Fungal CYP51 Inhibitors VT-1161 and VT-1129 Exhibit Strong In Vitro Activity against Candida glabrata and C. krusei Isolates Clinically Resistant to Azole and Echinocandin Antifungal Compounds
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The in vitro activities of fungal CYP51 inhibitors VT-1161 and VT-1129 were determined for Candida glabrata ( n = 34) and C. krusei ( n = 50). C. glabrata isolates were screened for FKS gene mutations. All isolates were resistant clinically and/or in vitro to at least one standard antifungal compound. VT-1161 and VT-1129 MICs for all isolates were at least 5-fold below achievable human plasma levels for VT-1161. VT-1161 and VT-1129 are promising for the treatment of resistant C. glabrata and C. krusei infections.
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Oteseconazole exhibited potent in vitro activity against most fluconazole-resistant C. albicans and C. krusei isolates (mean MIC ≤ 0.15 μg/mL) and echinocandin-resistant C. glabrata.
“It exhibited potent in vitro activity against most fluconazole-resistant C. albicans and C. krusei isolates (mean MIC ≤ 0.15 μg/mL) as well as echinocandin-resistant C. glabrata [44, 49].”
From Investigational Agents for the Treatment of Resistant Yeasts and Molds (2021) · cites this paper as [44]
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References 11 · Cited by 74
Research works printed but not linked: 2
- [11]Clinical and Laboratory Standards Institute. 2008. Reference method for broth dilution antifungal susceptibility testing of yeasts, 3rd ed M27-A3 Clinical and Laboratory Standards Institute, Wayne, PA. [Google Scholar]
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- Authors
- Schell, W. A., Jones, A. M., Garvey, E. P., Hoekstra, W. J., Schotzinger, R. J., & Alexander, B. D.
- Affiliations
- Duke Medical Center (US)
- Viamet Pharmaceuticals (United States) (US)
- ORCID
- Alexander, B. D.
- Venue
- Antimicrobial Agents and Chemotherapy
- Publisher
- American Society for Microbiology
- Published
- 2017-03
- Volume
- 61
- Issue
- 3
- ISSN
- 0066-4804 (ISSN-L)
- 1098-6596
- PMC
- PMC5328539
- OpenAlex
- W2565813012
- Cited by
- 74
- References
- 11
- Citations by year
- 2026: 4 · 2025: 10 · 2024: 7 · 2023: 9 · 2022: 9 · 2021: 13 · 2020: 8 · 2019: 4 · 2018: 6 · 2017: 3
- FWCI
- 4.00
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Antimicrobial Agents and Chemotherapy (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Infectious Diseases › Antifungal resistance and susceptibility
- Life Sciences › Agricultural and Biological Sciences › Ecology, Evolution, Behavior and Systematics › Fungal Plant Pathogen Control
- Health Sciences › Medicine › Epidemiology › Fungal Infections and Studies
- Keywords
- CYP51 inhibitors, Candida glabrata, Candida krusei, azole resistance, echinocandin resistance, antifungal resistance, in vitro antifungal activity, minimum inhibitory concentration
- MeSH terms
- Antifungal Agents, Azoles, Candida, Candidiasis, Fungal Proteins, Glucosyltransferases, Humans, Microbial Sensitivity Tests, Mutation, Pyridines, Tetrazoles, Gene Expression, Drug Resistance, Fungal, Candida glabrata, Echinocandins, 14-alpha Demethylase Inhibitors
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