Cyprotex Extends Cloe(R) Screen Mechanism-Based Inhibition Service to Include 4 Additional Cytochrome P450 Isoforms



    MANCHESTER, England, March 29 /CNW/ - Today, (29th March), Cyprotex
announces that it has enhanced its Cloe(R) Screen Mechanism-Based Inhibition
service to include 4 additional cytochrome P450 (CYP450) isoforms. These new
assays compliment the CYP3A4 isoform assay which was launched last year, and
provide information on 5 of the major CYP450 isoforms which are of interest in
drug discovery.
    The inhibition of human CYP450s is one of the most common mechanisms that
can lead to drug-drug interactions. Metabolic drug-drug interactions,
following the co-administration of drugs, can result in either reduced
efficacy or increased toxicity. In early drug discovery it is critical to
select candidates with a minimum potential of inhibition of CYP450 in order to
avoid late stage issues or failures. The consequences of mechanism-based
CYP450 inhibition are considered to be more serious than reversible inhibition
because the inactivated enzyme must be re-synthesised before activity is
restored.
    Within the Pharmaceutical Industry, the importance of identifying
compounds which are mechanism-based inhibitors at an early stage of drug
discovery is now being recognised. This has been further intensified by the
release of the draft FDA regulatory guidelines on drug interactions which
recommend that mechanism-based inhibition is investigated using in vitro
screening protocols. The assays have been designed using probe substrates
which are advocated by the draft FDA guidelines.
    Dr. Darwin Cheney, Cyprotex's Chief Scientific Officer, comments on the
launch of this new service. "We have developed these additional
mechanism-based inhibition assays in response to both customer demand and
regulatory guidelines. The prevalence and clinical implications of
mechanism-based CYP450 inhibition has placed greater emphasis on the early
detection of compounds with this potential."

    Cyprotex is a specialist provider of ADME data and pharmacokinetic
predictive services. Our unique Cloe(R) Screen technology which couples robust
protocols with state-of-the-art automation enables Cyprotex to offer an
unrivalled combination of high quality, cost effective data with rapid
turnaround. By using the Cloe(R) Screen mechanism-based inhibition assays in
conjunction with our existing Cloe(R) Screen CYP450 inhibition assays, it is
possible to investigate both reversible and irreversible inhibition. Used in
combination, these assays act as valuable tools in identifying potential
drug-drug interactions.




For further information:

For further information: Cyprotex PLC, Francesca Sadler, Marketing
Manager, Tel: +44-1625-505-100, f.sadler@cyprotex.com, www.cyprotex.com

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