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US4902505A
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Chimeric peptides for neuropeptide delivery through the blood-brain barrier
Assignee: Alkermes Inc
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Filing: 1988-04-25
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Granted: 1990-02-20
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Expires: 2008-04-25
Abstract
Abstract Chimeric peptides adapted for delivering neuropharmaceutical agents, such as neuropeptides into the brain by receptor-mediated transcytosis through the blood-brain barrier. The chimeric peptides include a peptide which by itself is capable of crossing the blood-brain barrier by transcytosis at a relatively high rate. The transportable peptide is conjugated to a hydrophilic neuropeptide which by itself is transportable only at a very low rate into the brain across the blood-brain barrier. The resulting chimeric peptide is transported into the brain at a much higher rate than the neuropeptide alone to thereby provide an effective means for introducing hydrophilic neuropeptides into the brain through the blood-brain barrier.
Inventors
- 👤 William M. Pardridge
- 👤 Paul R. Schimmel
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 20:35
CPC Classifications
C; C07; C07K; C07K1/00; C07K1/107; C07K1/1072; C07K1/1075; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/62; A61P; A61P25/00; A61P25/18; C07K14/00; C07K14/435; C07K14/575; C07K14/62; C07K14/655; C07K14/665; C07K14/675; C07K14/695; C07K7/00; C07K7/04; C07K7/16; A61K38/00
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
44 words
A chimeric peptide adapted for delivering a neuropharmaceutical agent into the brain by transcytosis through the blood-brain barrier, said chimeric peptide comprising a transportable peptide capable of crossing the blood-brain barrier by transcytosis conjugated with said neuropharmaceutical agent, wherein said transportable peptide is histone.
Claim 2
Dependent Claim
44 words
A chimeric peptide adapted for delivering a neuropharmaceutical agent into the brain by transcytosis through the blood-brain barrier, said chimeric peptide comprising a transportable peptide capable of crossing the blood-brain barrier by transcytosis conjugated with said neuropharmaceutical agent, wherein said transportable peptide is histone.
Claim 3
Dependent Claim
16 words
A chimeric peptide according to claim 1 wherein said histone is isolated from a human source.
Claim 4
Dependent Claim
19 words
A chimeric peptide according to claim 1 wherein said histone is selected from a class I-V type of histone.
Claim 5
Dependent Claim
19 words
A chimeric peptide according to claim 2 wherein said histone is selected from a class I-V type of histone.
Claim 6
Dependent Claim
15 words
A chimeric peptide according to claim 1 wherein said neuropharmaceutical agent is a hydrophilic peptide.
Claim 7
Dependent Claim
30 words
A chimeric peptide according to claim 5 wherein said neuropharmaceutical agent is selected from the group consisting of somatostatin, thyrotropin releasing hormone, vasopressin, alpha interferon, endorphin, muramyl dipeptide and L-methionyl(sulfone)-L-glytamyl-L-histidyl-L-phenylalanyl-D-lysyl-L-phenylalanine.
Claim 8
Dependent Claim
20 words
A chimeric peptide according to claim 1 wherein said transportable peptide and neuropharmaceutical agent are conjugated via a conjugation agent.
Claim 9
Dependent Claim
30 words
A chimeric peptide according to claim 1 wherein said conjugation agent is capable of conjugating the transportable peptide to said neuropharmaceutical agent by peptide thiolation or lysine coupling via glutaraldehyde.
Claim 10
Dependent Claim
21 words
A chimeric peptide according to claim 1 having the formula ##STR3## wherein A is a neuropharmaceutical agent and B is histone.
Claim 11
Dependent Claim
28 words
A chimeric peptide according to claim 9 wherein A is selected from the group consisting of somatostatin, thyrotropin releasing hormone, vasopressin, alpha interferon, endorphin, muramyl dipeptide and L-methionyl(sulfone)-L-glytamyl-L-histidyl-L-phenyl-alanyl-D-lysyl-L-phenylalanine.
Claim 12
Dependent Claim
19 words
A composition comprising a chimeric peptide according to claim 1 and a pharmaceutically acceptable carrier for said chimeric peptide.
Claim 13
Dependent Claim
14 words
A composition according to claim 11 wherein said pharmaceutically acceptable carrier is sterile saline.
Claim 14
Dependent Claim
52 words
A method for delivering a neuropharmaceutical agent into the brain of an animal by transcytosis through the blood-brain barrier comprising the step of introducing a chimeric peptide according to claim 1 into the bloodstream of said animal in a sufficient amount to provide transport of said chimeric peptide across said blood-brain barrier.
Claim 15
Dependent Claim
17 words
A method according to claim 13 wherein said chimeric peptide is introduced intranasally into the subject's bloodstream.
Claim 16
Dependent Claim
36 words
In a method for introducing a hydrophilic neuropeptide into the brain across the blood-brain barrier, wherein the improvement comprises increasing the rate at which said neuropeptide crosses the blood-brain barrier by conjugating said neuropeptide with histone.
Claim 17
Dependent Claim
36 words
In a method for introducing a hydrophilic neuropeptide into the brain across the blood-brain barrier, wherein the improvement comprises increasing the rate at which said neuropeptide crosses the blood-brain barrier by conjugating said neuropeptide with histone.
Claim 18
Dependent Claim
16 words
The improved method according to claim 15 wherein said histone is isolated from a human source.
Claim 19
Dependent Claim
19 words
The improved method according to claim 15 wherein said histone is selected from a class I-V type of histone.
Claim 20
Dependent Claim
19 words
The improved method according to claim 16 wherein said histone is selected from a class I-V type of histone.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1993-02-19 | 1993-08-21 | 1994-02-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-02-19 | 1997-08-21 | 1998-02-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-02-19 | 2001-08-21 | 2002-02-20 | $7700.00 | Window Closed / Lapsed |