# US 12,178,815 B2 · Regimens for treating HIV infections and aids

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- Number: US 12,178,815 B2
- Document ID: US12178815B2
- Status: Granted
- Kind: B2
- Application number: 18/762,939
- Filed: 2024-07-03
- Published: 2024-10-24
- Granted: 2024-12-31
- Earliest claimed: 2017-07-21
- Assignees: ViiV Healthcare Company; Janssen Sciences Ireland Unlimited Company
- Applicants: ViiV Healthcare Company; Janssen Sciences Ireland Unlimited Company
- Inventors: Herta Crauwels; David Margolis; William R. Spreen; Andrew Spaltenstein; Peter Williams
- Web page: https://patentgrep.com/patent/US12178815B2

## CPC

- A61K 31/4985: Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
- 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 31/505: Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K 31/7068: having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K 31/7076: containing purines, e.g. adenosine, adenylic acid
- A61P 31/18: for HIV
- 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

A method of treating HIV comprising intramuscular administration once every 4 weeks or less frequently of a combination of cabotegravir or a pharmaceutically acceptable salt thereof and rilpivirine or a pharmaceutically acceptable salt thereof, including the option of discontinuing administration of a first oral anti-retroviral regimen and intramuscularly administering, once four weeks or less often said combination of cabotegravir and rilpivirine.

## Claims

### Claim 1

A method of treating HIV-1 infection in a subject in need thereof, comprising intramuscularly administering into a gluteus medius muscle of the subject effective amounts of cabotegravir and rilpivirine resulting in the subject having a viral load of less than or equal to 50 copies of HIV-1 virus particles per mL of blood plasma (≤50 c/mL) in the subject after at least 96 weeks of administration,
wherein the effective amounts of cabotegravir and rilpivirine result in the subject having the viral load of ≤50 c/mL and comprise 400 mg of cabotegravir in a 2-mL injectable formulation and 600 mg of rilpivirine in a separate 2-mL injectable formulation administered once every four weeks or once a month.

### Claim 2 (depends on 1)

The method of claim 1, wherein the effective amounts of cabotegravir and rilpivirine which result in the subject having the viral load of ≤50 c/mL are administered once every four weeks.

### Claim 3 (depends on 1)

The method of claim 1, wherein the effective amounts of cabotegravir and rilpivirine which result in the subject having the viral load of ≤50 c/mL are administered once every month.

### Claim 4 (depends on 1)

The method of claim 1, wherein the effective amounts of cabotegravir and rilpivirine which result in the subject having the viral load of ≤50 c/mL are administered once every four weeks or once a month, with a 14-day dosing window.

### Claim 5 (depends on 1)

The method of claim 1, wherein the subject received oral anti-HIV therapy which was discontinued prior to the intramuscular administration.

### Claim 6 (depends on 5)

The method of claim 5, wherein the oral anti-HIV therapy comprised once daily administration of cabotegravir or a pharmaceutically acceptable salt thereof and/or once daily administration of rilpivirine or a pharmaceutically acceptable salt thereof.

### Claim 7 (depends on 6)

The method of claim 6, wherein the oral anti-HIV therapy comprised once daily administration of an amount by weight of the pharmaceutically acceptable salt of cabotegravir equivalent to 30 mg of cabotegravir and/or once daily administration of an amount by weight of the pharmaceutically acceptable salt of rilpivirine equivalent to 25 mg of rilpivirine.

### Claim 8 (depends on 1)

The method of claim 1, wherein the method comprises intramuscularly administering into a gluteus medius muscle of the subject effective amounts of cabotegravir and rilpivirine resulting in the subject having a viral load of less than 50 copies of HIV-1 virus particles per mL of blood plasma (<50 c/mL) in the subject after at least 96 weeks of administration,
wherein the effective amounts of cabotegravir and rilpivirine result in the subject having the viral load of <50 c/mL and comprise 400 mg of cabotegravir in a 2-mL injectable formulation and 600 mg of rilpivirine in a separate 2-mL injectable formulation administered once every four weeks or once a month.

### Claim 9

A method of treating HIV-1 infection in a subject in need thereof, comprising intramuscularly administering into a gluteus medius muscle of the subject effective amounts of cabotegravir and rilpivirine resulting in the subject having a viral load of less than or equal to 50 copies of HIV-1 virus particles per mL of blood plasma (≤50 c/mL) in the subject after at least 96 weeks of administration,
wherein the effective amounts of cabotegravir and rilpivirine result in the subject having the viral load of ≤50 c/mL and comprise 600 mg of cabotegravir in a 3-mL injectable formulation and 900 mg of rilpivirine in a separate 3-mL injectable formulation administered every once eight weeks or once every two months.

### Claim 10 (depends on 9)

The method of claim 9, wherein the effective amounts of cabotegravir and rilpivirine which result in the subject having the viral load of ≤50 c/mL are administered once every eight weeks.

### Claim 11 (depends on 9)

The method of claim 9, wherein the effective amounts of cabotegravir and rilpivirine which result in the subject having the viral load of ≤50 c/mL are administered once every two months.

### Claim 12 (depends on 9)

The method of claim 9, wherein the effective amounts of cabotegravir and rilpivirine which result in the subject having the viral load of ≤50 c/mL are administered once every eight weeks or once every 2 months, with a 14-day dosing window.

### Claim 13 (depends on 9)

The method of claim 9, wherein the subject received oral anti-HIV therapy which was discontinued prior to the intramuscular administration.

### Claim 14 (depends on 13)

The method of claim 13, wherein the oral anti-HIV therapy comprised once daily administration of cabotegravir or a pharmaceutically acceptable salt thereof and/or once daily administration of rilpivirine or a pharmaceutically acceptable salt thereof.

### Claim 15 (depends on 14)

The method of claim 14, wherein the oral anti-HIV therapy comprised once daily administration of an amount by weight of the pharmaceutically acceptable salt of cabotegravir equivalent to 30 mg of cabotegravir and/or once daily administration of an amount by weight of the pharmaceutically acceptable salt of rilpivirine equivalent to 25 mg of rilpivirine.

### Claim 16 (depends on 9)

The method of claim 9, wherein the method comprises intramuscularly administering into a gluteus medius muscle of the subject effective amounts of cabotegravir and rilpivirine resulting in the subject having a viral load of less than 50 copies of HIV-1 virus particles per mL of blood plasma (<50 c/mL) in the subject after at least 96 weeks of administration,
wherein the effective amounts of cabotegravir and rilpivirine result in the subject having the viral load of <50 c/mL and comprise 600 mg of cabotegravir in a 3-mL injectable formulation and 900 mg of rilpivirine in a separate 3-mL injectable formulation administered once every eight weeks or once every two months.

### Claim 17

A method of treating HIV-1 infection in a subject in need thereof, comprising intramuscularly administering into a gluteus medius muscle of the subject effective amounts of cabotegravir and rilpivirine which do not result in an emergent resistance-associated mutation in an HIV virus in the subject after at least 96 weeks of administration,
wherein the effective amounts of cabotegravir and rilpivirine comprise 400 mg of cabotegravir in a 2-mL injectable formulation and 600 mg of rilpivirine in a separate 2-mL injectable formulation administered every four weeks or once a month.

### Claim 18 (depends on 17)

The method of claim 17, wherein the effective amounts of cabotegravir and rilpivirine are administered once every four weeks.

### Claim 19 (depends on 17)

The method of claim 17, wherein the effective amounts of cabotegravir and rilpivirine are administered once every month.

### Claim 20 (depends on 17)

The method of claim 17, wherein the effective amounts of cabotegravir and rilpivirine are administered once every four weeks or once a month, with a 14-day dosing window.

### Claim 21 (depends on 17)

The method of claim 17, wherein the subject received oral anti-HIV therapy which was discontinued prior to the intramuscular administration.

### Claim 22 (depends on 21)

The method of claim 21, wherein the oral anti-HIV therapy comprised once daily administration of cabotegravir or a pharmaceutically acceptable salt thereof and/or once daily administration of rilpivirine or a pharmaceutically acceptable salt thereof.

### Claim 23 (depends on 22)

The method of claim 22, wherein the oral anti-HIV therapy comprised once daily administration of an amount by weight of the pharmaceutically acceptable salt of cabotegravir equivalent to 30 mg of cabotegravir and/or once daily administration of an amount by weight of the pharmaceutically acceptable salt of rilpivirine equivalent to 25 mg of rilpivirine.

### Claim 24

A method of treating HIV-1 infection in a subject in need thereof, comprising intramuscularly administering into a gluteus medius muscle of the subject effective amounts of cabotegravir and rilpivirine which do not result in an emergent resistance-associated mutation in an HIV virus in the subject after at least 96 weeks of administration,
wherein the effective amounts of cabotegravir and rilpivirine comprise 600 mg of cabotegravir in a 3-mL injectable formulation and 900 mg of rilpivirine in a separate 3-mL injectable formulation administered once every eight weeks or once every two months.

### Claim 25 (depends on 24)

The method of claim 24, wherein the effective amounts of cabotegravir and rilpivirine are administered once every eight weeks.

### Claim 26 (depends on 24)

The method of claim 24, wherein the effective amounts of cabotegravir and rilpivirine are administered once every two months.

### Claim 27 (depends on 24)

The method of claim 24, wherein the effective amounts of cabotegravir and rilpivirine are administered once every eight weeks or once every 2 months, with a 14-day dosing window.

### Claim 28 (depends on 24)

The method of claim 24, wherein the subject received oral anti-HIV therapy which was discontinued prior to the intramuscular administration.

### Claim 29 (depends on 28)

The method of claim 28, wherein the oral anti-HIV therapy comprised once daily administration of cabotegravir or a pharmaceutically acceptable salt thereof and/or once daily administration of rilpivirine or a pharmaceutically acceptable salt thereof.

### Claim 30 (depends on 29)

The method of claim 29, wherein the oral anti-HIV therapy comprised once daily administration of an amount by weight of the pharmaceutically acceptable salt of cabotegravir equivalent to 30 mg of cabotegravir and/or once daily administration of an amount by weight of the pharmaceutically acceptable salt of rilpivirine equivalent to 25 mg of rilpivirine.