A sublingual epinephrine treatment demonstrated efficacy in patients with anaphylaxis and might be a viable alternative to intravenous epinephrine, according to an abstract presented at the 2022 AAAAI Annual Meeting.

The randomized, single-ascending dose study was conducted with 12 male participants to evaluate the efficacy and safety of 2 formulations of epinephrine prodrug 109 (AQST-109). AQST-109 is “a polymer matrix-based film that can be applied sublingually (under the tongue) for the rapid delivery of epinephrine,” a press release from the meeting indicated.

Researchers recorded adverse events and tolerability, and measured systolic blood pressure (SBP), diastolic blood pressure (DBP), and heart rate (HR) before and after AQST-109 was administered. Dosing was 12 mg.

Previous data indicated intravenous epinephrine yielded an observed peak blood level (C_max) of 341 pg/mL and AUC_0-t of 328 hr*pg/mI. By comparison, AQST-109 Formulations 1 and 2 were associated with a geometric mean C_max of 552 pg/mL and 762 pg/mL, and AUC_0-t of 634 hr*pg/mI and 603 hr*pg/mI, respectively.

Authors noted the median time to reach maximum drug concentration was 15 minutes for AQST-109 vs 22 minutes for EpiPen.

“Dosing with AQST-109 resulted in meaningful and comparable changes in SBP, DBP, and HR. Both sublingual film formulations were safe and well-tolerated,” researchers concluded.

These phase 1 data were comparable to existing findings for treatment with EpiPen and Auvi-Q epinephrine autoinjectors1234567, according to the press release.

“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,” said lead author John Oppenheimer, MD, FAAAAI, clinical professor of medicine at UMDNJ Rutgers, Pulmonary and Allergy Associates NJ, in the press release.

References:

1. Oppenheimer J, Wargacki S, Kainthan R, Berg S, Leister C, Lepore M. A phase 1, randomized study evaluating the safety tolerability, pharmacokinetics (PK) and pharmacodynamics (PD) of single ascending doses of epinephrine prodrug 109 sublingual film (AQST-109) in healthy male volunteers. Abstract presented at: 2022 American Academy of Allergy, Asthma, & Immunology Meeting; February 25-28, 2022; Phoenix, AZ.
2. Phase 1 trial shows epinephrine can meet therapeutic thresholds when administered sublingually. News release. American Academy of Allergy, Asthma, & Immunology. February 1, 2022. Accessed March 10, 2022. https://www.aaaai.org/About/News/News/epineph