Trial reportAntimicrobial agents and chemotherapy2006
Single-ascending-dose pharmacokinetics and safety of the novel broad-spectrum antifungal triazole BAL4815 after intravenous infusions (50, 100, and 200 milligrams) and oral administrations (100, 200, and 400 milligrams) of its prodrug, BAL8557, in healthy volunteers.
Trial report in Antimicrobial agents and chemotherapy, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 80 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
80 citing papers in PubMed, 169 citations in OpenAlex.
- Pharmacokinetics, Safety, and Tolerability of Single and Multiple Doses of Isavuconazonium Sulfate in Healthy Adult Japanese Subjects.Clinical pharmacology in drug development · 2022Trial
- Pharmacokinetics and Bioequivalence of Isavuconazole Administered as Isavuconazonium Sulfate Intravenous Solution via Nasogastric Tube or Orally in Healthy Subjects.Antimicrobial agents and chemotherapy · 2021Trial
- Variability and exposure-response relationships of isavuconazole plasma concentrations in the Phase 3 SECURE trial of patients with invasive mould diseases.The Journal of antimicrobial chemotherapy · 2019Trial
- Population Pharmacokinetics of Isavuconazole from Phase 1 and Phase 3 (SECURE) Trials in Adults and Target Attainment in Patients with Invasive Infections Due to Aspergillus and Other Filamentous Fungi.Antimicrobial agents and chemotherapy · 2016Trial
- Population Pharmacokinetics of Isavuconazole in Subjects with Mild or Moderate Hepatic Impairment.Antimicrobial agents and chemotherapy · 2016Trial
- Safety and pharmacokinetics of isavuconazole as antifungal prophylaxis in acute myeloid leukemia patients with neutropenia: results of a phase 2, dose escalation study.Antimicrobial agents and chemotherapy · 2015Trial
- A phase 2, randomized, double-blind, multicenter trial to evaluate the safety and efficacy of three dosing regimens of isavuconazole compared with fluconazole in patients with uncomplicated esophageal candidiasis.Antimicrobial agents and chemotherapy · 2015Trial
- Effect of mild and moderate liver disease on the pharmacokinetics of isavuconazole after intravenous and oral administration of a single dose of the prodrug BAL8557.Antimicrobial agents and chemotherapy · 2009Trial
- Multiple-dose pharmacokinetics and safety of the new antifungal triazole BAL4815 after intravenous infusion and oral administration of its prodrug, BAL8557, in healthy volunteers.Antimicrobial agents and chemotherapy · 2006Trial
- The Activity of FDA-Approved Prodrug Isavuconazonium Sulfate and Its Major Metabolite Isavuconazole AgainstPharmaceutics · 2026Article
- Comparative Analysis of Isavuconazole DDIs With Other Azole Antifungal Drugs and PBPK Model-Informed Dosing Recommendations for Anticancer Drugs.CPT: pharmacometrics & systems pharmacology · 2025Article
- Low isavuconazole trough levels in critically ill patients with and without extracorporeal membrane oxygenation.Antimicrobial agents and chemotherapy · 2025Article
- Metamizole induces voriconazole metabolism and results in subtherapeutic voriconazole concentrations.British journal of clinical pharmacology · 2025Observational
- Single-Dose, Intravenous, and Oral Pharmacokinetics of Isavuconazole in Dogs.Journal of veterinary pharmacology and therapeutics · 2025Article
- Real-World Experience with Isavuconazole for Invasive Aspergillosis in Hematologic Patients with and Without COVID-19 in Brazil.Journal of fungi (Basel, Switzerland) · 2025Article
- Azole Combinations and Multi-Targeting Drugs That Synergistically InhibitJournal of fungi (Basel, Switzerland) · 2024Review
- Relative Performance of Volume of Distribution Prediction Methods for Lipophilic Drugs with Uncertainty in LogP Value.Pharmaceutical research · 2024Article
- The landscape of small-molecule prodrugs.Nature reviews. Drug discovery · 2024Review
- Pharmacokinetics of isavuconazonium sulfate and its active metabolite isavuconazole in healthy dogs.PloS one · 2024Article
- Isavuconazole use and TDM in real-world pediatric practice.Antimicrobial agents and chemotherapy · 2023Article
20 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BAL8557 is the water-soluble prodrug of a novel antifungal triazole, BAL4815. BAL4815 is active against a broad spectrum of major opportunistic and pathogenic fungi, including strains that are resistant to other azoles. Cohorts of healthy male subjects received single-ascending oral (p.o.) doses of BAL8557 that were equivalent to 100, 200, or 400 mg of BAL4815 or single-ascending, 1-h constant-rate intravenous (i.v.) infusions of BAL8557 which were equivalent to 50, 100, or 200 mg of BAL4815. In each cohort, six subjects were randomly assigned to receive active drug and two subjects were assigned to receive the placebo. All doses were well tolerated, and no severe or serious adverse events occurred. Maximum plasma concentrations of BAL4815 were observed 1.5 to 3 h after p.o. drug intake or at the end of the 1-h infusion. After both routes of administration, values for maximum drug concentration observed in plasma and area under the concentration-time curve increased slightly more than proportionally to the administered dose. Mean elimination half-lives were particularly long (56 to 77 h after p.o. administration and 76 to 104 h after i.v. administration). The volume of distribution was large (155 to 292 liters after p.o. administration and 304 to 494 liters after i.v. administration) and systemic clearance was low (1.9 to 2.8 liter/h after p.o. administration and 2.8 to 5.0 liter/h after i.v. administration). Urinary recovery of BAL4815 was less than 0.4% of the infused dose. Based on the exposure data, oral bioavailability of BAL4815 is assumed to be very high. The pharmacokinetics of BAL4815 are well suited to maintaining concentrations of BAL4815 for a long period of time in the body and to enabling an effective treatment of systemic mycoses.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.