# US 12,005,072 B2 · HIV drug combination for increasing barrier against resistance

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

- Number: US 12,005,072 B2
- Document ID: US12005072B2
- Status: Granted
- Kind: B2
- Application number: 17/258,649
- Filed: 2019-07-12
- Published: 2021-09-16
- Granted: 2024-06-11
- Earliest claimed: 2018-07-17
- Assignees: Merck Sharp & Dohme Corp.
- Applicants: Merck Sharp & Dohme LLC
- Inventors: Daria Jean Hazuda; Ming-Tain Lai
- Web page: https://patentgrep.com/patent/US12005072B2

## CPC

- A61K 31/7076: containing purines, e.g. adenosine, adenylic acid
- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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

The instant invention relates to a method for reducing the risk for development of anti-viral treatment resistance due to an HIV mutation in a human subject infected with HIV, comprising administering EFdA in combination with one or more anti-viral agents.

## Claims

### Claim 1

A method of reducing the risk for development of anti-viral treatment resistance due to an HIV mutation in a human subject infected with HIV, comprising administering an effective amount of EFdA in combination with one or more additional HIV antiviral drugs, wherein the additional antiviral drug is doravirine.

### Claim 2 (depends on 1)

The method of claim 1, wherein the HIV mutation is selected from the group consisting of F227C, F227C with one or more NNRTI-associated mutations, F227C with one or more NRTI-associated mutations, and combinations thereof.

### Claim 3 (depends on 2)

The method of claim 2 wherein the NNRTI-associated mutation is selected from the group consisting of L100I, K101E, K101P, K103N, K103S, V106A, V1061, V106M, V1081, E138A, E138G, E138K, E138Q, E138R, V179L, Y181C, Y1811, Y181V, Y188C, Y188H, Y188L, G190A, G190S, H221Y, L2341, P225H, F227C, F227L, F227V, M230L, M230I, P236L, Y318F, and combinations thereof.

### Claim 4 (depends on 2)

The method of claim 2 wherein the NRTI-associated mutation is selected from the group consisting of M184V/I, K65R, M41L, D67N, K70R/E, T69inst, Q151M, L210W, T215Y/F, K219Q/E, L74V, Y115F, and combinations thereof.

### Claim 5 (depends on 2)

The method of claim 2 wherein the HIV mutation is selected from the group consisting of F227C, A98G/F227C, V106I/F227C, C106M/F227C, V106/F227C/H221Y, and A98G/V106I/H221Y/F227C.

### Claim 6 (depends on 5)

The method of claim 5 wherein the HIV mutation is F227C.

### Claim 7 (depends on 3)

The method of claim 3 wherein the NRTI-associated mutation is selected from the group consisting of M184V/I, K65R, M41L, D67N, K70R/E, T69inst, Q151M, L210W, T215Y/F, K219Q/E, L74V, Y115F, and combinations thereof.

### Claim 8 (depends on 1)

The method of claim 1 wherein the HIV mutation exhibits hypersusceptibility to EFdA.

### Claim 9 (depends on 1)

The method of claim 1, wherein the doravirine is administered in an amount of 100 mg.

### Claim 10 (depends on 1)

The method of claim 1, wherein the EFdA is administered in an amount of 0.25 mg.

### Claim 11 (depends on 1)

The method of claim 1, wherein the EFdA and the doravirine are administered in a fixed combination of 0.25 mg EFdA and 100 mg doravirine.

### Claim 12

A method of reducing the risk for development of anti-viral treatment resistance due to an F227C HIV mutation in a human subject infected with HIV, comprising administering an effective amount of EFdA in combination with doravirine.

### Claim 13 (depends on 12)

The method of claim 12, wherein the doravirine is administered in an amount of 100 mg.

### Claim 14 (depends on 12)

The method of claim 12, wherein the EFdA is administered in an amount of 0.25 mg.

### Claim 15 (depends on 12)

The method of claim 12, wherein the EFdA and the doravirine are administered in a fixed combination of 0.25 mg EFdA and 100 mg doravirine.