PMID- 24802657
OWN - NLM
STAT- MEDLINE
DCOM- 20150330
LR  - 20211021
IS  - 1179-1918 (Electronic)
IS  - 1173-2563 (Linking)
VI  - 34
IP  - 7
DP  - 2014 Jul
TI  - Tolerability and pharmacokinetics of lobeglitazone, a novel peroxisome 
      proliferator-activated receptor-gamma agonist, after a single oral administration in 
      healthy female subjects.
PG  - 467-74
LID - 10.1007/s40261-014-0197-y [doi]
AB  - BACKGROUND AND OBJECTIVES: Lobeglitazone is a recently approved peroxisome 
      proliferator-activated receptor-gamma agonist for the treatment of type 2 diabetes 
      mellitus in Korea. The purpose of this study was to investigate the pharmaco 
      kinetic properties of lobeglitazone in healthy females and to compare these with 
      historical data in healthy males. METHODS: This study was designed as a 
      block-randomized, double-blind, placebo-controlled, parallel-group study. A 
      single 2 or 4 mg oral dose of lobeglitazone or a placebo was randomly 
      administered to 22 female subjects, and pharmacokinetic blood samples were 
      obtained after dosing. Pharmacokinetic parameters were calculated by a 
      non-compartmental method, and the results were compared with those previously 
      obtained from male subjects. Tolerability was assessed by clinical and laboratory 
      parameters. RESULTS: During the study, a total of 28 adverse events (AEs) were 
      observed in the lobeglitazone group (n = 16) and nine AEs in the placebo group (n 
      = 6). Serious AEs or significant clinical changes were not observed. After oral 
      administration, lobeglitazone was rapidly absorbed with the time to maximum 
      plasma concentration (t(max)) ranging from 0.5 to 4.0 h. The mean (standard 
      deviation) maximum plasma concentration (C(max)) and area under the plasma 
      concentration-time curve from time zero to infinity (AUC(infinity)) for the 2 mg dose 
      were 214.8 (56.4) microg/L and 2,251.3 (721.2) microg.h/L, respectively, and the 
      corresponding values for the 4 mg dose were 310.0 (47.8) microg/L and 6,942.6 
      (1,778.9) microg.h/L, respectively. The ratios (95 % CIs) for the geometric means 
      (female/male) of the C(max) and AUCinfinity were 1.23 (0.89-1.69) and 1.11 (0.73-1.68), 
      respectively (2 mg), and 1.28 (1.01-1.63) and 2.36 (1.60-3.47), respectively (4 
      mg). CONCLUSION: Lobeglitazone was well-tolerated in healthy females. There was 
      no sex difference for systemic lobeglitazone exposure at a 2 mg dose; however, 
      female subjects showed greater systemic exposure than males after the 
      administration of 4 mg of lobeglitazone. In spite of the pharmacokinetic 
      difference, dose adjustment based on sex alone is not needed in clinical use 
      because therapy should be individualized for each patient to achieve glycemic 
      control.
FAU - Park, Min Kyu
AU  - Park MK
AD  - Department of Clinical Pharmacology and Therapeutics, Seoul National University 
      College of Medicine and Hospital, 101 Daehak-ro, Jongno-gu, Seoul, 110-744, 
      Korea.
FAU - Kim, Tae-Eun
AU  - Kim TE
FAU - Kim, JaeWoo
AU  - Kim J
FAU - Kim, Chin
AU  - Kim C
FAU - Yoon, Seo Hyun
AU  - Yoon SH
FAU - Cho, Joo-Youn
AU  - Cho JY
FAU - Jang, In-Jin
AU  - Jang IJ
FAU - Yu, Kyung-Sang
AU  - Yu KS
FAU - Lim, Kyoung Soo
AU  - Lim KS
LA  - eng
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
PL  - New Zealand
TA  - Clin Drug Investig
JT  - Clinical drug investigation
JID - 9504817
RN  - 0 (PPAR gamma)
RN  - 0 (Pyrimidines)
RN  - 0 (Thiazolidinediones)
RN  - MY89F08K5D (lobeglitazone)
SB  - IM
MH  - Administration, Oral
MH  - Adult
MH  - Double-Blind Method
MH  - Drug Tolerance
MH  - Female
MH  - Healthy Volunteers
MH  - Humans
MH  - Male
MH  - PPAR gamma/*agonists
MH  - Pyrimidines/*administration & dosage/*pharmacokinetics
MH  - Thiazolidinediones/*administration & dosage/*pharmacokinetics
MH  - Young Adult
EDAT- 2014/05/08 06:00
MHDA- 2015/03/31 06:00
CRDT- 2014/05/08 06:00
PHST- 2014/05/08 06:00 [entrez]
PHST- 2014/05/08 06:00 [pubmed]
PHST- 2015/03/31 06:00 [medline]
AID - 10.1007/s40261-014-0197-y [doi]
PST - ppublish
SO  - Clin Drug Investig. 2014 Jul;34(7):467-74. doi: 10.1007/s40261-014-0197-y.