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Effect of food on the pharmacokinetic characteristics of a single oral dose of LCB01-0371, a novel oxazolidinone antibiotic.
- Source :
-
Drug design, development and therapy [Drug Des Devel Ther] 2018 Jun 11; Vol. 12, pp. 1707-1714. Date of Electronic Publication: 2018 Jun 11 (Print Publication: 2018). - Publication Year :
- 2018
-
Abstract
- Background: LCB01-0371 is a novel oxazolidinone antibiotic that blocks protein production by binding to bacterial 23S ribosomes. This antibiotic is active against Gram-positive bacteria. This study aimed to evaluate the effect of food on the pharmacokinetics (PKs) of LCB01-0371 and evaluate its safety profile.<br />Subjects and Methods: A randomized, open-label, two-way crossover study was performed in 18 healthy Korean male subjects. All subjects received a single oral 800 mg dose of LCB01-0371 in each period under fed or fasting condition with a 7-day washout in between. The fed condition was defined as consumption of a meal of 800-1,000 kcal containinį50% of fat content. Serial blood samples were collected over 24 h after dosing, and the PK parameters were calculated by noncompartment analysis. All available data of the subjects who received LCB01-0371 at least once were included in the safety data summaries.<br />Results: In the fed condition, both the maximum plasma concentration ( C <subscript>max</subscript> ) and the total systemic exposure (area under the plasma concentration-time curve from time zero to the last observed time point [AUC <subscript>last</subscript> ]) decreased by ~33% and 10%, respectively. The time to reach C <subscript>max</subscript> was delayed by ~1.25 h in the fed condition, whereas the mean elimination half-life remained similar in both conditions. In the fed/fasting condition, the geometric mean ratios and 90% CI of the C <subscript>max</subscript> and AUC <subscript>last</subscript> were 0.666 (0.470-0.945) and 0.897 (0.761-1.057), respectively. There were no drug-related adverse events (AEs) or serious AEs.<br />Conclusion: Although the T <subscript>max</subscript> after a single oral 800 mg dose of LCB01-0371 was slightly delayed under the fed condition compared to the fasting condition, the total systemic exposure was similar under both conditions. Therefore, LCB01-0371 could be administered regardless of food intake.<br />Competing Interests: Disclosure Heesook Nam and Young Lag Cho are LegoChem Biosciences, Inc. employees. The other authors report no conflicts of interest in this work.
- Subjects :
- Administration, Oral
Adult
Anti-Bacterial Agents blood
Area Under Curve
Cross-Over Studies
Fasting blood
Half-Life
Healthy Volunteers
Humans
Male
Metabolic Clearance Rate
Models, Biological
Oxazolidinones blood
Postprandial Period
Republic of Korea
Young Adult
Anti-Bacterial Agents administration & dosage
Anti-Bacterial Agents pharmacokinetics
Food-Drug Interactions
Oxazolidinones administration & dosage
Oxazolidinones pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 1177-8881
- Volume :
- 12
- Database :
- MEDLINE
- Journal :
- Drug design, development and therapy
- Publication Type :
- Academic Journal
- Accession number :
- 29928114
- Full Text :
- https://doi.org/10.2147/DDDT.S155657