Sigma-1 receptor agonist systolic blood pressure therapy

Inventors

Missling, Christopher U.

Assignees

Anavex Life Sciences Corp

Abstract

A method for lowering systolic blood pressure in a patient exhibiting resistance to a antihypertensive therapy with one or more drugs, the method comprising administering to the patient ANAVEX®2-73 at a dose and frequency effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, 24-hour ambulatory systolic, and maximum diurnal systolic blood pressures.

Core Innovation

The disclosed invention relates to methods of treating hypertension and lowering blood pressure by administering tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine, a salt thereof, and/or any combination thereof. The methods are directed to providing a therapeutically effective amount to a subject in need thereof. The document further identifies resistance to antihypertensive therapy with one or more antihypertensive drugs other than the therapeutic agent as a patient characteristic associated with the described approach.

The document describes lowering of blood pressure in terms of reductions of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, 24-hour ambulatory systolic, and maximum diurnal systolic blood pressures. These blood pressure parameters are presented together with the characterization of a subject who exhibits resistance to antihypertensive therapy with antihypertensive drugs other than the therapeutic agent. The described therapeutic agent is tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine, including salt forms such as tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX®2-73; A2-73).

The document also describes combination approaches in which the therapeutic agent is administered in combination with an antihypertensive drug, where the combination is administered at a dose and frequency effective to provide a reduction of at least about 3 mmHg in one or more of trough sitting systolic, 24-hour ambulatory systolic, and maximum diurnal systolic blood pressures. Co-administered antihypertensive drugs are restricted to classes including beta blockers, thiazine diuretics, ACE inhibitors, and calcium channel blockers, and the methods can specify administration frequency and intermittent dosing cycles comprising a dosing period and a resting period.

Claims Coverage

The independent claims cover three method categories: (i) treating hypertension by administering a therapeutically effective amount of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine (and/or salts/combination), (ii) lowering blood pressure in resistant subjects by achieving at least about a 3 mmHg reduction in specified blood pressure parameters, and (iii) lowering blood pressure by administering the therapeutic agent in combination with an antihypertensive drug to achieve at least about a 3 mmHg reduction in specified blood pressure parameters. Across these claims, the document ties the inventive scope to (a) selected blood pressure endpoints and thresholds and (b) patient resistance to other antihypertensive therapy in one branch, and (c) co-administration with specified antihypertensive drug classes in another branch.

The claim coverage focuses on hypertension treatment and blood-pressure lowering using tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine (including salts such as A2-73 hydrochloride). The core limiting features are a therapeutically effective amount for treating hypertension, achieving at least about a 3 mmHg reduction in defined trough sitting/24-hour ambulatory/maximum diurnal systolic endpoints, and tailoring the method to therapy-resistant subjects and/or co-administering the therapeutic agent with specified antihypertensive drug classes.

Stated Advantages

Documented Applications