Posters

The FDA guidance for industry states impurities under the ICH threshold may be exaluated for genotoxicity and carcinogenicity. This study uses an expert system to detect mutagens and compounds labeled as potent carcinogens by the FDA.

This poster outlines development of a novel screening method that is suitable for both the detection of known and unknown ED drugs and analogues. Comprehensive spectral data is collected and automatically compared to a prepared library if known drugs.

Recent studies have shown that an increasing number of drugs no longer on the market have negative effects on mitochondrial function in key organs such as the liver and heart. Therefore it is increasingly important to monitor the effects of lead compounds on mitochondrial function in relevant cell systems. The ability to incorporate a simple, rapid, multiplexed, predictive assay can make the detection of potential toxic effects easier to perform early on in the drug discovery process.

The Androgen Receptor (AR) is a member of the family of nuclear receptors responsive to steroid hormones. This poster aims to devise, validate and perform a preliminary automated HTS screening campaign to identify novel modulators of AR activity.

TNFa blocker biopharmaceuticals represent an important and successful class of protein drugs used in the treatment of several autoimmune diseases. Bioassays are indispensible tools in biopharmaceutical drug development and commercialization that are used to quantify biological activity and stability of drugs or drug candidates. The automation of these assays can serve to create an accurate, robust process which can allow the researcher to perform other more important functions.

Epigenetic processes are attracting considerable attention in drug discovery as their fundamental roles in controlling normal cell development and contributions to disease states become more clearly defined. This work combines a fluorescence-based assay with liquid handling and dispensing instrumentation and a multi-mode reader which can be used to monitor the biological activity of the histone methyltransferase (HMT) G9a, a model system.

Sotalol is a non specific adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmia. Its absorption, distribution and systemic PK or, collectively, ‘disposition’ was modeled and simulated using GastroPlus™ v7.0. Biopharmaceutical properties were obtained from in silico predictions and in vitro measurements.

Modeling hERG inhibition has gained significant popularity since 2005, when the FDA recognized the correlation between hERG inhibition and a prolonged QT interval by issuing guidance for the evaluation of new non-antiarrythmic drugs against the hERG channel.Long QT syndrome or LQTS is a risk factor for ventricular tachyarrhythmias and sudden death.

Hepatic first-pass metabolism of many drugs and pro drugs plays a key role in their oral bioavailability. The human cytochrome P450 enzymes are responsible for the metabolism of most drugs. Knowledge of likely sites of metabolic attack in a drug molecule can aid in designing out unwanted metabolic liabilities early on in the drug discovery process, as well as in the design of pro drugs where metabolic transformation is desired.