# US 10,479,839 B2 · Internalizing human monoclonal antibodies targeting prostate cancer cells in situ

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 10,479,839 B2
- Document ID: US10479839B2
- Status: Granted
- Kind: B2
- Application number: 15/418,588
- Filed: 2017-01-27
- Published: 2017-08-17
- Granted: 2019-11-19
- Earliest claimed: 2007-09-17
- Assignees: The Regents of the University of California
- Applicants: The Regents of the University of California
- Inventors: Bin Liu; James D. Marks
- Web page: https://patentgrep.com/patent/US10479839B2

## CPC

- C07K 16/3069: {Reproductive system, e.g. ovaria, uterus, testes, prostate}
- A61K 51/1072: {the tumor cell being from the reproductive system, e.g. ovaria, uterus, testes or prostate}
- A61P 35/00: Antineoplastic agents
- C07K 16/005: {constructed by phage libraries}
- C07K 16/18: against material from animals or humans
- C07K 16/2803: {against the immunoglobulin superfamily}
- C07K 16/30: from tumour cells
- G01N 33/5044: {involving specific cell types}
- G01N 33/57555: of the prostate
- G01N 33/6845: {Methods of identifying protein-protein interactions in protein mixtures}
- G01N 33/6854: {Immunoglobulins}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/21: from primates, e.g. man
- C07K 2317/56: variable (Fv) region, i.e. VH and/or VL
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/569: Single domain, e.g. dAb, sdAb, VHH, VNAR or nanobody®
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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 a method that allows selection of antibodies against cells (e.g., tumor cells) in situ using laser capture microdissection. By restricting antibody selection to binders of internalizing epitopes, a panel of phage antibodies was generated that targets clinically represented prostate cancer antigens.

## Claims

### Claim 1

A method of inhibiting the growth and/or proliferation of a prostate cancer cell, said method comprising contacting said cell with a chimeric moiety comprising an antibody attached to an anti-cancer drug or a radionuclide, where said antibody comprises the three variable heavy complementarity determining regions (VH CDRs) and the three variable light complementarity determining regions (VL CDRs) of the UA20 antibody (SEQ ID NO:8).

### Claim 2 (depends on 1)

The method of claim 1, wherein said cell is a metastatic cell.

### Claim 3 (depends on 1)

The method of claim 1, wherein said antibody comprises the variable heavy (VH) domain and the variable light (VL) domain of the UA20 antibody (SEQ ID NO:8).

### Claim 4 (depends on 1)

The method of claim 1, wherein said antibody is a single chain antibody.

### Claim 5 (depends on 4)

The method of claim 4, wherein the VL domain is attached to the VH domain by a (Gly4Ser)3 (SEQ ID NO: 1) linker.

### Claim 6 (depends on 1)

The method of claim 1, wherein said antibody is an antibody selected from the group consisting of a whole intact antibody, a Fab, a (Fab′)2, an scFv, and an (ScFv′)2.

### Claim 7 (depends on 6)

The method of claim 6, wherein said antibody is an scFv.

### Claim 8 (depends on 1)

The method of claim 1, wherein said chimeric moiety is internalized into a prostate cancer cell.

### Claim 9 (depends on 1)

The method of claim 1, wherein said cell is a refractory prostate cancer cell.

### Claim 10 (depends on 1)

The method of claim 1, wherein said chimeric moiety is formulated with a pharmaceutically acceptable excipient.

### Claim 11 (depends on 1)

The method of claim 1, wherein said antibody is an intact antibody.

### Claim 12 (depends on 11)

The method of claim 11, wherein said antibody is an IgG.