Selegiline Transdermal System

Selegiline Transdermal System (STS) is a transdermal patch formulation of selegiline, a selective and irreversible inhibitor of monoamine oxidase type B (MAO-B). Developed through a collaboration between the National Institute on Drug Abuse (NIDA) and Somerset Pharmaceuticals, the system was investigated as a pharmacotherapy for cocaine dependence. The therapeutic rationale was based on selegiline's ability to increase synaptic dopamine levels, potentially counteracting the dopaminergic deficits associated with chronic cocaine use and reducing withdrawal-related cravings. The transdermal delivery route was specifically utilized to maintain steady-state plasma concentrations and bypass the gastrointestinal and hepatic first-pass metabolism, thereby avoiding the hypertensive 'cheese effect' typically associated with oral MAO inhibitors. Despite reaching Phase 3 clinical trials, the STS failed to demonstrate a statistically significant reduction in cocaine use compared to placebo, leading to the termination of its development for this indication.

Brand names

Emsam

Other names

selegilineL-deprenyl