US2003124055A1PendingUtilityA1

Water soluble paclitaxel derivatives

63
Assignee: PG TXL CO LPPriority: Mar 12, 1996Filed: Dec 5, 2002Published: Jul 3, 2003
Est. expiryMar 12, 2016(expired)· nominal 20-yr term from priority
Inventors:Chun LiSidney WallaceDong-Fang YuDavid J. Yang
A61K 47/60A61K 47/59A61K 38/13A61L 2300/606C08G 73/1092A61L 2300/416A61K 31/337A61K 47/645A61P 35/02A61K 51/0497A61L 31/16A61K 51/065A61K 2121/00A61P 35/04A61L 31/10A61K 2123/00A61P 35/00A61K 41/0038A61K 47/547A61K 31/4375
63
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Claims

Abstract

Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble polymer such as poly-glutamic acid, poly-aspartic acid or poly-lysine. Also disclosed are methods of using the compositions for treatment of tumors, auto-immune disorders such as rheumatoid arthritis. Other embodiments include the coating of implantable stents for prevention of restenosis.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A method for determining the uptake of a chemotherapeutic drug by tumor tissue, comprising delivering a conjugate of a chemotherapeutic drug and a first water soluble chelator and detecting the presence of said conjugate in said tumor tissue.  
     
     
         2 . The method of  claim 1 , wherein said chemotherapeutic drug comprises a taxoid.  
     
     
         3 . The method of  claim 2 , wherein said taxoid comprises paclitaxel.  
     
     
         4 . The method of  claim 2 , wherein said taxoid comprises docetaxel.  
     
     
         5 . The method of  claim 1 , wherein said chemotherapeutic drug comprises etoposide.  
     
     
         6 . The method of  claim 1 , wherein said chemotherapeutic drug comprises teniposide.  
     
     
         7 . The method of  claim 1 , wherein said chemotherapeutic drug comprises camptothecin.  
     
     
         8 . The method of  claim 1 , wherein said chemotherapeutic drug comprises epothilone.  
     
     
         9 . The method of  claim 1 , wherein said chemotherapeutic drug comprises a radioactive isotope.  
     
     
         10 . The method of  claim 9 , wherein said chemotherapeutic drug comprises a taxoid.  
     
     
         11 . The method of  claim 10 , wherein said taxoid comprises paclitaxel.  
     
     
         12 . The method of  claim 10 , wherein said taxoid comprises docetaxel.  
     
     
         13 . The method of  claim 9 , wherein said chemotherapeutic drug comprises etoposide.  
     
     
         14 . The method of  claim 9 , wherein said chemotherapeutic drug comprises teniposide.  
     
     
         15 . The method of  claim 9 , wherein said chemotherapeutic drug comprises camptothecin.  
     
     
         16 . The method of  claim 9 , wherein said chemotherapeutic drug comprises epothilone.  
     
     
         17 . The method of  claim 9 , wherein said first water soluble chelator is selected from group consisting of diethylenetriaminepentaacetic acid (DTPA), ethylenediaminetetraacetic acid (EDTA), 1,4,7,10-tetraazacyclododecane-N,N′,N,″N′″ tetraacetate (DOTA), tetraazacyclotetradecane-N,N″,N′ ‘N′’-tetraacetic acid (TETA), hydroxyethylidene diphosphonate (HEDP), dimercaptosuccinic acid (DMSA), diethylenetriaminetetramethylenephosphonic acid (DTTP) and 1-(ρ-aminobenzyl)-DTPA, 1,6-diamino hexane-N,N,N′,N′-tetraacetic acid, DPDP, and ethylenebis (oxyethylenenitrilo)-tetraacetic acid.  
     
     
         18 . The method of  claim 17 , wherein said chemotherapeutic drug comprises a taxoid.  
     
     
         19 . The method of  claim 18 , wherein said taxoid comprises paclitaxel.  
     
     
         20 . The method of  claim 18 , wherein said taxoid comprises docetaxel.  
     
     
         21 . The method of  claim 17 , wherein said chemotherapeutic drug comprises etoposide.  
     
     
         22 . The method of  claim 17 , wherein said chemotherapeutic drug comprises teniposide.  
     
     
         23 . The method of  claim 17 , wherein said chemotherapeutic drug comprises camptothecin.  
     
     
         24 . The method of  claim 17 , wherein said chemotherapeutic drug comprises epothilone.  
     
     
         25 . The method of  claim 17 , wherein said conjugate further comprises a second water soluble chelator.  
     
     
         26 . The method of  claim 25 , wherein said chemotherapeutic drug comprises a taxoid.  
     
     
         27 . The method of  claim 26 , wherein said taxoid comprises paclitaxel.  
     
     
         28 . The method of  claim 26 , wherein said taxoid comprises docetaxel.  
     
     
         29 . The method of  claim 25 , wherein said chemotherapeutic drug comprises etoposide.  
     
     
         30 . The method of  claim 25 , wherein said chemotherapeutic drug comprises teniposide.  
     
     
         31 . The method of  claim 25 , wherein said chemotherapeutic drug comprises camptothecin.  
     
     
         32 . The method of  claim 25 , wherein said chemotherapeutic drug comprises epothilone.  
     
     
         33 . The method of  claim 25 , wherein said second water soluble chelator is a metal ion.  
     
     
         34 . The method of  claim 33 , wherein said chemotherapeutic drug comprises a taxoid.  
     
     
         35 . The method of  claim 34 , wherein said taxoid comprises paclitaxel.  
     
     
         36 . The method of  claim 34 , wherein said taxoid comprises docetaxel.  
     
     
         37 . The method of  claim 33 , wherein said chemotherapeutic drug comprises etoposide.  
     
     
         38 . The method of  claim 33 , wherein said chemotherapeutic drug comprises teniposide.  
     
     
         39 . The method of  claim 33 , wherein said chemotherapeutic drug comprises camptothecin.  
     
     
         40 . The method of  claim 33 , wherein said chemotherapeutic drug comprises epothilone.  
     
     
         41 . The method of  claim 33 , wherein said metal ion is selected from the group consisting of aluminum, boron, calcium, chromium, cobalt, copper, dysprosium, erbium, europium, gadolinium, gallium, germanium, holmium, indium, iridium, iron, magnesium, manganese, nickel, platinum, rhenium, rubidium, ruthenium, samarium, sodium, technetium, thallium, tin, yttrium or zinc.  
     
     
         42 . The method of  claim 41 , wherein said chemotherapeutic drug comprises a taxoid.  
     
     
         43 . The method of  claim 42 , wherein said taxoid comprises paclitaxel.  
     
     
         44 . The method of  claim 42 , wherein said taxoid comprises docetaxel.  
     
     
         45 . The method of  claim 41 , wherein said chemotherapeutic drug comprises etoposide.  
     
     
         46 . The method of  claim 41 , wherein said chemotherapeutic drug comprises teniposide.  
     
     
         47 . The method of  claim 41 , wherein said chemotherapeutic drug comprises camptothecin.  
     
     
         48 . The method of  claim 41 , wherein said chemotherapeutic drug comprises epothilone.  
     
     
         49 . The method of  claim 33 , wherein said metal ion comprises a radionuclide.  
     
     
         50 . The method of  claim 49 , wherein said chemotherapeutic drug comprises a taxoid.  
     
     
         51 . The method of  claim 50 , wherein said taxoid comprises paclitaxel.  
     
     
         52 . The method of  claim 50 , wherein said taxoid comprises docetaxel.  
     
     
         53 . The method of  claim 49 , wherein said chemotherapeutic drug comprises etoposide.  
     
     
         54 . The method of  claim 49 , wherein said chemotherapeutic drug comprises teniposide.  
     
     
         55 . The method of  claim 49 , wherein said chemotherapeutic drug comprises camptothecin.  
     
     
         56 . The method of  claim 49 , wherein said chemotherapeutic drug comprises epothilone.  
     
     
         57 . The method of  claim 49 , wherein said radionuclide is selected from the group consisting of of  67 Ga,  68 Ga,  166 Ho,  111 In,  99m Tc,  90 Y,  114m Sn and  193m Pt.  
     
     
         58 . The method of  claim 57 , wherein said chemotherapeutic drug comprises a taxoid.  
     
     
         59 . The method of  claim 58 , wherein said taxoid comprises paclitaxel.  
     
     
         60 . The method of  claim 58 , wherein said taxoid comprises docetaxel.  
     
     
         61 . The method of  claim 57 , wherein said chemotherapeutic drug comprises etoposide.  
     
     
         62 . The method of  claim 57 , wherein said chemotherapeutic drug comprises teniposide.  
     
     
         63 . The method of  claim 57 , wherein said chemotherapeutic drug comprises camptothecin.  
     
     
         64 . The method of  claim 57 , wherein said chemotherapeutic drug comprises epothilone.  
     
     
         65 . The method of  claim 57  wherein said conjugate comprises  111 In-DTPA paclitaxel.  
     
     
         66 . The method of  claim 41 , wherein said conjugate comprises Na-DTPA-paclitaxel.  
     
     
         67 . A conjugate comprising a chemotherapeutic drug and a water soluble chelator, wherein said water soluble chelator is a metal ion.  
     
     
         68 . The method of  claim 67 , wherein said chemotherapeutic drug comprises a taxoid.  
     
     
         69 . The method of  claim 68 , wherein said taxoid comprises paclitaxel.  
     
     
         70 . The method of  claim 68 , wherein said taxoid comprises docetaxel.  
     
     
         71 . The method of  claim 67 , wherein said chemotherapeutic drug comprises etoposide.  
     
     
         72 . The method of  claim 67 , wherein said chemotherapeutic drug comprises teniposide.  
     
     
         73 . The method of  claim 67 , wherein said chemotherapeutic drug comprises camptothecin.  
     
     
         74 . The method of  claim 67 , wherein said chemotherapeutic drug comprises epothilone.  
     
     
         75 . The method of  claim 67 , wherein said metal ion is selected from the group consisting of aluminum, boron, calcium, chromium, cobalt, copper, dysprosium, erbium, europium, gadolinium, gallium, germanium, holmium, indium, iridium, iron, magnesium, manganese, nickel, platinum, rhenium, rubidium, ruthenium, samarium, sodium, technetium, thallium, tin, yttrium or zinc.  
     
     
         76 . The method of  claim 75 , wherein said chemotherapeutic drug comprises a taxoid.  
     
     
         77 . The method of  claim 76 , wherein said taxoid comprises paclitaxel.  
     
     
         78 . The method of  claim 76 , wherein said taxoid comprises docetaxel.  
     
     
         79 . The method of  claim 75 , wherein said chemotherapeutic drug comprises etoposide.  
     
     
         80 . The method of  claim 75 , wherein said chemotherapeutic drug comprises teniposide.  
     
     
         81 . The method of  claim 75 , wherein said chemotherapeutic drug comprises camptothecin.  
     
     
         82 . The method of  claim 75 , wherein said chemotherapeutic drug comprises epothilone.  
     
     
         83 . The method of  claim 67 , wherein said metal ion comprises a radionuclide.  
     
     
         84 . The method of  claim 83 , wherein said chemotherapeutic drug comprises a taxoid.  
     
     
         85 . The method of  claim 84 , wherein said taxoid comprises paclitaxel.  
     
     
         86 . The method of  claim 84 , wherein said taxoid comprises docetaxel.  
     
     
         87 . The method of  claim 83 , wherein said chemotherapeutic drug comprises etoposide.  
     
     
         88 . The method of  claim 83 , wherein said chemotherapeutic drug comprises teniposide.  
     
     
         89 . The method of  claim 83 , wherein said chemotherapeutic drug comprises camptothecin.  
     
     
         90 . The method of  claim 83 , wherein said chemotherapeutic drug comprises epothilone.  
     
     
         91 . The method of  claim 83 , wherein said radionuclide is selected from the group consisting of of  67 Ga,  68 Ga,  166 Ho,  111 In,  99m Tc,  90 Y,  114m Sn and  193m Pt.  
     
     
         92 . The method of  claim 91 , wherein said chemotherapeutic drug comprises a taxoid.  
     
     
         93 . The method of  claim 92 , wherein said taxoid comprises paclitaxel.  
     
     
         94 . The method of  claim 92 , wherein said taxoid comprises docetaxel.  
     
     
         95 . The method of  claim 91 , wherein said chemotherapeutic drug comprises etoposide.  
     
     
         96 . The method of  claim 91 , wherein said chemotherapeutic drug comprises teniposide.  
     
     
         97 . The method of  claim 91 , wherein said chemotherapeutic drug comprises camptothecin.  
     
     
         98 . The method of  claim 91 , wherein said chemotherapeutic drug comprises epothilone.

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