CRX.L Regulatory News (CRX)

3rd May 2012

Cyprotex PLC

Cyprotex Strengthens Product Offering

Cyprotex PLC (AIM:CRX), the drug discovery ADME Tox services and information company, today announces the introduction of two new services in pre-clinical ADME Tox.

PXR and AhR Nuclear Receptor Activation Assay

PXR and AhR nuclear receptor activation is key in the regulation of certain drug metabolism pathways. Increase in such metabolism can cause lower plasma levels of co-administered drugs leading to reduced therapeutic effect, or increased metabolite production which may result in toxicity.

Nuclear receptors are unique from other types of receptors in the body in their ability to directly interact with and control the expression of genomic DNA. More specifically, PXR and AhR are two of the most common nuclear receptors involved in the induction of cytochrome P450 drug metabolising enzymes, CYP3A4 and CYP1A2. By identifying compounds that activate these nuclear receptors earlier in the drug discovery process, drug developers can ascertain the consequences of such interactions in a cost effective manner.

Lysosomal Trapping (Lysosomotropism) Service

Lysosomal trapping (lysosomotropism) has been implicated as a mechanism in drug-induced toxicity within lysosome-rich organs within the body. Drugs with particular chemical properties can become trapped within the acidic environment of a compartment within the cell called the lysosome causing high levels to accumulate. Cyprotex's assay provides a robust, sensitive and rapid approach to identify compounds that have a propensity for lysosomal trapping.

Research & Development

Cyprotex continues to invest in the research and development of cutting-edge technologies as well as continually improving the quality of their product offering to provide customers with a growing suite of pre-clinical ADME Tox services.

Dr Katya Tsaioun, Chief Scientific Officer of Cyprotex, said: "Cyprotex is at the forefront of scientific discovery in pre-clinical ADME Tox. Our knowledge of how certain drugs exhibit toxic effects is growing all the time. The latest additions to our growing suite of services further builds on our 'fail early/fail cheaply' approach to drug discovery, which is aimed at saving both time and money for drug developers." 

For further information:

Notes to Editors:

About Nuclear Receptor Activation

The nuclear receptor activation assay is a plate-based luciferase reporter gene system which offers enhanced throughput compared with other common techniques such as measuring catalytic activity and mRNA activity in primary hepatocytes. The service is, therefore, appropriate for evaluating larger numbers of compounds in early drug discovery. Validation data for the new assay correlates well with published data in the literature and the approach is widely used in the pharmaceutical industry.  A survey of current practices and recommendations within the industry (Chu et al., (2009) Drug Metab Dispos 37: 1339) indicated that 64% of the survey participants routinely used nuclear receptor transactivation assays to assess the potential of test compounds to cause enzyme induction.

About Lysosomal Trapping Service

The method at Cyprotex utilises our high content screening (HCS) technology to track a fluorescent dye which readily enters acidic organelles of the cell such as lysosomes. A separate dye simultaneously monitors for general health of the cells. The method is based on a protocol published recently by Pfizer (Nadanaciva et al., 2011), which describes a robust, sensitive and rapid approach for correctly identifying drugs which exhibit a propensity for lysosomal trapping. Data from our assay correlate very well with data generated in the publication.

Cyprotex PLC

Cyprotex is the world's largest contract research organisation (CRO) specialising in ADME Tox, which is the analysis of the Absorption, Distribution, Metabolism, Excretion, and Toxicity properties of potential drugs, cosmetics, and agrochemicals. It is the only company in the world with in-house capabilities for both in vitro (test tube) and in silico (computer modelling) ADME Tox. Cyprotex was founded in 1999 and listed on the AIM in 2002. It has laboratories in Macclesfield, Cheshire, UK (near Manchester), and Watertown, Massachusetts, USA (near Boston), making it one of only three ADME Tox CROs with international operations.