Kinetics of the Absorption, Distribution, Metabolism, and Excretion of Lobeglitazone, a Novel Activator of Peroxisome Proliferator-Activated Receptor Gamma in Rats

Journal of Pharmaceutical Sciences

Volumn 104, Issue 9, 2015, Pages 3049-3059

  Lee, Jong Hwa ^a,b   Noh, Chi Kyoung ^a   Yim, Chang Soon ^a   Jeong, Yoo Seong ^a   Ahn, Sung Hoon ^c   Lee, Wooin ^a   Kim, Dae Duk ^a   Chung, Suk Jae ^a  

^a Seoul National University   (South Korea)

^b Korea Institute of Toxicology   (South Korea)

^c Korea Research Institute of Chemical Technology   (South Korea)

Author keywords

ADME; CYP enzymes; microsomal stability; P glycoprotein; pharmacokinetics; transporters

Indexed keywords

CYTOCHROME P450 1A2; CYTOCHROME P450 2C19; CYTOCHROME P450 2C9; LOBEGLITAZONE; MULTIDRUG RESISTANCE PROTEIN 1; SOLUTE CARRIER ORGANIC ANION TRANSPORTER 1B1; 2,4 THIAZOLIDINEDIONE DERIVATIVE; 2,4-THIAZOLIDINEDIONE; CYTOCHROME P450; MULTIDRUG RESISTANCE PROTEIN; ORGANIC ANION TRANSPORTER; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA; PYRIMIDINE DERIVATIVE;

ADIPOSE TISSUE; ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; ARTIFICIAL MEMBRANE; CELL MEMBRANE PERMEABILITY; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG EXCRETION; DRUG METABOLISM; HEART; IN VITRO STUDY; LIVER MICROSOME; LUNG; MALE; MDCK CELL LINE; NONHUMAN; RAT; ANIMAL; BIOAVAILABILITY; CELL LINE; DOG; INTESTINE ABSORPTION; INTRAVENOUS DRUG ADMINISTRATION; KINETICS; METABOLISM; ORAL DRUG ADMINISTRATION; PHYSIOLOGY; SPRAGUE DAWLEY RAT; TISSUE DISTRIBUTION; TRANSPORT AT THE CELLULAR LEVEL;

ADMINISTRATION, INTRAVENOUS; ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; BIOLOGICAL TRANSPORT; CELL LINE; CELL MEMBRANE PERMEABILITY; CYTOCHROME P-450 ENZYME SYSTEM; DOGS; INTESTINAL ABSORPTION; KINETICS; MADIN DARBY CANINE KIDNEY CELLS; MALE; MICROSOMES, LIVER; ORGANIC ANION TRANSPORTERS; P-GLYCOPROTEIN; PPAR GAMMA; PYRIMIDINES; RATS; RATS, SPRAGUE-DAWLEY; THIAZOLIDINEDIONES; TISSUE DISTRIBUTION;

EID: 84939272467     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.24378     Document Type: Article

References (25)

1. Cox PJ, Ryan DA, Hollis FJ, Harris AM, Miller AK, Vousden M, Cowley H,. 2000. Absorption, disposition, and metabolism of rosiglitazone, a potent thiazolidinedione insulin sensitizer, in humans. Drug Metab Dispos 28 (7): 772-780.
2. Hanefeld M., 2001. Pharmacokinetics and clinical efficacy of pioglitazone. Int J Clin Pract Suppl (121): 19-25.
3. Loi CM, Young M, Randinitis E, Vassos A, Koup JR,. 1999. Clinical pharmacokinetics of troglitazone. Clin Pharm 37 (2): 91-104.
4. Zhu C, Jiang L, Chen TM, Hwang KK,. 2002. A comparative study of artificial membrane permeability assay for high throughput profiling of drug absorption potential. Eur J Med Chem 37 (5): 399-407.
5. Kerns EH, Di L, Petusky S, Farris M, Ley R, Jupp P,. 2004. Combined application of parallel artificial membrane permeability assay and Caco-2 permeability assays in drug discovery. J Pharm Sci 93 (6): 1440-1453.
6. 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. J Pharm Biomed Anal 50 (5): 872-877.
7. Ueki M, Galonic DP, Vaillancourt FH, Garneau-Tsodikova S, Yeh E, Vosburg DA, Schroeder FC, Osada H, Walsh CT,. 2006. Enzymatic generation of the antimetabolite gamma, gamma-dichloroaminobutyrate by NRPS and mononuclear iron halogenase action in a streptomycete. Chem Biol 13 (11): 1183-1191.
8. Li D, Au JL,. 2001. Mdr1 transfection causes enhanced apoptosis by paclitaxel: An effect independent of drug efflux function of P-glycoprotein. Pharm Res 18 (7): 907-913.
9. Soldner A, Benet LZ, Mutschler E, Christians U,. 2000. Active transport of the angiotensin-II antagonist losartan and its main metabolite EXP 3174 across MDCK-MDR1 and Caco-2 cell monolayers. Br J Pharmacol 129 (6): 1235-1243.
10. Obach RS, Baxter JG, Liston TE, Silber BM, Jones BC, MacIntyre F, Rance DJ, Wastall P,. 1997. The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data. J Pharmacol Exp Ther 283 (1): 46-58.
11. Gibaldi M, Perrier D,. 1982. Pharmacokinetics. 2nd ed. Taylor & Francis, New Jersey.
12. Feng B, Mills JB, Davidson RE, Mireles RJ, Janiszewski JS, Troutman MD, de Morais SM,. 2008. In vitro P-glycoprotein assays to predict the in vivo interactions of P-glycoprotein with drugs in the central nervous system. Drug Metab Dispos 36 (2): 268-275.
13. Irvine JD, Takahashi L, Lockhart K, Cheong J, Tolan JW, Selick HE, Grove JR,. 1999. MDCK (Madin-Darby canine kidney) cells: A tool for membrane permeability screening. J Pharm Sci 88 (1): 28-33.
14. Prueksaritanont T, Chu X, Gibson C, Cui D, Yee KL, Ballard J, Cabalu T, Hochman J,. 2013. Drug-drug interaction studies: Regulatory guidance and an industry perspective. AAPS J 15 (3): 629-645.
15. Sugano K, Hamada H, Machida M, Ushio H, Saitoh K, Terada K,. 2001. Optimized conditions of bio-mimetic artificial membrane permeation assay. Int J Pharm 228 (1-2): 181-188.
16. Hou T, Wang J, Zhang W, Xu X,. 2007. ADME evaluation in drug discovery. 7. Prediction of oral absorption by correlation and classification. J Chem Inf Model 47 (1): 208-218.
17. International, Transporter C, Giacomini KM, Huang SM, Tweedie DJ, Benet LZ, Brouwer KL, Chu X, Dahlin A, Evers R, Fischer V, Hillgren KM, Hoffmaster KA, Ishikawa T, Keppler D, Kim RB, Lee CA, Niemi M, Polli JW, Sugiyama Y, Swaan PW, Ware JA, Wright SH, Yee SW, Zamek-Gliszczynski MJ, Zhang L,. 2010. Membrane transporters in drug development. Nat Rev Drug Discov 9 (3): 215-236.
18. Yu KH, Lee YR, Ahn SH, Kim DD, Shim CK, Chung SJ,. 2009. Contribution of a significant first-pass effect of dimethyl-4,4′-dimethoxy-5,6,5′,6′-dimethylene dioxybiphenyl-2,2′-dicarboxylate in the liver to its poor bioavailability in rats. J Pharm Pharmacol 61 (9): 1197-1203.
19. Smith AL, Meeks CA, Koup JR, Opheim KE, Weber A, Vishwanathan CT,. 1990. Dicloxacillin absorption and elimination in children. Dev Pharmacol Ther 14 (1): 35-44.
20. Wempe MF, Wright C, Little JL, Lightner JW, Large SE, Caflisch GB, Buchanan CM, Rice PJ, Wacher VJ, Ruble KM, Edgar KJ,. 2009. Inhibiting efflux with novel non-ionic surfactants: Rational design based on vitamin E TPGS. Int J Pharm 370 (1-2): 93-102.
21. Bateman DN, Hobbs DC, Twomey TM, Stevens EA, Rawlins MD,. 1979. Prazosin, pharmacokinetics and concentration effect. Eur J Clin Pharmacol 16 (3): 177-181.
22. Brown RP, Delp MD, Lindstedt SL, Rhomberg LR, Beliles RP,. 1997. Physiological parameter values for physiologically based pharmacokinetic models. Toxicol Ind Health 13 (4): 407-484.
23. Falasca M, Linton KJ,. 2012. Investigational ABC transporter inhibitors. Exp Opin Invest Drugs 21 (5): 657-666.
24. Keogh JP., 2012. Membrane transporters in drug development. Adv Pharmacol 63: 1-42.
25. Slco1B2 Solute carrier organic anion transporter family, member 1B2 [Rattus norvegicus (Norway rat)]. Accessed on 12/24/2014, at: http://www.ncbi.nlm.nih.gov/gene/58978.