Evotec has announced the initiation of its first Phase I study with EVT 302. This open-label study is designed to access the presence of the monoamine oxidase B enzyme (MAO-B) in brain after administration of single oral doses of EVT 302 using dynamic positron emission tomography. This technique helps to determine the therapeutic dose range of EVT 302 for the upcoming safety and efficacy studies.

EVT 302 is an orally active, potent, highly selective and reversible inhibitor of MAO-B in development for smoking cessation. Its preclinical profile supports the potential for a superior safety profile over marketed MAO-B inhibitors and better tolerability compared with current treatments.

In a Phase I single-ascending-dose study by Roche, from whom the compound was in-licensed, EVT 302 was safe and well tolerated up to high dose levels and showed excellent pharmacokinetic properties with prolonged MAO-B inhibition, offering the potential for once-a-week dosing at very low exposure levels.

Evotec plans to start additional Phase I safety and tolerability studies during the first half of 2007. If the Phase I results are positive, a Phase II trial in smoking cessation is planned to begin in mid 2008.