Literature DB >> 21825291

In vitro activity of E1210, a novel antifungal, against clinically important yeasts and molds.

Mamiko Miyazaki1, Takaaki Horii, Katsura Hata, Nao-Aki Watanabe, Kazutaka Nakamoto, Keigo Tanaka, Syuji Shirotori, Norio Murai, Satoshi Inoue, Masayuki Matsukura, Shinya Abe, Kentaro Yoshimatsu, Makoto Asada.   

Abstract

E1210 is a new antifungal compound with a novel mechanism of action and broad spectrum of antifungal activity. We investigated the in vitro antifungal activities of E1210 compared to those of fluconazole, itraconazole, voriconazole, amphotericin B, and micafungin against clinical fungal isolates. E1210 showed potent activities against most Candida spp. (MIC(90) of ≤0.008 to 0.06 μg/ml), except for Candida krusei (MICs of 2 to >32 μg/ml). E1210 showed equally potent activities against fluconazole-resistant and fluconazole-susceptible Candida strains. E1210 also had potent activities against various filamentous fungi, including Aspergillus fumigatus (MIC(90) of 0.13 μg/ml). E1210 was also active against Fusarium solani and some black molds. Of note, E1210 showed the greatest activities against Pseudallescheria boydii (MICs of 0.03 to 0.13 μg/ml), Scedosporium prolificans (MIC of 0.03 μg/ml), and Paecilomyces lilacinus (MICs of 0.06 μg/ml) among the compounds tested. The antifungal action of E1210 was fungistatic, but E1210 showed no trailing growth of Candida albicans, which has often been observed with fluconazole. In a cytotoxicity assay using human HK-2 cells, E1210 showed toxicity as low as that of fluconazole. Based on these results, E1210 is likely to be a promising antifungal agent for the treatment of invasive fungal infections.

Entities:  

Mesh:

Substances:

Year:  2011        PMID: 21825291      PMCID: PMC3186989          DOI: 10.1128/AAC.00291-11

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.191


  20 in total

1.  Antifungal mechanism of FK463 against Candida albicans and Aspergillus fumigatus.

Authors:  Kazuo Hatano; Yoshihiko Morishita; Toru Nakai; Fumiaki Ikeda
Journal:  J Antibiot (Tokyo)       Date:  2002-02       Impact factor: 2.649

Review 2.  Echinocandin antifungal drugs.

Authors:  David W Denning
Journal:  Lancet       Date:  2003-10-04       Impact factor: 79.321

Review 3.  Epidemiology and outcome of zygomycosis: a review of 929 reported cases.

Authors:  Maureen M Roden; Theoklis E Zaoutis; Wendy L Buchanan; Tena A Knudsen; Tatyana A Sarkisova; Robert L Schaufele; Michael Sein; Tin Sein; Christine C Chiou; Jaclyn H Chu; Dimitrios P Kontoyiannis; Thomas J Walsh
Journal:  Clin Infect Dis       Date:  2005-07-29       Impact factor: 9.079

4.  Synthesis and evaluation of novel antifungal agents-quinoline and pyridine amide derivatives.

Authors:  Kazutaka Nakamoto; Itaru Tsukada; Keigo Tanaka; Masayuki Matsukura; Toru Haneda; Satoshi Inoue; Norio Murai; Shinya Abe; Norihiro Ueda; Mamiko Miyazaki; Naoaki Watanabe; Makoto Asada; Kentaro Yoshimatsu; Katsura Hata
Journal:  Bioorg Med Chem Lett       Date:  2010-06-08       Impact factor: 2.823

5.  In vitro activities of a new lipopeptide antifungal agent, FK463, against a variety of clinically important fungi.

Authors:  S Tawara; F Ikeda; K Maki; Y Morishita; K Otomo; N Teratani; T Goto; M Tomishima; H Ohki; A Yamada; K Kawabata; H Takasugi; K Sakane; H Tanaka; F Matsumoto; S Kuwahara
Journal:  Antimicrob Agents Chemother       Date:  2000-01       Impact factor: 5.191

6.  GWT1 gene is required for inositol acylation of glycosylphosphatidylinositol anchors in yeast.

Authors:  Mariko Umemura; Michiyo Okamoto; Ken-ichi Nakayama; Koji Sagane; Kappei Tsukahara; Katsura Hata; Yoshifumi Jigami
Journal:  J Biol Chem       Date:  2003-04-24       Impact factor: 5.157

7.  Antifungal susceptibility survey of 2,000 bloodstream Candida isolates in the United States.

Authors:  Luis Ostrosky-Zeichner; John H Rex; Peter G Pappas; Richard J Hamill; Robert A Larsen; Harold W Horowitz; William G Powderly; Newton Hyslop; Carol A Kauffman; John Cleary; Julie E Mangino; Jeannette Lee
Journal:  Antimicrob Agents Chemother       Date:  2003-10       Impact factor: 5.191

8.  Medicinal genetics approach towards identifying the molecular target of a novel inhibitor of fungal cell wall assembly.

Authors:  Kappei Tsukahara; Katsura Hata; Kazutaka Nakamoto; Koji Sagane; Nao-Aki Watanabe; Junro Kuromitsu; Junko Kai; Mamiko Tsuchiya; Fuminori Ohba; Yoshifumi Jigami; Kentaro Yoshimatsu; Takeshi Nagasu
Journal:  Mol Microbiol       Date:  2003-05       Impact factor: 3.501

9.  In vitro activity of the echinocandin antifungal agent LY303,366 in comparison with itraconazole and amphotericin B against Aspergillus spp.

Authors:  K L Oakley; C B Moore; D W Denning
Journal:  Antimicrob Agents Chemother       Date:  1998-10       Impact factor: 5.191

10.  Use of fatty acid RPMI 1640 media for testing susceptibilities of eight Malassezia species to the new triazole posaconazole and to six established antifungal agents by a modified NCCLS M27-A2 microdilution method and Etest.

Authors:  Aristea Velegraki; Evangelos C Alexopoulos; Stavroula Kritikou; George Gaitanis
Journal:  J Clin Microbiol       Date:  2004-08       Impact factor: 5.948

View more
  62 in total

1.  E1210, a new broad-spectrum antifungal, suppresses Candida albicans hyphal growth through inhibition of glycosylphosphatidylinositol biosynthesis.

Authors:  Nao-Aki Watanabe; Mamiko Miyazaki; Takaaki Horii; Koji Sagane; Kappei Tsukahara; Katsura Hata
Journal:  Antimicrob Agents Chemother       Date:  2011-12-05       Impact factor: 5.191

2.  Efficacy and Pharmacokinetics of Fosmanogepix (APX001) in the Treatment of Candida Endophthalmitis and Hematogenous Meningoencephalitis in Nonneutropenic Rabbits.

Authors:  Ruta Petraitiene; Vidmantas Petraitis; Bo Bo Win Maung; Robert S Mansbach; Michael R Hodges; Malcolm A Finkelman; Karen Joy Shaw; Thomas J Walsh
Journal:  Antimicrob Agents Chemother       Date:  2021-02-17       Impact factor: 5.191

Review 3.  The antifungal pipeline: a reality check.

Authors:  John R Perfect
Journal:  Nat Rev Drug Discov       Date:  2017-05-12       Impact factor: 84.694

Review 4.  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

Review 5.  The Future of Antifungal Drug Therapy: Novel Compounds and Targets.

Authors:  Caroline Mota Fernandes; Deveney Dasilva; Krupanandan Haranahalli; J Brian McCarthy; John Mallamo; Iwao Ojima; Maurizio Del Poeta
Journal:  Antimicrob Agents Chemother       Date:  2021-01-20       Impact factor: 5.191

6.  In Vitro Activity of APX001A (Manogepix) and Comparator Agents against 1,706 Fungal Isolates Collected during an International Surveillance Program in 2017.

Authors:  M A Pfaller; M D Huband; R K Flamm; P A Bien; M Castanheira
Journal:  Antimicrob Agents Chemother       Date:  2019-07-25       Impact factor: 5.191

Review 7.  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

8.  Endoplasmic reticulum localized PerA is required for cell wall integrity, azole drug resistance, and virulence in Aspergillus fumigatus.

Authors:  Dawoon Chung; Arsa Thammahong; Kelly M Shepardson; Sara J Blosser; Robert A Cramer
Journal:  Mol Microbiol       Date:  2014-05-09       Impact factor: 3.501

9.  In Vitro Activity of Manogepix against Multidrug-Resistant and Panresistant Candida auris from the New York Outbreak.

Authors:  YanChun Zhu; Shannon Kilburn; Mili Kapoor; Sudha Chaturvedi; Karen Joy Shaw; Vishnu Chaturvedi
Journal:  Antimicrob Agents Chemother       Date:  2020-10-20       Impact factor: 5.191

10.  In Vivo Pharmacokinetics and Pharmacodynamics of APX001 against Candida spp. in a Neutropenic Disseminated Candidiasis Mouse Model.

Authors:  Miao Zhao; Alexander J Lepak; Brian VanScoy; Justin C Bader; Karen Marchillo; Jamie Vanhecker; Paul G Ambrose; David R Andes
Journal:  Antimicrob Agents Chemother       Date:  2018-03-27       Impact factor: 5.191

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.