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Description: Lisdexamfetamine (L-lysine-d-amphetamine) is a prodrug of the psychostimulant d-amphetamine coupled with the essential amino acid L-lysine. It was developed so that the amphetamine psychostimulant is released and activated more slowly as the prodrug molecule is hydrolyzed consequently cleaving off the amino acid-during the first pass through the intestines and/or the liver. Amphetamines target the trace amine-associated receptor 1 (TAAR1). Amphetamine is also believed to exert its effects by binding to the monoamine transporters (the dopamine transporter or DAT) and increasing extracellular levels of the biogenic amines dopamine, norepinephrine (noradrenaline) and serotonin.
Drug Type: Small Molecule; Approved
Pharmacology: Lisdexamfetamine is a pro-drug of dextroamphetamine. It works primarily by inducing the release of the neurotransmitters dopamine and norepinephrine from their storage areas in nerve terminals. Both of these transmitters contribute to maintaining alertness, increasing focus, and sustaining thought, effort, and motivation.
Mechanism of Action: Lisdexamfetamine is a pro-drug of dextroamphetamine. Amphetamines are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space. Norepinephrine and dopamine contribute to maintaining alertness, increasing focus, and sustaining thought, effort, and motivation. However, the exact therapeutic action in ADHD is not known.
Indication: For the treatment of Attention Deficit/Hyperactivity Disorder (ADHD) in pediatric populations aged 6 to 12 years.
Half Life: The plasma elimination half-life of lisdexamfetamine typically averaged less
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View All Author iconAuthors
  • Suma Krishnan
  • Robert L Findling
  • Yuxin Zhang
  • Stephen V Faraone
  • Lenard A Adler
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • Shire Pharmaceutical Development
  • New River Pharmaceuticals
  • Massachusetts General Hospital
  • University of California, Irvine
  • Clinical Study Centers, LLC
View All Affiliations icon Organizations
  • Massachusetts General Hospital
  • New York University School of Medicine
  • Flinders University Rural Clinical School
  • University Hospitals Case Medical Center
  • Johns Hopkins University

Clinical Trials | 26 trials

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