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

Shawn R Lockhart1, Annette W Fothergill2, Naureen Iqbal1

  • 1Mycotic Diseases Branch, Centers for Disease Control and Prevention, Atlanta, Georgia, USA.

Antimicrobial Agents and Chemotherapy
|January 21, 2016
PubMed

Insights

The novel fungal Cyp51 inhibitor VT-1129 shows potent in vitro activity against Cryptococcus neoformans and Cryptococcus gattii. VT-1129 is more effective than fluconazole, especially against fluconazole-resistant strains.

Area of Science:

  • Mycology
  • Infectious Diseases
  • Antifungal Drug Discovery

Background:

  • Cryptococcus neoformans and Cryptococcus gattii are major fungal pathogens causing cryptococcosis.
  • Emergence of antifungal resistance necessitates development of novel therapeutic agents.
  • The enzyme lanosterol 14α-demethylase (Cyp51) is a validated target for antifungal drugs.

Purpose of the Study:

  • To evaluate the in vitro antifungal activity of VT-1129, a novel fungal Cyp51 inhibitor.
  • To compare the efficacy of VT-1129 against fluconazole in Cryptococcus species isolates.

Main Methods:

  • Broth microdilution method was used to determine the minimum inhibitory concentrations (MICs).
  • A large panel of Cryptococcus neoformans and Cryptococcus gattii isolates were tested.
  • Geometric mean MICs were calculated and compared between VT-1129 and fluconazole.

Main Results:

  • VT-1129 demonstrated potent in vitro activity against both C. neoformans and C. gattii, with low MIC50 and MIC90 values.
  • The in vitro potency of VT-1129 was consistent across all genotypes of C. gattii.
  • Significantly lower geometric mean MICs were observed for VT-1129 compared to fluconazole against C. neoformans, including fluconazole-resistant isolates.

Conclusions:

  • VT-1129 exhibits broad-spectrum in vitro activity against clinically relevant Cryptococcus species.
  • VT-1129 represents a promising therapeutic candidate for cryptococcosis, particularly in cases of fluconazole resistance.

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