US5087616A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Cytotoxic drug conjugates and their delivery to tumor cells
Assignee: Battelle Memorial Institute Inc
•
Filing: 1987-08-06
•
Granted: 1992-02-11
•
Expires: 2007-08-06
Abstract
Abstract A therapeutic composition comprising a chemical conjugatge including a first moiety, other than an immunoglobulin or fragment thereof, such as epidermal growth factor, which preferentially binds to a tumor cell, and is internalized by the cell, and a second moiety linked to the first moiety, and comprising a biodegradable polymeric carrier, such as polyglutamic acid, to which one or more cytotoxic molecules, for instance, daunomycin, are attached. The degradation of the carrier by intracellular enzymes releases a cytotoxic agent, resulting in selective destruction of the tumor cells.
Inventors
- 👤 Andre E. Myers
- 👤 Daniel Bichon
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 11:18
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/62; A61K47/64; A61K47/645; A61K47/642; A61P; A61P35/00
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
102 words
A therapeutic chemical conjugate including EGF as a first moiety, and a second moiety linked covalently to the EGF, said second moiety comprising a plurality of repeating units, each unit having the structure ##STR12## where L is selected from the group consisting of polyglutamic acid and polyaspartic acid, and T is selected from the group consisting of anthracycline drugs, bleomycin, melphalan, chlorambucil, cisplatin, adriamycin, daunomycin, and daunorubicin, and where said conjugate has a molecular weight of between 10,000 and 100,000 D and is effective in target cells in vivo and is internalized by tumor cells whereby the latter are inhibited or destroyed.
Claim 2
Dependent Claim
102 words
A therapeutic chemical conjugate including EGF as a first moiety, and a second moiety linked covalently to the EGF, said second moiety comprising a plurality of repeating units, each unit having the structure ##STR12## where L is selected from the group consisting of polyglutamic acid and polyaspartic acid, and T is selected from the group consisting of anthracycline drugs, bleomycin, melphalan, chlorambucil, cisplatin, adriamycin, daunomycin, and daunorubicin, and where said conjugate has a molecular weight of between 10,000 and 100,000 D and is effective in target cells in vivo and is internalized by tumor cells whereby the latter are inhibited or destroyed.
Claim 3
Dependent Claim
14 words
The conjugate of claim 1 wherein L is polyglutamic acid and T is daunomycin.
Claim 4
Dependent Claim
14 words
The conjugate of claim 1, where the EGF is essentially identical to human EGF.
Claim 5
Dependent Claim
22 words
The conjugate of claim 1, wherein the first moiety is directly linked to the second moiety by means of a peptidyl linkage.
Claim 6
Dependent Claim
45 words
The conjugate of claim 1 wherein the first moiety is linked to the second moiety by a structure having the formula: ##STR13## where R' is: alkylene (C 1 -C 4 ); 1,3-phenylene; cyclohexylene-4-methylene; or alkylene (C 1 -C 4 )-phenylene (1,4); and m=1 or 2.
Claim 7
Dependent Claim
15 words
The conjugate of claim 1, having a molecular weight of less than about 100,000 D.
Claim 8
Dependent Claim
22 words
The conjugate of claim 1 wherein the T is selected from the group consisting of anthracycline drugs, bleomycin, melphalan, chlorambucil, and cisplatin.
Claim 9
Dependent Claim
19 words
The conjugate of claim 7 wherein the T is selected from the group consisting of adriamycin, daunomycin, and daunorubicin.
Claim 10
Dependent Claim
10 words
The conjugate of claim 1 wherein the T is daunomycin.
Claim 11
Dependent Claim
25 words
A therapeutic composition comprising the chemical conjugate of claim 1 and a therapeutically acceptable carrier having a molecular weight of between 10,000 and 100,000 D.
References Cited (Backward Citations)
US3917824A
Cited
EP0046039A1
Cited
WO1983004030A1
Cited
US4528186A
Cited
US4485093A
Cited
EP0112720A2
Cited
EP0128733A1
Cited
WO1985000369A1
Cited
EP0131868A1
Cited
WO1985001284A1
Cited
US4545985A
Cited
EP0259904A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1995-02-10 | 1995-08-12 | 1996-02-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-02-10 | 1999-08-12 | 2000-02-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-02-10 | 2003-08-12 | 2004-02-11 | $7700.00 | Window Closed / Lapsed |