Methods and compositions using terfenadine metabolites in combination with leukotriene inhibitors

Abstract

Methods and pharmaceutical compositions employing a terfenadine metabolite and a leukotriene inhibitor for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof. Also included are methods and compositions employing a terfenadine metabolite, a leukotriene inhibitor, and a decongestant for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof.

Description

1. FIELD OF THE INVENTION[0001] The invention relates to methods of treating asthma, allergic conditions, and inflammation. In another aspect, this invention relates to the use of antihistamines and leukotriene inhibitors, and to compositions containing them.2. BACKGROUND OF THE INVENTION[0002] Terfenadine is an antagonist of the H-1 histamine receptor protein, which mediates the response antagonized by conventional antihistamines. Terfenadine is well absorbed but is extensively metabolized. See Okerholm et al., Biopharmaceutics and Drug Distribution, 2: 185-190 (1981). Two main metabolites have been identified and one of the metabolites, fexofenadine, chemically named 4-[1-hydroxy-4[4-(hydroxydiphenylmethyl-1--piperidinyl)butyl]-.alpha.,.alpha.-dimethylbenzeneacetic acid, is reported to have antihistaminic activity. See Gartiez et al., Arzneimittel Forschung / Drug-Research; 32: 1185-1190 (1982).[0003] Recently, the FDA has approved the use of fexofenadine as a prescription antihista...

AI Technical Summary

Benefits of technology

0021] The invention encompasses the treatment, prevention, and/or management of asthma, the symptoms of asthma, dermatitis, allergic rhinitis, or inflammation using a metabolite of terfenadine, preferably fexofenadine, and a leukotriene inhibitor. The invention also encompasses the treatment, prevention, and/or management of these disorders with a terfenadine metabolite, a leukotriene inhibitor, and optionally a decongestant. The invention encompasses the treatment, prevention, and/or management of these disorders using a single unit dosage form that contains a terfenadine metabolite, a leukotriene inhibitor and optionally a decongestant, such that a terfenadine metabolite and a leukotriene inhibitor or all three active ingredients are used. However, it should be recognized that combination th

Problems solved by technology

The study further mentioned a possible mechanism for loratadine and terfenadine, but concluded that the mechanism does not appear to warrant great attention for drug development.

Compounds within the class of non-sedating