Polypharmacology refers to the development and the use of pharmaceutical agents that act on multiple targets or disease pathways. It is generally thought that complex diseases – such as central nervous system diseases and cancer – may require complex therapeutic approaches. In this respect, a drug that hits multiple sensitive nodes belonging to a network of interacting targets offers the potential for higher efficacy and may limit drawbacks generally arising from the use of a single-target drug or a combination of multiple drugs.

Dual-target (or multi-target) ligands are generally designed using a strategy of molecular hybridization, a new concept in drug design and development based on the combination of pharmacophoric moieties of different bioactive substances to produce a new hybrid compound able to modulate multiple targets of interest. Using this strategy, we develop bifunctional ligands that target two different neurotransmitter receptors to tackle complex neurological disorders.

conceptual design of hybrid ligands

Selected Publications