# US 10,308,707 B2 · Bispecific HIV-1-neutralizing antibodies

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- Number: US 10,308,707 B2
- Document ID: US10308707B2
- Status: Granted
- Kind: B2
- Application number: 15/850,832
- Filed: 2017-12-21
- Published: 2018-08-23
- Granted: 2019-06-04
- Earliest claimed: 2013-12-02
- Assignees: The Aaron Diamond Aids Research Center
- Applicants: Aaron Diamond AIDS Research Center
- Inventors: David D. Ho; Yaoxing Huang; Jian Yu
- Web page: https://patentgrep.com/patent/US10308707B2

## CPC

- C07K 16/1145: {Env proteins, e.g. gp41, gp110/120, gp160, V3, principal neutralising domain [PND] or CD4-binding site}
- A61K 39/42: viral
- A61P 31/18: for HIV
- C07K 16/2812: {against CD4}
- C07K 16/2866: {against receptors for cytokines, lymphokines, interferons}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/31: multispecific
- C07K 2317/52: Constant or Fc region; Isotype
- C07K 2317/567: Framework region [FR]
- C07K 2317/66: comprising a swap of domains, e.g. CH3-CH2, VH-CL or VL-CH1
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- C07K 2317/94: Stability, e.g. half-life, pH, temperature or enzyme-resistance
- 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

In various embodiments, the present invention relates generally to using bispecific antibodies in the prevention and treatment of HIV.

## Claims

### Claim 1

A bispecific antibody in a CrossMab format capable of neutralizing HIV, wherein the antibody comprises a light chain and heavy chain portion of a first antibody 10E8, or a variant thereof, that binds to a HIV envelope protein, and a light chain and heavy chain portion of a second antibody ibalizumab, or a variant thereof, that binds to a cell membrane receptor protein or a cell membrane co-receptor protein, wherein
the light chain portion of the first antibody 10E8 comprises an amino acid sequence having at least 97% identity with SEQ ID NO: 46 and the heavy chain portion of the first antibody 10E8 comprises an amino acid sequence having at least 97% identity with SEQ ID NO: 47; and
the light chain portion of the second antibody ibalizumab comprises an amino acid sequence having at least 97% identity with SEQ ID NO: 1, and the heavy chain portion of the second antibody ibalizumab comprises an amino acid sequence having at least 97% with SEQ ID NO: 2; and wherein any variations relative to SEQ ID NOs:1, 2, 46 and 47 are outside the variable regions.

### Claim 2 (depends on 1)

The bispecific antibody of claim 1, wherein the antibody comprises a light chain portion of an ibalizumab antibody comprising the amino acid sequence of SEQ ID NO: 1 and a heavy chain portion of an ibalizumab antibody comprising the amino acid sequence of SEQ ID NO: 2.

### Claim 3 (depends on 1)

The bispecific antibody of claim 1, wherein the antibody comprises a light chain portion of a 10E8 antibody comprising the amino acid sequence of SEQ ID NO: 46 and a heavy chain portion of a 10E8 antibody comprising the amino acid sequence of SEQ ID NO: 47.

### Claim 4 (depends on 1)

A pharmaceutical composition comprising the bispecific antibody of claim 1, and a pharmaceutically acceptable carrier.

### Claim 5 (depends on 4)

The pharmaceutical composition of claim 4, wherein the composition is formulated for oral, intranasal, pulmonary, intradermal, transdermal, subcutaneous, intramuscular, intraperitoneal, or intravenous delivery.
