ArticleAntimicrobial agents and chemotherapy2001
Compartmental pharmacokinetics and tissue distribution of the antifungal echinocandin lipopeptide micafungin (FK463) in rabbits.
Article in Antimicrobial agents and chemotherapy, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers, 1 of them a synthesis that pooled it.
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Who cites it
44 citing papers in PubMed, 1 synthesis or guideline pooled it, 131 citations in OpenAlex.
- Clinical Practice Guideline for the Management of Candidiasis: 2016 Update by the Infectious Diseases Society of America.Clinical infectious diseases : an official publication of the Infectious Diseases Society of America · 2016Guideline
- Safety, tolerability, and pharmacokinetics of Micafungin (FK463) in febrile neutropenic pediatric patients.Antimicrobial agents and chemotherapy · 2005Trial
- Central Nervous System Fungal Diseases in Children with Malignancies: A 16-Year Study from the Infection Working Group of the Hellenic Society of Pediatric Hematology Oncology.Journal of fungi (Basel, Switzerland) · 2024Article
- Combination of Systemic and Lock-Therapies with Micafungin Eradicate Catheter-Based Biofilms and Infections Caused byJournal of fungi (Basel, Switzerland) · 2024Article
- Strategic Approaches to Improvise Peptide Drugs as Next Generation Therapeutics.International journal of peptide research and therapeutics · 2023Review
- Risk Factors and Clinical Characteristics of Patients with Ocular Candidiasis.Journal of fungi (Basel, Switzerland) · 2022Article
- Multicenter prospective observational study of fungal keratitis in Japan: analyses of in vitro susceptibility tests for combinations of drugs.Japanese journal of ophthalmology · 2022Observational
- Human Tissue Distribution of Anidulafungin and Micafungin.Antimicrobial agents and chemotherapy · 2021Article
- Anidulafungin and Micafungin Concentrations in Cerebrospinal Fluid and in Cerebral Cortex.Antimicrobial agents and chemotherapy · 2020Article
- Delamanid Central Nervous System Pharmacokinetics in Tuberculous Meningitis in Rabbits and Humans.Antimicrobial agents and chemotherapy · 2019Article
- SCY-078, a Novel Fungicidal Agent, Demonstrates Distribution to Tissues Associated with Fungal Infections during Mass Balance Studies with Intravenous and Oral [Antimicrobial agents and chemotherapy · 2019Article
- Invasive Candidiasis in Infants and Children: Recent Advances in Epidemiology, Diagnosis, and Treatment.Journal of fungi (Basel, Switzerland) · 2019Review
- Clinical and Microbiological Characteristics of Candida guilliermondii and Candida fermentati.Antimicrobial agents and chemotherapy · 2018Article
- Clinical Pharmacokinetics and Pharmacodynamics of Micafungin.Clinical pharmacokinetics · 2018Review
- Pharmacokinetics of antifungal drugs: practical implications for optimized treatment of patients.Infection · 2017Review
- Unraveling Drug Penetration of Echinocandin Antifungals at the Site of Infection in an Intra-abdominal Abscess Model.Antimicrobial agents and chemotherapy · 2017Article
- Preclinical Pharmacokinetics and Pharmacodynamic Target of SCY-078, a First-in-Class Orally Active Antifungal Glucan Synthesis Inhibitor, in Murine Models of Disseminated Candidiasis.Antimicrobial agents and chemotherapy · 2017Article
- Micafungin treatment and eradication of candiduria among hospitalized patients.International urology and nephrology · 2016Article
- Approach to the Solid Organ Transplant Patient with Suspected Fungal Infection.Infectious disease clinics of North America · 2016Review
- Micafungin in the treatment of candiduria: A case series.Medical mycology case reports · 2016Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The plasma pharmacokinetics and tissue distribution of the novel antifungal echinocandin-like lipopeptide micafungin (FK463) were investigated in healthy rabbits. Cohorts of three animals each received micafungin at 0.5, 1, and 2 mg/kg of body weight intravenously once daily for a total of 8 days. Serial plasma samples were collected on days 1 and 7, and tissue samples were obtained 30 min after the eighth dose. Drug concentrations were determined by validated high-performance liquid chromatographic methods. Plasma drug concentration data were fit to a two-compartment pharmacokinetic model, and pharmacokinetic parameters were estimated using weighted nonlinear least-square regression analysis. Micafungin demonstrated linear plasma pharmacokinetics without changes in total clearance and dose-normalized area under the concentration-time curve from 0 h to infinity. After administration of single doses to the rabbits, mean peak plasma drug concentrations ranged from 7.62 microg/ml at 0.5 mg/kg to 16.8 microg/ml at 2 mg/kg, the area under the concentration-time curve from 0 to 24 h ranged from 5.66 to 21.79 microg x h/ml, the apparent volume of distribution at steady state ranged from 0.296 to 0.343 liter/kg, and the elimination half-life ranged from 2.97 to 3.20 h, respectively. No significant changes in pharmacokinetic parameters and no accumulation was noted after multiple dosing. Mean tissue micafungin concentrations 30 min after the last of eight daily doses were highest in the lung (2.26 to 11.76 microg/g), liver (2.05 to 8.82 microg/g), spleen (1.87 to 9.05 microg/g), and kidney (1.40 to 6.12 microg/g). While micafungin was not detectable in cerebrospinal fluid, the concentration in brain tissue ranged from 0.08 to 0.18 microg/g. These findings indicate linear disposition of micafungin at dosages of 0.5 to 2 mg/kg and achievement of potentially therapeutic drug concentrations in plasma and tissues that are common sites of invasive fungal infections.
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