Cited by 81Antifungal resistance and susceptibilityFungal Plant Pathogen ControlFungal and yeast genetics research

CD101: a novel long-acting echinocandin

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Zhao, Yanan, Perez, Winder B., Jiménez‐Ortigosa, Cristina, Hough, Grayson, Locke, Jeffrey B., Ong, Voon, Bartizal, Ken, Perlin, David S.·2016·Cellular Microbiology

Abstract

CD101 is a novel echinocandin drug being developed to treat severe fungal infections including invasive candidiasis. We have performed a series of studies to evaluate the antifungal properties of CD101 against both echinocandin-susceptible and -resistant Candida strains. Antifungal susceptibility testing performed on a collection of 95 Candida strains including 30 caspofungin-resistant isolates containing fks mutations demonstrated comparable antifungal potency of CD101 relative to micafungin (MCF) across different Candida species. Comparable kinetic inhibition of glucan synthase activity was also observed for CD101 and MCF on both wild-type (WT) and resistant fks mutant Candida strains. Similarly, both drugs yielded nearly identical values for a mutant prevention concentration. In a murine model of invasive candidiasis, CD101 displayed better or at least comparable efficacy relative to MCF in treating WT or fks mutant Candida albicans. An exceptional long-lived pharmacokinetic profile was observed in mice following a single dose of CD101. Collectively, CD101 has great potential not only in treating invasive Candida infections but also in preventing emergence of resistance to currently approved echinocandin drugs.

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  • Rezafungin is a new long-acting echinocandin with improved stability and extended half-life compared to first-generation echinocandins, potentially allowing once-a-week dosing.

    “Rezafungin (formerly CD101) is a new long-acting echinocandin with improved stability and extended half life as compared to the first generation drugs within this class, thereby potentially allowing for once a week dosing [41].”

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  1. Ong, V., Hough, G., Schlosser, M., Bartizal, K., Balkovec, J., James, K., Krishnana, R. (2015a) Preclinical evaluation shows CD101, a novel echinocandin, is highly stable with no hepatotoxicity in rats. A‐015. In the Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) and the International Congress of Chemotherapy (ICC) joint meeting. San Diego.
  2. Ong, V., Miesel, L., Bartizal, K., Huang, H.H., Chien, J.C. (2015b) Prolonged efficacy following one dose of a novel echinocandin, CD101, in a neutropenic mouse model of disseminated candidiasis. F‐761. In the Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) and the International Society of Chemotherapy (ICC) joint meeting.
  3. Rubino, C.M., O.V., Thye, D., Ambrose, P.G. (2015) Pharmacokinetics–Pharmacodynamics (PK–PD) of a Novel Echinocandin, CD101 (Biafungin), in a Neutropenic Murine Disseminated Candidiasis Model. Slide Session 044. In the Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) and the International Society of Chemotherapy (ICC) joint meeting. San Diego.

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Authors
Zhao, Y., Perez, W. B., Jiménez‐Ortigosa, C., Hough, G., Locke, J. B., Ong, V., Bartizal, K., & Perlin, D. S.
Affiliations
  • Rutgers Health (US)
  • Cidara Therapeutics (United States) (US)
Corresponding author
Perlin, David S.
Venue
Cellular Microbiology
Publisher
Wiley
Published
2016-07-22
Volume
18
Issue
9
Pages
1308-1316
ISSN
  • 1462-5814 (ISSN-L)
  • 1462-5822
OpenAlex
W2467264597
Cited by
81
References
36
Citations by year
2026: 2 · 2025: 6 · 2024: 7 · 2023: 8 · 2022: 5 · 2021: 6 · 2020: 10 · 2019: 10 · 2018: 7 · 2017: 17 · 2016: 3
FWCI
11.38
Type
journal article
Language
en
Open access
Locations
  • Cellular Microbiology (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
Funders
Cidara Therapeutic, Inc.
Topics
  • Health Sciences › Medicine › Infectious Diseases › Antifungal resistance and susceptibility
  • Life Sciences › Agricultural and Biological Sciences › Ecology, Evolution, Behavior and Systematics › Fungal Plant Pathogen Control
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Fungal and yeast genetics research
Keywords
CD101, echinocandins, invasive candidiasis, Candida albicans, caspofungin resistance, micafungin, antifungal susceptibility, mutant prevention concentration, antifungal drug development
MeSH terms
Animals, Antifungal Agents, Candida albicans, Candidiasis, Female, Half-Life, Mice, Inbred BALB C, Microbial Sensitivity Tests, Inhibitory Concentration 50, Drug Resistance, Fungal, Echinocandins

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