US5116944A
Expired / Lapsed
US
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Conjugates having improved characteristics for in vivo administration
Assignee: Poniard Pharmaceuticals Inc
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Filing: 1989-12-29
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Granted: 1992-05-26
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Expires: 2009-12-29
Abstract
Abstract Conjugates comprising a therapeutically effective proteinaceous active moiety linked to an albumin moiety which exhibit enhanced serum half-life and stability properties are disclosed. The conjugates may additionally comprise targeting moieties to facilitate selective localization of the active moiety at a target site. Conjugates of the present invention comprising an albumin moiety additionally exhibit reduced toxicity, yet maintain a high degree of selectivity and potency.
Inventors
- 👤 Gowsala P. Sivam
- 👤 A. Charles Morgan, Jr.
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 19:50
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/68; A61K47/6801; A61K47/6803; A61K47/6811; A61K47/6817; Y; Y10; Y10S; Y10S530/00; Y10S530/866
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
122 words
A conjugate of a proteinaceous toxin, targeting moiety and albumin moiety wherein: a proteinaceous toxin selected from the group consisting of: ricin; abrin; diphtheria toxin; Pseudomonas exotoxin A; and modified forms thereof that exhibit toxic properties that are substantially equivalent to those of a native form of the corresponding proteinaceous toxin; a targeting moiety linked to said proteinaceous toxin, said targeting moiety selected from the group consisting of: antibodies; antibody fragments; and modified antibodies and fragments having binding activities substantially equivalent to that of a native form of the corresponding antibody or fragment; and an albumin moiety linked to one of said targeting moiety and said proteinaceous toxin wherein the molar ratio of targeting moiety:proteinaceous toxin:albumin moiety is about 1:1:1 to 2.
Claim 2
Dependent Claim
122 words
A conjugate of a proteinaceous toxin, targeting moiety and albumin moiety wherein: a proteinaceous toxin selected from the group consisting of: ricin; abrin; diphtheria toxin; Pseudomonas exotoxin A; and modified forms thereof that exhibit toxic properties that are substantially equivalent to those of a native form of the corresponding proteinaceous toxin; a targeting moiety linked to said proteinaceous toxin, said targeting moiety selected from the group consisting of: antibodies; antibody fragments; and modified antibodies and fragments having binding activities substantially equivalent to that of a native form of the corresponding antibody or fragment; and an albumin moiety linked to one of said targeting moiety and said proteinaceous toxin wherein the molar ratio of targeting moiety:proteinaceous toxin:albumin moiety is about 1:1:1 to 2.
Claim 3
Dependent Claim
39 words
A conjugate according to claim 1, wherein said proteinaceous toxin comprises Pseudomonas exotoxin A (PE), modified forms thereof, or therapeutically active fragments thereof that exhibit toxic properties that are substantially equivalent to those of a native form of PE.
Claim 4
Dependent Claim
17 words
A conjugate according to claim 1, having a molar ratio of approximately 1:1:1, targeting moiety:proteinaceous toxin:albumin moiety.
Claim 5
Dependent Claim
16 words
A conjugate according to claim 1, wherein said albumin moiety is linked to said proteinaceous toxin.
Claim 6
Dependent Claim
16 words
A conjugate according to claim 1, wherein said albumin moiety is linked to said targeting moiety.
Claim 7
Dependent Claim
21 words
A conjugate according to claim 1, wherein an albumin moiety is linked to both said targeting moiety and said active moiety.
Claim 8
Dependent Claim
28 words
A conjugate according to claim 1, wherein said antibody fragment is selected from the group consisting of: Fab; Fab'; F(ab') 2 ; Fv; and single chain antibody fragments.
Claim 9
Dependent Claim
22 words
A conjugate according to claim 1, wherein said albumin moiety is linked to said proteinaceous toxin by means of a thioether linkage.
Claim 10
Dependent Claim
22 words
A conjugate according to claim 8, wherein said targeting moiety is linked to said proteinaceous toxin by means of a thioether linkage.
Claim 11
Dependent Claim
124 words
A conjugate according to claim 1 of: a proteinaceous toxin selected from the group consisting of: diphtheria toxin; Pseudomonas exotoxin A; inactivating proteins; and combinations and modified forms thereof that exhibit toxic properties that are substantially equivalent to those of a native form of the corresponding proteinaceous toxin; a targeting moiety linked to said proteinaceous toxin, said targeting moiety selected from the group consisting of: antibodies; antibody fragments; and modified antibodies and fragments having binding activities substantially equivalent to that of a native form of the corresponding antibody or fragment; and an albumin moiety linked to at least one of said targeting moiety and said proteinaceous toxin there should be no fee for the above amendment, since the number of claims has been reduced.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1995-05-26 | 1995-11-25 | 1996-05-26 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-05-26 | 1999-11-25 | 2000-05-26 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-05-26 | 2003-11-25 | 2004-05-26 | $7700.00 | Window Closed / Lapsed |