The Investigational Fungal Cyp51 Inhibitor VT-1129 Demonstrates Potent In Vitro Activity against Cryptococcus neoformans and Cryptococcus gattii

Thein vitroactivities of the novel fungal Cyp51 inhibitor VT-1129 were evaluated against a large panel ofCryptococcus neoformansandCryptococcus gattiiisolates. VT-1129 demonstrated potent activities against bothCryptococcusspecies as demonstrated by low MIC50and MIC90values. ForC. gattii, thein vitr...

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Veröffentlicht in:	Antimicrobial agents and chemotherapy 2016-04, Vol.60 (4), p.2528-2531
Hauptverfasser:	Lockhart, Shawn R, Fothergill, Annette W, Iqbal, Naureen, Bolden, Carol B, Grossman, Nina T, Garvey, Edward P, Brand, Stephen R, Hoekstra, William J, Schotzinger, Robert J, Ottinger, Elizabeth, Patterson, Thomas F, Wiederhold, Nathan P
Format:	Artikel
Sprache:	eng
Schlagworte:	14-alpha Demethylase Inhibitors 14-alpha Demethylase Inhibitors - chemical synthesis 14-alpha Demethylase Inhibitors - pharmacology Antifungal Agents Antifungal Agents - chemical synthesis Antifungal Agents - pharmacology Cryptococcus gattii - drug effects Cryptococcus gattii - enzymology Cryptococcus gattii - genetics Cryptococcus neoformans - drug effects Cryptococcus neoformans - enzymology Cryptococcus neoformans - genetics Drug Resistance, Fungal - genetics Drugs, Investigational Drugs, Investigational - chemical synthesis Drugs, Investigational - pharmacology Fluconazole - pharmacology Fungal Proteins Fungal Proteins - antagonists & inhibitors Fungal Proteins - genetics Fungal Proteins - metabolism Gene Expression Genotype Microbial Sensitivity Tests Pyridines Pyridines - chemical synthesis Pyridines - pharmacology Sterol 14-Demethylase Sterol 14-Demethylase - genetics Sterol 14-Demethylase - metabolism Susceptibility Tetrazoles Tetrazoles - chemical synthesis Tetrazoles - pharmacology
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Zusammenfassung:	Thein vitroactivities of the novel fungal Cyp51 inhibitor VT-1129 were evaluated against a large panel ofCryptococcus neoformansandCryptococcus gattiiisolates. VT-1129 demonstrated potent activities against bothCryptococcusspecies as demonstrated by low MIC50and MIC90values. ForC. gattii, thein vitropotency was maintained against all genotypes. In addition, significantly lower geometric mean MICs were observed for VT-1129 than for fluconazole againstC. neoformans, including isolates with reduced fluconazole susceptibility.
ISSN:	0066-4804 1098-6596
DOI:	10.1128/AAC.02770-15