Ligand id: 8284

Name: CPP-115

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 3
Hydrogen bond donors 2
Rotatable bonds 1
Topological polar surface area 63.32
Molecular weight 177.06
XLogP -0.44
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
The hydrochloride salt of CPP-115 (PubChem CID 71252718) has been granted orphan drug designation by the EMA for the treatment of West syndrome, an epileptic disorder of young children which causes developmental problems. West syndrome is a long-term debilitating disease which may be life threatening as it can lead to severe damage to motor and cognitive functions. CPP-115 may have additional therapeutic applications for treating other neurological disorders, including drug addiction [4]. A single Phase I clinical trial has assessed CPP-115 as a treatment for cocaine addiction [3], but development has not progressed further.
Mechanism Of Action and Pharmacodynamic Effects
CPP-115 inhibits GABA aminotransferase [2,5] activity, which is responsible for the catabolic degradation of the principal inhibitory neurotransmitter GABA. Inhibition of GABA aminotransferase leads to increased concentrations of GABA in the brain and is able to terminate seizures [1] which are the result of pathophysiologically low GABA levels.