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Ganstigmine
- Development stage
- Discontinued
- Lead developer
- Chiesi
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
- Administration
- Oral (investigational)
01
Overview
Ganstigmine is an experimental drug that was developed as a cholinesterase inhibitor for the potential treatment of Alzheimer's disease and other dementias. It is a carbamate derivative structurally related to physostigmine and neostigmine, designed to inhibit both acetylcholinesterase and butyrylcholinesterase enzymes. By inhibiting these enzymes, ganstigmine increases the levels of acetylcholine in synaptic clefts, thereby enhancing cholinergic neurotransmission in the brain. This mechanism was intended to address cognitive deficits associated with Alzheimer's disease. Despite early clinical development, ganstigmine did not progress beyond Phase 2/3 trials due to lack of sufficient efficacy.
02
Targets
AcetylcholinesteraseButyrylcholinesterase
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