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Volumn 102, Issue 3, 2013, Pages 1106-1115

Presystemic metabolism of AZ'0908, a novel mPGES-1 inhibitor: An in vitro and in vivo cross-species comparison

Author keywords

ABC transporters; Bioavailability; CYP2J2; First pass metabolism; Interspecies correlation; Intestinal loss; Intestinal metabolism; Pharmacokinetics

Indexed keywords

1 AMINOBENZOTRIAZOLE; AZ 0908; BREAST CANCER RESISTANCE PROTEIN; CYTOCHROME P450 2J2; ISOMERASE INHIBITOR; UNCLASSIFIED DRUG;

EID: 84878124595     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23443     Document Type: Article
Times cited : (8)

References (40)
  • 2
    • 34748817976 scopus 로고    scopus 로고
    • Membrane prostaglandin E synthase-1: A novel therapeutic target
    • Samuelsson B, Morgenstern R, Jakobsson PJ. 2007. Membrane prostaglandin E synthase-1: A novel therapeutic target. Pharmacol Rev 59:207-224.
    • (2007) Pharmacol Rev , vol.59 , pp. 207-224
    • Samuelsson, B.1    Morgenstern, R.2    Jakobsson, P.J.3
  • 3
    • 0030444901 scopus 로고    scopus 로고
    • Interpatient variability in bioavailability is related to the extent of absorption: Implications for bioavailability and bioequivalence studies
    • Hellriegel ET, Bjornsson TD, Hauck WW. 1996. Interpatient variability in bioavailability is related to the extent of absorption: Implications for bioavailability and bioequivalence studies. Clin Pharmacol Ther 60:601-607.
    • (1996) Clin Pharmacol Ther , vol.60 , pp. 601-607
    • Hellriegel, E.T.1    Bjornsson, T.D.2    Hauck, W.W.3
  • 4
    • 35348856278 scopus 로고    scopus 로고
    • The role of the intestine in drug metabolism and pharmacokinetics: An industry perspective
    • Fisher MB, Labissiere G. 2007. The role of the intestine in drug metabolism and pharmacokinetics: An industry perspective. Curr Drug Metab 8:694-699.
    • (2007) Curr Drug Metab , vol.8 , pp. 694-699
    • Fisher, M.B.1    Labissiere, G.2
  • 6
    • 35348860160 scopus 로고    scopus 로고
    • Modeling gastrointestinal drug absorption requires more in vivo biopharmaceutical data: Experience from in vivo dissolution and permeability studies in humans
    • Lennernäs H. 2008. Modeling gastrointestinal drug absorption requires more in vivo biopharmaceutical data: Experience from in vivo dissolution and permeability studies in humans. Curr Drug Metab 8:645-657.
    • (2008) Curr Drug Metab , vol.8 , pp. 645-657
    • Lennernäs, H.1
  • 8
    • 77953737073 scopus 로고    scopus 로고
    • Prediction of human intestinal first-pass metabolism of 25 CYP3A4 substrates from in vitro clearance and permeability data
    • Gertz M, Harrison A, Houston JB, Galetin A. 2010. Prediction of human intestinal first-pass metabolism of 25 CYP3A4 substrates from in vitro clearance and permeability data. Drug Metab Dispos 38:1147-1158.
    • (2010) Drug Metab Dispos , vol.38 , pp. 1147-1158
    • Gertz, M.1    Harrison, A.2    Houston, J.B.3    Galetin, A.4
  • 9
    • 77953777072 scopus 로고    scopus 로고
    • Quantitative prediction of intestinal metabolism in humans from a simplified intestinal availability model and empirical scaling factor
    • Kadono K, Akabane T, Tabata K, Gato K, Terashita S, Teramura T. 2010. Quantitative prediction of intestinal metabolism in humans from a simplified intestinal availability model and empirical scaling factor. Drug Metab Dispos 38:1230-1237.
    • (2010) Drug Metab Dispos , vol.38 , pp. 1230-1237
    • Kadono, K.1    Akabane, T.2    Tabata, K.3    Gato, K.4    Terashita, S.5    Teramura, T.6
  • 10
    • 84855219592 scopus 로고    scopus 로고
    • Prediction of the intestinal first-pass metabolism of CYP3A and UGT substrates in humans from in vitro data
    • Nishimuta H, Sato K, Yabuki M, Komura S. 2011. Prediction of the intestinal first-pass metabolism of CYP3A and UGT substrates in humans from in vitro data. Drug Metab Pharmacokinet 26:592-601.
    • (2011) Drug Metab Pharmacokinet , vol.26 , pp. 592-601
    • Nishimuta, H.1    Sato, K.2    Yabuki, M.3    Komura, S.4
  • 11
    • 79851476433 scopus 로고    scopus 로고
    • Interplay of metabolism and transport in determining oral drug absorption and gut wall metabolism: A simulation assessment using the Advanced Dissolution, Absorption, Metabolism (ADAM) model
    • Darwich AS, Neuhoff S, Jamei M, Rostami-Hodjegan A. 2010. Interplay of metabolism and transport in determining oral drug absorption and gut wall metabolism: A simulation assessment using the Advanced Dissolution, Absorption, Metabolism (ADAM) model. Curr Drug Metab 11:716-729.
    • (2010) Curr Drug Metab , vol.11 , pp. 716-729
    • Darwich, A.S.1    Neuhoff, S.2    Jamei, M.3    Rostami-Hodjegan, A.4
  • 12
    • 68149170038 scopus 로고    scopus 로고
    • The role of transporters in the pharmacokinetics of orally administered drugs
    • Shugarts S, Benet LZ. 2009. The role of transporters in the pharmacokinetics of orally administered drugs. Pharm Res 26:2039-2054.
    • (2009) Pharm Res , vol.26 , pp. 2039-2054
    • Shugarts, S.1    Benet, L.Z.2
  • 13
    • 84865178172 scopus 로고    scopus 로고
    • Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics
    • Zamek-Gliszczynski MJ, Bedwell DW, Bao JQ, Higgins JW. 2012. Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics. Drug Metab Dispos 40:1825-1833.
    • (2012) Drug Metab Dispos , vol.40 , pp. 1825-1833
    • Zamek-Gliszczynski, M.J.1    Bedwell, D.W.2    Bao, J.Q.3    Higgins, J.W.4
  • 16
    • 84878155918 scopus 로고    scopus 로고
    • Rat predicts the combined non-absorbed and presystemically metabolised fractions in human poorly. Xenobiotica, In press.
    • Bueters T, Juric S, Sohlenius-Sternbeck A-K, Hu Y, Bylund J. Rat predicts the combined non-absorbed and presystemically metabolised fractions in human poorly. Xenobiotica, In press.
    • Bueters, T.1    Juric, S.2    Sohlenius-Sternbeck, A.-K.3    Hu, Y.4    Bylund, J.5
  • 17
    • 0031786518 scopus 로고    scopus 로고
    • Linear correlation of the fraction of oral dose absorbed of 64 drugs between human and rats
    • Chiou WL, Barve A. 1998. Linear correlation of the fraction of oral dose absorbed of 64 drugs between human and rats. Pharm Res 15:1792-1795.
    • (1998) Pharm Res , vol.15 , pp. 1792-1795
    • Chiou, W.L.1    Barve, A.2
  • 19
    • 0024571757 scopus 로고
    • The absolute oral bioavailability of selected drugs
    • Sietsema WK. 1989. The absolute oral bioavailability of selected drugs. Int J Clin Pharmacol Ther Toxicol 27:179-211.
    • (1989) Int J Clin Pharmacol Ther Toxicol , vol.27 , pp. 179-211
    • Sietsema, W.K.1
  • 20
    • 80054948359 scopus 로고    scopus 로고
    • In vitro and in vivo small intestinal metabolism of CYP3A and UGT substrates in preclinical animals species and humans: Species differences
    • Komura H, Iwaki M. 2011. In vitro and in vivo small intestinal metabolism of CYP3A and UGT substrates in preclinical animals species and humans: Species differences. Drug Metab Rev 43:476-498.
    • (2011) Drug Metab Rev , vol.43 , pp. 476-498
    • Komura, H.1    Iwaki, M.2
  • 21
    • 84856372013 scopus 로고    scopus 로고
    • Validation of quinidine as a probe substrate for the in vitro P-gp inhibition assay in Caco-2 cell monolayer
    • Patil AG, D'Souza R, Dixit N, Damre A. 2011. Validation of quinidine as a probe substrate for the in vitro P-gp inhibition assay in Caco-2 cell monolayer. Eur J Drug Metab Pharmacokinet 36:115-119.
    • (2011) Eur J Drug Metab Pharmacokinet , vol.36 , pp. 115-119
    • Patil, A.G.1    D'Souza, R.2    Dixit, N.3    Damre, A.4
  • 22
    • 67650084777 scopus 로고    scopus 로고
    • Identification of novel specific and general inhibitors of the three major human ATP-binding cassette transporters P-gp, BCRP and MRP2 among registered drugs
    • Matsson P, Pedersen JM, Norinder U, Bergström CA, Artursson P. 2009. Identification of novel specific and general inhibitors of the three major human ATP-binding cassette transporters P-gp, BCRP and MRP2 among registered drugs. Pharm Res 26:1816-1831.
    • (2009) Pharm Res , vol.26 , pp. 1816-1831
    • Matsson, P.1    Pedersen, J.M.2    Norinder, U.3    Bergström, C.A.4    Artursson, P.5
  • 23
    • 84864299679 scopus 로고    scopus 로고
    • Differential selectivity of effluxtransporter inhibitors in Caco-2 and MDCK-MDR1 monolayers: A strategy to assess the interaction of a new chemical entity with P-gp, BCRP, and MRP2
    • Mease K, Sane R, Podila L, Taub ME. 2012. Differential selectivity of effluxtransporter inhibitors in Caco-2 and MDCK-MDR1 monolayers: A strategy to assess the interaction of a new chemical entity with P-gp, BCRP, and MRP2. J Pharm Sci 101:1888-1897.
    • (2012) J Pharm Sci , vol.101 , pp. 1888-1897
    • Mease, K.1    Sane, R.2    Podila, L.3    Taub, M.E.4
  • 25
    • 79956145323 scopus 로고    scopus 로고
    • High-throughput analysis of standardized pharmacokinetic studies in the rat using sample pooling and UPLC-MS/MS
    • Bueters T, Dahlström J, Kvalvågnaes K, Betner I, Briem S. 2011. High-throughput analysis of standardized pharmacokinetic studies in the rat using sample pooling and UPLC-MS/MS. J Pharm Biomed Anal 55:1120-1126.
    • (2011) J Pharm Biomed Anal , vol.55 , pp. 1120-1126
    • Bueters, T.1    Dahlström, J.2    Kvalvågnaes, K.3    Betner, I.4    Briem, S.5
  • 26
    • 0036785501 scopus 로고    scopus 로고
    • Effective dosing regimen of 1-aminobenzotriazole for inhibition of antipyrine clearance in rats, dogs, and monkeys
    • Balani SK, Zhu T, Yang TJ, Liu Z, He B, Lee FW. 2002. Effective dosing regimen of 1-aminobenzotriazole for inhibition of antipyrine clearance in rats, dogs, and monkeys. Drug Metab Dispos 30:1059-1062.
    • (2002) Drug Metab Dispos , vol.30 , pp. 1059-1062
    • Balani, S.K.1    Zhu, T.2    Yang, T.J.3    Liu, Z.4    He, B.5    Lee, F.W.6
  • 27
    • 47249159896 scopus 로고    scopus 로고
    • The use of 1-aminobenzotriazole in differentiating the role of CYP-mediated first pass metabolism and absorption in limiting drug oral bioavailability: A case study
    • El-Kattan AF, Poe J, Buchholz L, Thomas HV, Brodfuehrer J, Clark A. 2008. The use of 1-aminobenzotriazole in differentiating the role of CYP-mediated first pass metabolism and absorption in limiting drug oral bioavailability: A case study. Drug Metab Lett 2:120-124.
    • (2008) Drug Metab Lett , vol.2 , pp. 120-124
    • El-Kattan, A.F.1    Poe, J.2    Buchholz, L.3    Thomas, H.V.4    Brodfuehrer, J.5    Clark, A.6
  • 28
    • 23944451585 scopus 로고    scopus 로고
    • A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomes
    • Riley RJ, McGinnity DF, Austin RP. 2005. A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomes. Drug Metab Dispos 33:1304-1311.
    • (2005) Drug Metab Dispos , vol.33 , pp. 1304-1311
    • Riley, R.J.1    McGinnity, D.F.2    Austin, R.P.3
  • 29
    • 0027275566 scopus 로고
    • Physiological parameters in laboratory animals and humans
    • Davies B, Morris T. 1993. Physiological parameters in laboratory animals and humans. Pharm Res 10:1093-1095.
    • (1993) Pharm Res , vol.10 , pp. 1093-1095
    • Davies, B.1    Morris, T.2
  • 30
    • 79952343050 scopus 로고    scopus 로고
    • Methodologies for investigating drug metabolism at the early drug discovery stage: Prediction of hepatic drug clearance and P450 contribution
    • Emoto C, Murayama N, Rostami-Hodjegan A, Yamazaki H. 2010. Methodologies for investigating drug metabolism at the early drug discovery stage: Prediction of hepatic drug clearance and P450 contribution. Curr Drug Metab 11:678-685.
    • (2010) Curr Drug Metab , vol.11 , pp. 678-685
    • Emoto, C.1    Murayama, N.2    Rostami-Hodjegan, A.3    Yamazaki, H.4
  • 31
    • 58149460394 scopus 로고    scopus 로고
    • Is 1-aminobenzotriazole an appropriate in vitro tool as a nonspecific cytochrome P450 inactivator
    • Linder CD, Renaud NA, Hutzler JM. 2009. Is 1-aminobenzotriazole an appropriate in vitro tool as a nonspecific cytochrome P450 inactivator? Drug Metab Dispos 37:10-13.
    • (2009) Drug Metab Dispos , vol.37 , pp. 10-13
    • Linder, C.D.1    Renaud, N.A.2    Hutzler, J.M.3
  • 32
    • 33745049731 scopus 로고    scopus 로고
    • In vivo use of the P450 inactivator 1-aminobenzotriazole in the rat: Varied dosing route to elucidate gut and liver contributions to first-pass and systemic clearance
    • Strelevitz TJ, Foti RS, Fisher MB. 2006. In vivo use of the P450 inactivator 1-aminobenzotriazole in the rat: Varied dosing route to elucidate gut and liver contributions to first-pass and systemic clearance. J Pharm Sci 95:1334-1341.
    • (2006) J Pharm Sci , vol.95 , pp. 1334-1341
    • Strelevitz, T.J.1    Foti, R.S.2    Fisher, M.B.3
  • 33
    • 32644436135 scopus 로고    scopus 로고
    • Impact of extracellular protein binding on passive and active drug transport across Caco-2 cells
    • Neuhoff S, Artursson P, Zamora I, Ungell AL. 2006. Impact of extracellular protein binding on passive and active drug transport across Caco-2 cells. Pharm Res 23:350-359.
    • (2006) Pharm Res , vol.23 , pp. 350-359
    • Neuhoff, S.1    Artursson, P.2    Zamora, I.3    Ungell, A.L.4
  • 34
    • 67650227457 scopus 로고    scopus 로고
    • Preparation and characterization of rodent intestinal microsomes: Comparative assessment of two methods
    • Damre A, Mallurwar SR, Behera D. 2009. Preparation and characterization of rodent intestinal microsomes: Comparative assessment of two methods. Indian J Pharm Sci 71:75-77.
    • (2009) Indian J Pharm Sci , vol.71 , pp. 75-77
    • Damre, A.1    Mallurwar, S.R.2    Behera, D.3
  • 35
    • 33747599176 scopus 로고    scopus 로고
    • Intestinal and hepatic metabolic activity of five cytochrome P450 enzymes: Impact on prediction of first-pass metabolism
    • Galetin A, Houston JB. 2006. Intestinal and hepatic metabolic activity of five cytochrome P450 enzymes: Impact on prediction of first-pass metabolism. J Pharmacol Exp Ther 318:1220-1229.
    • (2006) J Pharmacol Exp Ther , vol.318 , pp. 1220-1229
    • Galetin, A.1    Houston, J.B.2
  • 36
    • 68949103975 scopus 로고    scopus 로고
    • Cytochrome P450-mediated metabolism in the human gut wall
    • Thelen K, Dressman JB. 2009. Cytochrome P450-mediated metabolism in the human gut wall. J Pharm Pharmacol 61:541-558.
    • (2009) J Pharm Pharmacol , vol.61 , pp. 541-558
    • Thelen, K.1    Dressman, J.B.2
  • 37
    • 0030063499 scopus 로고    scopus 로고
    • Molecular cloning and expression of CYP2J2, a human cytochrome P450 arachidonic acid epoxygenase highly expressed in heart
    • Wu S, Moomaw CR, Tomer KB, Falck JR, Zeldin DC. 1996. Molecular cloning and expression of CYP2J2, a human cytochrome P450 arachidonic acid epoxygenase highly expressed in heart. J Biol Chem 271:3460-3468.
    • (1996) J Biol Chem , vol.271 , pp. 3460-3468
    • Wu, S.1    Moomaw, C.R.2    Tomer, K.B.3    Falck, J.R.4    Zeldin, D.C.5


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