Cilofungin
Also known as: Cilofungin, Echinocandin B p-octylphenyl ether, LY121019
Source Cilofungin at Peptiology
Save 10% with code PEPTI-BOSSRABBIT-10
Tapping Shop Now & Save 10% copies your 10% off code PEPTI-BOSSRABBIT-10 to your clipboard. Paste it at the Peptiology checkout to claim the discount.
Summary
Cilofungin (LY121019) was the first echinocandin antifungal agent to enter clinical trials in humans. It demonstrated potent in vitro and in vivo activity against Candida species by inhibiting 1,3-beta-D-glucan synthase. Clinical development was halted in the late 1980s due to formulation-related toxicity (nephrotoxicity and polyethylene glycol vehicle toxicity) rather than intrinsic drug toxicity, paving the way for later echinocandins such as caspofungin, micafungin, and anidulafungin.
Mechanism of Action
Non-competitive inhibition of 1,3-beta-D-glucan synthase, disrupting fungal cell wall synthesis by blocking glucan polymer formation, leading to osmotic instability and fungal cell death
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
No sources recorded yet.
Frequently Asked Questions
What is Cilofungin?
Cilofungin (LY121019) was the first echinocandin antifungal agent to enter clinical trials in humans. It demonstrated potent in vitro and in vivo activity against Candida species by inhibiting 1,3-beta-D-glucan synthase. Clinical development was halted in the late 1980s due to formulation-related toxicity (nephrotoxicity and polyethylene glycol vehicle toxicity) rather than intrinsic drug toxicity, paving the way for later echinocandins such as caspofungin, micafungin, and anidulafungin.
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.