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Human Microdosing Greater Than 80% Predictive in 25 Tested Molecules

Human Microdosing Greater Than 80% Predictive in 25 Tested Molecules
Latest microdose data from 7 new compounds to be showcased at EUMAPP Conference June 16th in Germany

York, UK and Germantown, MD USA – May 29, 2008 – Xceleron, the global leader in predictive clinical research to enable smarter, safer drug development decisions, announced today microdose data for 25 clinical candidates proved more than 80% predictive of pharmacokinetics (PK) compared to pharmacological dose.  Latest microdose data from 7 new compounds will be presented as part of the June 16, 2008 European Federation of Pharmaceutical Sciences (EUFEPS) Conference in Bad Homburg, Germany.

“Microdosing is gaining acceptance as it is a new and more precise method for evaluating a drug candidate’s profile earlier than traditional practices,” said Dr. Colin Garner, CEO of Xceleron. “With 1 out-of-every 5,000 compounds making it from bench to bedside, the intrinsic value of microdosing is that it enables companies to select and advance only those compounds to clinical trials which demonstrate optimal drug profiles predictive of success.”

Of the 25 molecules reported, 19 are in the public domain and 6 remain proprietary compounds.  All compounds are small molecules, exhibiting different ADME properties and cover a variety of therapeutic areas including anti-infectives, CNS, oncology, anti-coagulant, cardio-respiratory, hypertension and analgesia. 
“The completion of 25 molecules is an important milestone,” said Dr. Garner.  “Establishing a data library which consistently demonstrates the predictive value of microdosing aids in building greater market acceptance of this approach.”

Consistent with the FDA’s Critical Path Initiative, it is believed that human microdosing offers a faster, more accurate method of developing drugs -- bridging the gap between the laboratory and the clinic.

In January 2006, Xceleron was asked to lead the European Union Microdose AMS Partnership Programme (EUMAPP) consortium and establish a path to faster, more efficient drug development.  The results of the 30-month, €2 million project will be presented by ten organizations from five different countries (United Kingdom, Sweden, Netherlands, France and Poland) at the EUMAPP Workshop on June 16, 2008 in Germany.  The results of the EUMAPP Project will also be put into a wider context, comparing the reliability, accuracy and predictive value of microdose studies to the classic drug development model.

“Past studies suggest that in vivo animal models are not necessarily reliable predictors of drug absorption and elimination in humans and we have found human microdosing data to be more than 80% predictive,” said Dr. Garner.  “The benefits of microdosing in terms of cost savings, improved candidate selection, pipeline productivity, and risk mitigation are significant.”

In April 2008, Professor Malcolm Rowland, Chairman of Xceleron’s Scientific Advisory Board, presented information on Fexofenadine, one of the seven drugs tested in the EUMAPP study, at the American Society for Clinical Pharmacology and Therapeutics Conference in Orlando, Florida.  The findings established linear pharmacokinetics (PK) between a microdose of Fexofenadine and its therapeutic dose.  Additionally, prior to the EUMAPP study, it had not been possible to administer Fexofenadine intravenously. The absolute bioavailability was previously estimated to be 11% based on unchanged drug in urine, however the IV microdose showed the oral absolute bioavailability to be 33% implying a higher degree of biliary excretion than originally thought.

During the EUMAPP conference, Professor Rowland will expand on this evidentiary research, as well as be joined by other experts to provide findings on six other molecules.  The presentation of these data is expected to continue the process of discovery with regard to the validity and value of microdosing as an alternative to traditional compound evaluation through animal models.

For more details on the EUMAPP Workshop please visit: http://www.eufeps.org/. 

Xceleron will present preliminary details of the EUMAPP data at the upcoming Biotechnology Industry Organization’s International Conference and Exhibition in San Diego, California the week of June 17th. 

-END-

Notes to Editors:
An article in Drug Discovery Today, Vol. 6, No. 12 (Supplement) 2001 entitled
“Effects of diverse datasets on the predictive capability of ADME models in drug discovery” concluded that animal models can be unreliable measures of drug behavior in humans as there as there is often no apparent relationship between bioavailability in humans and animals.  The article further notes that traditional development models tested drug viability sequentially:  first oral absorption; then metabolism; then distribution; then elimination.  Microdosing allows these drug profile attributes to be tested simultaneously in one study. 

According to a recent study conducted at Oxford University’s Saïd Business School, “the value created [by Microdosing] is substantial and originates from reduced development time and improved clinical success rates for compounds using a microdose protocol.”

Microdosing enables researchers to determine factors like PK properties of a compound including oral absorption, rate of metabolism, and excretion characteristics at the earliest point possible in the drug development cycle. The data from EUMAPP’s seven molecules is expected to strengthen support by:

o Demonstrating the value of microdosing for predicting PK at pharmacological doses;
o Certifying Accelerator Mass Spectrometry (AMS) as the most accurate, appropriate and powerful technology for reproducible measurements required by microdosing studies;
o Developing in silico modelling application to predict PK parameters from data derived from microdosing studies.

About Xceleron
Leveraging its proprietary methods and ultra-sensitive technology platform, Xceleron delivers the earliest possible, most relevant human insights to its clients enabling smarter and safer drug development decision-making in terms of productivity, pipeline value and profit.  Xceleron maintains ongoing client engagements with 15 of the 20 largest pharmaceutical companies in the world and analyzed more than 200 molecules to date.  For more information, log on to www.xceleron.com 
About EUMAPP
EUMAPP is the European Union Microdose AMS Partnership Programme, coordinated by Xceleron Ltd., York UK, and funded by the European Commission. It comprises 10 organisations from 5 different countries (United Kingdom, Sweden, The Netherlands, France and Poland). The aim is to evaluate microdosing for drug development and to arrive at recommendations about how and when it could and should be used.
About EUFEPS
EUFEPS is the European Federation for Pharmaceutical Sciences, the mission of which is to advance excellence in the pharmaceutical sciences and innovative drug research and to represent the interests of scientists engaged in drug research and development, drug regulation and drug policymaking. Currently, it links scientific societies and associations in 24 European Countries, and 10+ member institutions. There are around 600 individual members, and EUFEPS Networks are growing in numbers.

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