# US 11,773,183 B2 · MUC16 monoclonal antibody and uses thereof

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- Number: US 11,773,183 B2
- Document ID: US11773183B2
- Status: Granted
- Kind: B2
- Application number: 17/048,119
- Filed: 2019-04-30
- Published: 2021-04-08
- Granted: 2023-10-03
- Earliest claimed: 2018-05-09
- Assignees: Quest Pharmatech Inc.
- Applicants: Quest Pharmatech Inc.
- Inventors: Ragupathy Madiyalakan; Michael Hollingsworth; Prakash Radhakrishnan
- Web page: https://patentgrep.com/patent/US11773183B2

## CPC

- A61K 39/395: Antibodies (agglutinins A61K38/36 {; as drug carriers A61K47/50}); Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- C07K 16/3092: {against tumour-associated mucins}
- A61K 31/337: having four-membered rings, e.g. taxol
- A61K 31/517: ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
- A61K 31/7068: having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K 39/39558: {against tumor tissues, cells, antigens}
- A61P 35/00: Antineoplastic agents
- G01N 33/57525: of the liver or pancreas
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/567: Framework region [FR]
- C07K 2317/569: Single domain, e.g. dAb, sdAb, VHH, VNAR or nanobody®
- C07K 2317/622: Single chain antibody (scFv)
- C07K 2317/73: Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
- G01N 2400/02: involving antibodies to sugar part of glycoproteins
- 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)
- 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)
- 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

The present document describes an antibody or an antigen-binding fragment that bind to O-glycan mucin-type glycoprotein MUC16 comprising three variable heavy domain complementarity determining regions (CDR)(CDR H1, H2 and H3), and three variable lighy domain CDR (CDR L1, L2 and L3). The present invention also relates to pharmaceutical compositions, nucleic acid vectors, cells comprising the nucleic acid vectors, and methods of inhibiting tumor growth of a tumor expressing O-glycan mucin-type glycoprotein MUC16.

## Claims

### Claim 1

An antibody or an antigen-binding fragment thereof that binds to O-glycan mucin-type glycoprotein MUC16, comprising three variable heavy domain complementarity determining regions (CDR) (CDR H1, H2, and H3), and three variable light domain CDR (CDR L1, L2, and L3), wherein the CDR H1, H2, H3, L1, L2, and L3 comprise the amino acid sequence:
CDR H1:
(SEQ ID NO: 1)
GFTFSTF,
CDR H2:
(SEQ ID NO: 2)
SSGSST,
CDR H3:
(SEQ ID NO: 3)
SGYDYDPIYYALDY,
CDR L1:
(SEQ ID NO: 4)
RASESVDNYGISFMN,
CDR L2:
(SEQ ID NO: 5)
GASNQGS,
and
CDR L3:
(SEQ ID NO: 6)
QQTKEVPWT.

### Claim 2 (depends on 1)

The antibody or the antigen binding fragment thereof of claim 1, further comprising four variable heavy domain framework regions (HFR)(HFR 1, 2, 3, and 4), wherein the HFR 1, 2, 3, and 4 comprise the amino acid sequence:
HFR 1:
(SEQ ID NO: 7)
EVQLVESGGGLVQPGGSRKLSCAAS,
HFR 2:
(SEQ ID NO: 8)
GMHWVRQAPEKGLEWVAYI,
HFR 3:
(SEQ ID NO: 9)
IYYGDTLQGRFIISRDNPKNTLFLQMTSLRSEDTAMYYCAR,
and
HFR 4:
(SEQ ID NO: 10)
WGQGTSVTVSS.

### Claim 3 (depends on 1)

The antibody or the antigen binding fragment thereof of claim 1, further comprising four variable light domain framework regions (LFR) (LFR 1, 2, 3, and 4), wherein the LFR 1, 2, 3, and 4 comprise the amino acid sequence:
LFR 1:
(SEQ ID NO: 11)
DIVLTQSPASLAVSLGQRATISC,
LFR 2:
(SEQ ID NO: 12)
WFQQKPGHPPKLLIY,
LFR 3:
(SEQ ID NO: 13)
GVPARFSGSGSGTDFSLNIHPMEEDDAAMYFC,
and
LFR 4:
(SEQ ID NO: 14)
FGGGTKVEIKR.

### Claim 4 (depends on 1)

The antibody or the antigen binding fragment thereof of claim 1, comprising a variable heavy domain (VH) comprising the amino acid sequence:
(SEQ ID NO: 15)
EVQLVESGGGLVQPGGSRKLSCAASGFTFSTFGMHWVRQAPEKGLEWVAY
ISSGSSTIYYGDTLQGRFIISRDNPKNTLFLQMTSLRSEDTAMYYCARSG
YDYDPIYYALDYWGQGTSVTVSS.

### Claim 5 (depends on 1)

The antibody or the antigen binding fragment thereof of claim 1, comprising a variable light domain (VL) comprising the amino acid sequence:
(SEQ ID NO: 16)
DIVLTQSPASLAVSLGQRATISCRASESVDNYGISFMNWFQQKPGHPPKL
LIYGASNQGSGVPARFSGSGSGTDFSLNIHPMEEDDAAMYFCQQTKEVPW
TFGGGTKVEIKR.

### Claim 6 (depends on 1)

The antibody or the antigen binding fragment thereof of claim 1, comprising a variable heavy domain (VH) comprising the amino acid sequence:
(SEQ ID NO: 15)
EVQLVESGGGLVQPGGSRKLSCAASGFTFSTFGMHWVRQAPEKGLEWVAY
ISSGSSTIYYGDTLQGRFIISRDNPKNTLFLQMTSLRSEDTAMYYCARSG
YDYDPIYYALDYWGQGTSVTVSS,
and
a variable light domain (VL) comprising the amino acid sequence:
(SEQ ID NO: 16)
DIVLTQSPASLAVSLGQRATISCRASESVDNYGISFMNWFQQKPGHPPKL
LIYGASNQGSGVPARFSGSGSGTDFSLNIHPMEEDDAAMYFCQQTKEVPW
TFGGGTKVEIKR.

### Claim 7 (depends on 1)

The antibody or the antigen binding fragment thereof of claim 1, wherein the antibody is an IgA, IgD, IgE, IgG, or IgM.

### Claim 8 (depends on 1)

The antibody or the antigen binding fragment thereof of claim 1, wherein the antigen-binding fragment is a single domain antibody (sdAb) or a single-chain variable fragment (scFv).

### Claim 9 (depends on 1)

The antibody or the antigen binding fragment thereof of claim 1, wherein the antibody or the antigen-binding fragment thereof is humanized or partially humanized.

### Claim 10 (depends on 1)

The antibody or the antigen binding fragment thereof of claim 1, wherein the antibody is POCmAb.

### Claim 11 (depends on 1)

A composition, comprising the antibody or the antigen binding fragment thereof of claim 1 and a pharmaceutically acceptable diluent, carrier, or excipient.

### Claim 12 (depends on 1)

A method of inhibiting tumor growth of a tumor expressing O-glycan mucin-type glycoprotein MUC16 in a subject in need thereof, comprising administering to the subject the antibody or the antigen binding fragment thereof that targets O-glycan mucin-type glycoprotein MUC16 of claim 1.

### Claim 13 (depends on 12)

The method of claim 12, wherein the antibody or the antigen binding fragment thereof is an antibody.

### Claim 14 (depends on 13)

The method of claim 13, wherein the antibody is a monoclonal antibody.

### Claim 15 (depends on 12)

The method of claim 12, further comprising administering a second therapeutic agent comprising at least one of a cytotoxic agent, an additional antibody or a therapeutically active fragment thereof, or a chemotherapy regimen.

### Claim 16 (depends on 15)

The method of claims 15, wherein the cytotoxic agent is at least one of an inhibitor of ErbB signaling, an inhibitor of phosphoinositide 3-kinases (PI3Ks)/Akt signaling, gemcitabine and abraxane or combinations thereof;
wherein the additional antibody or therapeutically fragment thereof is oregovomab antibody B43.13, AR9.6 antibody, or combinations thereof; and
wherein the chemotherapy regimen is Folfirinox.

### Claim 17 (depends on 12)

The method of claim 12, wherein the tumor is chosen from a pancreatic tumor, a gall bladder tumor, a gastric tumor, a colon tumor, an ovarian tumor, a breast tumor, and a liver tumor.

### Claim 18 (depends on 12)

The method of claim 12, wherein the method is for the treatment of a cancer.