Cytochrome P450 isoforms

Aprepitant, which inhibits the cytochrome P450 isoform, CYP3A4, is metabolised by it. As a result,... 

Fuhr U, Strobl G, Manaut F, Anders E-M, Sorgel F, Lopez-de-brinas E, et al. Quinolone antibacterial agents relationship between structure and in vitro inhibition of human cytochrome P450 isoform CYP1A2. Mol Pharmacol 1993 43 191-9. 

Olesen, O. V. Linnet, K. (2001). Contributions of five human cytochrome P450 isoforms to the N-demethylation of clozapine in vitro at low and high concentrations. /. Clin. Pharmacol., 41, 823-32. 

Easterbrook, J., Liu, C., Sakai, Y. and Li, A.P. (2001) Effects of organic solvents on the activities of cytochrome P450 isoforms, UDP-dependent glucuronyl transferase, and phenol sulfotransferase in human hepatocytes. Drug Metabolism and Disposition The Biological Fate of Chemicals, 29, 141-144. 

Scollon EJ, Starr JM, Godin SJ, DeVito MJ, Hughers MF (2009) In vitro metabolism of pyrethroid pesticides by rats and human hepatic microsomes and cytochrome p450 isoforms. Dmg Metab Dispos 37 221-228... 

Godin SJ, Crow JA, Scollon EJ, Hughes MF, DeVito MJ, Ross MK (2007) Identification of rat and human cytochrome p450 isoforms and a rat serum esterase that metabolize the pyrethroid insecticides deltamethrin and esfenvalerate. Drug Metab Dispos 35 1664-1671... 

Nishimura M, Yaguti H, Yoshitsugu H, Naito S, Satoh T (2003) Tissue distribution of mRNA expression of human cytochrome P450 isoforms assessed by high-sensitivity real-time reverse transcription PCR. Yakugaku Zasshi 123(5) 369-375. 

Rosenbrock H, Hagemeyer CE, Singec I, Knoth R, Volk B. 1999. Testosterone metabolism in rat brain is differentially enhanced by phenytoin-inducible cytochrome P450 isoforms. J Neuroendocrinol 11 597-604. 

Upadhya SC, Chinta SJ, Pai HV, Boyd MR, Ravindranath V. 2002. Toxicological consequences of differential regulation of cytochrome p450 isoforms in rat brain regions by phe-nobarbital. Arch Biochem Biophys 399 56-65. 

Tam TW, Liu R, Amason IT et al (2009) Actions of ethnobotanicaUy selected Cree antidiabetic plants on human cytochrome P450 isoforms and flavin-containing monooxygenase 3. 1 Ethnopharmacol 126 119-126... 

The first studies with isolated human hepatocytes concentrated on the characterization of these hepatocytes, as well as on the improvement of the isolation procedure, and the possibilities of culturing these cells [16,19-24]. Thereafter studies were performed to investigate the metabolism of drugs [25-28], in which emphasis was often put on the activity and concentration of cytochrome P450 isoforms. Nowadays, hepatocytes are more generally used in metabolic studies of specific compounds, in order to unravel potential species differences and... 

The inhibitor has excellent pharmacokinetics in both mice and rats, with high bioavailabilities (82 and 74%, respectively) [113]. Additionally, the potential for drug-drug interactions after administration of ARRY-142886 is low as it does not inhibit any of the major cytochrome p450 isoforms below 20 xM. 

The cytochrome P450 isoform CYP3A4 is partially responsible for the metabolism of pioglitazone. 

Metabolism - Unchanged nelfinavir comprised 82% to 86% of the total plasma. In vitro multiple cytochrome P450 isoforms including CYP3A and CYP2C19 are responsible for metabolism of nelfinavir. One major and several minor oxidative... 

Lewis, D. F. V., Wiseman, A., and Tarbit, M. H. (1999) Molecular modeling of lanosterol 14-alpha-demethylase (CYP51) from Saccharomyces cerevisiae via homology with CYP102, a unique bacterial cytochrome P450 isoform quantitative structure-activity relationships (QSARs) within two related series of antifungal azole derivatives../. Enz. Inhib. 14, 175-192. 

Table 3. Some drug substrates, inducers and inhibitors of the major cytochrome P450 isoforms...

Desta, Z., Kerbusch, T, Soukhova, N., Richard, E., Ko, J.W., and Flockhart, D.A. (1998) Identification and characterization of human cytochrome P450 isoforms interacting with pimozide. / Pharmacol Exp Ther 285 428-437. 

Prakash, C., Kamel, A., Cui, D., Whalen, R.D., Miceli, J.J., and Tweedie, D. (2000) Identification of the major human liver cytochrome P450 isoform(s) responsible for the formation of zi-prasidone and prediction of possible drug interactions. Br Clin Pharmacol 49 35S-42S. 

Shader RI, Granda BW, von Moltke LL, Giancarlo GM, Greenblatt DJ. Inhibition of human cytochrome P450 isoforms in vitro by zafirlukast. Biopharm Drug Dispos 1999 20(8) 385-388. 

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