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

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

March 29, 2007

    MANCHESTER, England, March 29 /Xinhua-PRNewswire/ --
Today, 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 complement 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 more information, please contact:

     Francesca Sadler
     Marketing Manager
     Cyprotex Discovery Ltd
     Tel:   [phone]
     Email: [e-mail]