UCB 44212, the second analogue of UCB Pharma’s anti-epileptic, KEPPRA*, enters clinical study phase

Tuesday 27th April 2004 - UCB Pharma's 44212, a more potent analogue of the potential blockbuster antiepileptic, KEPPRA (levetiracetam), has entered Phase I, the first phase of clinical development.

Animal studies have shown that UCB 44212 is several orders of magnitude more potent in preventing seizures in epilepsy models than KEPPRA, and has a 10 times higher affinity at the levetiracetam binding site.^{1, 2} In addition, based on all the available animal data it could be suggested that UCB 44212 may be not only more effective and better tolerated but also easier to administer than other anti-epileptic drugs (AEDs).

This new compound joins UCB 34714, another UCB Pharma pyrrolidone derivative that recently entered clinical trials. Besides its high affinity at the levetiracetam binding site, UCB 34714 also exhibits additional mechanisms of action, which may result in a broad therapeutic value in neurological disorders beyond epilepsy. ^{3, 4, 5, 6} In 2004, phase II clinical trials of UCB 34714 will take place in epilepsy, neuropathic pain and essential tremor.

UCB 44212 is the latest in the family of CNS molecules designed around UCB Pharma's flagship brand KEPPRA, which should provide the company with major competitive assets well into the next decade.

UCB 44212 and UCB34714 are a further demonstration of UCB Pharma's commitment to investment in CNS research using the levetiracetam binding site as a unique research pathway.

- ENDS –

* KEPPRA is a registered trademark of the UCB Group. Please consult your national product information as the trademark, as well as the prescribing information, may differ from one country to the other.

• UCB Pharma is one of Europe's leading pharmaceutical companies. It is active in all the world's major markets, specialising in the fields of treatments for disorders of the central nervous system and for allergy and respiratory diseases. Among products developed by UCB Pharma are KEPPRA® (levetiracetam), an adjunctive treatment of partial onset seizures in adults with epilepsy, and XYZAL® (levocetirizine) a novel antihistamine for the treatment of allergic rhinitis and chronic idiopathic urticaria.
• With over 6,500 employees operating in over 100 countries, UCB Pharma's global headquarters are in Brussels, capital of Europe. In 2003 it achieved a consolidated turnover of €1.463 billion.
• In 2003 UCB Group invested €270 millions in research and development, an increase of 3% over 2002
• In 2003, KEPPRA reached a total turnover of €314 million, a 36% increase over 2002 (up 55% at constant exchange rates)
• KEPPRA is registered in 51 countries including Argentina, Australia, Austria, Belgium, Bulgaria, Canada, Czech Republic, Denmark, Finland, France, Germany, Greece, Hong Kong, Ireland, Italy, Luxembourg, Mexico, Netherlands, Norway, Poland, Singapore, South Africa, Spain, Sweden, Switzerland, UK and USA
• KEPPRA is currently available as adjunctive treatment of partial onset seizures, with or without secondary generalisation, in adults with epilepsy
• A partial seizure involves just part of the brain, and can be either ‘simple' when consciousness is not affected, ‘complex' when consciousness is affected, or secondary generalised when either a simple or complex seizure spreads to involve the whole brain
• Clinical research with KEPPRA is ongoing, including studies in paediatric, primary generalised seizure and monotherapy use
• For further information please visit www.ucb-group.com and www.ucbpharma.com

References

1. Data on file (RRLE03A2101)
2. Data on file (RRLE03B2402)
3. Kenda B et al. Discovery of 4-Substituted Pyrrolidone Butanamides as New Agents with Significant Antiepileptic Activity. J. Med. Chem. 2004;47: 530-549
4. De Ryck M et al. UCB 34714, A New Pyrrolidone Derivative, Antagonizes Harmalineinduced Tremor In Rats: Comparison To Drugs For Essential Tremor And Anti-Epileptic Drugs. Neuroscience 2003. Abstract: 33rd annual meeting of the Society for Neuroscience, New Orleans, Nov 8-12 2003.
5. Lamberty et al. UCB 34714, A New Pyrrolidone Derivative, Is effective In Two Models Of Human Neuropathy In The Rat: Comparison To Gabapentin. Neuroscience 2003. Abstract: 33rd annual meeting of the Society for Neuroscience, New Orleans, Nov 8-12 2003.
6. Matagne et al. UCB 34714, A New Pyrrolidone Derivative, Reveals Potent Activity In In Vitro and In Vivo Models Of Epilepsy. Neuroscience 2003. Abstract: 33rd annual meeting of the Society for Neuroscience, New Orleans, Nov 8-12 2003.