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Table 2. Metabolism and transport of pharmacologic agents used in BPH and prostate cancer

Drug   Enzyme/Transporter Implicated   References   Antiandrogens           Bicalutamide   Inhibits CYP3A4   Cockshott, 2004       Flutamide   Metabolized by CYP1A and CYP3A   Berson et al, 1993; Shet et al, 1997     Inhibits CYP1B1   Rochat et al, 2001   5-reductase inhibitors           Dutasteride   Metabolized by CYP3A4   Andriole and Kirby, 2003       Finasteridex   Metabolized by CYP3A4   Huskey et al, 1995     Induces GST-   Montironi et al, 1999   -adrenergic antagonists           Doxazosin   Transported by MDR1   Takara et al, 2002       Indoramin   Metabolized by CYP (unspecified); sulfonation   Pierce, 1990       Prazosin   Inhibitor of hOCT1 and hOCT3   Hayer-Zillgen et al, 2002     Transported by BCRP   Ozvegy et al, 2001       Tamsulosin   Metabolized by CYP3A4 and CYP2D6   Kamimura et al, 1998   Miscellaneous cytotoxic agents           Cyclophosphamide   Activation by CYP2Cs   Chang et al, 1997     Metabolized by CYP3A4   Huang et al, 2000; Murray et al, 1994       Dacarbazine   Activation by CYP1A; CYP2E at higher concentrations   Long and Dolan, 2001; Reid et al, 1999       Docetaxel   Metabolized by CYP3A4 and CYP3A5   Cresteil et al, 2002; Shou et al, 1998       Doxazosin   Transported by MDR1   Takara et al, 2002       Etoposide   Metabolized by CYP3A4   Relling et al, 1994; Kawashiro et al, 1998     Transported by P-gp   Shapiro and Ling, 1998       Flavopiridol   Transported by ABCG2   Doyle and Ross, 2003     Metabolized by UGT1A1, UGT1A9, UGT1A10   Hagenauer et al, 2001       Ifosfamide   Activation by CYP2Cs   Chang et al, 1997     Metabolized by CYP3A4   Huang et al, 2000; Murray et al, 1994     Metabolized by CYP2B6   Huang et al, 2000       JM216   Inhibited CYP2C8 and CYP3A4   Ando et al, 1998       Lilopristone   Metabolized by CYP3A4   Jang and Benet, 1997       Methotrexate   Transported by MRP1-4   Chen et al, 2003     Transported by ABCG2(BCRP)   Chen et al, 2003; Doyle and Ross, 2003       Mifepristone   Metabolized by CYP3A4   Heikinheimo, 1997; Jang et al, 1996     Metabolized by CYP3A4 and CYP3A5   Khan et al, 2002       Mitoxantrone   Transported by ABCG2(BCRP)   Cooray et al, 2004; Doyle and Ross, 2003       Navelbine   Inhibits CYP3A4   Zhou et al, 1993       Onapristone   Metabolized by CYP3A4   Jang and Benet, 1997       Paclitaxel   Metabolized by CYP3A4 and CYP2C8   Cresteil et al, 2002       Tamoxifen   -hydroxylation by CYP3A4   Boocock et al, 2002     4-hydroxylation by CYP2D6 and CYP2B6 at high substrate concentrations   Boocock et al, 2002; Crewe et al, 2002     N-demethylation by CYP2D6, CYP1A1, CYP3A4   Crewe et al, 2002     Trans-cis isomerization by CYP1B1   Crewe et al, 2002

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