Literature DB >> 23190764

Activity of MK-3118, a new oral glucan synthase inhibitor, tested against Candida spp. by two international methods (CLSI and EUCAST).

Michael A Pfaller1, Shawn A Messer, Mary R Motyl, Ronald N Jones, Mariana Castanheira.   

Abstract

OBJECTIVES: To evaluate the activity of the orally bioavailable enfumafungin derivative MK-3118 and comparator antifungal agents tested against a collection of 113 clinical isolates of Candida spp. using CLSI and EUCAST broth microdilution (BMD) methods.
METHODS: Candida spp. isolates (n=113) were tested by CLSI and EUCAST methods. The collection contained 29 Candida albicans, 29 Candida glabrata, 21 Candida tropicalis, 15 Candida parapsilosis and 19 Candida krusei, including azole- and echinocandin-resistant isolates. CLSI and EUCAST MIC endpoints of 50% and 100% inhibition were determined using visual reading at 24 and 48 h of incubation and spectrophotometric reading at 24 h of incubation, respectively.
RESULTS: MK-3118 CLSI MIC results ranged from 0.06 to 16 mg/L depending on species, duration of incubation and endpoint criteria (EC) used. Comparison of CLSI and EUCAST following 24 h of incubation and either 50% or 100% inhibition revealed an essential agreement (EA; ± 2 doubling dilutions) of 99.1% using the 50% inhibition EC and 93.2% using the 100% inhibition EC. MK-3118 (24 h of incubation and 50% EC) was active against all the species tested and displayed similar potency to caspofungin (using CLSI BMD) against C. albicans (MIC90, 1 and 2 mg/L, respectively), C. tropicalis (1 and 1 mg/L, respectively), C. parapsilosis (0.5 and 0.5 mg/L, respectively) and C. krusei (2 and 1 mg/L, respectively), but was 8-fold more potent than caspofungin against C. glabrata strains (MIC90, 2 and 16 mg/L, respectively). MK-3118 was active against fluconazole-resistant strains as well as caspofungin-resistant strains with documented fks mutations.
CONCLUSIONS: MK-3118 was documented to have potent in vitro activity against Candida spp. when tested by both CLSI and EUCAST BMD methods, with the highest overall EA (99.1%) obtained when MK-3118 MIC results were read after 24 h of incubation using a partial inhibition EC (50%).

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Year:  2012        PMID: 23190764     DOI: 10.1093/jac/dks466

Source DB:  PubMed          Journal:  J Antimicrob Chemother        ISSN: 0305-7453            Impact factor:   5.790


  30 in total

1.  Enfumafungin derivative MK-3118 shows increased in vitro potency against clinical echinocandin-resistant Candida Species and Aspergillus species isolates.

Authors:  Cristina Jiménez-Ortigosa; Padmaja Paderu; Mary R Motyl; David S Perlin
Journal:  Antimicrob Agents Chemother       Date:  2013-12-09       Impact factor: 5.191

Review 2.  Echinocandin prophylaxis in patients undergoing haematopoietic cell transplantation and other treatments for haematological malignancies.

Authors:  David J Epstein; Susan K Seo; Janice M Brown; Genovefa A Papanicolaou
Journal:  J Antimicrob Chemother       Date:  2018-01-01       Impact factor: 5.790

3.  In Vitro Activity of a Novel Glucan Synthase Inhibitor, SCY-078, against Clinical Isolates of Candida auris.

Authors:  Elizabeth L Berkow; David Angulo; Shawn R Lockhart
Journal:  Antimicrob Agents Chemother       Date:  2017-06-27       Impact factor: 5.191

4.  De Novo Acquisition of Resistance to SCY-078 in Candida glabrata Involves FKS Mutations That both Overlap and Are Distinct from Those Conferring Echinocandin Resistance.

Authors:  Cristina Jiménez-Ortigosa; Winder B Perez; David Angulo; Katyna Borroto-Esoda; David S Perlin
Journal:  Antimicrob Agents Chemother       Date:  2017-08-24       Impact factor: 5.191

5.  Oral glucan synthase inhibitor SCY-078 is effective in an experimental murine model of invasive candidiasis caused by WT and echinocandin-resistant Candida glabrata.

Authors:  Nathan P Wiederhold; Laura K Najvar; Rosie Jaramillo; Marcos Olivo; Jason Pizzini; Gabriel Catano; Thomas F Patterson
Journal:  J Antimicrob Chemother       Date:  2018-02-01       Impact factor: 5.790

Review 6.  Antifungal drug development: challenges, unmet clinical needs, and new approaches.

Authors:  Terry Roemer; Damian J Krysan
Journal:  Cold Spring Harb Perspect Med       Date:  2014-05-01       Impact factor: 6.915

Review 7.  Emerging drugs and vaccines for candidemia.

Authors:  Brad Moriyama; Lori A Gordon; Matthew McCarthy; Stacey A Henning; Thomas J Walsh; Scott R Penzak
Journal:  Mycoses       Date:  2014-10-08       Impact factor: 4.377

8.  Antifungal Activity of SCY-078 and Standard Antifungal Agents against 178 Clinical Isolates of Resistant and Susceptible Candida Species.

Authors:  Wiley A Schell; A M Jones; Katyna Borroto-Esoda; Barbara D Alexander
Journal:  Antimicrob Agents Chemother       Date:  2017-10-24       Impact factor: 5.191

Review 9.  Drugs in Clinical Development for Fungal Infections.

Authors:  Maria F Gonzalez-Lara; Jose Sifuentes-Osornio; Luis Ostrosky-Zeichner
Journal:  Drugs       Date:  2017-09       Impact factor: 9.546

10.  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

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