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Atorvastatin Treatment Induces Uptake and Efflux Transporters in Human Liver [Short Communications] 13 Aug 2013 | 07:40 pm
The metabolism and disposition of statins are highly dependent on different cytochrome P450 enzymes, such as CYP3A4 and CYP2C9, as well as membrane transporters SLCO1B1, SLCO2B1, ABCB1, and ABCG2. Int...
The Human UDP-Glucuronosyltransferase UGT2A1 and UGT2A2 Enzymes Are Highly Active in Bile Acid Glucuronidation [Short Communications] 13 Aug 2013 | 07:40 pm
Bile acids (BA) are essential modulators of lipid, glucose, and cholesterol homeostasis, but they exert cytotoxic effects in the cholestatic liver. Glucuronidation, catalyzed by the UDP-glucuronosyltr...
Characterization of Microsomal Glutathione S-Transferases MGST1, MGST2, and MGST3 in Cynomolgus Macaque [Short Communications] 13 Aug 2013 | 07:40 pm
The glutathione S-transferase (GST) family comprises cytosolic, mitochondrial, and microsomal GSTs, all essential enzymes that metabolize a wide range of endogenous and exogenous substrates. Among the...
Metabolism and Disposition of the Metabotropic Glutamate Receptor 5 Antagonist (mGluR5) Mavoglurant (AFQ056) in Healthy Subjects [Articles] 13 Aug 2013 | 07:40 pm
The disposition and biotransformation of 14C-radiolabeled mavoglurant were investigated in four healthy male subjects after a single oral dose of 200 mg. Blood, plasma, urine, and feces collected over...
Downregulation of Sulfotransferase Expression and Activity in Diseased Human Livers [Articles] 13 Aug 2013 | 07:40 pm
Sulfotransferase (SULT) function has been well studied in healthy human subjects by quantifying mRNA and protein expression and determining enzyme activity with probe substrates. However, it is not we...
The Relative Contributions of CYP3A4 and CYP3A5 to the Metabolism of Vinorelbine [Articles] 13 Aug 2013 | 07:40 pm
Vinorelbine is a semisynthetic vinca alkaloid used in the treatment of advanced breast and non-small cell lung cancers. Vincristine, a related vinca alkaloid, is 9-fold more efficiently metabolized by...
A Systematic Approach to Evaluate Herb-Drug Interaction Mechanisms: Investigation of Milk Thistle Extracts and Eight Isolated Constituents as CYP3A In... 13 Aug 2013 | 07:40 pm
Despite increasing recognition of potential untoward interactions between herbal products and conventional medications, a standard system for prospective assessment of these interactions remains elusi...
Formation of Threohydrobupropion from Bupropion Is Dependent on 11{beta}-Hydroxysteroid Dehydrogenase 1 [Articles] 13 Aug 2013 | 07:40 pm
Bupropion is widely used for treatment of depression and as a smoking-cessation drug. Despite more than 20 years of therapeutic use, its metabolism is not fully understood. While CYP2B6 is known to fo...
An Assessment of Pharmacokinetics and Antioxidant Activity of Free Silymarin Flavonolignans in Healthy Volunteers: A Dose Escalation Study [Articles] 13 Aug 2013 | 07:40 pm
Milk thistle (Silybum marianum) extracts, one of the most widely used dietary supplements, contain a mixture of six major flavonolignans (silybin A, silybin B, isosilybin A, isosilybin B, silychristin...
The Role of Human Cytochrome P450 Enzymes in the Formation of 2-Hydroxymetronidazole: CYP2A6 is the High Affinity (Low Km) Catalyst [Articles] 13 Aug 2013 | 07:40 pm
Despite metronidazole’s widespread clinical use since the 1960s, the specific enzymes involved in its biotransformation have not been previously identified. Hence, in vitro studies were conducted to i...
