Unit aerosol doses for anticoagulation
Inventors
Narasimhan, Rangachari • Marcus, Gregory
Assignees
Incarda Therapeutics Inc • University of California San Diego UCSD
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Publication Number
US-11547663-B2
Publication Date
2023-01-10
Expiration Date
Abstract
Disclosed herein are methods for prophylactic treatment of acute coronary syndrome (ACS) comprising administering, by inhalation, an effective amount of a pharmaceutical composition comprising at least one anticoagulant or antiplatelet agent to a subject in need thereof, wherein the anticoagulant or antiplatelet agent first enters the heart via the left atrium.
Core Innovation
The invention provides methods for treatment of acute coronary syndrome and/or thrombosis and methods for prevention of acute coronary syndrome and/or thrombosis by administering pharmaceutical compositions by inhalation to a subject or patient in need thereof. The pharmaceutical composition includes a univalent direct thrombin inhibitor selected from argatroban, melagatran, ximelagatran, and dabigatran, and at least about 5% of the univalent direct thrombin inhibitor is delivered to the coronary arteries.
In prophylaxis, the antithrombotic compound is delivered such that at least about 5% of the univalent direct thrombin inhibitor is delivered to the coronary arteries and/or about 10% to about 80% of the antithrombotic compound is delivered to the left atrium. The approach is directed to anticoagulant and antithrombotic effects in the heart and coronary arteries while using inhalation as the administration route.
Dependent aspects refine the inhalation delivery and formulation constraints for these methods, including inhalation delivery devices and inhalation-based dosing constraints expressed as numbers of inhalations and/or dose ranges expressed in mg/kg. Additional embodiments include adding a direct factor Xa inhibitor to the pharmaceutical composition, extending the antithrombotic composition beyond the univalent direct thrombin inhibitor.
Claims Coverage
The partial content identifies two independent claims. Both require inhalation administration of an antithrombotic pharmaceutical composition containing a univalent direct thrombin inhibitor, with a specified minimum delivery fraction to the coronary arteries, and the prevention claim additionally introduces a distribution range to the left atrium.
Inhalation treatment with coronary delivery of univalent direct thrombin inhibitor
A method for treatment of acute coronary syndrome and/or thrombosis comprising administering, by inhalation, an effective amount of a pharmaceutical composition to a subject in need thereof, wherein the pharmaceutical composition comprises a univalent direct thrombin inhibitor selected from argatroban, melagatran, ximelagatran, and dabigatran, and wherein at least about 5% of the univalent direct thrombin inhibitor is delivered to the coronary arteries.
Inhalation prevention with coronary and left atrium delivery of univalent direct thrombin inhibitor
A method for prevention of acute coronary syndrome and/or thrombosis in a patient comprising inhaling an effective amount of a pharmaceutical composition, the pharmaceutical composition comprising an antithrombotic compound, wherein the antithrombotic compound comprises a univalent direct thrombin inhibitor selected from argatroban, melagatran, ximelagatran, and dabigatran, wherein at least about 5% of the univalent direct thrombin inhibitor is delivered to the coronary arteries and/or wherein about 10% to about 80% of the antithrombotic compound is delivered to the left atrium.
Across the independent claims, the core inventive coverage is inhalation administration of a pharmaceutical composition containing a univalent direct thrombin inhibitor with a required delivery threshold to the coronary arteries, and in the prevention method a further distribution option to the left atrium.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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