Cilofungin
Also known as: Cilofungin, Echinocandin B p-octylphenyl ether, LY121019
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Summary
Cilofungin is an investigational echinocandin lipopeptide antifungal administered intravenously. Developed as a semisynthetic analogue of echinocandin B, it inhibits fungal cell‑wall synthesis and has been studied primarily for candidiasis in animal models and early clinical trials.
Mechanism of Action
Cilofungin targets the fungal (1,3)-β‑glucan synthase complex, blocking synthesis of the essential β‑glucan polymer that forms the cell wall. Fluorescence studies suggest the drug also perturbs the surrounding membrane lipid environment, enhancing inhibition of the synthase complex.
What the Research Shows
Early reviews highlighted cilofungin as a representative echinocandin with low toxicity and clinical testing. In vitro combination studies with amphotericin B or flucytosine showed occasional synergistic inhibition of Candida growth but frequent antagonism. In a murine disseminated candidiasis model, cilofungin alone improved survival at high dose, and combined therapy with amphotericin B produced markedly better survival, lower organ fungal burdens, and occasional sterile organs, indicating additive or modest synergistic effects. Pharmacokinetic data showed higher serum levels when combined, without overt toxicity. Additional animal work demonstrated that non‑linear pharmacokinetics could augment its activity, and fluorescence probing confirmed stronger membrane interaction with C. albicans than with S. cerevisiae, supporting its mechanism of glucan‑synthase inhibition.
Reported Benefits
Animal studies provide evidence that cilofungin can clear Candida infections, especially when paired with amphotericin B, leading to higher survival rates and reduced organ fungal loads. The compound exhibits selective toxicity toward fungal cells and has shown low overt toxicity in mouse experiments.
Limitations of the Evidence
Clinical development was halted, and cilofungin is withdrawn, so human efficacy and safety data are limited. In vitro combination tests revealed frequent antagonism with other antifungals, and synergistic effects were inconsistent. Evidence is confined to animal models and early laboratory studies, lacking large‑scale clinical trials.
Safety Considerations
Mouse studies reported no overt toxicity at therapeutic doses, but comprehensive safety data in humans are unavailable. The observed antagonism in some drug combinations suggests potential for reduced efficacy when used with certain agents. Caution is warranted pending further toxicological evaluation.
How It Is Administered
Cilofungin has been investigated for intravenous infusion. Formulations described in the literature are lipopeptide solutions suitable for parenteral delivery.
Routes of Administration
Goals & Uses
- Treatment of invasive candidiasisAntifungalModerate
- Treatment of disseminated fungal infectionsAntifungal TherapyLow
- Prototype for echinocandin class developmentDrug DiscoveryHigh
Contraindications
- Hypersensitivity to echinocandinsAllergyHigh
- Renal impairmentOrgan DysfunctionHigh
Adverse Effects
- NauseaGastrointestinalUncommonFeeling of sickness or urge to vomit
- Elevated liver enzymesHepaticUncommonIncrease in AST/ALT or other hepatic markers
- Infusion-related reactionsHypersensitivityUncommon
- NephrotoxicityRenalCommon
Drug Interactions
- Nephrotoxic agentsHigh
Population Constraints
- Pediatric patientsAgeRelative
- Patients with renal impairmentOrgan ImpairmentAbsolute
- Pregnant womenReproductiveRelative
Regulatory Status
- European UnionUnapprovedNever received European regulatory approval; trials halted before submission
- United StatesUnapprovedClinical development discontinued circa 1989; never submitted for FDA approval
- United KingdomUnapprovedNo regulatory application made; compound remains a research reference only
Never received regulatory approval in any jurisdiction. Phase II clinical trials were discontinued circa 1989 due to vehicle-related toxicity (polyethylene glycol 400 solvent). Served as the prototype compound for the echinocandin class.
Evidence & Sources
- Journal ArticleModerateDebono M, Gordee RS1994-01-01T00:00:00.000000Z
- Journal ArticleModerateZhao P, et al.2019-01-01T00:00:00.000000Z
- Journal ArticleLowBulo AN, Bradley SF, Kauffman CA1989-01-01T00:00:00.000000Z
- Journal ArticleLowHanson LH, et al.1991-01-01T00:00:00.000000Z
- Journal ArticleModerateWalsh TJ, et al.1992-01-01T00:00:00.000000Z
- Journal ArticleLowKo YT, et al.1994-01-01T00:00:00.000000Z
Frequently Asked Questions
What type of infections has cilofungin been studied for?
Research has focused on invasive candidiasis, particularly disseminated Candida albicans infections in murine and rabbit models.
How does cilofungin differ from other antifungals?
It inhibits (1,3)-β‑glucan synthase, a cell‑wall target absent in human cells, and appears to interact directly with fungal membranes, unlike many azoles or polyenes.
Is cilofungin approved for clinical use?
No. The compound was withdrawn during development and remains an investigational agent with no regulatory approval.
Can cilofungin be used together with amphotericin B?
Animal studies suggest additive or modest synergistic effects when combined, improving survival and reducing fungal burden, though in vitro data show occasional antagonism.
What are the known safety concerns?
Limited data indicate no overt toxicity in mice, but human safety is uncharacterized, and antagonistic interactions with other antifungals have been reported.
What is Cilofungin?
Cilofungin is an investigational echinocandin lipopeptide antifungal administered intravenously. Developed as a semisynthetic analogue of echinocandin B, it inhibits fungal cell‑wall synthesis and has been studied primarily for candidiasis in animal models and early clinical trials.
What is Cilofungin used for?
Cilofungin is educationally associated with: Treatment of invasive candidiasis, Treatment of disseminated fungal infections, Prototype for echinocandin class development. Educational only — not medical advice.
How is Cilofungin administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Cilofungin?
Reported adverse effects include: Nausea, Elevated liver enzymes, Infusion-related reactions, Nephrotoxicity. This list is not exhaustive — consult a qualified clinician.
Who should avoid Cilofungin?
Recorded contraindications: Hypersensitivity to echinocandins, Renal impairment. Consult a qualified clinician before use.