Evotec’s EVT 101 is an NR2B subtype-specific NMDA receptor antagonist developed for the treatment of Alzheimer’s disease and/or neuropathic pain.
A total of 90 healthy subjects, both young and elderly, received single and multiple ascending doses of the compound. In all subjects EVT 101 was well absorbed, achieved good exposure levels, and was very well tolerated, with no significant adverse events.
In both the young and elderly subjects, the compound had a good pharmacokinetic profile, with an 11 hour half-life consistent with once- or twice-daily oral dosing.
Evotec was keen to point out that the good tolerability of EVT 101 is significant given the unfavorable side-effect profile of non-selective NMDA antagonists. These drugs, which have shown potential in the treatment of Alzheimer’s disease, Parkinson’s disease, neuropathic pain and epilepsy, have also been associated with side-effects such as hallucinations.
In preclinical models, EVT 101 has also demonstrated potent beneficial effects and an improved side effect profile compared to non-selective NMDA receptor antagonists, and has shown good oral bioavailability and in vivo pharmacokinetics.