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-10668015-B2
Publication Date
2020-06-02
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 disclosure provides a method for prophylactic treatment of acute coronary syndrome (ACS) by administering, by inhalation, an aerosolized liquid pharmaceutical composition comprising argatroban to a subject in need thereof. The subject is suffering from acute coronary syndrome, and the prophylactic method includes administering an effective amount of the composition. The effective amount is between about 0.1 and 150 mg/kg.
The disclosure further requires that at least about 5% of the pharmaceutical composition is delivered to the coronary arteries. In addition, delivery constraints to cardiac structures are emphasized, including a delivery fraction of 10% to 80% to the left atrium. The disclosure also specifies a left atrium peak constraint in which the amount reaches peak in the left atrium between 30 seconds and 180 minutes after starting administration.
The disclosure supports prophylactic outcomes by focusing on pharmacokinetic and pharmacodynamic behavior in the left atrium rather than only systemic exposure. The disclosure includes quantitative pharmacodynamic constraints, such as producing a ratio of factor Xa to factor IIa activity of at least 0.07 in the left atrium. The inhaled aerosol is described as an aerosolized liquid pharmaceutical composition, with dependent refinements including aerosol particle size constraints such as a mass median aerodynamic diameter of less than 10 μm.
Claims Coverage
One independent method claim is provided, focused on prophylactic ACS treatment by inhalation of an aerosolized liquid argatroban composition with coronary-artery delivery requirements.
Prophylactic ACS inhalation of argatroban aerosol
A method for prophylactic treatment of acute coronary syndrome (ACS) comprising administering, by inhalation, an effective amount of an aerosolized liquid pharmaceutical composition comprising argatroban to a subject in need thereof where the subject is suffering from acute coronary syndrome.
Effective argatroban dose range
The method wherein the effective amount is between about 0.1 and 150 mg/kg.
Coronary-artery delivery fraction
The method wherein at least about 5% of the pharmaceutical composition is delivered to the coronary arteries.
Left atrium delivery fraction
The method wherein 10% to 80% of the administered pharmaceutical composition reaches the left atrium.
Left atrium peak timing after administration
The method wherein the administered pharmaceutical composition reaches peak amount in the left atrium between 30 seconds and 180 minutes after starting administration.
Left atrium factor activity ratio
The method wherein the pharmaceutical composition produces, in the left atrium, a ratio of factor Xa to factor IIa activity of at least 0.07.
Aerosol particle size constraint
A method including aerosolizing a liquid composition having a mass median aerodynamic diameter of less than 10 μm.
The independent claim focuses on prophylactic ACS treatment by inhalation of an aerosolized liquid pharmaceutical composition comprising argatroban, with an effective dose range and a required delivery fraction to the coronary arteries. The claimed features further constrain left atrium delivery fraction, left atrium peak timing, left atrium factor Xa to factor IIa activity ratio, and aerosol particle size.
Stated Advantages
Documented Applications
No documented applications found
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