Lobeglitazone is used to assist regulation of blood glucose level of diabetes mellitus type 2 patients. It can be used alone or in combination with metformin.[4]
The absolute bioavailability of lobeglitazone is about 95% in rat.[1] In human, the mean steady state clearance (CLss/F) was 1.13 L/h across in 1 to 4 mg dose range. In the dose range, the mean half-life was 10.3 h.[2] Urine excretion was negligible amount in elimination of lobeglitazone in rat and human.[1][2]
The plasma protein binding of the drug is over 99%.[1][6] The average blood-to-plasma concentration ratio was 0.636. The unbound fraction of lobeglitazone in microsomal incubation medium was 0.479.[6]
Lobeglitazone was primarily distributed to the liver with tissue-to-plasma concentration ratio as 5.59, and less to heart, lung, and fat. The tissue to plasma concentration ratios were ranged from about 0.25 to 4.0 for major tissues, in rat.[1]
Among six major membrane transporters recommended by the United States Food and Drug Administration, lobeglitazone interacts with OATP1B1, OAT3, and MDR1.[1] In vitro, lobeglitazone was a substrate of rodent OATP1B2.[6] Lobeglitazone interacted with CYP1A2, 2C9 and 2C19.[1]
Distribution to liver of lobeglitazone was inhibited by atorvastatin, in rats.[6]
^abcKim JW, Kim JR, Yi S, Shin KH, Shin HS, Yoon SH, Cho JY, Kim DH, Shin SG, Jang IJ, Yu KS (2011). "Tolerability and pharmacokinetics of lobeglitazone (CKD-501), a peroxisome proliferator-activated receptor-γ agonist: a single- and multiple-dose, double-blind, randomized control study in healthy male Korean subjects".Clinical Therapeutics.33 (11):1819–1830.doi:10.1016/j.clinthera.2011.09.023.PMID22047812.
^Lee JH, Woo YA, Hwang IC, Kim CY, Kim DD, Shim CK, Chung SJ (2009). "Quantification of CKD-501, lobeglitazone, in rat plasma using a liquid-chromatography/tandem mass spectrometry method and its applications to pharmacokinetic studies".Journal of Pharmaceutical and Biomedical Analysis.50 (5):872–877.doi:10.1016/j.jpba.2009.06.003.PMID19577404.
