Trazpiroben (TAK-906), a peripherally selective dopamine D2/D3 receptor antagonist, is being developed for the treatment of patients with gastroparesis. The potential trazpiroben to act as perpetrator or victim cytochrome P450 (CYP)- transporter- mediated drug–drug interactions (DDIs) was evaluated following latest regulatory guidelines.In vitro studies revealed that metabolised mainly through ...

Delamanid is a new drug for the treatment of multidrug-resistant tuberculosis. Individuals who are co-infected with human immunodeficiency virus and Mycobacterium tuberculosis may require treatment with a number of medications that might interact significantly with the CYP enzyme system as inhibitors or inducers. It is therefore important to understand how drugs in development for the treatment...

We investigated the effect of a novel synthetic analogue of a constituent from the Chinese medicinal herb Isodon excisus, 3-(3-methoxy-phenyl)-N-(3, 4, 5-trimethoxy-phenyl)-acrylamide (compound 343), on the carcinogen activation pathway mediated by the aryl hydrocarbon receptor (AhR) in human hepatoma HepG2 cells. We found that compound 343 inhibited the upregulation of cytochrome P-450 (CYP) e...

In arthropods, periodic molting plays an important role in the growth, reproduction and morphogenesis. Periodic ecdysis is affected by a variety of environmental own factors, most which controlled concentration steroid hormones, ecdysone (Ecd) whose mainly active form 20-hydroxyecdysone(20E) hormone. Moreover, ecdysteroids play roles regulating development reproduction, CYP302al key enzyme bios...

PURPOSE Preclinical studies suggested that green tea or green tea catechins can modulate the activities of drug-metabolizing enzymes. We conducted this clinical study to determine the effect of repeated green tea catechin administration on human cytochrome P450 (CYP) enzyme activities. METHODS Forty-two healthy volunteers underwent a 4-week washout period by refraining from tea or tea-related...

Cytochrome P450 (CYP) enzymes catalyze the generation of reactive species capable of binding with cellular macromolecules, leading to acute and delayed toxicity. Since individual CYP forms differ markedly in their substrate preferences and regulation, the expression profiles of CYP in various cell types are important determinants in tissue-specific toxicity. The highest concentrations of most f...

Aristolochic acid (AA), a naturally occurring nephrotoxin and carcinogen, has been found to be implicated in an unique type of renal fibrosis, designated Chinese herbs nephropathy (CHN), and associated with the development of urothelial cancer in CHN patients. Understanding, which enzymes are involved in AA activation and/or detoxication is important in the assessment of individual susceptibili...

Introduction The cytochromes P450 (CYP) are oxidative enzymes involved in multiple biochemical pathways, including drug metabolism and clearance of toxicants from the body [1]. Certain drugs or chemicals can inhibit CYP enzyme function, which alters their ability to metabolize drugs. The resulting toxic effects are referred to as drug-drug interactions and are a major concern for drug developme...

In insects molting and metamorphosis are primarily under the control of two insect hormones, ecdysone and juvenile hormone (JH). Physiological and biochemical studies of insect hormone metabolic pathways suggested the involvement of P450 (CYP) enzymes in the pathways, but molecular details of the enzymes were unclear. In recent years, the genome information and studies using molecular biology a...

Oltipraz (OPZ) is currently being considered for human use to protect against aflatoxin B, (AFB)-induced hepatocarcinogenesis based on its proven protective effect in rats. The effectiveness of this treatment pre sumes that orthologous cytochrome P450 and glutathione S-transferase (GST) isozymes metabolize AFB in humans as they do in rats. In this study, alterations in the expression of multipl...