SCHOOL OF MEDICINE

Department of Medicine

Clinical Pharmacology

2B6 REFERENCES

 2B6 SUBSTRATES: 

BUPROPION
Validation of bupropion hydroxylation as a selective marker of human cytochrome P450 2B6 catalytic activity. [ PMID 10997944 ]
Faucette SR, Hawke RL, Lecluyse EL, Shord SS, Yan B, Laethem RM, Lindley CM.
Drug Metab Dispos 2000 Oct;28(10):1222-30

CYCLOPHOSPHAMIDE
Differential activation of cyclophosphamide and ifosphamide by cytochromes P-450 2B and 3A in human liver microsomes. [ PMID 8242617 ]
Chang TK, Weber GF, Crespi CL, Waxman DJ
Cancer Res 1993 Dec 1;53(23):5629-37.

EFAVIRENZ
Pharmacokinetics of efavirenz when co-administered with rifampin in TB/HIV co-infected patients: pharmacogenetic effect of CYP2B6 variation. [ PMID 18728241 ]
Kwara A, Lartey M, Sagoe KW, Xexemeku F, Kenu E, Oliver-Commey J, Boima V, Sagoe A, Boamah I, Greenblatt DJ, Court MH.
J Clin Pharmacol. 2008 Sep;48(9):1032-40.

High prevalence of the CYP2B6 516G-->T(*6) variant and effect on the population pharmacokinetics of efavirenz in HIV/AIDS outpatients in Zimbabwe. [ PMID 18057928 ]
Nyakutira C, Röshammar D, Chigutsa E, Chonzi P, Ashton M, Nhachi C, Masimirembwa C.
Eur J Clin Pharmacol. 2008 Apr;64(4):357-65.

IFOSPHAMIDE
Differential activation of cyclophosphamide and ifosphamide by cytochromes P-450 2B and 3A in human liver microsomes. [ PMID 8242617 ]
Chang TK, Weber GF, Crespi CL, Waxman DJ
Cancer Res 1993 Dec 1;53(23):5629-37.

Role of CYP2B6 and CYP3A4 in the in vitro N-dechloroethylation of (R)- and (S)-ifosfamide in human liver microsomes. [ PMID 10101149 ]
Granvil CP, Madan A, Sharkawi M, Parkinson A, Wainer IW
Drug Metab Dispos 1999 Apr;27(4):533-41.

METHADONE
Role of CYP2B6 in stereoselective human methadone metabolism. [ PMID 18292673 ]
Totah RA, Sheffels P, Roberts T, Whittington D, Thummel K, Kharasch ED.
Anesthesiology. 2008 Mar;108(3):363-74.

SORAFENIB
Prescribing Information
 

 2B6 INHIBITORS: 

THIOTEPA
Triethylenethiophosphoramide is a specific inhibitor of cytochrome P450 2B6: Implications for cyclophosphamide metabolism. [ PMID 11950782 ]
Rae JM, Soukhova NV, Flockhart DA, Desta Z.
Drug Metab Dispos 2002;30(5)

TICLOPIDINE
Mechanism-based inhibition of human cytochrome P450 2B6 by ticlopidine, clopidogrel, and the thiolactone metabolite of prasugrel. [ PMID 19047469 ]
Nishiya Y, Hagihara K, Ito T, Tajima M, Miura SI, Kurihara A, Farid NA, Ikeda T.
Drug Metab Dispos. 2008 Dec 1.
 

 2B6 INDUCERS: 

PHENOBARBITAL
Enhanced cyclophosphamide and ifosfamide activation in primary human hepatocyte cultures: Response to cytochrome P-450 inducers and autoinduction by oxazaphosphorines. [ PMID 9157990 ]
Chang TK, Yu L, Maurel P, Waxman DJ
Cancer Res 1997 May 15;57(10):1946-54

PHENYTOIN
Phenytoin-induced alteration in the N-dechloroethylation of ifosfamide stereoisomers. [ PMID 9332469 ]
Ducharme MP, Bernstein ML, Granvil CP, Gehrcke B, Wainer IW
Cancer Res 1997 May 15;40(6):531-3

RIFAMPIN
Enhanced cyclophosphamide and ifosfamide activation in primary human hepatocyte cultures: Response to cytochrome P-450 inducers and autoinduction by oxazaphosphorines. [ PMID 9157990 ]
Chang TK, Yu L, Maurel P, Waxman DJ
Cancer Res 1997 May 15;57(10):1946-54