COL-204 for Wake Promotion
COL-204 is the lead candidate from the Conjugated Stigmine Program. Pre-clinical data demonstrated an attractive profile for wake promotion, notably a marked increase in duration of wakefulness without rebound hypersomnolence or amphetamine-like stimulant effects.
Conjugated Stigmines
The Conjugated Stigmine Program is built on novel and proprietary chemistry technology. This technology results in a new chemical entity (NCE) which can deliver and release two active therapeutic agents in the CNS. The Program has yielded a library of cholinesterase inhibitors conjugated to targeted CNS therapeutics. It includes product candidates for pain, Alzheimer’s disease, cognition disorders, anxiety, depression and psychiatric indications.
Concept
Conjugate therapeutically active entities to stigmine acetylcholinesterase inhibitors to allow delivery of 2 active agents to the CNS.
Rationale
- Stigmines are carbamoyl esters which inhibit cholinesterases, such as AChE
- Inhibition occurs when the stigmine binds to the active site of the cholinesterase, where it is eventually hydrolyzed, thereby releasing an amine
- By conjugating the stigmine to a therapeutically active amine, the hydrolysis event will result in delivery of a second active drug to the CNS
- Thus the conjugated stigmine provides the ability to deliver two different drugs to the CNS with a single chemical entity
- The conjugated stigmine is a NEW chemical entity, providing the opportunity for commercial exclusivity
