Targacept Inc., a clinical-stage biopharmaceutical company developing a new class of drugs known as NNR Therapeutics, has initiated a phase I clinical trial of TC-5619, a novel small molecule that modulates the activity of the neuronal nicotinic receptor (NNR) subtype known as alpha7. TC-5619 was discovered using Targacept's proprietary drug design technology known as Pentad and is the lead product candidate in its alpha7 NNR programme.

"The entry of TC-5619 into the clinic further demonstrates the breadth and pharmacological diversity of our pipeline of NNR Therapeutics," said J Donald deBethizy, PhD., Targacept's president and CEO. "The broad therapeutic application of the alpha7 NNR is well established and presents multiple opportunities for potential later stage development of TC-5619. We are also excited by the promise of other alpha7 compounds in our portfolio."

The phase I study is designed to evaluate the safety, tolerability and pharmacokinetics of TC-5619. The trial is a double-blind, placebo-controlled study with single escalating doses of TC-5619 administered orally to healthy volunteers.

The alpha7 NNR is associated with a variety of biological functions. In particular, the alpha7 NNR has been shown in animal studies to be an essential regulator of both inflammation arising from injury or infection and cognitive functions. Published in vitro studies have also suggested that the alpha7 NNR plays a role in protecting neuronal cells from deterioration and death, a process known as neuroprotection.