Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2014;58(2):1248-51.
doi: 10.1128/AAC.02145-13. Epub 2013 Dec 9.

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

Cristina Jiménez-Ortigosa  1 , Padmaja Paderu, Mary R Motyl, David S Perlin
Affiliations

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

Cristina Jiménez-Ortigosa et al. Antimicrob Agents Chemother. 2014.

Abstract

MK-3118 is as an orally active new antifungal in the early stage of clinical development that inhibits the biosynthesis of β-(1,3)-glucan. We evaluated the in vitro activity of this compound against wild-type and echinocandin-resistant (ER) isolates containing mutations in the FKS gene(s) of Candida spp. and Aspergillus spp. MK-3118 demonstrated enhanced efficacy for most C. albicans and C. glabrata ER isolates relative to caspofungin, with decreased MICs and half-maximal inhibitory concentrations (IC50s).

PubMed Disclaimer

Figures

FIG 1
FIG 1
Structures of enfumafungin and MK-3118, a semisynthetic enfumafungin derivative.
FIG 2
FIG 2
Antifungal inhibition profiles for product-entrapped 1,3-β-glucan synthase enzyme complexes (GS) for caspofungin (CAS) and MK-3118 for wild-type and ER clinical isolates. GS inhibition was assessed by the incorporation of [3H]glucose into radiolabeled product. (A) Candida albicans. (B) Aspergillus fumigatus.
See this image and copyright information in PMC

References

    1. Pappas PG, Kauffman CA, Andes D, Benjamin DK, Jr, Calandra TF, Edwards JE, Jr, Filler SG, Fisher JF, Kullberg BJ, Ostrosky-Zeichner L, Reboli AC, Rex JH, Walsh TJ, Sobel JD; Infectious Diseases Society of America 2009. Clinical practice guidelines for the management of candidiasis: 2009 update by the Infectious Diseases Society of America. Clin. Infect. Dis. 48:503–535. 10.1086/596757 - DOI - PMC - PubMed
    1. Denning DW. 2003. Echinocandin antifungal drugs. Lancet 362:1142–1151. 10.1016/S0140-6736(03)14472-8 - DOI - PubMed
    1. Perlin DS. 2007. Resistance to echinocandin-class antifungal drugs. Drug Resist. Updat. 10:121–130. 10.1016/j.drup.2007.04.002 - DOI - PMC - PubMed
    1. Onishi J, Meinz M, Thompson J, Curotto J, Dreikorn S, Rosenbach M, Douglas C, Abruzzo G, Flattery A, Kong L, Cabello A, Vicente F, Pelaez F, Diez MT, Martin I, Bills G, Giacobbe R, Dombrowski A, Schwartz R, Morris S, Harris G, Tsipouras A, Wilson K, Kurtz MB. 2000. Discovery of novel antifungal (1,3)-beta-D-glucan synthase inhibitors. Antimicrob. Agents Chemother. 44:368–377. 10.1128/AAC.44.2.368-377.2000 - DOI - PMC - PubMed
    1. Peel M, Fan W, Mamai A, Hong J, Orr M, Ouvry G, Perrey D, Liu H, Jones M, Nelson K, Ogbu C, Lee S, Li K, Kirwan R, Noe A, Sligar J, Martensen P, Balkove J, Greenlee CM, Meng D, Parker D, Wildonger K, Liberator P, Abruzzo G, Flattery A, Galgoci A, Giacobbe R, Gill C, Hsu MJ, Misura A, Nielsen J, Powles M, Racine F, Dragovic J, Habulihaz B, Balkovec J. 2010. Enfumafungin derivatives: orally active glucan synthase inhibitors, abstr F1-845. Abstr. Intersci. Conf. Antimicrob. Agents Chemother., Boston, MA

Publication types

MeSH terms