Dissolution of Arterial Cholesterol Plaques by Pharmacologically Induced Elevation of Endogenous Bile Salts
AssigneeZ & Z Medical Holdings, Inc.
InventorsFiliberto P. Zadini, Giorgio C. Zadini
Life of this patent
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Abstract
A group of pharmaceutical substances induce elevation of endogenous bile salts and acids via different mechanisms. The elevated circulating bile salts exert a beneficial effect in atherosclerosis by acting both as atherolytic and antiatherogenic agents. The result of the elevated circulating endogenous bile salt is the dissolution of cholesterol/lipidic aggregates of the atherosclerotic plaques.
Claims36
The use of at least two of (i)-(vii) below:
- (i) ketoconazole or a pharmaceutically acceptable salt, conjugate, hydrate, solvate, polymorph, or mixture thereof;
- (ii) trichloroethylene or a pharmaceutically acceptable salt, conjugate, hydrate, solvate, polymorph, or mixture thereof;
- (iii) troglitazone or a pharmaceutically acceptable salt, conjugate, hydrate, solvate, polymorph, or mixture thereof;
- (iv) bosentan or a pharmaceutically acceptable salt, conjugate, hydrate, solvate, polymorph, or mixture thereof;
- (v) saquinavir or a pharmaceutically acceptable salt, conjugate, hydrate, solvate, polymorph, or mixture thereof;
- (vi) ritonavir or a pharmaceutically acceptable salt, conjugate, hydrate, solvate, polymorph, or mixture thereof;
- and
- (vii) efavirenz or a pharmaceutically acceptable salt, conjugate, hydrate, solvate, polymorph, or mixture thereof;
- for the manufacture of a medicament useful for treating atherosclerotic plaque.
A pharmaceutical formulation, for treating atherosclerosis in a mammal, comprising:
- a combination of at least two of (i)-(vii) below:
- (i) ketoconazole or a pharmaceutically acceptable salt, conjugate, hydrate, solvate, polymorph, or mixture thereof;
- (ii) trichloroethylene or a pharmaceutically acceptable salt, conjugate, hydrate, solvate, polymorph, or mixture thereof;
- (iii) troglitazone or a pharmaceutically acceptable salt, conjugate, hydrate, solvate, polymorph, or mixture thereof;
- (iv) bosentan or a pharmaceutically acceptable salt, conjugate, hydrate, solvate, polymorph, or mixture thereof;
- (v) saquinavir or a pharmaceutically acceptable salt, conjugate, hydrate, solvate, polymorph, or mixture thereof;
- (vi) ritonavir or a pharmaceutically acceptable salt, conjugate, hydrate, solvate, polymorph, or mixture thereof;
- (vii) efavirenz or a pharmaceutically acceptable salt, conjugate, hydrate, solvate, polymorph, or mixture thereof;
- wherein the combination is in an amount effective to result in an amount of increased diversion of a bile acid, from an enterohepatic circulation to the systemic circulation of the mammal, sufficient to result in an amount of emulsification of an atherosclerotic plaque in an artery of the mammal sufficient to result in regression of the plaque.
A method, of treating atherosclerosis in a mammal, comprising administering to a mammal a pharmaceutical formulation in an amount effective to result in an amount of increased diversion of a bile acid, from an enterohepatic circulation to the systemic circulation of the mammal, sufficient to result in an amount of emulsification of an atherosclerotic plaque in an artery of the mammal sufficient to result in regression of the plaque.
Dependencies are inferred from the claim text.