N. P.
- Affiliations
- Centers for Disease Control and Prevention (US)
- The University of Texas at San Antonio Health Science Center (US)
- Viamet Pharmaceuticals (United States) (US)
- National Institutes of Health (US)
- ORCID
- Venue
- Antimicrobial Agents and Chemotherapy
- Publisher
- American Society for Microbiology
- Published
- 2016-04
- Volume
- 60
- Issue
- 4
- Pages
- 2528-2531
- ISSN
- 0066-4804 (ISSN-L)
- 1098-6596
- PMC
- PMC4808209
- OpenAlex
- W2326587704
- Cited by
- 67
- References
- 16
- Citations by year
- 2026: 3 · 2025: 5 · 2024: 1 · 2023: 4 · 2022: 5 · 2021: 9 · 2020: 6 · 2019: 10 · 2018: 10 · 2017: 10 · 2016: 4
- FWCI
- 10.62
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Antimicrobial Agents and Chemotherapy (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institutes of Health (n01ai25475-8-0-1)
- National Institute of Allergy and Infectious Diseases (N01-AI-25475, N01 AI025475)
- Topics
- Health Sciences › Medicine › Epidemiology › Fungal Infections and Studies
- Health Sciences › Medicine › Infectious Diseases › Antifungal resistance and susceptibility
- Life Sciences › Agricultural and Biological Sciences › Ecology, Evolution, Behavior and Systematics › Fungal Plant Pathogen Control
- Keywords
- CYP51 inhibitors, Cryptococcus neoformans, Cryptococcus gattii, antifungal activity, fluconazole resistance, minimum inhibitory concentration
- MeSH terms
- Antifungal Agents, Cryptococcus neoformans, Fungal Proteins, Genotype, Microbial Sensitivity Tests, Pyridines, Tetrazoles, Drugs, Investigational, Fluconazole, Gene Expression, Drug Resistance, Fungal, Cryptococcus gattii, Sterol 14-Demethylase, 14-alpha Demethylase Inhibitors
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