INHIBITION OF HIV INFECTION THROUGH CHEMOPROPHYLAXIS

• US 20170143745A1
• Filed: 01/13/2017
• Published: 05/25/2017
• Est. Priority Date: 02/03/2006
• Status: Active Grant

• Current Assignee: United States Department Of Health And Human Services
• Original Assignee: The United States of America As Represented By The Secretary of Agriculture
• Inventors: Heneine, Walid, Otten, Ronald A., Garcia Lerma, Jose Gerardo, Folks, Thomas M., Janssen, Robert
• Granted Patent: US 9,937,191 B2
• Time in Patent Office: Days
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/513 having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• CPC Class Codes: A61K 31/675 having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• CPC Class Codes: A61K 31/683 Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
• CPC Class Codes: A61K 31/7072 having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/0034 Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61P 31/18 for HIV

Abstract

A process is provided for protecting a primate host from a self-replicating infection by an immunodeficiency retrovirus. Protection is achieved by administering to the primate host a combination of a pharmaceutically effective amount of a nucleoside reverse transcriptase inhibitor and a pharmaceutically effective amount of a nucleotide reverse transcriptase inhibitor prior to exposure to the immunodeficiency retrovirus. The administration is effective if provided in a single dose within 24 hours of the exposure. A regime of regular daily doses is also effective in providing protection against an immunodeficiency retrovirus becoming self-replicating after infecting a primate host. A process for controlling retrovirus transmission within a population includes the administration to a subpopulation at high risk for contracting an immunodeficiency retroviral infection the detailed combination prior to sexual exposure to a source of immunodeficiency retrovirus so as to preclude the immunodeficiency retrovirus from becoming self-replicating in a member of the subpopulation.

Claims

1. A process of protecting a primate host from a self-replicating infection by an immunodeficiency retrovirus comprising:

(a) selecting a primate host not infected with the immunodeficiency retrovirus, and

(b) administering directly to an uninfected primate host a combination comprising;

i. a pharmaceutically effective amount of emtricitabine; and

ii. a pharmaceutically effective amount of tenofovir or a tenofovir prodrug,

wherein the combination is administered orally prior to the exposure of the primate host to the immunodeficiency retrovirus,

thereby protecting the primate host from infection with the immunodeficiency retrovirus.

2. The process of claim 1, wherein selecting a primate host comprises selecting an adult human not infected with the immunodeficiency retrovirus.

3. The process of claim 2, wherein the adult human is a male.

4. The process of claim 2, wherein the pharmaceutically effective amount of emtricitabine and the pharmaceutically effective amount of tenofovir or the tenofovir prodrug, are administered directly to the human in a combined single dosage formulation.

5. The process of claim 2, wherein immunodeficiency retrovirus is a human immunodeficiency virus.

6. The process of claim 5, wherein a human immunodeficiency virus (HIV) is HIV-1.

7. The process of claim 1, wherein the combination is administered as preexposure prophylactic treatment prior to rectal and/or vaginal exposure of the primate host to the immunodeficiency retrovirus.

8. The process of claim 1, comprising administering 200 milligrams (mg) of emtricitabine to the primate host.

9. The process of claim 1, wherein the combination is administered daily for several days, weeks or months.

10. The process of claim 9, wherein the combination is administered daily for several days, weeks or months both before after an exposure of the primate host to the immunodeficiency retrovirus.

11. The process of claim 1, wherein administration of the combination results in an absence of persistent viremia and seroconversion of the primate host.

19. The process of claim 1, wherein the combination comprises the tenofovir prodrug.

12. A process for inhibiting establishment of a human immunodeficiency virus self-replicating infection of human immunodeficiency virus infection in a human, comprising:

(a) selecting an uninfected human that does not have the self-replicating infection; and

(b) administering to the uninfected human a combination comprising;

i. a pharmaceutically effective amount of emtricitabine; and

ii. a pharmaceutically effective amount of tenofovir or a tenofovir prodrug;

thereby inhibiting the establishment of the self-replicating infection with the immunodeficiency virus in the human.

13. The process of claim 12, wherein the combination is administered prior to a potential exposure of the human to the human immunodeficiency retrovirus.

14. The process of claim 12, wherein the combination is compounded into a single combination formulation.

15. The process of claim 12, wherein an inhibition of infection in the host is determined by an absence of persistent viremia and seroconversion in the human following the exposure to the immunodeficiency retrovirus.

16. The process of claim 12, wherein the combination is administered following potential exposure of the primate host to the human immunodeficiency retrovirus.

17. The process of claim 16, wherein the potential exposure to the human immunodeficiency retrovirus comprises sexual intercourse, medical worker skin puncture inoculation, hypodermic needle sharing, or blood transfusion.

18. The process of claim 12, wherein the combination comprises the tenofovir prodrug.