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Anaphylm (dibutepinephrine)

Type I allergic reactions including anaphylaxis

Also known as AQST-109
Regulatory submission
NDA resubmitted September 2026
Launch
Not announced
Last updated
121 sources

Product information and disease descriptionProduct descriptionProduct informationPharmacology

Mechanism of action

11 evidence topics · 10 sources

Epinephrine actions at alpha- and beta-adrenergic receptors in anaphylaxis

“Epinephrine acts on both alpha and beta-adrenergic receptors.” (opens the source at this quote in a new tab)

“Through its action on alpha-adrenergic receptors, epinephrine lessens the vasodilation and increased vascular permeability that occurs during anaphylaxis, which can lead to loss of intravascular fluid volume and hypotension.” (opens the source at this quote in a new tab)

“Through its action on beta-adrenergic receptors, epinephrine causes bronchial smooth muscle relaxation and helps alleviate bronchospasm, wheezing and dyspnea that may occur during anaphylaxis.” (opens the source at this quote in a new tab)

“Epinephrine alleviates pruritus, urticaria, and angioedema. It may also relieve gastrointestinal and genitourinary symptoms associated with anaphylaxis because of its relaxer effects on the smooth muscle of the stomach, intestine, uterus, and urinary bladder.” (opens the source at this quote in a new tab)

Receptor subtypes: alpha-1 vasoconstriction, beta-1 cardiac stimulation, beta-2 bronchial relaxation

“Epinephrine increases cardiac output by stimulating β1-adrenergic receptors within the heart and causes vasoconstriction by the activation of α1-adrenergic receptor.” (opens the source at this quote in a new tab)

“Although systemic IM or IV administered epinephrine binds to α- and β-adrenergic receptors nonselectively, inhaled epinephrine is delivered to the pulmonary airways that predominantly contain β2-adrenergic receptors in the bronchial smooth muscles.” (opens the source at this quote in a new tab)

Combined alpha- and beta-adrenergic effects as the basis of first-line treatment

“Through its combined α- and β-adrenergic effects, epinephrine counteracts vasodilation and increased vascular permeability, improves blood pressure and coronary perfusion, relaxes bronchial smooth muscle, and reduces mucosal edema in the upper airway.” (opens the source at this quote in a new tab)

Dibutepinephrine as a polymer matrix-based epinephrine prodrug

“Anaphylm™ (dibutepinephrine) sublingual film is a polymer matrix-based epinephrine prodrug investigational product.” (opens the source at this quote in a new tab)

“Anaphylm is similar in size to a postage stamp, weighs less than an ounce, and begins to dissolve on contact.” (opens the source at this quote in a new tab)

Sublingual film application and delivery of epinephrine

“AQST-109 is a polymer matrix-based epinephrine prodrug administered as a sublingual film that is applied under the tongue for the rapid delivery of epinephrine.” (opens the source at this quote in a new tab)

Prodrug formulation delivered on PharmFilm technology

“Aquestive Therapeutics is developing a sublingual (SL) film containing AQST - 109 (a prodrug of Epinephrine) delivered using PharmFilm technology” (opens the source at this quote in a new tab)

AdrenaVerse platform: control of absorption and conversion rates

“Our AdrenaVerse™ platform contains a library of over twenty epinephrine prodrug product candidates intended to control absorption and conversion rates across a variety of possible dosage forms and delivery sites.” (opens the source at this quote in a new tab)

“Epinephrine plays a critical role in immune suppression but, until now, its role has been limited due to issues in the absorption and conversion of epinephrine in the human body.” (opens the source at this quote in a new tab)

“The AdrenaVerse platform makes it possible to deliver epinephrine locally across mucosal surfaces and the skin and, therefore, we believe that it has the potential to yield multiple product candidates focused on treating a range of diseases.” (opens the source at this quote in a new tab)

Conversion of the prodrug to epinephrine after administration

“epinephrine prodrugs can control conversion rate” (opens the source at this quote in a new tab)

“In vitro data showing instant conversion of AQST-109” (opens the source at this quote in a new tab)

Ester prodrug lipophilicity: log P of the first-generation epinephrine prodrug dipivefrin
PropertyEpinephrineDipivefrin
Log P“-0.43”“3.71”
Rationale for a prodrug: overcoming the barrier properties of the oral mucosa

“Mucosal surfaces, such as the oral mucosa, are a convenient route for delivering drugs to the body due to the fact that they are highly vascularized and permeable, providing increased bioavailability and rapid onset of action because it does not pass through the digestive system and thereby avoids first pass metabolism.” (opens the source at this quote in a new tab)

“In particular, the buccal and sublingual tissues offer advantageous sites for drug delivery because they are highly permeable regions of the oral mucosa, allowing drugs diffusing from the oral mucosa to have direct access to systemic circulation.” (opens the source at this quote in a new tab)

“Since drug delivery through the buccal mucosa is limited by the barrier nature of the epithelium and the area available for absorption, various enhancement strategies are required in order to deliver therapeutically relevant amounts of drug to the systemic circulation. Various methods, including the use of chemical penetration enhancers, prodrugs, and physical methods may be employed to overcome the barrier properties of the buccal mucosa.” (opens the source at this quote in a new tab)

Sublingual delivery of a prodrug of epinephrine in an investigational film

“This medicine is a polymer‐based adrenaline prodrug in the form of a sublingual (SL) film.” (opens the source at this quote in a new tab)