US2006269594A1PendingUtilityA1

Liposomal antineoplastic drugs and uses thereof

60
Assignee: INEX PHARMACEUTICALS CORPPriority: Jun 30, 2000Filed: May 8, 2006Published: Nov 30, 2006
Est. expiryJun 30, 2020(expired)· nominal 20-yr term from priority
Inventors:Thomas D. MaddenSean C. SempleQuet Ahkong
A61P 7/02A61P 35/00A61K 9/127A61K 9/1272A61K 9/1278A61K 31/4745A61K 45/06
60
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Claims

Abstract

This invention relates to liposomal antineoplastic agents (e.g., camptothecin) compositions and methods of using such compositions for treating neoplasia and for inhibiting angiogenesis. The compositions and methods are useful for modulating the plasma circulation half-life of an active agent.

Claims

exact text as granted — not AI-modified
1 . A method for modulating the plasma circulation half-life of an active agent, said method comprising: 
 (a) providing a liposome having free active agent and precipitated active agent encapsulated therein; and    (b) varying the amount of said active agent that is precipitated in said liposome.    
   
   
       2 . The method of  claim 1 , wherein step (b) comprises varying said active agent to lipid ratio.  
   
   
       3 . The method of  claim 2 , wherein said active agent to lipid ratio is varied by the addition of an empty liposome.  
   
   
       4 . The method of  claim 1 , wherein step (b) comprises varying the size of said liposome.  
   
   
       5 . The method of  claim 1 , wherein step (b) comprises adding a component that enhances precipitation of said active agent.  
   
   
       6 . The method of  claim 5 , wherein said component is a mono-, di-, tri-, or polyvalent anion.  
   
   
       7 . The method of  claim 1 , wherein step (b) comprises varying both said active agent to lipid ratio and the size of the liposome.  
   
   
       8 . The method of  claim 1 , wherein said active agent is an antineoplastic drug.  
   
   
       9 . The method of  claim 8 , wherein said antineoplastic drug is a camptothecin.  
   
   
       10 . The method of  claim 9 , wherein said camptothecin is a member selected from the group consisting of irinotecan, topotecan, 9-amino camptothecin, 10,11-methylenedioxy camptothecin, 9-nitro camptothecin, TAS 103, 7-(4-methyl-piperazino-methylene)-10,11-ethylenedioxy-20(S)-camptothecin and 7-(2-N-isopropylamino)ethyl)-20(S)-camptothecin.  
   
   
       11 . The method of  claim 10 , wherein said camptothecin is topotecan.  
   
   
       12 . The method of  claim 1 , wherein said active antineoplastic drug is a vinca alkaloid.  
   
   
       13 . The method of  claim 12 , wherein said vinca alkaloid is a member selected from the group consisting of vincristine, vinblastine, vinorelbine and vindesine.  
   
   
       14 . The method of  claim 1 , wherein the precipitated active agent encapsulated in said liposome is at least 50% of said total active agent.  
   
   
       15 . The method of  claim 14 , wherein the precipitated active agent encapsulated in said liposome is at least 60% of said total active agent.  
   
   
       16 . The method of  claim 15 , wherein the precipitated active agent encapsulated in said liposome is at least 70% of said total active agent.  
   
   
       17 . The method of  claim 1 , wherein said liposome comprises sphingomyelin and cholesterol.  
   
   
       18 . The method of  claim 17 , wherein said liposome comprises sphingomyelin and cholesterol in a 55:45 ratio.  
   
   
       19 . The method of  claim 1 , wherein the plasma circulation half-life of said active agent is modulated for optimum efficacy.  
   
   
       20 . The method of  claim 1 , wherein the ratio of said active agent to lipid is about 0.005-1:1 (w/w).  
   
   
       21 . The method of  claim 20 , wherein the ratio of said active agent to lipid is about 0.05-0.9:1 (w/w).  
   
   
       22 . The method of  claim 21 , wherein the ratio of said active agent to lipid is about 0.1-0.5:1 (w/w).  
   
   
       23 . A method for modulating the plasma circulation half-life of an active agent, said method comprising: 
 (a) providing a liposome having free active agent and precipitated active agent encapsulated therein; and    (b) adding a liposome with no encapsulated active agent.    
   
   
       24 . The method of  claim 23 , wherein the ratio of liposomes containing active agent to liposomes with no encapsulated agent is from about 1:0.5 to 1:1000.  
   
   
       25 . The method of  claim 24 , wherein the ratio of liposomes containing active agent to liposomes with no encapsulated agent is from about 1:1 to 1:100.  
   
   
       26 . The method of  claim 25 , wherein the ratio of liposomes containing active agent to liposomes with no encapsulated agent is from about 1:2 to 1:10.  
   
   
       27 . The method of  claim 26 , wherein the ratio of liposomes containing active agent to liposomes with no encapsulated agent is from about 1:3 to 1:5.  
   
   
       28 . The method of  claim 23 , wherein said active agent is an antineoplastic drug.  
   
   
       29 . The method of  claim 28 , wherein said antineoplastic drug is a camptothecin.  
   
   
       30 . The method of  claim 29 , wherein said camptothecin is a member selected from the group consisting of irinotecan, topotecan, 9-amino camptothecin, 10,11-methylenedioxy camptothecin, 9-nitro camptothecin, TAS 103, 7-(4-methyl-piperazino-methylene)-10,11-ethylenedioxy-20(S)-camptothecin and 7-(2-N-isopropylamino)ethyl)-20(S)-camptothecin.  
   
   
       31 . The method of  claim 30 , wherein said camptothecin is topotecan.  
   
   
       32 . A liposomal formulation, said liposomal formulation comprising: 
 a) an antineoplastic drug; and    b) a liposome having free antineoplastic drug and precipitated antineoplastic drug, wherein the precipitated antineoplastic drug in said liposome is at least 50% of the total antineoplastic drug.    
   
   
       33 . The liposomal formulation of  claim 32 , wherein said antineoplastic drug is a camptothecin.  
   
   
       34 . The liposomal formulation of  claim 33 , wherein said camptothecin is a member selected from the group consisting of irinotecan, topotecan, 9-amino camptothecin, 10,11-methylenedioxy camptothecin, 9-nitro camptothecin, TAS 103, 7-(4-methylpiperazino-methylene)-10,11-ethylenedioxy-20(S)-camptothecin and 7-(2-N-isopropylamino)ethyl)-20(S)-camptothecin.  
   
   
       35 . The liposomal formulation of  claim 34 , wherein said camptothecin is topotecan.  
   
   
       36 . The liposomal formulation of  claim 33 , wherein said antineoplastic drug is a vinca alkaloid.  
   
   
       37 . The liposomal formulation of  claim 32 , wherein the free antineoplastic drug and the precipitated antineoplastic drug are different.  
   
   
       38 . The liposomal formulation of  claim 36 , wherein said vinca alkaloid is a member selected from the group consisting of vincristine, vinblastine, vinorelbine and vindesine.  
   
   
       39 . The liposomal formulation of  claim 32 , wherein the ratio of said antineoplastic drug to lipid is about 0.005-1:1 (w/w).  
   
   
       40 . The liposomal formulation of  claim 39 , wherein the ratio of said antineoplastic drug: said lipid is about 0.05-0.9:1 (w/w).  
   
   
       41 . The liposomal formulation of  claim 40 , wherein the ratio of said antineoplastic drug: said lipid is about 0.1-0.5:1 (w/w).  
   
   
       42 . The liposomal formulation of  claim 32 , wherein said liposome comprises sphingomyelin and cholesterol.  
   
   
       43 . The liposomal formulation of  claim 42 , wherein said liposome comprises sphingomyelin and cholesterol in a 55:45 ratio.  
   
   
       44 . The liposomal formulation of  claim 32 , further comprising a liposome with no encapsulated active agent.  
   
   
       45 . The liposomal formulation of  claim 44 , wherein the ratio of liposomes containing active agent to liposomes with no encapsulated agent is from about 1:0.5 to 1:1000.  
   
   
       46 . The liposomal formulation of  claim 45 , wherein the ratio of liposomes containing active agent to liposomes with no encapsulated agent is from about 1:1 to 1:100.  
   
   
       47 . The liposomal formulation of  claim 46 , wherein the ratio of liposomes containing active agent to liposomes with no encapsulated agent is from about 1:2 to 1:10.  
   
   
       48 . The liposomal formulation of  claim 47 , wherein the ratio of liposomes containing active agent to liposomes with no encapsulated agent is from about 1:3 to 1:5.  
   
   
       49 . A liposomal formulation, said liposomal formulation comprising: 
 a) an active agent;    b) a liposome having free active agent and precipitated active agent encapsulated therein; and    c) an empty liposome.    
   
   
       50 . The liposomal formulation of  claim 49 , wherein the ratio of liposomes containing said active agent to said empty liposomes is from about 1:0.5 to 1:1000.  
   
   
       51 . The liposomal formulation of  claim 50 , wherein the ratio of liposomes containing said active agent to said empty liposomes is from about 1:1 to 1:100.  
   
   
       52 . The liposomal formulation of  claim 51 , wherein the ratio of liposomes containing said active agent to said empty liposomes is from about 1:2 to 1:10.  
   
   
       53 . The liposomal formulation of  claim 52 , wherein the ratio of liposomes containing said active agent to said empty liposomes is from about 1:3 to 1:5.  
   
   
       54 . The liposomal formulation of  claim 49 , wherein said active agent is an antineoplastic drug.  
   
   
       55 . The liposomal formulation of  claim 54 , wherein said antineoplastic drug is a camptothecin.  
   
   
       56 . The liposomal formulation of  claim 55 , wherein said camptothecin is a member selected from the group consisting of irinotecan, topotecan, 9-amino camptothecin, 10,11-methylenedioxy camptothecin, 9-nitro camptothecin, TAS 103, 7-(4-methylpiperazino-methylene)-10,11-ethylenedioxy-20(S)-camptothecin and 7-(2-N-isopropylamino)ethyl)-20(S)-camptothecin.  
   
   
       57 . The liposomal formulation of  claim 56 , wherein said camptothecin is topotecan.  
   
   
       58 . The liposomal formulation of  claim 57 , wherein said antineoplastic drug is a vinca alkaloid.  
   
   
       59 . The liposomal formulation of  claim 58 , wherein said vinca alkaloid is a member selected from the group consisting of vincristine, vinblastine, vinorelbine and vindesine.  
   
   
       60 . The liposomal formulation of  claim 49 , wherein the ratio of said active agent to lipid is about 0.005-1:1 (w/w).  
   
   
       61 . The liposomal formulation of  claim 60 , wherein the ratio of said active agent to lipid is about 0.05-0.9:1 (w/w).  
   
   
       62 . The liposomal formulation of  claim 61 , wherein the ratio of said active agent to lipid is about 0.1-0.5:1 (w/w).  
   
   
       63 . The liposomal formulation of  claim 49 , wherein said liposome comprises sphingomyelin and cholesterol.

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