# US 2014/0155583 A1 · Monoclonal antibodies and single chain antibody fragments against cell-surface prostate specific membrane antigen

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- Number: US 2014/0155583 A1
- Document ID: US20140155583A1
- Status: Published application
- Kind: A1
- Application number: 14/105,808
- Filed: 2013-12-13
- Published: 2014-06-05
- Earliest claimed: 2005-05-27
- Assignees: Universitatsklinikum Freiburg
- Applicants: UniversitäTsklinikum Freiburg
- Inventors: Ursula Elsässer-Beile; Philipp Wolf; Dorothee Gierschner; Patrick Bühler; Ulrich Wetterauer
- Web page: https://patentgrep.com/patent/US20140155583A1

## CPC

- C07K 16/3069: {Reproductive system, e.g. ovaria, uterus, testes, prostate}
- A61K 47/6869: {the tumour determinant being from a cell of the reproductive system: ovaria, uterus, testes, prostate}
- A61K 51/1072: {the tumor cell being from the reproductive system, e.g. ovaria, uterus, testes or prostate}
- A61P 13/08: of the prostate
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 35/00: Antineoplastic agents
- A61K 2039/505: {comprising antibodies}
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/622: Single chain antibody (scFv)
- C07K 2317/626: Diabody or triabody
- C07K 2317/77: Internalization into the cell
- C07K 2317/80: remaining in the (producing) cell, i.e. intracellular antibodies or intrabodies
- C07K 2317/92: Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Isolated monoclonal antibodies or an antigen binding portion thereof which bind to prostate specific membrane antigen in its native form occurring on the surface of tumor cells characterized in that it is linked to a label or a cytotoxic agent or constructed as a part of a bispecific antibody or a recombinant diabody.

## Claims

### Claim 1

An isolated monoclonal antibody or an antigen-binding portion thereof which
a) binds to a prostate specific membrane antigen in its native form,
b) binds strongly to LNCAP cells but not or only minimally to cells which lack expression of prostate specific membrane antigen, and
c) comprises at least three sequences selected from the group consisting of SEQ ID NO:25, 31, 27, 32, 33 and 30, or at least three sequences from the group consisting of SEQ ID NO:25, 26, 27, 28, 29 and 30.

### Claim 2 (depends on 1)

Isolated monoclonal antibody or an antigen-binding portion thereof according to claim 1 which can be internalized by a tumor cell.

### Claim 3 (depends on 1)

Isolated monoclonal antibody or an antigen-binding portion thereof according to claim 1 characterized in that it is linked to label or a cytotoxic agent.

### Claim 4 (depends on 1)

Monoclonal antibody or an antigen-binding portion thereof according to claim 1 wherein the prostate specific antigen in its native form occurs on the surface of tumor cells.

### Claim 5 (depends on 1)

Monoclonal antibody or an antigen-binding portion thereof according to claim 1 which shows a high binding activity to LNCAP cells reaching 50% saturation of PSMA sites at concentrations between 1 nM and 120 nM.

### Claim 6 (depends on 3)

Monoclonal antibody or an antigen-binding portion thereof according to claim 3 characterized in that the cytotoxic agent is a cytotoxic cell substance.

### Claim 7 (depends on 6)

Monoclonal antibody or an antigen-binding portion thereof according to claim 6 characterized in that the cytotoxic agent is a cell toxic substance selected from the group consisting of taxol, cytocalasin B, gramicidin D, ethidium bromid, emetine, mitomycin, etopside, tenopside, vincristine, vinblastine, colchicin, doxorubicin, daunorubicin, dihydroxy antracin dione, mitoxantrone, mithramycin, actinomycin D, 1-dehydrotestosteron, glycocorticoids, procain, tetracaine, lidokaine, propranolol, puromycin, and combinations thereof.

### Claim 8 (depends on 3)

Monoclonal antibody or an antigen-binding portion thereof according to claim 3 characterized in that the label is a particle which emits radioactive or fluorescence radiation.

### Claim 9 (depends on 3)

Diagnostic kit for the detection of tumor cells comprising an isolated monoclonal antibody or an antigen-binding portion thereof according to claim 3.

### Claim 10 (depends on 8)

Diagnostic kit for the detection of tumor cells comprising an isolated monoclonal antibody or antigen-binding portion thereof according to claim 8.