# US 10,307,463 B2 · Method for administering omega-conopeptide

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

- Number: US 10,307,463 B2
- Document ID: US10307463B2
- Status: Granted
- Kind: B2
- Application number: 15/651,655
- Filed: 2017-07-17
- Published: 2017-11-02
- Granted: 2019-06-04
- Earliest claimed: 2003-10-02
- Assignees: TerSera Therapeutics LLC
- Applicants: TerSera Therapeutics LLC
- Inventors: David J. Ellis; George P. Miljanich; David E. Shields
- Web page: https://patentgrep.com/patent/US10307463B2

## CPC

- A61K 38/1767: {from invertebrates}
- A61K 9/0085: {Brain, e.g. brain implants; Spinal cord}
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 31/195: having an amino group
- A61K 31/4168: having a nitrogen attached in position 2, e.g. clonidine
- A61K 31/445: Non condensed piperidines, e.g. piperocaine
- A61K 31/4468: having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
- A61K 31/451: having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
- A61K 31/4535: containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 38/17: from animals; from humans {(enzyme inhibitors A61K38/005)}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/20: containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 14/43504: {from invertebrates}
- 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
- 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)

## Abstract

The present invention is directed to a method of producing analgesia in a mammalian subject. The method includes administering to the subject an omega conopeptide, preferably ziconotide, in combination with an analgesic selected from the group consisting of morphine, bupivacaine, clonidine, hydromorphone, baclofen, fentanyl 1, buprenorphine, and sufentanil, or its pharmaceutically acceptable salts thereof, wherein the ω-conopeptide retains its potency and is physically and chemically compatible with the analgesic compound. A preferred route of administration is intrathecal administration, particularly continuous intrathecal infusion. The present invention is also directed to a pharmaceutical formulation comprising an omega conopeptide, preferably ziconotide, an antioxidant, in combination with an analgesic selected from the group consisting of morphine, bupivacaine, clonidine, hydromorphone, baclofen, fentanyl, buprenorphine, and sufentanil.

## Claims

### Claim 1

A method for treating severe chronic pain in a human patient, comprising:
(a) selecting a human patient who is suffering from severe chronic pain and is being administered a therapeutically effective amount of an opioid; and
(b) administering ziconotide to the human patient by continuous intrathecal infusion with a dose starting at 0.6 μg/day, titrating upward by up to 2.4 μg/day per week, and up to a maximum of 7.2 μg/day, or until improved analgesia is obtained.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the patient is treated for 14-35 days.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the cumulative dose of the ziconotide is 8.8-118.6 μg.

### Claim 4 (depends on 1)

The method according to claim 1, wherein said ziconotide is administered in a pharmaceutical composition comprising an antioxidant.

### Claim 5 (depends on 4)

The method according to claim 4, wherein said antioxidant is methionine.

### Claim 6 (depends on 4)

The method according to claim 4, wherein said pharmaceutical formulation has pH between 4 and 4.5.

### Claim 7 (depends on 4)

The method according to claim 4, wherein said ziconotide is supplied in a single dose vial.

### Claim 8 (depends on 7)

The method according to claim 7, wherein said ziconotide has a concentration of 100 μg/mL in the vial.

### Claim 9 (depends on 1)

The method according to claim 1, wherein the ziconotide is administered via a drug dispensing implantable pump.