Potential First-in-Class Compound, Reveals New Approach to the Treatment of Pain (D3)

The preclinical study by the Drug Discovery and Development (D3) unit of the Italian Institute of Technology and the University of California, Irvine, showed that URB937, a potent, second-generation inhibitor of the enzyme fatty acid amide hydrolase (FAAH), controlled pain and inflammation locally at site by boosting levels of anandamide in peripheral tissues, part of the analgesic and anti-inflammatory endocannabinoid system. The compound is the first FAAH inhibitor produced with restricted access to the central nervous system (CNS), whereas current FAAH inhibitors readily cross the blood-brain barrier.1

Dr Daniele Piomelli, Scientific Director of D3, and lead investigator said: "These findings are significant because they show for the first time how FAAH inhibitors may enable the body to harness its own analgesic and anti-inflammatory powers right where the pain relief is needed and avoid side effects often seen in other painkillers. This has great potential to give patients more treatment options to relieve a wide spectrum of pain, such as rheumatoid arthritis and peripheral neuropathic pain."

By circumventing the CNS, the compound may have numerous therapeutic advantages over current pain treatments such as opiates and non-steroidal anti-inflammatory drugs (NSAIDs) that can cause unwanted side effects in some patients such as nausea, bowel irritation and dependency.2,3

Andrew Rice, Professor of Pain Research at Imperial College London, said: "This paper represents an important advance in the development of clinically useful cannabinoids. The existing laboratory and clinical data unequivocally demonstrate that cannabinoids have pain relieving properties, but their therapeutic index needs to be improved. By using a strategy of inhibiting an enzyme which inactivates endogenous cannabinoid only outside the brain and showing that this approach is still sufficient to retain an analgesic effect, Professor Piomelli and his colleagues have made a significant advance."

D3 is continuing the development programme of URB937 and plans to begin clinical studies in 2012.

Investigators from other institutions were also involved in the study, including the universities of Urbino, Parma, Naples, and the Complutense University in Madrid.

About the D3

The D3 is a specialist unit of the Italian Institute of Technology dedicated to the discovery of new medicines. The organisation focuses its research efforts on drug discovery in the three key therapeutic areas of pain, inflammation and dementia. By collaborating with private partners, the D3 brings together excellence in basic science from academia with the focus of the pharmaceutical industry to accelerate research in important areas of unmet medical need.

Funded by the Italian government, the D3 will employ over 70 scientists and technical staff by December 2010. The organisation's state-of-the-art facilities include 2000m2 of laboratory and office space completed in December 2009. For more information, visit www.iit.it/en/drug-discovery-and-development.

About the IIT

The Italian Institute of Technology (IIT) is a foundation established jointly by the Italian Ministry of Education, Universities and Research and the Ministry of Economy and Finance to promote excellence in basic and applied research and to contribute to the economic development of Italy. The primary goals of the IIT are the creation and dissemination of scientific knowledge as well as the strengthening of Italy's technological competitiveness. To achieve these two goals, the IIT will cooperate with both academic institutions and private organisations, fostering through these partnerships scientific development, technological advances and training in high technology. For more information visit www.iit.it/en.

About the University of California, Irvine

Founded in 1965, UCI is a top-ranked university dedicated to research, scholarship and community service. Led by Chancellor Michael Drake since 2005, UCI is among the most dynamic campuses in the University of California system, with nearly 28,000 undergraduate and graduate students, 1,100 faculty and 9,000 staff. Orange County's largest employer, UCI contributes an annual economic impact $3.9 billion. For more UCI news, visit www.today.uci.edu.