Ketoconazole enantiomer in humans

Abstract

Treatment of patients with the 2S,4R ketoconazole enantiomer or its pharmaceutically acceptable salts, and solvates is useful for reducing systemic inflammation and cholesterol levels and improving glycemic control.

1 . A method of treating a patient that is diabetic, non-diabetic with elevated cortisol, or non-diabetic with elevated cholesterol comprising
 co-administering a 3-hydroxy 3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor and a composition to said patient, wherein the composition comprises a therapeutically effective amount of a 2S,4R ketoconazole enantiomer, wherein the composition does not comprise a therapeutically effective amount of a 2R,4S ketoconazole enantiomer.   
     
     
         2 . The method of  claim 1 , wherein administration of the HMG-CoA reductase inhibitor is contraindicated in the patient in the absence of administration of the ketoconazole enantiomer. 
     
     
         3 . The method of  claim 1 , wherein the HMG-CoA reductase inhibitor is selected from the group consisting of lovastatin, simvastatin, pravastatin, fluvastatin, atorvastatin, rosuvastatin, itavastatin, ZD-4522, and rivastatin. 
     
     
         4 . The method of  claim 1 , wherein the patient is non-diabetic with elevated cortisol. 
     
     
         5 . The method of  claim 1 , wherein the HMG CoA reductase inhibitor is a cholesterol-lowering HMG CoA reductase inhibitor. 
     
     
         6 . The method of  claim 1 , wherein the patient is non-diabetic with elevated cholesterol. 
     
     
         7 . The method of  claim 1 , wherein the therapeutically effective amount of the 2S,4R ketoconazole enantiomer is a daily dose of from 100 mg to 600 mg. 
     
     
         8 . The method of  claim 1 , wherein the therapeutically effective amount of the 2S,4R ketoconazole enantiomer is a daily dose of 400 mg. 
     
     
         9 . The method of  claim 1 , wherein the composition is free of the 2R,4S ketoconazole enantiomer.