# US 7,744,879 B2 · Blood-brain barrier targeting antibodies

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- Number: US 7,744,879 B2
- Document ID: US7744879B2
- Status: Granted
- Kind: B2
- Application number: 11/759,723
- Filed: 2007-06-07
- Published: 2008-01-24
- Granted: 2010-06-29
- Earliest claimed: 2006-06-07
- Assignees: Wisconsin Alumni Research Foundation
- Inventors: Eric V. Shusta; Xin X. Wang; Yongku P. Cho
- Web page: https://patentgrep.com/patent/US7744879B2

## CPC

- C07K 16/28: against receptors, cell surface antigens or cell surface determinants
- A61K 47/6849: {the antibody targeting a receptor, a cell surface antigen or a cell surface determinant}
- G01N 33/6854: {Immunoglobulins}
- C07K 2317/21: from primates, e.g. man
- C07K 2317/622: Single chain antibody (scFv)
- C07K 2317/77: Internalization into the cell
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

This invention provides antibodies that bind brain endothelial cell receptors resulting in endocytosis/transcytosis of the receptor and bound ligands. In some embodiments, the ligand comprises the antibody in combination with a pharmaceutically active compound and the antibody directs delivery of the compound across the blood brain barrier (BBB). The invention also provides methods of identifying endothelial cell specific antibodies by panning the library against cultured cell monolayers. The invention further allows for identifying endothelial cell receptors that bind the antibody thereby providing target receptors against which to isolate further cognate ligands and their associated transport systems and by which to identify transcytosis transporters targeted by the antibodies.

## Claims

### Claim 1

An isolated polypeptide comprising an antibody fragment having an amino acid sequence set forth in any one of SEQ ID NOs. 1-5.

### Claim 2 (depends on 1)

The isolated polypeptide of claim 1, wherein the antibody fragment has the amino acid sequence set forth in SEQ ID NO. 1.

### Claim 3 (depends on 1)

The isolated polypeptide of claim 1, wherein the antibody fragment binds to a brain endothelial cell.

### Claim 4 (depends on 1)

The isolated polypeptide of claim 1, wherein the antibody fragment is a single chain fragment variable (scFv) antibody.

### Claim 5

A composition comprising: an isolated antibody fragment set forth in any one of SEQ ID NOs. 1-5 and a pharmaceutically active compound linked thereto.

### Claim 6 (depends on 5)

The composition of claim 5, wherein the antibody fragment is set forth in SEQ ID NO. 1.