CD101, a novel echinocandin with exceptional stability properties and enhanced aqueous solubility
Open accessAbstract
The echinocandins are an important class of antifungal agents. However, instability and, in some cases, lack of solubility have restricted their use to situations in which daily infusions are acceptable. CD101 is a novel echinocandin in development for topical and weekly i.v. administration that exhibits prolonged stability in plasma and aqueous solutions up to 40 °C. After incubation for 44 h in rat, dog, monkey and human plasma at 37 °C, the percent of CD101 remaining (91%, 79%, 94% and 93%, respectively) was consistently greater than that of anidulafungin (7%, 15%, 14% and 7%, respectively). Similarly, after incubation in phosphate-buffered saline at 37 °C, the CD101 remaining (96%) was greater than that of anidulafungin (42%). CD101 exhibited <2% degradation after long-term storage at 40 °C as a lyophilized powder (9 months) and at room temperature in 5% dextrose (15 months), 0.9% saline (12 months) and sterile water (18 months). Degradation was <7% at 40 °C in acetate and lactate buffers (6 to 9 months at pH 4.5-5.5). The chemical stability and solubility of CD101 contribute to dosing, pharmacokinetic, formulation and safety advantages over other echinocandins and should expand utility beyond daily i.v.
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Rezafungin is the latest echinocandin, with structural modifications that enhance chemical stability and solubility, granting a long half-life that enables once-weekly intravenous dosing.
“Structural modifications have enhanced its chemical stability and solubility granting a long half-life enabling once-weekly IV dosing [31].”
From Investigational Agents for the Treatment of Resistant Yeasts and Molds (2021) · cites this paper as [31]
RZF can be dosed once weekly as an echinocandin for treatment or prevention in immunocompromised patients.
“RZF offers convenient, once-weekly dosing for echinocandin for the treatment or prophylaxis in immunocompromised patients.”
From Investigational Agents for the Treatment of Resistant Yeasts and Molds (2021) · cites this paper as [31]
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- Authors
- Krishnan, B. R., James, K. D., Polowy, K., Bryant, B. J., Vaidya, A., Smith, S., & Laudeman, C. P.
- Affiliations
- Cidara Therapeutics (United States) (US)
- Corresponding author
- James, Kenneth D
- Venue
- The Journal of Antibiotics
- Published
- 2016-08-10
- Volume
- 70
- Issue
- 2
- Pages
- 130-135
- ISSN
- 0021-8820 (ISSN-L)
- 1881-1469
- OpenAlex
- W2489758720
- Cited by
- 98
- References
- 18
- Citations by year
- 2026: 8 · 2025: 10 · 2024: 8 · 2023: 10 · 2022: 8 · 2021: 9 · 2020: 15 · 2019: 13 · 2018: 5 · 2017: 9 · 2016: 3
- FWCI
- 9.23
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- The Journal of Antibiotics (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Infectious Diseases › Antifungal resistance and susceptibility
- Physical Sciences › Chemistry › Analytical Chemistry › Analytical Methods in Pharmaceuticals
- Health Sciences › Medicine › Pharmacology › Antibiotics Pharmacokinetics and Efficacy
- Keywords
- CD101, echinocandins, antifungal agents, drug stability, water solubility, anidulafungin, plasma stability, thermal degradation, storage stability, topical administration, intravenous administration, drug formulation
- MeSH terms
- Animals, Antifungal Agents, Buffers, Drug Stability, Hydrogen-Ion Concentration, Phosphates, Plasma, Powders, Solubility, Solutions, Molecular Structure, Echinocandins
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