Drug intelligence / Profile preview

dextroamphetamine + tranylcypromine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Dextroamphetamine + tranylcypromine is a combination of two small molecule drugs, each with distinct mechanisms of action. Dextroamphetamine is a central nervous system stimulant primarily used to treat attention deficit hyperactivity disorder (ADHD) and narcolepsy; it works by increasing the release and blocking the reuptake of dopamine and norepinephrine in the brain[6][8]. Tranylcypromine is an irreversible monoamine oxidase inhibitor (MAOI), mainly used for treatment-resistant depression; it increases levels of serotonin, norepinephrine, and dopamine by inhibiting their breakdown[4][5][10]. The combination has been explored off-label for treatment-resistant major depressive disorder (MDD), particularly when other therapies have failed. While some case reports suggest efficacy in refractory depression, this combination carries significant risk due to potential severe drug interactions—most notably hypertensive crisis or serotonin syndrome—because MAOIs can dangerously potentiate the effects of stimulants like dextroamphetamine[2][3]. This regimen should only be considered under strict medical supervision.

02

Targets

NET (Norepinephrine Transporter)VMAT2 (Synaptic vesicular monoamine transporter 2)TAAR1 (Trace amine-associated receptor 1)SERT (Sodium-dependent serotonin transporter)DAT (Dopamine plasma membrane transport protein)KDM1A (LSD1)MAOB (Monoamine oxidase B)MAOA (Monoamine oxidase A)

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