Drug intelligence / Profile preview

neostigmine + glycopyrrolate

Development stage
Unknown
Lead developer
Endo International
Modality
Small Molecules
Administration
Intranasal, Sublingual, Intravenous, Intramuscular, Subcutaneous, Transdermal
01

Overview

This is an investigational dual-drug combination of neostigmine and glycopyrrolate being developed by the US Department of Veterans Affairs for the treatment of neurogenic bowel dysfunction in patients with spinal cord injury. Neostigmine is a cholinesterase inhibitor that increases cholinergic tone by blocking acetylcholine metabolism, thereby stimulating colonic motility and promoting bowel evacuation. Glycopyrrolate is an anticholinergic agent co-administered to attenuate peripheral cholinergic side effects of neostigmine, such as bradycardia and bronchoconstriction, while preserving its beneficial effects on the colon. The combination has been evaluated in multiple delivery routes, including intravenous, intramuscular, and transdermal administration, with a recent Phase 2 study focusing on an intranasal spray formulation to provide a more practical administration route for patients with spinal cord injuries.

Other names
neostigmine and glycopyrrolateintranasal neostigmine and glycopyrrolate
02

Targets

M1 (Muscarinic acetylcholine receptor M1)CHRM2 (M2)Acetylcholinesterase

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