Technology Bundle ID

Analogues of Modafinil for treating sleep and attention disorders

Lead Inventors
Amy Newman (NIDA)
Development Status
Discovery (Lead Identification)

Modafinil has attracted attention for the treatment of cognitive dysfunction in disorders such as attention-deficit/hyperactivity disorder (ADHD) as well as cocaine and methamphetamine dependence.  However, modafinil has relatively low affinity for binding to the dopamine transporter (DAT) to block dopamine reuptake, and is water-insoluble, thus requiring large doses to achieve pharmacological effects.

Investigators at the National Institute of Drug Abuse have synthesized a series of modafinil analogues that have higher affinity for the dopamine (DAT), serotonin (SERT) and/or norepinephrine (NET) transporters and improved water solubility.  These novel analogues present the advantage of higher potency, which may translate into lower effective doses and better bioavailability over modafinil.

Commercial Applications
  • Therapeutic agent for substance abuse (such as nicotine, cocaine, methamphetamine, opioids), for attention/cognitive disorders (such as ADHD), and for sleep disorders.
Competitive Advantages
  • Higher affinity for monoamine transporters (DAT, SERT, and NET) compared to modafinil
  • Analogues have lower effective doses
  • Better bioavailability than modafinil
  • Improved water solubility over modafinil

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