# US 2012/0230994 A1 · Bladder cancer specific ligand peptides

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- Number: US 2012/0230994 A1
- Document ID: US20120230994A1
- Status: Published application
- Kind: A1
- Application number: 13/497,041
- Filed: 2010-09-23
- Published: 2012-09-13
- Earliest claimed: 2009-09-24
- Assignees: The Regents Of The University Of California Office Of Technology
- Inventors: Chong-xian Pan; Hongyong Zhang; Kit S. Lam; Olulanu H. Aina
- Web page: https://patentgrep.com/patent/US20120230994A1

## CPC

- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/51: Nanocapsules; {Nanoparticles; (nanotubes A61K9/0092; polymeric micelles A61K9/1075; polymersomes A61K9/1273; pure drug nanoparticles A61K9/14; drug nanoparticles with adsorbed surface modifiers A61K9/141; conjugates, e.g. between drug and non-active nanoparticles, A61K47/50; preparations for in vivo diagnosis A61K49/00; with radioactive substances A61K51/00)}
- A61K 47/51: the non-active ingredient being a modifying agent
- A61K 47/64: Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent (peptidic linkers A61K47/65)
- A61K 47/66: the modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells
- A61K 49/0002: {General or multifunctional contrast agents, e.g. chelated agents}
- A61K 49/0032: {Methine dyes, e.g. cyanine dyes}
- A61K 49/0056: {Peptides, proteins, polyamino acids}
- A61K 51/088: {conjugates with carriers being peptides, polyamino acids or proteins (antibodies A61K51/10)}
- A61P 13/10: of the bladder
- A61P 35/00: Antineoplastic agents
- B82Y 5/00: Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
- C07K 7/06: having 5 to 11 amino acids
- G01N 33/57557: {of other specific parts of the body, e.g. brain}
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- B82Y: SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
- 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)
- 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

The present invention is directed to bladder cancer specific ligand peptides, comprising the amino acid sequence X1DGRX5GF (SEQ ID NO:1), and methods of their use, e.g., for imaging detection for diagnosis of bladder, tumor localization to guide transurethral resection of bladder cancer, imaging detection of bladder cancer for follow-up after the initial treatment that can replace or complement costly cystoscopy, imaging detection of metastatic bladder cancer, and targeted therapy for superficial and metastatic bladder cancer.

## Claims

### Claim 1

A peptide comprising the amino acid sequence X1DGRX5GF, wherein X1 and X5 are any amino acid, wherein the peptide is no longer than 10 amino acids in length and binds to bladder cancer cells.

### Claim 2

A peptide comprising the amino acid sequence X1DGRX5GF, wherein X1 and X5 are any amino acid, wherein:
i) one or more of the amino acid residues are D-amino acids;
ii) the peptide comprises protecting groups at one or both of the N-terminus or the C terminus;
iii) the peptide is fully or partially retro-inverso;
iv) the peptide comprises 2 or more repeats of the amino acid sequence X1DGRX5GF (SEQ ID NO:1); or
v) the peptide is circularized.

### Claim 3 (depends on 1)

The peptide of claim 1, wherein X1 is Gln, Gly or Ala.

### Claim 4 (depends on 1)

The peptide of claim 1, wherein X5 is Met, Lys, Gly, Ala or Gly-Gly.

### Claim 5 (depends on 1)

The peptide of claim 1, wherein the peptide has the amino acid sequence QDGRMGF.

### Claim 6 (depends on 1)

The peptide of claim 1, wherein the peptide does not bind to normal bladder tissue.

### Claim 7 (depends on 1)

The peptide of claim 1, wherein the peptide further comprises from 1 to 5 flanking amino acid residues at the amino and/or carboxyl termini.

### Claim 8 (depends on 1)

The peptide of claim 1, wherein the peptide further comprises a cysteine residue at the amino terminus and a cysteine residue at the carboxyl terminus.

### Claim 9 (depends on 1)

The peptide of claim 1, wherein the peptide is linked to a therapeutic moiety or a detectable label.

### Claim 10 (depends on 9)

The peptide of claim 9, wherein the detectable label is a bead, a fluorophore, a chemiluminescent moiety, a magnetic particle, a metal particle or a radioisotope.

### Claim 11 (depends on 9)

The peptide of claim 9, wherein the therapeutic moiety is an Fc portion of an immunoglobulin, a cytotoxin, or an anticancer agent.

### Claim 12 (depends on 1)

A method of detecting the presence of bladder cancer comprising contacting a bladder cell or bladder tissue with a peptide of claim 1 linked to a detectable label, and detecting the binding of the peptide to the bladder cell or bladder tissue, wherein detecting binding of the peptide to the bladder cell or bladder tissue is indicative of bladder cancer.

### Claim 13 (depends on 12)

The method of claim 12, wherein the peptide is linked to a detectable label.

### Claim 14 (depends on 12)

The method of claim 12, wherein the detectable label is selected from the group consisting of a bead, a fluorophore, a chemiluminescent moiety, a magnetic particle, a metal particle or a radioisotope.

### Claim 15 (depends on 12)

The method of claim 12, wherein the bladder cell or bladder tissue is in vitro.

### Claim 16 (depends on 12)

The method of claim 12, wherein the bladder cell or bladder tissue is in a urine sample.

### Claim 17 (depends on 12)

The method of claim 12, wherein the bladder cell or bladder tissue is in vivo.

### Claim 18 (depends on 12)

The method of claim 12, wherein the bladder cell or bladder tissue is detected in situ within a subject.

### Claim 19 (depends on 1)

A method of inhibiting or preventing the growth of a bladder cancer cell in a subject in need thereof, comprising contacting bladder tissue with a peptide of claim 1, linked to a therapeutic moiety, wherein the peptide binds to bladder cancer cells and the therapeutic moiety inhibits or prevents the growth of the bladder cancer cells.

### Claim 20 (depends on 19)

The method of claim 19, wherein the subject is a mammal.

### Claim 21 (depends on 19)

The method of claim 19, wherein the therapeutic moiety is an Fc portion of an immunoglobulin, a cytotoxin, an anticancer agent, or a radioisotope.

### Claim 22 (depends on 19)

The method of claim 19, wherein the peptide linked to the therapeutic moiety is administered to the subject intravenously, intratumorally or intraurethrally.