ArticleAntimicrobial agents and chemotherapy2017
Structure-Activity Relationships of a Series of Echinocandins and the Discovery of CD101, a Highly Stable and Soluble Echinocandin with Distinctive Pharmacokinetic Properties.
Article in Antimicrobial agents and chemotherapy, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed.
- Natural Product-Inspired Antifungal Drugs Introduced for Human Use from 1872 to August 2026.Antibiotics (Basel, Switzerland) · 2026Review
- Cryo-EM structures of Candida albicans chitin synthase Chs1 reveal a druggable translocation channel.Nature microbiology · 2026Article
- Intravitreal rezafungin and anidulafungin in a rabbit model of Aspergillus fumigatus endophthalmitis.Scientific reports · 2026Article
- Ultrastructural and Immunohistochemical Study on the Nephrotoxicity Following Intravitreal Administration of the Antifungal Agents Voriconazole and Micafungin in New Zealand White Rabbits.International journal of molecular sciences · 2025Article
- Rezafungin: A Review in Invasive Candidiasis.Drugs · 2025Review
- FDA-approved drugs featuring macrocycles or medium-sized rings.Archiv der Pharmazie · 2025Review
- Novel antifungals and treatment approaches to tackle resistance and improve outcomes of invasive fungal disease.Clinical microbiology reviews · 2024Review
- Amphotericin B in the Era of New Antifungals: Where Will It Stand?Journal of fungi (Basel, Switzerland) · 2024Review
- Advancements and challenges in antifungal therapeutic development.Clinical microbiology reviews · 2024Review
- Pharmacokinetic and pharmacodynamic considerations for antifungal therapy optimisation in the treatment of intra-abdominal candidiasis.Critical care (London, England) · 2023Review
- Recent developments in membrane targeting antifungal agents to mitigate antifungal resistance.RSC medicinal chemistry · 2023Review
- Cyclic Peptides in Pipeline: What Future for These Great Molecules?Pharmaceuticals (Basel, Switzerland) · 2023Review
- Pharmacodynamics, Mechanisms of Action and Resistance, and Spectrum of Activity of New Antifungal Agents.Journal of fungi (Basel, Switzerland) · 2022Review
- Invasive candidiasis: investigational drugs in the clinical development pipeline and mechanisms of action.Expert opinion on investigational drugs · 2022Article
- The Antifungal Pipeline: Fosmanogepix, Ibrexafungerp, Olorofim, Opelconazole, and Rezafungin.Drugs · 2021Review
- Antifungal Pipeline.Frontiers in cellular and infection microbiology · 2021Review
- Review of the Novel Echinocandin Antifungal Rezafungin: Animal Studies and Clinical Data.Journal of fungi (Basel, Switzerland) · 2020Review
- Antifungal Resistance inAntibiotics (Basel, Switzerland) · 2020Review
- RezafunginAntimicrobial agents and chemotherapy · 2020Article
- Activity of a Long-Acting Echinocandin, Rezafungin, and Comparator Antifungal Agents Tested against Contemporary Invasive Fungal Isolates (SENTRY Program, 2016 to 2018).Antimicrobial agents and chemotherapy · 2020Article
Corrections and comments
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Authors and funding
5 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Echinocandins are a first-line therapy for candidemia and invasive candidiasis. They are generally safe with few drug interactions, but the stability and pharmacokinetic properties of currently approved echinocandins are such that each was developed for daily intravenous infusion. We sought to discover a novel echinocandin with properties that would enable more flexible dosing regimens, alternate routes of delivery, and expanded utility. Derivatives of known echinocandin scaffolds were generated, and an iterative process of design and screening led to the discovery of CD101, a novel echinocandin that has since demonstrated improved chemical stability and pharmacokinetics. Here, we report the structure-activity relationships (including preclinical efficacy and pharmacokinetic data) for the series of echinocandin analogs from which CD101 was selected. In a mouse model of disseminated candidiasis, the test compounds displayed clear dose responses and were generally associated with lower fungal burdens than that of anidulafungin. Single-dose pharmacokinetic studies in beagle dogs revealed a wide disparity in the half-lives and volumes of distribution, with one compound (now known as CD101) displaying a half-life that is nearly 5-fold longer than that of anidulafungin (53.1 h versus 11.6 h, respectively). In vitro activity data against panels of Candida spp. and Aspergillus spp. demonstrated that CD101 behaved similarly to approved echinocandins in terms of potency and spectrum of activity, suggesting that the improved efficacy observed in vivo for CD101 is a result of features beyond the antifungal potency inherent to the molecule. Factors that potentially contribute to the improved in vivo efficacy of CD101 are discussed.
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