Literature DB >> 33668824

Ibrexafungerp: A First-in-Class Oral Triterpenoid Glucan Synthase Inhibitor.

Sabelle Jallow1, Nelesh P Govender1,2.   

Abstract

Ibrexafungerp (formerly SCY-078 or MK-3118) is a first-in-class triterpenoid antifungal or "fungerp" that inhibits biosynthesis of β-(1,3)-D-glucan in the fungal cell wall, a mechanism of action similar to that of echinocandins. Distinguishing characteristics of ibrexafungerp include oral bioavailability, a favourable safety profile, few drug-drug interactions, good tissue penetration, increased activity at low pH and activity against multi-drug resistant isolates including C. auris and C. glabrata. In vitro data has demonstrated broad and potent activity against Candida and Aspergillus species. Importantly, ibrexafungerp also has potent activity against azole-resistant isolates, including biofilm-forming Candida spp., and echinocandin-resistant isolates. It also has activity against the asci form of Pneumocystis spp., and other pathogenic fungi including some non-Candida yeasts and non-Aspergillus moulds. In vivo data have shown IBX to be effective for treatment of candidiasis and aspergillosis. Ibrexafungerp is effective for the treatment of acute vulvovaginal candidiasis in completed phase 3 clinical trials.

Entities:  

Keywords:  MK-3118; SCY-078; aspergillosis; candidiasis; fungal cell wall; fungerp; glucan synthase inhibitor; ibrexafungerp (IBX); invasive fungal disease; triterpenoid antifungal; β-(1,3)-D-glucan

Year:  2021        PMID: 33668824      PMCID: PMC7996284          DOI: 10.3390/jof7030163

Source DB:  PubMed          Journal:  J Fungi (Basel)        ISSN: 2309-608X


  103 in total

1.  Surface coatings with covalently attached caspofungin are effective in eliminating fungal pathogens.

Authors:  Bryan R Coad; Stephanie J Lamont-Friedrich; Lauren Gwynne; Marek Jasieniak; Stefani S Griesser; Ana Traven; Anton Y Peleg; Hans J Griesser
Journal:  J Mater Chem B       Date:  2015-10-07       Impact factor: 6.331

2.  Differential Activity of the Oral Glucan Synthase Inhibitor SCY-078 against Wild-Type and Echinocandin-Resistant Strains of Candida Species.

Authors:  Michael A Pfaller; Shawn A Messer; Paul R Rhomberg; Katyna Borroto-Esoda; Mariana Castanheira
Journal:  Antimicrob Agents Chemother       Date:  2017-07-25       Impact factor: 5.191

3.  In Vitro Activity of Ibrexafungerp, a Novel Glucan Synthase Inhibitor against Candida glabrata Isolates with FKS Mutations.

Authors:  Natalie S Nunnally; Kizee A Etienne; David Angulo; Shawn R Lockhart; Elizabeth L Berkow
Journal:  Antimicrob Agents Chemother       Date:  2019-10-22       Impact factor: 5.191

4.  SCY-078, a Novel Fungicidal Agent, Demonstrates Distribution to Tissues Associated with Fungal Infections during Mass Balance Studies with Intravenous and Oral [14C]SCY-078 in Albino and Pigmented Rats.

Authors:  Stephen Wring; Katyna Borroto-Esoda; Eric Solon; David Angulo
Journal:  Antimicrob Agents Chemother       Date:  2019-01-29       Impact factor: 5.191

5.  Analysis of a Candida auris Outbreak Provides New Insights into an Emerging Pathogen.

Authors:  Brian L Wickes
Journal:  J Clin Microbiol       Date:  2020-03-25       Impact factor: 5.948

6.  Evidence for the presence of "metabolic sterols" in Pneumocystis: identification and initial characterization of Pneumocystis carinii sterols.

Authors:  E S Kaneshiro; J E Ellis; K Jayasimhulu; D H Beach
Journal:  J Eukaryot Microbiol       Date:  1994 Jan-Feb       Impact factor: 3.346

7.  Effect of Candida glabrata FKS1 and FKS2 mutations on echinocandin sensitivity and kinetics of 1,3-beta-D-glucan synthase: implication for the existing susceptibility breakpoint.

Authors:  Guillermo Garcia-Effron; Samuel Lee; Steven Park; John D Cleary; David S Perlin
Journal:  Antimicrob Agents Chemother       Date:  2009-06-22       Impact factor: 5.191

8.  A Novel 1,3-Beta-d-Glucan Inhibitor, Ibrexafungerp (Formerly SCY-078), Shows Potent Activity in the Lower pH Environment of Vulvovaginitis.

Authors:  E L Larkin; L Long; N Isham; K Borroto-Esoda; S Barat; D Angulo; S Wring; M Ghannoum
Journal:  Antimicrob Agents Chemother       Date:  2019-04-25       Impact factor: 5.191

9.  SCY-078 Is Fungicidal against Candida Species in Time-Kill Studies.

Authors:  Bernard Scorneaux; David Angulo; Katyna Borroto-Esoda; Mahmoud Ghannoum; Michael Peel; Stephen Wring
Journal:  Antimicrob Agents Chemother       Date:  2017-02-23       Impact factor: 5.191

10.  Comparison of echinocandin antifungals.

Authors:  Gregory Eschenauer; Daryl D Depestel; Peggy L Carver
Journal:  Ther Clin Risk Manag       Date:  2007-03       Impact factor: 2.423

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