Budesonide 21-phosphate salts and pharmaceutical compositions containing the same
Inventors
Caliendo, Giuseppe • CIRINO, GIUSEPPE • FIORINO, Ferdinando • FRECENTESE, Francesco • MUSCARÀ, Marcelo Nicolas • PERISSUTTI, Elisa • Petti, Antonio • ROVIEZZO, Fiorentina • Santagada, Vincenzo • SEVERINO, Beatrice • MAGLI, Elisa
Assignees
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Publication Number
US-12465614-B2
Publication Date
2025-11-11
Expiration Date
Abstract
The present invention relates to salts of budesonide 21-phosphate with β2 adrenergic agonists, preferably with formoterol, pharmaceutical compositions containing the same and the use thereof in the treatment of respiratory inflammatory pathologies, obstructive pathologies and allergen-induced airway dysfunctions. The invention further relates to the process for preparing said salts.
Core Innovation
The invention relates to salts of budesonide 21-phosphate with a β2 adrenergic agonist, wherein the β2 adrenergic agonist is Formoterol. Formoterol is present as a crystalline form IV, characterized by an X-ray powder diffraction spectrum obtained using CuKα radiation and specified 2θ angle characteristic peaks.
The disclosure addresses treatment of respiratory inflammatory, obstructive, and allergen-induced airway dysfunctions, including asthma, COPD, and pulmonary fibrosis. Budesonide 21-phosphate is used as a water-soluble phosphate ester, and the invention provides combinations of budesonide 21-phosphate with Formoterol.
Pharmaceutical compositions are described for treating respiratory inflammatory pathologies, obstructive pathologies, and allergen-induced airway dysfunctions by including the described salt with physiologically acceptable excipients. The disclosure also includes crystalline and analytical identification of the budesonide 21-phosphate/Formoterol salt, with additional characterization mentioned as NMR and FT-IR.
Claims Coverage
The claims cover a budesonide 21-phosphate/Formoterol salt defined by Formoterol crystalline form IV and a therapeutic use of the defined salt for specified respiratory conditions.
Formoterol crystalline form IV characterized by XRPD peak set
A salt of budesonide 21-phosphate with a β2 adrenergic agonist wherein the β2 adrenergic agonist is Formoterol, and Formoterol is in crystalline form IV characterized by an X-ray powder diffraction spectrum obtained using CuKα radiation and represented by 2θ angle with specified characteristic peaks.
Budesonide 21-phosphate and Formoterol salt for respiratory treatment
A method for treating respiratory inflammatory pathologies, obstructive pathologies, and allergen-induced airway dysfunctions by administering an effective amount of the defined salt, optionally with physiologically acceptable excipients.
The claim set centers on a defined budesonide 21-phosphate/Formoterol salt where Formoterol is in crystalline form IV with a specified XRPD peak pattern, and it further covers use of the defined salt to treat respiratory inflammatory, obstructive, and allergen-induced airway dysfunctions.
Stated Advantages
Improved airway hyperreactivity and bronchoconstriction in OVA-induced allergic asthma models.
Reduction in plasma IgE.
Reduction in inflammatory cell recruitment in BAL fluid, including eosinophils and macrophages.
Increased anti-inflammatory potency versus parent budesonide in a cutaneous edema model.
Documented Applications
Treatment of respiratory inflammatory pathologies, obstructive pathologies, and allergen-induced airway dysfunctions, including asthma, COPD, and pulmonary fibrosis.
Preclinical evaluation in OVA-induced allergic asthma models to assess airway hyperreactivity, bronchoconstriction, and inflammatory endpoints.
Use in a cutaneous edema model to evaluate anti-inflammatory potency versus parent budesonide.
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