Use of an angiogenesis inhibitor as a lead compound in drug development

Abstract

The present invention provides a treatment for angiogenic diseases, including solid tumors. The treatment consists of administering therapeutically active dosages of FC101, resulting in a reduction in endothelial cell proliferation and inhibition of new blood vessel formation. FC101 can also be used as a lead compound to develop other pharmacologically-active compounds, by adding or substituting different functional groups for those already present on the FC101 molecule.

What is claimed is:  
     
         1 . A method for inhibiting angiogenesis in human or animal patients, comprising administering to said patients a therapeutically active dosage of a water soluble fusarochromanone isolated from fungal cultures, wherein said water soluble fusarochromanone is administered via a pharmaceutically or veterinarily acceptable carrier, for a time effective to inhibit the formation of new blood vessels in said patient.  
     
     
         2 . A method according to    claim 1   , wherein said water soluble fusarochromanone is chosen from the group consisting of FC101 and an FC101 analog.  
     
     
         3 . A method according to    claim 1   , wherein said water soluble fusarochromanone is FC101.  
     
     
         4 . A method according to    claim 1   , wherein said water soluble fusarochromanone is isolated from fungal cultures chosen from the group consisting of members of the Fusarium genera.  
     
     
         5 . A method according to    claim 4   , wherein said water soluble fusarochromanone is isolated from  Fusarium equiseti  fungal cultures.  
     
     
         6 . A method according to    claim 1   , wherein said water soluble fusarochromanone is a synthetic form of FC101.  
     
     
         7 . A method according to    claim 1   , wherein said administration is chosen from the group consisting of administration via mucosal administration (e.g., oral, nasal, anal, vaginal) or a parenteral route (e.g., intradermal, intramuscular, subcutaneous, intravenous, intraperitoneal).  
     
     
         8 . A method according to    claim 1   , wherein the therapeutic dosage is in the range of about 0.2 μg to about 200 g.  
     
     
         9 . A method for treating angiogenic diseases in human or animal patients comprising administering to said patients a therapeutically active dosage of a water soluble fusarochromanone, wherein said water soluble fusarochromanone is administered via a pharmaceutically or veterinarily acceptable carrier for a time effective to treat the angiogenic disease.  
     
     
         10 . A method according to    claim 9   , wherein said water soluble fusarochromanone is chosen from the group consisting of FC101 and an FC101 analog.  
     
     
         11 . A method according to    claim 9   , wherein said water soluble fusarochromanone is FC101.  
     
     
         12 . A method according to    claim 9   , wherein said water soluble fusarochromanone is a synthetic form of FC101.  
     
     
         13 . A method according to    claim 9   , wherein said water soluble fusarochromanone is isolated from fungal cultures chosen from the group consisting of members of the Fusarium genera.  
     
     
         14 . A method according to    claim 13   , wherein said water soluble fusarochromanone is isolated from  Fusarium equiseti  fungal cultures.  
     
     
         15 . A method according to    claim 9   , wherein said angiogenic disease is chosen from the group consisting of solid tumors, psoriasis, arthritis, and diabetic retinopathy.  
     
     
         16 . A method according to    claim 9   , wherein the therapeutic dosage is in the range of about 0.2 μg to about 200 g.  
     
     
         17 . A method for using FC101 as a lead compound to develop therapeutically active analogs, said method comprising the steps of: 
 a) identifying a functional group member attached via a chemical bond to the structural backbone of the FC101 parent molecule, said members chosen from the group consisting of methyl, hydroxyl, amino, and acetyl functional groups.    b) breaking the chemical bond joining said functional group member to said structural backbone of said FC101 parent molecule;    c) removing said functional group member; and    d) chemically joining a second member of said functional group to said structural backbone of said FC101 parent molecule.    
     
     
         18 . A method for selectively inhibiting endothelial cell proliferation in human or animal patients, comprising treating said cells with a therapeutically active dosage of a water soluble fusarochromanone isolated from fungal cultures, wherein said fusarochromanone is administered in a pharmaceutically or veterinarily acceptable carrier for a time effective to inhibit endothelial cell proliferation in said patient.  
     
     
         19 . A method according to    claim 18   , wherein said water soluble fusarochromanone is chosen from the group consisting of FC101 and an FC101 analog.  
     
     
         20 . A method according to    claim 18   , wherein said water soluble fusarochromanone is FC101.  
     
     
         21 . A method according to    claim 18   , wherein said water soluble fusarochromanone is a synthetic form of FC101.  
     
     
         22 . A method according to    claim 18   , wherein said water soluble fusarochromanone is isolated from fungal cultures chosen from the group consisting of members of the Fusarium genera.  
     
     
         23 . A method according to    claim 22   , wherein said water soluble fusarochromanone is isolated from  Fusarium equiseti  fungal cultures.