Current Drug Metabolism - Volume 11, Issue 6, 2010

Positron emission tomography (PET) is a very sensitive molecular imaging technique that when employed with an appropriate radioligand has the ability to quantititate physiological processes in a non-invasive manner. Since the imaging technique detects all radioactive emissions in the field of view, the presence and biological activity of radiolabeled metabolites must be determined for each radioligand in order to validate the u Read More

Dihydrocodeine (DHC) is a semi-synthetic analogue of codeine which was formed by the hydrogenation of the double tie in the main chain of the codeine molecule. DHC is used as an analgesic, antitussive and antidiarrhoeal agent; it is also used for the treatment of opioid addiction. Limited data is available on the relative potency of DHC to other opioids. The analgesic effect of DHC is probably twice as potent as codeine for t Read More

Cisplatin is one of the commonly-used chemotherapeutic drugs to efficiently treat malignant tumors in clinic, however, the adverse effects of cisplatin such as nephrotoxicity, neurotoxcity, and hemolytic uremic syndrome are often observed at its clinical doses (~60 mg/m2), which limit its broader application. In earlier studies, little attention was paid to the subtle changes in the architecture of lymphatic organs after low do Read More

Background: The metabolic/biotransformation pathways of atypical antipsychotics (aripiprazole, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, and ziprasidone) have been characterized and reviewed. However, comparisons of excretory pathways remain unexplored. Objective: To analyze the excretion profile of atypical antipsychotic agents and compare the overall magnitude of metabolism (changed Read More

An understanding of dose proportionality is essential in drug development, and the results are of great clinical importance for predicting the effects of dose adjustments. However, little consensus exists with regard to study design and analysis. The aim of this paper was to produce a detailed profile of the information on dose proportionality studies in the last 10 years and to provide a foundation for reflection and debate on fut Read More

Cytosolic sulfotransferases (SULTs) are traditionally known as the Phase II drug-metabolizing or detoxifying enzymes that serve for the detoxification of drugs and other xenobiotics. These enzymes in general catalyze the transfer of a sulfonate group from the active sulfate, 3'-phophoadenosine 5'-phosphosulfate (PAPS), to low-molecular weight substrate compounds containing hydroxyl or amino group(s). Despite considerable eff Read More

Chirality is a ubiquitous feature present in all biological systems that plays a very important role in many processes. Drug metabolism is one of these and is the subject of this review. Chiral drugs can be metabolized without changes in their chiral characteristics, but also their biotransformation may give rise to a new chiral center. On the other hand, prochiral drugs are always metabolized to chiral metabolites. Read More

This addendum was compiled by the authors to clarify some points presented in the review article titled “Expression, Function and Regulation of Mouse Cytochrome P450 Enzymes: Comparison With Human Cytochrome P450 Enzymes”, which appeared in Current Drug Metabolism (2009) 10 (10), 1151-1183. Table 1 lists Cyp2c22, Cyp2c23, Cyp2c51 and Cyp2b20 as mouse P450 genes. Mouse Cyp2c22 and Cyp2c23 genes (ref. Read More