TABLE 3

Fractions of the drugs cleared by CYP3A4 (fm, CYP3A4) estimated by fi, CYP3A4 from clinical DDIs associated with CYP3A4 inhibition (eq. 18)

Substrate
fm a
Reference
Substrate
fm
Reference
Alfentanilb 871 Kharasch et al., 2005 Midazolam 89 Chen et al., 2006
Alprazolam 69 Greenblatt et al., 1998 Nifedipine 634 Kremens et al., 1999
Amprenavir 22 Polk et al., 1999 Omeprazole 37 He et al., 2003
Antipyrine 25 D'Mello et al., 1985 Pravastatinb 526 Jacobson, 2004
Atorvastatin 605 Mazzu et al., 2000 Prednisoloneb 27 Zurcher and Frey, 1989
Budesonide 765 Raaska et al., 2002 Quetiapine 84 Grimm et al., 2006
Buspirone 93-955 Kivistö et al., 1997 Quinidine 615 Damkier et al., 1999
Cyclophosphamideb 434 Yule et al., 1999 Quinine 461 Wanwimolruk et al., 2002
Cyclosporine 79 Gomez et al., 1995 Repaglinideb 306 Niemi et al., 2001
Diazepam 245 Ahonen et al., 1996 Ritonavir 23 Khaliq et al., 2000
Ethinyl estradiol 194 Hilbert et al., 2001 Ropivacaine 55 Jokinen et al., 2001a
Etizolam 355 Araki et al., 2004 Saquinavir 66 Grub et al., 2001
Everolimus 778 Kovarik et al., 2005 Sildenafilb 667 Muirhead et al., 2000
Gefitinib 445 Swaisland et al., 2005 Simvastatin 915 Neuvonen et al., 1998
Glyburide 256 Lilja et al., 2007 Tacrolimus 58 Tuteja et al., 2001
Imatinib 29 Dutreix et al., 2004 Tirilazadb 41 Fleishaker et al., 1996
Indinavir 67-902 Hsu et al., 1998 Triazolam 91 Greenblatt et al., 1998
Losartan 21 Kaukonen et al., 1998 Verapamil 309 Fuhr et al., 2002
Methadone
254
Cobb et al., 1998
Zolpidem
262
Greenblatt et al., 2000

  • ↵ a fm, CYP3A4 values were calculated (eq. 18) by decreased oral clearance (or systemic clearance) or increased AUC of the drugs in the presence of ketoconazole or other individual CYP3A4 inhibitors (fi, CYP3A4) as denoted by 1troleandomycin, 2ritonavir, 3mibefradil, 4fluconazole, 5itraconazole, 6clarithromycin, 7saquinavir, 8erythromycin, and 9grapefruit juice.

  • ↵ b Drugs were given i.v.