2016/08/10 by B Radha Krishnan, Kenneth D. James, Kenneth D James +6 · 1 citation
Chemistry · Medicine · #Amphotericin B #Anesthesia #Anidulafungin #Antifungal #Antifungal resistance and susceptibility #Aqueous solution #Biochemistry #Chemistry #Chromatography #Dosing #Echinocandin #Echinocandins #Fungal Biology and Applications #Incubation #Medicine #Nail Diseases and Treatments #Organic chemistry #Pharmacokinetics #Pharmacology #Saline #Solubility
paper · pdf · doi:10.1038/ja.2016.89
crossref issued 2016/08/10 · crossref published 2016/08/10 · crossref published-online 2016/08/10 · openalex publication_date 2016/08/10 · crossref created 2016/08/10 · crossref published-print 2017/02/01 · crossref deposited 2025/06/04 · openalex created_date 2025/10/10 · crossref indexed 2026/07/30 · openalex updated_date 2026/07/30
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.