Debiopharm\'s novel cholinesterase inhibitor, for the treatment of Alzheimer\'s disease
Lausanne-based Debiopharm is to start a Phase II trial for dose-finding and efficacy assessment of a once daily oral formulation of ZT-1, a novel cholinesterase inhibitor, for the treatment of Alzheimer\'s disease (AD). The multicentre trial will be conducted in France, Belgium and Switzerland, and will enroll 180 patients suffering from mild to moderate AD.
ZT-1\'s dual pharmacological mechanism of action is said to offer the potential to slow deterioration, while improving cognitive function. In addition to its established anti-acetylcholinesterase (AChE) activity, ZT-1 has neuroprotective properties, one of them being mediated possibly by the N-methyl-D-aspartate (NMDA) receptor. After oral administration, ZT-1 is progressively hydrolysed into the active compound huperzine A (hup A). Hup A is one of the most potent AChE inhibitors and was originally isolated by Chinese scientists from the club moss Huperzia serrata.
Debiopharm is developing an injectable sustained-release formulation of ZT-1. The pharmacokinetic results in animals showed a stable release pattern over several weeks. This has the potential to further benefit AD patients due to improved compliance and a close medical follow-up with monthly injections.