Two Phase 1, Open-Label, Mass Balance Studies to Determine the Pharmacokinetics of ¹⁴ C-Labeled Isavuconazonium Sulfate in Healthy Male Volunteers.

ABSTRACT: Isavuconazonium sulfate is the water-soluble prodrug of the active triazole isavuconazole. Two phase 1 studies were conducted to identify the metabolic profile and mass balance of isavuconazole and BAL8728 (inactive cleavage product). Seven subjects in study 1 (isavuconazole mass balance) received a single oral dose of [cyano-¹⁴ C]isavuconazonium sulfate corresponding to 200 mg isavuconazole. Six subjects in study 2 (BAL8728 mass balance) received a single intravenous dose of [pyridinylmethyl-¹⁴ C]isavuconazonium sulfate corresponding to 75 mg BAL8728. Pharmacokinetic parameters of radioactivity in whole blood and plasma and of isavuconazole and BAL8728 in plasma were assessed. Radioactivity ratio of blood/plasma, percentage of dose, and cumulative percentage of radio

SUBMITTER: Townsend R 

PROVIDER: S-EPMC5811773 | biostudies-literature | 2018 Feb

REPOSITORIES: biostudies-literature