▪ Abstract Cytochrome P4503A (CYP3A) is importantly involved in the metabolism of many
chemically diverse drugs administered to humans. Moreover, its localization in high amounts …

The human CYP3A subfamily plays a dominant role in the metabolic elimination of more
drugs than any other biotransformation enzyme. CYP3A enzyme is localized in the liver and …

… M where V max =k 2 ·E t and K M = k 1 k −1 +k 2 Despite a generally complex molecular
mechanism for most enzyme-catalyzed drug metabolism processes, the rate of product …

Background The management of warfarin therapy is complicated by a wide variation among
patients in drug response. Variants in the gene encoding vitamin K epoxide reductase …

… m for each intestinal region was similar to the median hepatic K m , ∼4 μM. In contrast, the
… Intrinsic clearance (V max /K m ) followed a similar trend for the intestinal regions; median …

… It also appears that the systemic clearance of midazolam exhibits little variability within a
subject over a period similar to that of this study (Thummel KE and Kharasch ED, unpublished …

Tacrolimus is the mainstay immunosuppressant drug used after solid organ and hematopoietic
stem cell transplantation. Individuals who express CYP3A5 (extensive and intermediate …

… (K,) for fentanyl (a CYP3A4 substrate) is not known, the related opioid alfentanil exhibits a
K, … (10 to 20 nmol/L) than the expected K,; thus no competitive interaction with midazolam is …

… would either remain unaffected by the addition of the alternatively labeled substrate or be
inhibited if the concentration of the alternative substrate approached the enzyme K,,, for car…

We recently demonstrated that a variant allele of CYP3A5(CYP3A5*3) confers low CYP3A5
expression as a result of improper mRNA splicing. In this study, we further evaluated the …