Evotec AG has announced that it has successfully completed a Phase I safety and tolerability study with EVT 302. The preliminary results confirm the good tolerability profile of EVT 302 and are an encouraging basis for further clinical development.
EVT 302, a reversible and highly selective inhibitor of MAO-B in development for smoking cessation, was investigated in an ascending dose study with repeated daily dosing in a total of 84 healthy young and elderly subjects.
Healthy young male subjects were treated with EVT 302 2.5, 5, 15 mg, or placebo for two weeks, and healthy elderly male and female subjects were treated with EVT 302 2.5 mg, 10 mg, or placebo for four weeks. Each treatment was received by 12 young and/or elderly subjects as appropriate.
The highest dose levels exceed the expected maximum therapeutic dose planned to be used in further clinical trials. For the treatment period and part of the subsequent washout phase the subjects were confined to the clinical research unit.
The study was aimed at investigating safety/tolerability, pharmacokinetics, and pharmacodynamics (inhibition of MAO-B in platelets) during prolonged dosing with EVT 302 as compared to placebo. The study was conducted and successfully completed as planned per protocol. The results are still blinded and will become available as final evaluated data over the next two months.
The preliminary data indicate that EVT 302 was well tolerated in young and elderly subjects up to the highest dose levels tested in this study. Adverse events (AEs) classified as possibly treatment related were transient and mostly of mild intensity; only very few moderate AEs were reported. No severe or serious AEs occurred.
No clinically relevant changes in lab values of haematology or clinical chemistry were noted. In particular, there were no changes in liver function tests, in any subjects.