US2006040903A1PendingUtilityA1

Methods of use related to xerostomia

54
Assignee: STOGNIEW MARTINPriority: Dec 9, 1997Filed: Oct 25, 2005Published: Feb 23, 2006
Est. expiryDec 9, 2017(expired)· nominal 20-yr term from priority
Inventors:Martin StogniewDavid S. AlbertsEdward H. Kaplan
A61P 9/10A61P 43/00A61P 39/02A61P 29/00A61P 27/16A61P 25/00A61P 25/02A61P 35/00A61P 31/12A61P 31/04A61K 31/135A61K 31/195A61K 31/13A61P 21/00A61K 45/06A61P 13/12A61P 17/14A61P 19/02A61P 11/00A61P 1/02A61P 17/16A61K 31/661A61K 31/426A61P 15/08A61K 31/66A61K 31/16A61K 31/145
54
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Claims

Abstract

The present invention relates to new uses of thermally stable, crystalline S-2-(3-aminopropylamino)ethyl dihydrogen phosphorothioate, (amifostine) and other aminothiol compounds to treat and reverse toxicities caused by radiation treatment. In particular, the invention provides a method for treating or preventing xerostomia associated with the administration of radiation treatment of head and neck cancer.

Claims

exact text as granted — not AI-modified
1 . A method for treating xerostomia associated with radiation therapy for head and neck cancer in a human, which comprises administering to said human a therapeutically effective amount of a dosage form comprising a thermally stable, sterile, crystalline compound of the formula:  
       R 1 NH(CH 2 ) n NH(CH 2 ) m SR 2    
     or a pharmaceutically acceptable addition salt or hydrate thereof, wherein 
 R 1  is hydrogen, C 5 -C 7  aryl, C 2 -C 7  acyl, or C 1 -C 7  alkyl;  
 R 2  is hydrogen, PO 3 H 2  or R 3  wherein R 3  is R 1 NH(CH 2 ) n NH(CH 2 ) m S—;  
 n is an integer from 1 to 10; and  
 m is an integer from 1 to 10.  
 
   
   
       2 . The method of  claim 1 , wherein R 2  is PO 3 H 2 .  
   
   
       3 . The method of  claim 2 , wherein R 1  is hydrogen.  
   
   
       4 . The method of  claim 3 , wherein n is 3 and m is 2.  
   
   
       5 . The method of  claim 4 , wherein the compound is a thermally stable, sterile, crystalline amifostine hydrate.  
   
   
       6 . The method of  claim 5 , wherein the compound is thermally stable, sterile, crystalline amifostine trihydrate.  
   
   
       7 . The method of  claim 6 , wherein the crystalline amifostine trihydrate exhibits substantially the crystal structure having a space group of P2 1 2 1 2, and cell dimensions of about a=8.46 Å, b=21.55 Å and c=6.76 Å.  
   
   
       8 . The method of  claim 6 , wherein the crystalline amifostine trihydrate forms less than about 2% 2-[(3-aminopropyl)amino]ethane thiol when sealed in a nitrogen filled vial and heated to 40° C. for one week.  
   
   
       9 . The method of  claim 6 , wherein the crystalline amifostine trihydrate forms less than about 2% 2-[(3-aminopropyl)amino]ethane thiol when sealed in a nitrogen filled vial and heated to 40° C. for four weeks.  
   
   
       10 . The method of  claim 6 , wherein the crystalline amifostine trihydrate is thermally stable at about 4° C. for at least two years.  
   
   
       11 . The method of  claim 6 , wherein the crystalline amifostine trihydrate is thermally stable at about ambient temperature for at least two years.  
   
   
       12 . The method of  claim 1 , wherein the dosage form further comprises an excipient.  
   
   
       13 . The method of  claim 12 , wherein the excipient is mannitol.  
   
   
       14 . The method of  claim 1 , wherein the dosage form is lyophilized.  
   
   
       15 . The method of  claim 6 , wherein the dosage form comprises 500 mg of amifostine on an anhydrous basis.  
   
   
       16 . The method of  claim 1 , wherein the amount of the crystalline compound administrated is from about 10 to 1000 mg/m 2 .  
   
   
       17 . The method of  claim 1 , wherein the amount of the crystalline compound administrated is from about 200 to 750 mg/m 2 .  
   
   
       18 . The method of  claim 1 , wherein the amount of the crystalline compound administrated is about 750 mg/m 2 .  
   
   
       19 . The method of  claim 1 , wherein the dosage form is administrated before the radiation therapy.  
   
   
       20 . The method of  claim 1 , wherein the dosage form is administrated after the radiation therapy.  
   
   
       21 . The method of  claim 1 , wherein the dosage form is administrated during the radiation therapy.  
   
   
       22 . A method for treating xerostomia associated with radiation therapy for head and neck cancer in a human, which comprises administering to said human a therapeutically effective amount of a dosage form comprising a thermally stable, sterile, crystalline amifostine.  
   
   
       23 . The method of  claim 22 , wherein the crystalline amifostine is an amifostine hydrate.  
   
   
       24 . The method of  claim 23 , wherein the crystalline amifostine is an amifostine trihydrate.  
   
   
       25 . The method of  claim 24 , wherein the crystalline amifostine trihydrate exhibits substantially the crystal structure having a space group of P2 1 2 1 2 1  and cell dimensions of about a=8.46 Å, b=21.55 Å and c=6.76 Å.  
   
   
       26 . The method of  claim 25 , wherein the crystalline amifostine trihydrate forms less than about 2% 2-[(3-aminopropyl)amino]ethane thiol when sealed in a nitrogen filled vial and heated to 40° C. for one week.  
   
   
       27 . The method of  claim 25 , wherein the crystalline amifostine trihydrate forms less than about 2% 2-[(3-aminopropyl)amino]ethane thiol when sealed in a nitrogen filled vial and heated to 40° C. for four weeks.  
   
   
       28 . The method of  claim 25 , wherein the crystalline amifostine trihydrate is thermally stable at about 4° C. for at least two years.  
   
   
       29 . The method of  claim 25 , wherein the crystalline amifostine trihydrate is thermally stable at about ambient temperature for at least two years.  
   
   
       30 . The method of  claim 22  where the dosage form is lyophilized.  
   
   
       31 . The method of  claim 22 , wherein the dosage form further comprises an excipient.  
   
   
       32 . The method of  claim 31 , wherein the excipient is mannitol.  
   
   
       33 . The method of  claim 22 , wherein the dosage form comprises 500 mg of amifostine on an anhydrous basis.  
   
   
       34 . The method of  claim 22 , wherein the amount of the crystalline compound administrated is from about 10 to 1000 mg/m 2 .  
   
   
       35 . The method of  claim 22 , wherein the amount of the crystalline compound administrated is from about 200 to 750 mg/m 2 .  
   
   
       36 . The method of  claim 22 , wherein the amount of the crystalline compound administrated is about 750 mg/m 2 .  
   
   
       37 . The method of  claim 22 , wherein the dosage form is administrated before the radiation therapy.  
   
   
       38 . The method of  claim 22 , wherein the dosage form is administrated after the radiation therapy.  
   
   
       39 . The method of  claim 22 , wherein the dosage form is administrated during the radiation therapy.

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