Regimens for treating HIV infections and AIDS

Patent metadata

Field	Value
Publication number	US-11564921-B2
Application number	US-201816631868-A
Country	US
Kind code	B2
Filing date	Jul 18, 2018
Priority date	Jul 21, 2017
Publication date	Jan 31, 2023
Grant date	Jan 31, 2023

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.

First claim

What is claimed is:

1. A method of treating HIV comprising intramuscularly administering to a subject in need thereof a dosage regimen consisting of either
(a) 400 mg of cabotegravir or a pharmaceutically acceptable salt thereof and 600 mg of rilpivirine or a pharmaceutically acceptable salt thereof administered every four weeks or once a month in two separate 2-mL injections, or
(b) 600 mg of cabotegravir or a pharmaceutically acceptable salt thereof and 900 mg of rilpivirine or a pharmaceutically acceptable salt thereof administered every 8 weeks or once every two months in two separate 3-mL injections.

2. The method according to claim 1 , wherein the dosage regimen for administration is every month or 4 weeks.

3. The method according to claim 2 , wherein the dosage regimen for administration is every 4 weeks.

4. A method of modifying an anti-HIV dosage regimen for a subject in need thereof comprising
discontinuing administration of a first oral anti-HIV regimen to the subject; and
intramuscularly administering to the subject, once every month or four weeks a dosage regimen consisting of
600 mg rilpivirine, or a pharmaceutically acceptable salt thereof in a 2-mL injection; and
400 mg cabotegravir, or a pharmaceutically acceptable salt thereof in a 2-mL injection.

5. The method of claim 4 , wherein the dosage regimen is two separate 2-mL injections administered every four weeks.

6. The method according to claim 1 , wherein the dosage regimen for administration is every 8 weeks or 2 months.

7. The method according to claim 6 , wherein the dosage regimen for administration is every 8 weeks.

8. A method of modifying an anti-HIV dosage regimen for a subject in need thereof comprising
discontinuing administration of a first oral anti-HIV regimen to the subject; and
intramuscularly administering to the subject, once every two months or eight weeks a dosage regimen consisting of
900 mg rilpivirine, or a pharmaceutically acceptable salt thereof in a 3-mL injection; and
600 mg cabotegravir, or a pharmaceutically acceptable salt thereof in a 3-mL injection.

9. The method according to claim 1 , wherein the subject exhibits a viral load of less than or equal to 50 copies of HIV-1 virus particles per mL of blood plasma (≤50 c/mL) after at least 96 weeks of administration of the dosage regimen.

10. The method of claim 4 , wherein the first oral anti-HIV regimen comprises
cabotegravir; and
two nucleoside reverse transcriptase inhibitors.

11. The method of claim 10 , wherein the first oral anti-HIV regimen comprises
cabotegravir; and
abacavir and lamivudine.

12. The method of claim 1 , wherein the subject is infected with HIV-1.

13. The method of claim 1 , wherein the subject exhibits a viral load of less than or equal to 50 copies of HIV-1 virus particles per mL of blood plasma (≤50 c/mL) prior to the administration of the dosage regimen.

14. The method of claim 1 , wherein the subject exhibits the same or an improved cluster of differentiation (CD) 4+cell count after at least 96 weeks, of once every month or 4 weeks, or once every two months or eight weeks, administration of the dosage regimen, as compared to the subject's CD4+count prior to the administration.

15. The method of claim 1 , wherein the subject does not exhibit an emergent resistance-associated mutation in an HIV virus after at least 96 weeks, of once every month or four weeks, or once every two months or eight weeks administration of the dosage regimen.

16. The method of claim 1 , wherein the method comprises intramuscularly administering to the subject in need thereof a dosage regimen consisting of either
(a) 400mg of cabotegravir and 600mg of rilpivirine or a pharmaceutically acceptable salt thereof administered every four weeks or once a month in two separate 2-mL injections, or
(b) 600mg of cabotegravir and 900mg of rilpivirine or a pharmaceutically acceptable salt thereof administered every 8 weeks or once every two months in two separate 3-mL injections.

17. The method of claim 1 , wherein the method comprises intramuscularly administering to the subject in need thereof a dosage regimen consisting of either
(a) 400mg of cabotegravir or a pharmaceutically acceptable salt thereof and 600mg of rilpivirine administered every four weeks or once a month in two separate 2-mL injections, or
(b) 600mg of cabotegravir or a pharmaceutically acceptable salt thereof and 900mg of rilpivirine administered every 8 weeks or once every two months in two separate 3-mL injections.

18. The method according to claim 2 , wherein the dosage regimen for administration is once every month.

19. The method according to claim 4 , wherein the dosage regimen is two separate 2-mL injections, administered once every month.

20. The method according to claim 6 , wherein the dosage regimen for administration is once every two months.

21. The method according to claim 8 , wherein the dosage regimen for administration is once every two months.

22. The method according to claim 8 , wherein the dosage regimen for administration is once every eight weeks.

23. The method of claim 1 , wherein the method comprises intramuscularly administering to the subject in need thereof a dosage regimen consisting of either
(a) 400mg of cabotegravir and 600mg of rilpivirine administered every four weeks or once a month in two separate 2-mL injections, or
(b) 600mg of cabotegravir and 900mg of rilpivirine administered every 8 weeks or once every two months in two separate 3-mL injections.

Assignees

• Viiv Healthcare Co
• Janssen Sciences Ireland Unlimited Co

Inventors

• Crauwels Herta
• Margolis David
• Spreen William R
• Spaltenstein Andrew
• Williams Peter

Classifications

• A61K31/7068

  having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid · CPC title

• A61K31/4985 Primary

  Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems · CPC title

• A61K31/505 Primary

  Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim · CPC title

• A61K9/0019

  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) · CPC title

• A61K31/7076

  containing purines, e.g. adenosine, adenylic acid · CPC title