PMID- 29928114
OWN - NLM
STAT- MEDLINE
DCOM- 20181105
LR  - 20220330
IS  - 1177-8881 (Electronic)
IS  - 1177-8881 (Linking)
VI  - 12
DP  - 2018
TI  - Effect of food on the pharmacokinetic characteristics of a single oral dose of 
      LCB01-0371, a novel oxazolidinone antibiotic.
PG  - 1707-1714
LID - 10.2147/DDDT.S155657 [doi]
AB  - 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. 
      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 containing50% 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. RESULTS: In 
      the fed condition, both the maximum plasma concentration (C(max)) and the total 
      systemic exposure (area under the plasma concentration-time curve from time zero 
      to the last observed time point [AUC(last)]) decreased by ~33% and 10%, 
      respectively. The time to reach C(max) 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(max) and AUC(last) 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. 
      CONCLUSION: Although the T(max) 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.
FAU - Sunwoo, Jung
AU  - Sunwoo J
AD  - Department of Clinical Pharmacology and Therapeutics, Seoul National University 
      College of Medicine and Hospital, Seoul.
FAU - Kim, Yu Kyong
AU  - Kim YK
AD  - Department of Clinical Pharmacology and Therapeutics, Seoul National University 
      College of Medicine and Hospital, Seoul.
FAU - Choi, Yewon
AU  - Choi Y
AD  - Department of Clinical Pharmacology and Therapeutics, Seoul National University 
      College of Medicine and Hospital, Seoul.
FAU - Yu, Kyung-Sang
AU  - Yu KS
AD  - Department of Clinical Pharmacology and Therapeutics, Seoul National University 
      College of Medicine and Hospital, Seoul.
FAU - Nam, Heesook
AU  - Nam H
AD  - LegoChem Biosciences, Inc., Daejeon.
FAU - Cho, Young Lag
AU  - Cho YL
AD  - LegoChem Biosciences, Inc., Daejeon.
FAU - Yoon, Seonghae
AU  - Yoon S
AD  - Department of Clinical Pharmacology and Therapeutics, Seoul National University 
      College of Medicine and Bundang Hospital, Seongnam, Republic of Korea.
FAU - Chung, Jae-Yong
AU  - Chung JY
AD  - Department of Clinical Pharmacology and Therapeutics, Seoul National University 
      College of Medicine and Bundang Hospital, Seongnam, Republic of Korea.
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Randomized Controlled Trial
DEP - 20180611
PL  - New Zealand
TA  - Drug Des Devel Ther
JT  - Drug design, development and therapy
JID - 101475745
RN  - 0 (Anti-Bacterial Agents)
RN  - 0 (Oxazolidinones)
RN  - 43EP6XV33E (delpazolid)
SB  - IM
MH  - Administration, Oral
MH  - Adult
MH  - Anti-Bacterial Agents/*administration & dosage/blood/*pharmacokinetics
MH  - Area Under Curve
MH  - Cross-Over Studies
MH  - Fasting/blood
MH  - *Food-Drug Interactions
MH  - Half-Life
MH  - Healthy Volunteers
MH  - Humans
MH  - Male
MH  - Metabolic Clearance Rate
MH  - Models, Biological
MH  - Oxazolidinones/*administration & dosage/blood/*pharmacokinetics
MH  - Postprandial Period
MH  - Republic of Korea
MH  - Young Adult
PMC - PMC6001845
OTO - NOTNLM
OT  - antibiotic resistance
OT  - clinical trial
OT  - gram-positive bacteria
COIS- Disclosure Heesook Nam and Young Lag Cho are LegoChem Biosciences, Inc. 
      employees. The other authors report no conflicts of interest in this work.
EDAT- 2018/06/22 06:00
MHDA- 2018/11/06 06:00
PMCR- 2018/06/11
CRDT- 2018/06/22 06:00
PHST- 2018/06/22 06:00 [entrez]
PHST- 2018/06/22 06:00 [pubmed]
PHST- 2018/11/06 06:00 [medline]
PHST- 2018/06/11 00:00 [pmc-release]
AID - dddt-12-1707 [pii]
AID - 10.2147/DDDT.S155657 [doi]
PST - epublish
SO  - Drug Des Devel Ther. 2018 Jun 11;12:1707-1714. doi: 10.2147/DDDT.S155657. 
      eCollection 2018.