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Phase 1 Trial Shows Epinephrine Can Meet Therapeutic Thresholds When Administered Sublingually

AAAAI News Release

April Presnell
AAAAI Executive Office: (414) 272-6071

February 1, 2022

Treatment shows promise as a viable alternative for the treatment of anaphylaxis, according to new research from the 2022 AAAAI Annual Meeting.

Milwaukee, WI – A phase 1 study demonstrated for the first time that epinephrine can reach therapeutic plasma concentrations via sublingual administration. The full abstract (#L37) will be presented at the 2022 Annual Meeting of the American Academy of Allergy, Asthma & Immunology (AAAAI).

“The results from this study are encouraging, indicating that an epinephrine treatment alternative, which can be administered sublingually for cases of life-threatening allergic reactions, has the potential to meet the therapeutic window required to treat anaphylaxis, while providing patients a needle-free, pocket-sized medication option,” remarked the study’s lead author, John Oppenheimer, MD, FAAAAI, Clinical Professor of Medicine at UMDNJ Rutgers, Pulmonary and Allergy Associates NJ.

This Phase 1 randomized, single-ascending dose study was performed in order to assess the safety, tolerability and pharmacologic profile of AQST-109. Developed by Aquestive Therapeutics (Nasdaq: AQST), AQST-109 (epinephrine prodrug sublingual film) is a polymer matrix-based film that can be applied sublingually (under the tongue) for the rapid delivery of epinephrine. The product is similar in size to a postage stamp and begins to dissolve on contact. In the Phase 1 study, all study volunteers were monitored for adverse events and local tolerability. Systolic blood pressure (SBP), diastolic blood pressure (DBP) and heart rate (HR) were taken before and up to six hours after dosing. Data from prior studies of EpiPen and Auvi-Q were used for historic comparison.

This study indicated that AQST-109 was absorbed and rapidly converted to epinephrine with an observed median time to reach maximum drug concentration (Tmax) of 15 minutes and an observed peak blood level (Cmax) of 762 pg/mL. These findings are comparable to published study results for both EpiPen and Auvi-Q epinephrine auto-injectors1234567. In addition, dosing with AQST-109 resulted in changes in blood pressure and heart rate that were comparable to epinephrine auto-injectors.

Safety data indicated that AQST-109 was generally well tolerated with no serious adverse events, significant medical events, or treatment-related severe adverse events reported within the trial.

Visit to learn more about anaphylaxis. Research presented at the AAAAI Annual Meeting, February 25-28 in Phoenix, Arizona, is published in an online supplement to The Journal of Allergy and Clinical Immunology.

The American Academy of Allergy, Asthma & Immunology (AAAAI) is the leading membership organization of more than 7,100 allergists, asthma specialists, clinical immunologists, allied health professionals and others with a special interest in the research and treatment of allergic and immunologic diseases. The AAAAI is the go-to resource for patients living with allergies, asthma and immune deficiency disorders. Established in 1943, the AAAAI has more than 7,100 members in the United States, Canada and 72 other countries. The AAAAI’s Find an Allergist/Immunologist service is a trusted resource to help you find a specialist close to home.

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2 Aquestive Therapeutics, Study 160455, on file.
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