The Galantos Approach

Galantos is exploring a novel class of drugs, so-called allosteric potentiating ligands (APLs). The company´s founders discovered this novel mechanism in 1995 when studying the mechanism of action of galantamine and other inhibitors of acetylcholinesterase. Galantamine (Reminyl) has been marketed for the treatment of mild to moderate Alzheimer's disease (AD) since 2000. Originally established as a reversible inhibitor of the enzyme acetylcholinesterase (AChE), galantamine was found to mainly act as an allosteric modulator of nicotinic receptors.

Allosteric modulators interact with the receptor through binding sites that are distinct from those for acetylcholine and nicotinic agonists. Because these modulators only enhance natural cholinergic neurotransmission without acting as agonists, they do not induce compensatory processes as agonists do. As a result, they do not carry the same risk of receptor desensitization as nicotinic agonists and potent AChE inhibitors. Moreover, they do not carry a risk of inducing AChE up-regulation when regularly applied, either.

As galantamine and similar molecules modulate nicotinic cholinergic receptors through an alternative binding site to increase cholinergic neruotransmission, they are called an allosteric potentiating ligands (APL) of nicotinic acetylcholine receptors.

Galantos Pharma has chosen to identify and develop nicotinic APLs with higher efficacy and improved AE profile.