Drug Metabolism in Drug Design and Development Basic Concepts and Practice

(nextflipdebug2) #1

Desai PB, Nallani SC, Sane RS, Moore LB, Goodwin BJ, Buckley DJ, Buckley AR.
Induction of cytochrome P450 3A4 in primary human hepatocytes and activation of
the human pregnane X receptor by tamoxifen and 4-hydroxytamoxifen. Drug Metab
Dispos 2002;30:608–612.
Dilger K, Denk A, Heeg MH, Beuers U. No relevant effect of ursodeoxycholic acid on
cytochrome P450 3A metabolism in primary biliary cirrhosis. Hepatology
2005;41:595–602.
Durr D, Stieger B, Kullak-Ublick GA, Rentsch KM, Steinert HC, Meier PJ, Fattinger
K. St John’s wort induces intestinal P-glycoprotein/MDR1 and intestinal and hepatic
CYP3A4. Clin Pharmacol Ther 2000;68:598–604.
Eloranta JJ, Meier PJ, Kullak-Ublick GA. Coordinate transcriptional regulation of
transport and metabolism. Methods Enzymol 2005;400:511–530.
El-Sankary W, Plant NJ, Gibson GG, Moore DJ. Regulation of the CYP3A4 gene by
hydrocortisone and xenobiotics: role of the glucocorticoid and pregnane X receptors.
Drug Metab Dispos 2000;28:493–496.
Fabre G, Rahmani R, Placidi M, Combalbert J, Covo J, Cano JP, Coulange C, Ducros
M, Rampal M. Characterization of midazolam metabolism using human hepatic
microsomal fractions and hepatocytes in suspension obtained by perfusing whole
human livers. Biochem Pharmacol 1988;37:4389–4397.
Floyd MD, Gervasini G, Masica AL, Mayo G, George AL, Bhat K Jr, Kim RB,
Wilkinson GR. Genotype-phenotype associations for common CYP3A4 and
CYP3A5 variants in the basal and induced metabolism of midazolam in European-
and African-American men and women. Pharmacogenetics 2003;13:595–606.
Furster C, Wikvall K. Identification of CYP3A4 as the major enzyme responsible for
25-hydroxylation of 5beta-cholestane-3alpha,7alpha, 12alpha-triol in human liver
microsomes. Biochim Biophys Acta 1999;1437:46–52.
Gerbal-Chaloin S, Pascussi JM, Pichard-Garcia L, Daujat M, Waechter F, Fabre JM,
Carrere N, Maurel P. Induction of CYP2C genes in human hepatocytes in primary
culture. Drug Metab Dispos 2001;29:242–251.
Goodwin B, Hodgson E, Liddle C. The orphan human pregnane X receptor mediates
the transcriptional activation of CYP3A4 by rifampicin through a distal enhancer
module. Mol Pharmacol 1999;56:1329–1339.
Goodwin B, Moore LB, Stoltz CM, McKee DD, Kliewer SA. Regulation of the human
CYP2B6 gene by the nuclear pregnane X receptor. Mol Pharmacol 2001;60:427–431.
Goodwin B, Redinbo MR, Kliewer SA. Regulation of cyp3a gene transcription by the
pregnane x receptor. Annu Rev Pharmacol Toxicol 2002;42:1–23.
Handschin C, Podvinec M, Amherd R, Looser R, Ourlin JC, Meyer UA. Cholesterol
and bile acids regulate xenosensor signaling in drug-mediated induction of
cytochromes P450. J Biol Chem 2002;277:29561–29567.
Hankinson O. The aryl hydrocarbon receptor complex. Annu Rev Pharmacol Toxicol
1995;35:307–340.
Hariparsad N, Nallani SC, Sane RS, Buckley DJ, Buckley AR, Desai PB. Induction of
CYP3A4 by efavirenz in primary human hepatocytes: comparison with rifampin and
phenobarbital. J Clin Pharmacol 2004;44:1273–1281.
He K, Woolf TF, Hollenberg PF. Mechanism-based inactivation of cytochrome P450–
3A4 by mifepristone (RU486). J Pharmacol Exp Ther 1999;288:791–797.


REFERENCES 567

Free download pdf