Seeking Future Cures

Fighting deadly infectious diseases

Fungerp: Triterpenoid antifungals

When working in the field of life-threatening infectious diseases, you are racing against rapidly evolving pathogens.

Of the dozens of potential assets within the fungerp family of triterpenoid antifungals, we have narrowed the focus to the most promising of the antifungal compounds to investigate powerful systemic therapeutic options.

SCY-247: Advanced chemistry and favorable tolerability with enormous potential in the fight against deadly fungi

Some of the key advantages of triterpenoid are the broad spectrum of activity, safety and high tissue penetration compared to other antifungals. SCY-247 is a second generation triterpenoid showing significant promise. The collective attributes of broad spectrum of activity, favorable tolerability and high tissue penetration make SCY-247 an attractive development candidate for the treatment and prevention of difficult to treat and emerging fungal infections like C. auris, and those in anatomic areas not adequately reached by other antifungals.

SCY-247 Key attributes

  • Broad-spectrum activity against yeasts, molds, pneumocystis and dimorphic fungi
  • Fungicidal against Candida spp. and potentially Aspergillus spp.
  • Extensive tissue penetration
  • Active against multi-drug resistant (MDR) pathogens, including potent activity against C. auris
  • Suitable for both IV and oral formulations
  • Potential for Qualified Infectious Disease Product (QIDP), Orphan Drug and Fast Track designations
  • Validated mechanism of action (MOA): Glucan synthase inhibition – click here to see how our MOA works

How are the fungerps different?

The structures of the fungerp class of antifungals and echinocandins are very different, allowing for:

  • Different enzyme-inhibition properties than the echinocandins
  • Most gene mutations (FKS) that confer resistance to echinocandins do not affect the activity of fungerps
  • Administration orally and IV (echinocandins are only available IV)
  • Extensive distribution into key tissues associated with fungal infections, often achieving tissue concentration severalfold above the plasma concentrations (echinocandins have a limited tissue distribution achieving tissue concentration at or below plasma concentrations)

The MOA of the novel fungerp antifungals is different from the azoles and polyenes, allowing for:

  • Retention of activity against azole and polyene-resistant strains
  • More favorable safety profile
  • Lower risk for drug-drug interaction (vs. azoles)
  • Retained activity at vaginal pH (4.5)
  • Synergistic antifungal activity when combined with azoles or polyenes, particularly relevant for the treatment of invasive aspergillosis

Ibrexafungerp:

Ibrexafungerp was the first representative of a novel class of structurally-distinct glucan synthase inhibitors, triterpenoids.

Ibrexafungerp has been licensed to GSK.

The U.S. Food and Drug Administration (FDA) approved BREXAFEMME® (ibrexafungerp tablets) in June 2021, for its first indication in vulvovaginal candidiasis (VVC), followed by a second indication in November 2022, for reduction in the incidence of recurrent VVC.

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