A5002542670- Pharmacogenetics and Drug Metabolism
- Computational Drug Discovery Methods
- Drug Transport and Resistance Mechanisms
- Analytical Chemistry and Chromatography
- Pharmaceutical studies and practices
- Drug-Induced Hepatotoxicity and Protection
- Metabolomics and Mass Spectrometry Studies
- Pharmacological Effects and Toxicity Studies
- Receptor Mechanisms and Signaling
- Pharmaceutical Economics and Policy
- Antibiotics Pharmacokinetics and Efficacy
- Synthesis of Organic Compounds
- Analytical Methods in Pharmaceuticals
- Crystallization and Solubility Studies
- Sensor Technology and Measurement Systems
- Biotechnology and Related Fields
- Drug Solubulity and Delivery Systems
- Cancer Treatment and Pharmacology
- X-ray Diffraction in Crystallography
- Health Systems, Economic Evaluations, Quality of Life
- Eicosanoids and Hypertension Pharmacology
- Statistical Methods in Clinical Trials
- Chemical Synthesis and Analysis
- Oxidative Organic Chemistry Reactions
- Biosimilars and Bioanalytical Methods
Oldham Council
2024
Independent Age
2024
TGS (United Kingdom)
2024
Roche (Ireland)
2023
Ollscoil na Gaillimhe – University of Galway
2018-2021
Pfizer (United States)
2001-2019
University of Cape Town
2012-2019
University of Manchester
2019
King's College London
2019
University of Cambridge
2019
Volume of distribution is one the most important pharmacokinetic properties a drug candidate. It major determinant half-life and dosing frequency drug. For similar log P, basic molecule will tend to exhibit higher volume than neutral molecule. Acids often low volumes distribution. Although design strategy against can be advantageous in achieving desirable regimen, it must well-directed order avoid detrimental effects other properties. Strategies increase include adding lipophilicity...
Voriconazole is a triazole antifungal agent with potent activity against broad spectrum of clinically significant pathogens. In vivo and in vitro studies have demonstrated that voriconazole extensively metabolized, the major circulating metabolite resulting from<i>N-</i>oxidation. present study, we report on human cytochrome P450 enzymes responsible for generation this metabolite. liver microsomes voriconazole<i>N</i>-oxidation exhibited biphasic kinetics with<i>K</i><sub>m1</sub> 8.1 μM,...
Voriconazole is a new triazole antifungal agent with potent, wide-spectrum activity. Its pharmacokinetics and metabolism have been studied in mouse, rat, rabbit, dog, guinea pig, humans after single multiple administration by both oral intravenous routes. Absorption of voriconazole essentially complete all species. The elimination characterized non-linear Consequently, pharmacokinetic parameters are dependent upon dose, superproportional increase area under the curve seen increasing dose rat...
An early understanding of key metabolites drugs is crucial in drug discovery and development. As a result, several vitro models typically derived from liver are frequently used to study metabolism. It presumed that these systems provide an accurate view the potential vivo metabolic pathways. However, no formal analysis has been conducted validate their use. The goal present was conduct comprehensive assess if three commonly systems, pooled human microsomes, S-9 fraction, hepatocytes,...
Drug half-life has important implications for dosing regimen and peak-to-trough ratio at the steady state. A of 12-48 h is generally ideal once daily oral drugs. If too short, it may require more frequent in order to maintain desired exposures avoid unnecessarily high peak concentrations. This pose challenges achieving optimal efficacy, safety, patient compliance. long, time over which accumulation subsequent elimination occur be prolonged. problems with managing adverse effects design...
The 2-aminopyridine MMV048 was the first drug candidate inhibiting Plasmodium phosphatidylinositol 4-kinase (PI4K), a novel target for malaria, to enter clinical development. In an effort identify next generation of PI4K inhibitors, series optimized improve properties such as solubility and antiplasmodial potency across parasite life cycle, leading 2-aminopyrazine UCT943.
Abstract Background Modelling and simulation are being increasingly utilized to support the discovery development of new anti-malarial drugs. These approaches require reliable in vitro data for physicochemical properties, permeability, binding, intrinsic clearance cytochrome P450 inhibition. This work was conducted generate an toolbox using standardized methods a set 45 drugs assess changes properties relation changing target product candidate profiles. Methods Ionization constants were...
To characterize the cytochrome P450 (CYP) enzymes responsible for N-demethylation of sildenafil to its main metabolite, UK-103 320, investigate potential inhibitory effects on CYP and evaluate selected drugs affect metabolism.The metabolic pathways were studied using human liver microsomes, as well microsomes expressing individual enzymes. Further studies identify performed at 2.5 250 microM sildenafil, employed a combination chemical inhibition, correlation analysis, metabolism by expressed...
UK-427,857 (4, 4-difluoro-<i>N</i>-{(1<i>S</i>)-3-[<i>exo</i>-3-(3-isopropyl-5-methyl-4<i>H</i>-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]oct-8-yl]-1-phenylpropyl}cyclohexanecarboxamide) is a novel CCR5 antagonist undergoing investigation for use in the treatment of human immunodeficiency virus (HIV) infection. Pharmacokinetic and metabolism studies have been performed mouse, rat, dog, after single multiple administration by oral intravenous routes. The compound has physicochemical properties...