Alzheimer's disease is a dreaded disease for the elderly. In the direction of its treatment , the effort of Evotec AG (Frankfurt Stock Exchange: EVT, TecDAX 30, "Evotec") has successfully completed the single ascending dose component of the Phase I clinical study with EVT 101, a subtype-specific NMDA receptor antagonist Alzheimer's disease.
The study comprised 48 young healthy subjects of whom 36 received EVT 101. These showed that EVT 101 was well absorbed, extremely well tolerated with no significant adverse events and had a good pharmacokinetic profile consistent with once or twice daily oral dosing.
The finding is of great importance as non-selective NMDA antagonists have unfavourable side-effect profile.
The EVT 101 has now moved into the multiple ascending dose stage of the Phase I study in both young and elderly volunteers.
EVT 101 is a highly potent and selective antagonist of NR2B subunit containing NMDA receptors.
NMDA receptors are important players in certain pathological disease states such as Alzheimer's disease, Parkinson's disease, neuropathic pain and epilepsy. However, the clinical development of non-selective antagonists has been limited by unfavourable side-effects, such as hallucinations. In the early 1990's it was found that multiple NMDA receptor subtypes exist which contain different NR2(A-D) subunits.
In this direction this trial is stepping stone for success. It would be greatly beneficial in treating patients suffering from Alzheimer's.