# US 11,028,163 B2 · Heavy chain only antibodies to PDGF

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- Number: US 11,028,163 B2
- Document ID: US11028163B2
- Status: Granted
- Kind: B2
- Application number: 16/425,140
- Filed: 2019-05-29
- Published: 2020-04-23
- Granted: 2021-06-08
- Earliest claimed: 2015-08-14
- Assignees: Allergan, Inc.
- Applicants: Allergan, Inc.
- Inventors: Yanbin Liang; Daniel W. Gil
- Web page: https://patentgrep.com/patent/US11028163B2

## CPC

- C07K 16/22: against growth factors {; against growth regulators}
- A61K 39/395: Antibodies (agglutinins A61K38/36 {; as drug carriers A61K47/50}); Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 27/02: Ophthalmic agents
- A61P 35/00: Antineoplastic agents
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/52: Constant or Fc region; Isotype
- C07K 2317/522: CH1 domain
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/569: Single domain, e.g. dAb, sdAb, VHH, VNAR or nanobody®
- C07K 2317/64: comprising a combination of variable region and constant region components
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- 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

Disclosed herein are monospecific HCAb antibodies with antigen-binding specificity to PDGF and bispecific antibodies with antigen-binding specificities to PDGF-2 and VEGF or to PDGF and ANG-2.

## Claims

### Claim 1

A method of treating an ophthalmologic disorder comprising administering to a subject in need thereof a heavy-chain only antibody (HCAb) comprising homodimeric variable heavy chain (VH) regions wherein each VH region comprises:
a CDR1 having the amino acid sequence of SEQ ID NO:23;
a CDR2 having the amino acid sequence of SEQ ID NO:24; and
a CDR3 having the amino acid sequence of SEQ ID NO:25;
wherein the HCAb retains its specificity for PDGF-BB; and
wherein the HCAB binds to PDGF-BB and treats the ophthalmologic disorder, and wherein the ophthalmologic disorder is selected from the group consisting of dry age-related macular degeneration, wet age-related macular degeneration, choroidal neovascularization (CNV), cystoid macula edema (CME), myopia-associated choroidal neovascularization, vascular streaks, diabetic macular edema (DME), macular edema, retinal vein occlusion, abnormal corneal angiogenesis, pterygium conjunctivae, subretinal edema, or intraretinal edema.

### Claim 2 (depends on 1)

The method of claim 1, wherein the VH region has at least 85% identity to SEQ ID NO:22.

### Claim 3 (depends on 2)

The method of claim 2, wherein the VH region has at least 90% identity to SEQ ID NO:22.

### Claim 4 (depends on 2)

The method of claim 2, wherein the VH region has at least 93% identity to SEQ ID NO:22.

### Claim 5 (depends on 2)

The method of claim 2, wherein the VH region has at least 96% identity to SEQ ID NO:22.

### Claim 6 (depends on 2)

The method of claim 2, wherein the VH region has at least 98% identity to SEQ ID NO:22.

### Claim 7 (depends on 1)

The method of claim 1, wherein the VH region comprises SEQ ID NO:22.

### Claim 8 (depends on 1)

The method of claim 1, wherein the abnormal corneal angiogenesis is as a result of keratitis, corneal transplantation, keroplasty or hypoxia.
