title: The Investigational Fungal Cyp51 Inhibitor VT-1129 Demonstrates Potent In Vitro Activity against Cryptococcus neoformans and Cryptococcus gattii.
abstract: 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.
authors.affiliation: Mycotic Diseases Branch, Centers for Disease Control and Prevention, Atlanta, Georgia, USA.
authors.forename: Shawn R
authors.initials: SR
authors.lastname: Lockhart
authors.affiliation: University of Texas Health Science Center at San Antonio, San Antonio, Texas, USA.
authors.forename: Annette W
authors.initials: AW
authors.lastname: Fothergill
authors.affiliation: Mycotic Diseases Branch, Centers for Disease Control and Prevention, Atlanta, Georgia, USA.
authors.forename: Naureen
authors.initials: N
authors.lastname: Iqbal
authors.affiliation: Mycotic Diseases Branch, Centers for Disease Control and Prevention, Atlanta, Georgia, USA.
authors.forename: Carol B
authors.initials: CB
authors.lastname: Bolden
authors.affiliation: Mycotic Diseases Branch, Centers for Disease Control and Prevention, Atlanta, Georgia, USA.
authors.forename: Nina T
authors.initials: NT
authors.lastname: Grossman
authors.affiliation: Viamet Pharmaceuticals, Inc., Durham, North Carolina, USA.
authors.forename: Edward P
authors.initials: EP
authors.lastname: Garvey
authors.affiliation: Viamet Pharmaceuticals, Inc., Durham, North Carolina, USA.
authors.forename: Stephen R
authors.initials: SR
authors.lastname: Brand
authors.affiliation: Viamet Pharmaceuticals, Inc., Durham, North Carolina, USA.
authors.forename: William J
authors.initials: WJ
authors.lastname: Hoekstra
authors.affiliation: Viamet Pharmaceuticals, Inc., Durham, North Carolina, USA.
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Schotzinger
authors.affiliation: National Institutes of Health, Therapeutics for Rare and Neglected Diseases, Bethesda, Maryland, USA.
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Ottinger
authors.affiliation: University of Texas Health Science Center at San Antonio, San Antonio, Texas, USA South Texas Veterans Health Care System, San Antonio, Texas, USA.
authors.forename: Thomas F
authors.initials: TF
authors.lastname: Patterson
authors.affiliation: University of Texas Health Science Center at San Antonio, San Antonio, Texas, USA wiederholdn@uthscsa.edu.
authors.forename: Nathan P
authors.initials: NP
authors.lastname: Wiederhold
mesh_terms: D058888:14-alpha Demethylase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D056285:Cryptococcus gattii / Q000187:drug effects / Q000201:enzymology / Q000235:genetics; D003455:Cryptococcus neoformans / Q000187:drug effects / Q000201:enzymology / Q000235:genetics; D025141:Drug Resistance, Fungal / Q000235:genetics; D015507:Drugs, Investigational / Q000138:chemical synthesis / Q000494:pharmacology*; D015725:Fluconazole / Q000494:pharmacology; D005656:Fungal Proteins / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D015870:Gene Expression; D005838:Genotype; D008826:Microbial Sensitivity Tests; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology*; D058886:Sterol 14-Demethylase / Q000235:genetics / Q000378:metabolism*; D013777:Tetrazoles / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D058888:14-alpha Demethylase Inhibitors; D000935:Antifungal Agents; D015507:Drugs, Investigational; D005656:Fungal Proteins; D011725:Pyridines; D013777:Tetrazoles; C000612857:VT-1129; D015725:Fluconazole; D058886:Sterol 14-Demethylase