# US 12,594,319 B2 · Pharmaceutical development

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- Number: US 12,594,319 B2
- Document ID: US12594319B2
- Status: Granted
- Kind: B2
- Application number: 17/630,645
- Filed: 2020-07-28
- Published: 2022-08-18
- Granted: 2026-04-07
- Earliest claimed: 2019-07-29
- Assignees: Helperby Therapeutics Limited
- Applicants: Helperby Therapeutics Limited
- Inventors: Professor Anthony Coates; Yanmin Hu
- Web page: https://patentgrep.com/patent/US12594319B2

## CPC

- 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 38/12: Cyclic peptides {, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C (A61K38/043 - A61K38/046 take precedence)}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 9/19: lyophilised {, i.e. freeze-dried, solutions or dispersions (lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00)}
- A61K 31/7072: having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
- A61P 31/04: Antibacterial agents
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The present invention relates to a pharmaceutical product in the form of a storage stable lyophilisate or a pharmaceutical formulation in the form of a sterile solution for parenteral administration. Both the lyophilisate and solution consist essentially of a polymyxin selected from polymyxin E, polymyxin B, or a pharmaceutically acceptable derivative thereof, and zidovudine or a pharmaceutically acceptable derivative thereof. The solution further includes an aqueous carrier.

## Claims

### Claim 1

A pharmaceutical product comprising:
i) a polymyxin that is colistin methane sulfonate or a pharmaceutically acceptable salt thereof;
ii) zidovudine or a pharmaceutically acceptable salt thereof; and
iii) optionally one or more of a buffering agent,
wherein the pharmaceutical product is formulated as a storage stable lyophilizate.

### Claim 2 (depends on 1)

The pharmaceutical product of claim 1, wherein the storage stable lyophilizate consists of the polymyxin and the zidovudine.

### Claim 3 (depends on 1)

The pharmaceutical product of claim 1, wherein the polymyxin is colistin methane sulfonate sodium.

### Claim 4 (depends on 1)

The pharmaceutical product of claim 1, wherein the polymyxin is present in an amount between about 0.5 MIU and about 14 MIU.

### Claim 5 (depends on 1)

The pharmaceutical product of claim 1, wherein the zidovudine is present in a therapeutically effective amount of between about 50 mg and about 1500 mg.

### Claim 6 (depends on 1)

The pharmaceutical product of claim 1, wherein the polymyxin is present in an amount, the zidovudine is present in a therapeutically effective amount, and the amount of polymyxin is greater than the therapeutically effective amount of zidovudine, on a % w/w basis.

### Claim 7 (depends on 6)

The pharmaceutical product of claim 6, wherein the weight ratio of polymyxin to zidovudine is between about 8:1 to about 11:10.

### Claim 8 (depends on 1)

The pharmaceutical product of claim 1, for use in treating a gram-negative bacterial infection.

### Claim 9 (depends on 8)

The pharmaceutical product for use of claim 8, wherein the gram-negative bacterial infection is caused by Enterobacteriaceae, Enterobacter, Pseudomonas, or Acinetobacter.

### Claim 10 (depends on 8)

The pharmaceutical product for use of claim 8, wherein the gram-negative bacterial infection is caused by a (multi)-drug-resistant strain of bacteria.

### Claim 11 (depends on 1)

A sealed vial containing the pharmaceutical product of claim 1.

### Claim 12 (depends on 1)

The pharmaceutical product of claim 1, wherein the therapeutically effective amount of zidovudine is between about 150 mg and about 500 mg.

### Claim 13 (depends on 1)

The pharmaceutical product of claim 1, wherein the amount of the polymyxin is between about 40 mg and about 400 mg.

### Claim 14 (depends on 1)

A method of treating a gram-negative bacterial infection comprising administering an effective amount of the pharmaceutical product of claim 1 to a subject in need thereof.

### Claim 15 (depends on 14)

The method of claim 14, wherein the gram-negative bacterial infection is caused by Enterobacteriaceae, Enterobacter, Pseudomonas, or Acinetobacter.

### Claim 16 (depends on 14)

The method of claim 14, wherein the gram-negative bacterial infections is caused by a (multi)-drug-resistant strain of bacteria.

### Claim 17 (depends on 1)

A process for preparing the pharmaceutical product of claim 1, wherein the process comprises: mixing a therapeutically effective amount of the polymyxin, a therapeutically effective amount of zidovudine or the pharmaceutically acceptable salt thereof, and an aqueous carrier, to form a sterile solution, sterile filtering the solution, filling a vial with the filtered solution, and subjecting the filled vial to lyophilization.

### Claim 18 (depends on 17)

The process of claim 17, wherein the polymyxin is colistin methane sulfonate sodium.

### Claim 19 (depends on 17)

The process of claim 17, wherein the fill volume per vial is between about 10 ml and about 20 ml.