IIBR has launched a major R&D program focused on the design, development and testing of novel, proprietary drug compounds for the treatment of central nervous system disorders, such as Alzheimer's disease (AD). The program is based on manipulation of specific neurotransmitter systems believed to be involved in a range of CNS and PNS disorders.
Achievements
- The discovery of novel CNS drugs (protected by worldwide patents).
- Generation and evaluation of AF102B, an M1 selective muscarinic agonist, developed in cooperation with a major Japanese company. AF102B was approved by the FDA (January, 2001) and in Japan (June, 2001) for treatment of dry mouth in Sjorgen's Syndrome and is now marketed in the USA and Japan under the name Cevimeline (EVOXACTM) by Daiichi-Sankyo.
Treatment of AD patients with AF102B resulted in a considerable decrease of beta-amyloids in the cerebrospinal fluid. This seminal finding indicates that AF102B may reduce the beta-amyloid burden in brains of AD patients.
- Generation and evaluation of AF267B, a second generation of M1 agonist. AF267B was tested successfuly by TorreyPines Therapeutics, USA, in Phase I and Phase II studies in healthy volunteers and is currently in Phase II testing for xerostomia , secondary to Sjogren's Syndrome.
AF267B may also be developed for the treatment of cognitive disorders.
The design and production of unique proprietary structures with potential therapeutic activity are an outcome of an extensive effort in rational drug design and pharmacological screening. A number of lead compounds that appeared to have the clinical potential to be effective in treating both acute and chronic neurodegenerative diseases were identified and comprehensively evaluated at IIBR. These compounds can be useful both in treatment and as disease modifying-agents in AD and other related disorders.
These compounds can beneficially affect major hallmarks involved in AD pathology (cognitive dysfunction, beta-amyloids, tangles and cell death).
Drugs that address cholinergic dysfunction are believed to provide potential benefit not only for those suffering from AD; they are also considered useful in treatment of additional disease states such as dementia with Lewy Bodies, minimal cognitive impairment, cerebral amyloid angiopathy, schizophrenia, mania, stroke, head injury and post-operative delirium.
|
| |
|
|