Drug intelligence / Profile preview

Dextroamphetamine + lisdexamfetamine

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

Dextroamphetamine + lisdexamfetamine is a combination of two central nervous system (CNS) stimulants, both used primarily in the treatment of attention deficit hyperactivity disorder (ADHD). Lisdexamfetamine is a prodrug that is converted in the body to dextroamphetamine, which then exerts its pharmacological effects. Both drugs increase synaptic concentrations of dopamine and norepinephrine by blocking their reuptake and promoting their release from presynaptic neurons. Dextroamphetamine also acts as an agonist at trace amine-associated receptor 1 and inhibits vesicular monoamine transporter 2. Lisdexamfetamine was developed to provide a longer duration of action with reduced abuse potential compared to immediate-release stimulants. The primary indications for these agents are ADHD and, for lisdexamfetamine specifically, moderate to severe binge eating disorder[1][3][4][5].

02

Targets

DAT (Dopamine plasma membrane transport protein)TAAR1 (Trace amine-associated receptor 1)SERT (Sodium-dependent serotonin transporter)NET (Norepinephrine Transporter)VMAT2 (Vesicular monoamine transporter 2)

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