Cholinomimetic drugs in clinical development for Alzheimer’s disease including European registrations

PhaseDrug nameCompanyMechanism of action
RegisteredCognex (tacrine)Parke-DavisAChE inhibitor
RegisteredAricept (donepezil)Eisai Inc/Pfizer IncAChE inhibitor
RegisteredExelon (rivastigmine)Novartis IncAChE inhibitor
Awaiting approvalMetrifonateBayer AGAChE inhibitor
Awaiting approvalSynapton (physostigmine)Forest Laboratories IncAChE inhibitor
3SB-202026SmithKline Beecham plcM1 agonist
3AmridinNikken Chemicals Co LtdAChE inhibitor
3TalsaclidineBoehringer Ingelheim CorpM1 agonist, nootropic agent
3GalantamineJanssen Ltd and Shire LtdAChE inhibitor
3MontirelinGruchenthal GmbHACh release stimulator
3FKS-508Nippon Shinyaku Co LtdACh modulator
3NefiracetamDaijchi Sciyaku Co LtdACh receptor agonist
3AF-1025B (cevimeline)Snow Brand Milk Products Co LtdM1agonist
3EptastigmineMediolanum Farmaceutical SpAAChE inhibitor
3MilamelineParke Davis and CoM1 agonist
2ABT-418Abbot LaboratoriesnAChR agonist
2KA-672Dr Wilmar Schwabe GmbH and CoAChE inhibitor
2HuperzineMayo FoundationAChE inhibitor
2P-11012Hoechst AGAChE inhibitor
2P-11149Hoechst AGAChE inhibitor
2SR-46559ASanofi Recherche SAM1 agonist
2T-588Toyama Chemical Co LtdACh release stimulator
2TAK-147Takeda Chemical Industries LtdAChE inhibitor
2YM-796Yamanouchi Pharmaceutical Co LtdM1 agonist, nootropic agent
2ZifrosiloneHoechst Marion Roussel IncAChE inhibitor
2Methanesulfonyl chlorideUniversity of Texas systemAChE inhibitor
2S-9977ServierAChE inhibitor
1LU-25109H Lundbeck A/SmAChR agonist
1GTS-21 (DMXB-anabaseine)University of FloridaNicotinic agonist
1NS-2330NeuroSearch A/SAChR agonist
  • ACh=acetylcholine; AChR=acetylcholine receptor; AChE=acetylcholinesterase; nAChR=nicotonic cholinergic receptor; M=muscarinic receptor.[118]