IP Library Granted Patent US 12,005,072
Granted Patent B2
US 12,005,072 · App. 17/258,649 · Granted Jun 11, 2024

HIV drug combination for increasing barrier against resistance

Inventors: Daria Jean Hazuda (Doylestown, PA); Ming-Tain Lai (Lansdale, PA)
Assignee: Merck Sharp & Dohme LLC
A61K31/7076A61K31/4439A61P31/18
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Quick Facts
Patent No.
US 12,005,072
App. No.
17/258,649
Granted
Jun 11, 2024
Kind
B2
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 (15)

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.

2. 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.

3. 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.

4. 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.

5. 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.

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

7. 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.

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

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

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

11. 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.

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.

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

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

15. 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.

Assignments (2)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 7, 2021
From: HAZUDA, DARIA JEAN; LAI, MING-TAIN
To: MERCK SHARP & DOHME CORP.
Reel/Frame 054847/0826 →