# US 12,215,144 B2 · Acute treatment and rapid treatment of headache using anti-CGRP antibodies

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- Number: US 12,215,144 B2
- Document ID: US12215144B2
- Status: Granted
- Kind: B2
- Application number: 18/609,223
- Filed: 2024-03-19
- Published: 2024-08-15
- Granted: 2025-02-04
- Earliest claimed: 2019-01-08
- Assignees: H. Lundbeck A/S
- Applicants: H. Lundbeck A/S
- Inventors: Roger K. Cady; Jeffrey T.L. Smith; Joseph Hirman; Barbara Schaeffler; Lahar Mehta
- Web page: https://patentgrep.com/patent/US12215144B2

## CPC

- C07K 16/18: against material from animals or humans
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 31/4172: Imidazole-alkanecarboxylic acids, e.g. histidine
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61P 25/06: Antimigraine agents
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- A61K 2039/505: {comprising antibodies}
- A61K 2039/54: {characterised by the route of administration}
- A61K 2039/545: {characterised by the dose, timing or administration schedule}
- C07K 2317/14: Specific host cells or culture conditions, e.g. components, pH or temperature
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/41: Glycosylation, sialylation, or fucosylation
- C07K 2317/526: CH3 domain
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/71: Decreased effector function due to an Fc-modification
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- 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

Methods for rapid treatment of chronic migraine are provided. Exemplary methods provide relief from migraine within 24 hours of administration. Also provided are methods for acute treatment of migraine. Exemplary methods comprise administration of an anti-CGRP antagonist antibody to a patient in need thereof.

## Claims

### Claim 1

A method of acute treatment of migraine in a patient in need thereof, the method comprising intravenously administering to the patient:
(A) about 100 mg or about 300 mg of a monoclonal antibody comprising:
(a) a variable light chain polypeptide comprising light chain complementary determining region (CDR) 1, 2, and 3 polypeptide sequences of SEQ ID NO: 224, SEQ ID NO: 226, and SEQ ID NO: 228, respectively, and
(b) a variable heavy chain polypeptide comprising heavy chain CDR 1, 2, and 3 polypeptide sequences of SEQ ID NO: 204, SEQ ID NO: 206, and SEQ ID NO: 208, respectively; and
(B) one or more acute migraine medications,
wherein the administering begins while the patient is experiencing a headache, and wherein the administering is followed by preventive treatment once every three months using about 100 mg or about 300 mg of said monoclonal antibody.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the one or more acute migraine medications comprise triptan, an analgesic such as non-opioids or opioids/narcotics, acetaminophen, an non-steroidal anti-inflammatory drug (NSAID), a combination medication, an ergotamine, and/or an ergot derivative.

### Claim 3 (depends on 2)

The method according to claim 2, wherein the patient suffers from chronic migraine.

### Claim 4 (depends on 3)

The method according to claim 3, wherein the about 100 mg or about 300 mg of the monoclonal antibody is administered to the patient once every three months, for at least six months.

### Claim 5 (depends on 2)

The method according to claim 2, wherein the patient suffers from episodic migraine.

### Claim 6 (depends on 5)

The method according to claim 5, wherein the about 100 mg or about 300 mg of the monoclonal antibody is administered to the patient once every three months, for at least twelve months.

### Claim 7 (depends on 2)

The method according to claim 2, wherein the monoclonal antibody comprises a human IgG1 constant region and is produced in Chinese hamster ovary (CHO) cells.

### Claim 8 (depends on 2)

The method according to claim 2, wherein the monoclonal antibody comprises a human IgG1 constant region and is produced in Pichia pastoris yeast cells.

### Claim 9 (depends on 2)

The method according to claim 2, wherein the monoclonal antibody is a humanized IgG1 monoclonal antibody.

### Claim 10 (depends on 2)

The method according to claim 2, wherein:
(A) the variable light chain polypeptide comprises the amino acid sequence of SEQ ID NO: 222; and
(B) the variable heavy chain polypeptide comprises the amino acid sequence of SEQ ID NO: 202.

### Claim 11 (depends on 10)

The method according to claim 10, wherein the monoclonal antibody is produced in CHO cells.

### Claim 12 (depends on 10)

The method according to claim 10, wherein the monoclonal antibody further comprises the heavy chain constant region polypeptide sequence of SEQ ID NO: 565.

### Claim 13 (depends on 2)

The method according to claim 2, wherein the monoclonal antibody comprises:
(A) a light chain polypeptide comprising the amino acid sequence of SEQ ID NO: 221; and
(B) a heavy chain polypeptide comprising the amino acid sequence of SEQ ID NO: 201.

### Claim 14 (depends on 2)

The method according to claim 2, wherein the monoclonal antibody comprises:
(A) a light chain polypeptide comprising the amino acid sequence of SEQ ID NO: 221; and
(B) a heavy chain polypeptide comprising the amino acid sequence of SEQ ID NO: 566.

### Claim 15 (depends on 2)

The method according to claim 2, wherein the patient experiences:
(i) a reduction in the number of migraine days per month in the one-month period following the administration of the monoclonal antibody, relative to the number of migraine days per month experienced by the patient during the previous one-month period prior to said administration;
(ii) a reduction in the number of migraine days per month in the three-month period following the administration of the monoclonal antibody, relative to the baseline number of migraine days per month experienced by the patient prior to said administration, wherein said baseline number of migraine days per month is determined over a period of one month or longer; and/or
(iii) a reduction in migraine prevalence in the one-month period after being administered the monoclonal antibody, relative to the patient's migraine prevalence during the previous one-month period prior to said administration.

### Claim 16 (depends on 1)

The method according to claim 1, wherein said administering is completed within 1-2 hours.

### Claim 17

A method of reducing the occurrence of migraine in a patient in need thereof, the method comprising intravenously administering to the patient, about 100 mg or about 300 mg of a monoclonal antibody comprising:
(A) a variable light chain polypeptide comprising light chain complementary determining region (CDR) 1, 2, and 3 polypeptide sequences of SEQ ID NO: 224, SEQ ID NO: 226, and SEQ ID NO: 228, respectively, and
(B) a variable heavy chain polypeptide comprising heavy chain CDR 1, 2, and 3 polypeptide sequences of SEQ ID NO: 204, SEQ ID NO: 206, and SEQ ID NO: 208, respectively,
wherein the administering begins while the patient is experiencing a headache, and wherein the administering is followed by administration of about 100 mg or about 300 mg of said monoclonal antibody once every three months.

### Claim 18 (depends on 17)

The method according to claim 17, wherein the patient suffers from chronic migraine.

### Claim 19 (depends on 18)

The method according to claim 18, wherein the about 100 mg or about 300 mg of the monoclonal antibody is intravenously administered to the patient once every three months, for at least six months.

### Claim 20 (depends on 17)

The method according to claim 17, wherein the patient suffers from episodic migraine.

### Claim 21 (depends on 20)

The method according to claim 20, wherein the about 100 mg or about 300 mg of the monoclonal antibody is intravenously administered to the patient once every three months, for at least twelve months.

### Claim 22 (depends on 17)

The method according to claim 17, wherein the monoclonal antibody comprises a human IgG1 constant region and is produced in CHO cells.

### Claim 23 (depends on 17)

The method according to claim 17, wherein the monoclonal antibody comprises a human IgG1 constant region and is produced in Pichia pastoris yeast cells.

### Claim 24 (depends on 17)

The method according to claim 17, wherein the monoclonal antibody is a humanized IgG1 monoclonal antibody.

### Claim 25 (depends on 17)

The method according to of claim 17, wherein:
(A) the variable light chain polypeptide comprises the amino acid sequence of SEQ ID NO: 222; and
(B) the variable heavy chain polypeptide comprises the amino acid sequence of SEQ ID NO: 202.

### Claim 26 (depends on 25)

The method according to claim 25, wherein the monoclonal antibody is produced in CHO cells.

### Claim 27 (depends on 25)

The method according to claim 25, wherein the monoclonal antibody further comprises the heavy chain constant region polypeptide sequence of SEQ ID NO: 565.

### Claim 28 (depends on 17)

The method according to claim 17, wherein the monoclonal antibody comprises:
(A) a light chain polypeptide comprising the amino acid sequence of SEQ ID NO: 221; and
(B) a heavy chain polypeptide comprising the amino acid sequence of SEQ ID NO: 201.

### Claim 29 (depends on 17)

The method according to claim 17, wherein the monoclonal antibody comprises:
(A) a light chain polypeptide comprising the amino acid sequence of SEQ ID NO: 221; and
(B) a heavy chain polypeptide comprising the amino acid sequence of SEQ ID NO: 566.

### Claim 30 (depends on 17)

The method according to claim 17, wherein the patient experiences:
(i) a reduction in the number of migraine days per month in the one-month period following the administration of the monoclonal antibody, relative to the number of migraine days per month experienced by the patient during the previous one-month period prior to said administration;
(ii) a reduction in the number of migraine days per month in the three-month period following the administration of the monoclonal antibody, relative to the baseline number of migraine days per month experienced by the patient prior to said administration, wherein said baseline number of migraine days per month is determined over a period of one month or longer; and/or
(iii) a reduction in migraine prevalence in the one-month period following the administration of the monoclonal antibody, relative to the patient's migraine prevalence during the previous one-month period prior to said administration.

### Claim 31 (depends on 17)

The method according to claim 17, wherein said administering is completed within 1-2 hours.