Single Ascending-Dose Study To Evaluate the Safety, Tolerability, and Pharmacokinetics of Sutezolid in Healthy Adult Subjects

• Published in: Antimicrobial agents and chemotherapy Vol. 66; no. 4; p. e0210821
• Main Authors: Bruinenberg, Paul, Nedelman, Jerry, Yang, Tian J, Pappas, Fran, Everitt, Dan
• Format: Journal Article
• Language: English
• Published: United States American Society for Microbiology 19-04-2022
• Subjects: Administration, Oral; Adult; Antimicrobial Chemotherapy; Area Under Curve; Clinical Therapeutics; Dose-Response Relationship, Drug; Healthy Volunteers; Humans; Oxazolidinones - adverse effects; Tablets; pharmacokinetics; sutezolid; phase 1; safety; tuberculosis; antimicrobial safety
• ISSN: 0066-4804; 1098-6596
• DOI: 10.1128/aac.02108-21

The primary objective of the study was to evaluate the safety and tolerability of single oral doses of sutezolid tablets administered under fasting conditions in healthy adult subjects. The secondary objective was to determine the pharmacokinetics (PK) of sutezolid and two metabolites, PNU-101603 and PNU-101244. Overall, sutezolid was well tolerated when administered as a 300-mg, 600-mg, 1,200-mg, or 1,800-mg dose in healthy adult subjects under fasting conditions. Maximum concentration (
) of sutezolid, PNU-101603, and PNU-101244 increased in a less-than-proportional manner with an increase in sutezolid dose between 300 mg and 1,800 mg. Total exposure (AUC
[area under the concentration-time curve from time zero to the time of the last quantifiable concentration] and AUC
[area under the plasma concentration time curve from time zero extrapolated to infinity]) of sutezolid, PNU-101603, and PNU-101244 increased proportionally with an increase in sutezolid dose.