GABAA Receptor Agonists for Oral Treatment of Asthma


Target Problems

Over one-half of pediatric patients and three-fourths of adults are reported to be non-compliant with current asthma medications. This technology improves compliance over inhaled medications with small molecule drugs that are orally active.


Asthma pill avoids inhaler delivery and corticosteroid side effects

Key Features

  • Improved Dosing– Compounds are orally available; can avoid inhaler delivery, improve dosing, and promote better compliance.
  • Reduced Side Effects– Avoiding corticosteroid use will improve safety and avoid potential resistance and immunosuppression.
  • Efficacy Demonstrated– Lead compounds reduce airway hyper-responsiveness in isolated human and rodent airway smooth muscle.
  • Target Selectivity–Lead drugs are designed to act in the lung tissue to suppress inflammation and airway hyper-responsiveness but are designed to avoid off-target effects and central nervous system distribution.
  • Known Drug Target– GABAAR structure and function are well characterized and have been drugged for 50 years for other indications; safety profile well established.


Inventors at the University of Wisconsin-Milwaukee and Columbia University have developed lead drug compounds for asthma based on a fundamentally novel mechanism of action. These small molecule drugs are orally active, improving compliance over inhaled medications. The drugs target functional gamma-amino butyric acid type A receptors (GABAAR) expressed on airway smooth muscle and immune/inflammatory cells, avoiding the use of corticosteroids and adrenergic agonists.

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UWM scientists developing asthma pill

Intellectual Property

US9879020B2 “GABAA agonists and methods of using to control airway hyperresponsiveness and inflammation in asthma” (expiration 2033)

US11447495B2 “Substituted benzo[f]imidazo[1,5-a][1,4]diazepines as GABA(a) receptor modulators” (expiration 2039)

AU2017313753A1 “GABA(A) receptor modulators and methods to control airway hyperresponsiveness and inflammation in asthma” (expiration 2037)

EP3500573B1 “Gaba(a) receptor modulators and methods to control airway hyperresponsiveness and inflammation in asthma” (expiration 2037)


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