Single centered crossover, two cycles volunteer study was performed on 12 healthy male volunteers. Both reference and test, immediate release nimesulide formulation was given in a randomized manner with a washout period of 15 days and 5 mL of blood s...
Alcoholism, clinical and experimental research
29689131
BACKGROUND: A statistical pipeline was developed and used for determining candidate genes and candidate gene coexpression networks involved in 2 alcohol (i.e., ethanol [EtOH]) metabolism phenotypes, namely alcohol clearance and acetate area under the...
A key consideration at the screening stages of drug discovery is in vitro metabolic stability, often measured in human liver microsomes. Computational prediction models can be built using a large quantity of experimental data available from public da...
Lower clearance of immune checkpoint inhibitors is a predictor of improved overall survival (OS) in patients with advanced cancer. We investigated a novel approach using machine learning to identify a baseline composite cytokine signature via clearan...
The in vitro-in vivo extrapolation (IVIVE) approach for predicting total plasma clearance (CL) has been widely used to rank order compounds early in discovery. More recently, a computational machine learning approach utilizing physicochemical descrip...
Journal of clinical pharmacy and therapeutics
33201513
WHAT IS KNOWN AND OBJECTIVE: Febuxostat is a well-known drug for treating hyperuricemia and gout. The published methods for determination of febuxostat in human plasma might be unsuitable for high-throughput determination and widespread application. ...
Measurement of stimulus-induced dopamine release and other types of transient neurotransmitter response (TNR) from dynamic positron emission tomography (PET) images typically suffers from limited detection sensitivity and high false positive (FP) rat...
Research into pharmacokinetics plays an important role in the development process of new drugs. Accurately predicting human pharmacokinetic parameters from preclinical data can increase the success rate of clinical trials. Since clearance (CL) which ...
We constructed machine learning-based pharmacokinetic prediction models with very high performance. The models were trained on 26138 and 16613 compounds involved in metabolic stability and cytochrome P450 inhibition, respectively. Because the compoun...
Animal pharmacokinetic (PK) data as well as human and animal in vitro systems are utilized in drug discovery to define the rate and route of drug elimination. Accurate prediction and mechanistic understanding of drug clearance and disposition in anim...