Abstract Pharmaceutical compositions containing a 57 amino acid protease inhibitor and uses for those compositions are taught. The protease inhibitor is referred to as A4i which is associated with Alzheimer's disease. In addition to the A4i protease, other analogs are taught as are pharmaceutical compositions containing such analogs and their uses in treating a variety of abnormalities associated with Kunitz-type basic protease inhibitors. For example, it has been found that pharmaceutical compositions containing A4i protease and analogs thereof inhibit plasmin and tryptase, and also inhibit pancreatic trypsin, alpha-chymotrypsin, tissue kallikrein and serum kallikrein. In that certain diseases are associated with a general release of proteases such as trypsin, chymotrypsin and elastase into the circulatory system pharmaceutical compositions containing A4i and analogs thereof can be used in the management of such diseases.
A method of treating an individual having excessive activity of serine proteases, comprising: administering to the individual in need thereof a pharmaceutically effective amount of the composition, comprising: a pharmaceutically acceptable carrier; and a protein analog wherein the amino acid corresponding to arginine at position 13 in the sequence ##STR9## is substituted with a neutral hydrophobic amino acid.
Claim 2
Independent Claim
58 words
A method of treating an individual having excessive activity of serine proteases, comprising: administering to the individual in need thereof a pharmaceutically effective amount of the composition, comprising: a pharmaceutically acceptable carrier; and a protein analog wherein the amino acid corresponding to arginine at position 13 in the sequence ##STR9## is substituted with a neutral hydrophobic amino acid.
Claim 3
Dependent Claim
26 words
The method as claimed in claim 1, wherein the serine protease inhibited by the protein analog is elastase and the neutral hydrophobic amino acids is valine.
Claim 4
Dependent Claim
18 words
The method as claimed in claim 1, wherein the excessive activity of serine proteases is associated with emphysema.