Drug intelligence / Profile preview

Venlafaxine + lisdexamfetamine

Development stage
Unknown
Lead developer
Takeda
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Venlafaxine + lisdexamfetamine is a combination of two pharmaceutical agents used primarily in psychiatric and neurobehavioral disorders. Venlafaxine is a selective serotonin and norepinephrine reuptake inhibitor (SNRI) that increases synaptic concentrations of serotonin and norepinephrine by inhibiting their reuptake at the presynaptic terminal. It also weakly inhibits dopamine reuptake. Lisdexamfetamine is an inactive prodrug that is converted in the body to dextroamphetamine, which acts as a central nervous system stimulant by increasing the release of monoamines (dopamine and norepinephrine) via Trace amine-associated receptor 1 (TAAR1) agonism and vesicular monoamine transporter 2 inhibition. This combination may be considered for treatment-resistant depression or comorbid attention-deficit hyperactivity disorder (ADHD) with mood disorders; however, coadministration requires careful monitoring due to potential additive side effects such as increased blood pressure, heart rate, anxiety, or jitteriness[1][3][8][6].

Brand names
VyvanseEffexorVensirVencarmVenlalixEfexorVenlablue
Other names
venlafaxinelisdexamfetamine dimesylate
02

Targets

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

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