Drug metabolism

Administration of poly (ADP-ribose) polymerase (PARP) inhibitors after achieving a response to platinum-containing drugs significantly prolonged relapse-free survival compared to placebo administration. PARP inhibitors have been used in clinical practice. However, patients with platinum-resistant relapsed ovarian cancer still have a poor prognosis and there is an unmet need.

11p vielonmusk 21-01-2022 11 2   Download

Biotherapeutics (BTs), one of the fastest growing classes of drug molecules, offer several advantages over the traditional small molecule pharmaceuticals because of their relatively high specificity, low off-target effects, and biocompatible metabolism, in addition to legal and logistic advantages. However, their clinical utility is limited, among other things, by their high immunogenic potential and/or variable therapeutic efficacy in different patient populations.

7p caothientrangnguyen 09-05-2020 22 0   Download

Quantifying the multiple processes which control and modulate the extent of oral bioavailability for drug candidates is critical to accurate projection of human pharmacokinetics (PK). Understanding how gut wall metabolism and hepatic elimination factor into first-pass clearance of drugs has improved enormously. Typically, the cytochrome P450s, uridine 5′- diphosphate-glucuronosyltransferases and sulfotransferases, are the main enzyme classes responsible for drug metabolism. Knowledge of the isoforms functionally expressed within organs of first-pass clearance, their anatomical topology (e.

16p caothientrangnguyen 09-05-2020 18 0   Download

The cytochrome P450 family of enzymes has long been known tometabolize a wide range of compounds, including many of today’s most common drugs. A novel nuclear receptor called PXR has been established as an activator of several of the cytochrome P450 genes, including CYP3A4. This enzyme is believed to account for the metabolism of more than 50% of all prescription drugs. PXR is therefore used as a negative selector target and discriminatory filter in preclinical drug development.

9p research12 29-04-2013 42 3   Download

Glofish is the first transgenic animal approved to be consumed by human in the USA  The insertion of different constructs of GFP into the fish genomes to give different green colors.The idea for recombinant DNA was first proposed by Peter Lobban, a graduate student of Prof. Dale Kaiser in the Biochemistry Department at Stanford University Medical School. The first publications describing the successful production and intracellular replication of recombinant DNA appeared in 1972 and 1973.

54p zingzing09 24-04-2013 77 5   Download

Liver microsomal preparations are routinely used to predict drug interactions that can occurin vivo as a result of inhi-bition of cytochrome P450 (CYP)-mediated metabolism. However, the concentration of free drug (substrate and inhibitor)at its intrahepatic site of action, a variable that cannot be directly measured, may be significantly different from that in microsomal incubation systems.

10p tumor12 20-04-2013 47 4   Download

Malaria remains a major health problem especially in trop-ical and subtropical regions of the world, and therefore developing new antimalarial drugs constitutes an urgent challenge. Lipid metabolism has been attracting a lot of attention as an application for malarial chemotherapeutic purposes in recent years. However, little is known about glycosphingolipid biosynthesis inPlasmodium falciparum. In this report we describe for the first time the presence of an active glucosylceramide synthase in the intraerythrocytic stages of the parasite....

11p dell39 03-04-2013 31 4   Download

Prolonged exposure of pancreatic beta cells to the sulfonylureas glibenca-mide and tolbutamide induces subsequent desensitization to the actions of these drugs. The precise mechanisms underlying this desensitization remain unknown, prompting the present study, which investigated the impact of prolonged sulfonylurea exposure on glucose and energy metabolism using clonal pancreatic BRIN-BD11 beta cells.

9p inspiron33 23-03-2013 42 4   Download

In the search for new drug targets in the human parasite Entamoeba histolytica, metabolic control analysis was applied to determine, experimen-tally, flux control distribution of amebal glycolysis. The first (hexokinase, hexose-6-phosphate isomerase, pyrophosphate-dependent phosphofructo-

16p galaxyss3 07-03-2013 52 4   Download

Branched-chain lipids are important components of the human diet and are used as drug molecules, e.g. ibuprofen. Owing to the presence of methyl groups on their carbon chains, they cannot be metabolized in mitochon-dria, and instead are processed and degraded in peroxisomes. Several dif-ferent oxidative degradation pathways for these lipids are known, including a-oxidation, b-oxidation, and x-oxidation.

14p media19 06-03-2013 39 3   Download

Constitutively expressed human cytochrome P450 2D6 (CYP2D6; EC 1.14.14.1) is responsible for the metabolism of approximately 25% of drugs in common clinical use. It is widely accepted that CYP2D6 is localized in the endoplasmic reticulum of cells; however, we have identified this enzyme in the mitochondria of human liver samples and found that extensive inter-individual variability exists with respect to the level of the mitochondrial enzyme.

14p viettel02 22-02-2013 44 4   Download

The present study aimed to determine the role of Kupffer cells (KCs) in cytochrome P450 (CYP) isozyme activity and the expression of its gene during polymicrobial sepsis. For ablation of KCs, rats were pretreated with gadolinium chloride (GdCl3 ) at 48 and 24 h before cecal ligation and punc-ture (CLP). The depletion of KCs was confirmed by measuring the mRNA level of the KC marker gene CD163.

11p cosis54 05-01-2013 42 4   Download

Tuyển tập các báo cáo nghiên cứu về hóa học được đăng trên tạp chí sinh học quốc tế đề tài : Metabolically stable bradykinin B2 receptor agonists enhance transvascular drug delivery into malignant brain tumors by increasing drug half-life

15p dauphong3 03-01-2012 41 5   Download

Tuyển tập các báo cáo nghiên cứu về y học được đăng trên tạp chí y học Critical Care giúp cho các bạn có thêm kiến thức về ngành y học đề tài: Drug metabolizing enzyme activities versus genetic variances for drug of clinical pharmacogenomic relevance...

9p thulanh17 27-10-2011 38 2   Download

Tuyển tập các báo cáo nghiên cứu về y học được đăng trên tạp chí y học Critical Care giúp cho các bạn có thêm kiến thức về ngành y học đề tài: Clinical review: Drug metabolism and nonrenal clearance in acute kidney injury...

9p coxanh_3 27-10-2011 55 3   Download

Thyroiditis is the inflammation of the thyroid gland. The thyroid gland is located on the front of the neck below the laryngeal prominence, and makes hormones that control metabolism. There are many different types of thyroiditis, with the most common being Hashimoto's thyroiditis. Other forms of the disease are postpartum thyroiditis, subacute thyroiditis, silent thyroiditis, drug-induced thyroiditis, radiation-induced Association, 2008).

4p truongthiuyen2 10-06-2011 90 2   Download

The peptide hormones of the anterior pituitary are essential for the regulation of growth and development, reproduction, responses to stress, and intermediary metabolism. Their synthesis and secretion are controlled by hypothalamic hormones and by hormones from the peripheral endocrine organs. A large number of disease states as well as a diverse group of drugs also affect their secretion.

260p vanass 01-04-2011 100 11   Download

The absorption, distribution, metabolism, and excretion of a drug all involve its passage across cell membranes. Mechanisms by which drugs cross membranes and the physicochemical properties of molecules and membranes that influence this transfer are, therefore, important. The determining characteristics of a drug are its molecular size and shape, degree of ionization, relative lipid solubility of its ionized and nonionized forms, and its binding to tissue proteins.

149p vanass 01-04-2011 71 11   Download

Macrolides and Ketolides Erythromycin, clarithromycin, and telithromycin inhibit CYP3A4, the hepatic P450 enzyme that metabolizes many drugs, including cyclosporine, certain statins (lovastatin, simvastatin), theophylline, carbamazepine, warfarin, certain antineoplastic agents (e.g., vincristine, irinotecan), and ergot alkaloids. In ~10% of patients receiving digoxin, concentrations increase significantly when erythromycin or telithromycin is coadministered, and this increase may lead to digoxin toxicity. Azithromycin has little effect on the metabolism of other drugs. Many drugs (e.g.

9p colgate_colgate 21-12-2010 81 3   Download

Table 81-2 Commonly Used Cancer Chemotherapy Agents Drug Exam ples of Usual Doses Toxicity Issues Interactions, Direct DNA-Interacting Agents Alkylators Cyclophospha 2000 400– mg/m2 Marrow (relative Liver metabolism required mide IV platelet sparing) to activate to phosphoramide 100 mg/m2 PO qd Common alkylatora Mesna protects Cardiac dose) against Cystitis mustard + acrolein (high "high-dose" bladder damage Mechloretha mine 6 mg/m2 IV day Marrow Topical use in cutaneous lymphoma Vesicant 1 and day 8 Nausea Chlorambucil 1–3 mg/m2 qd PO Marrow Common alkylatora ...

28p konheokonmummim 03-12-2010 69 3   Download