Granted Patent B2

US 12,606,638 · App. 18/301,638 · Granted Apr 21, 2026

Inventors: Marie Baccara-Dinet (Paris, FR); Laurence Bessac (Paris, FR); Corinne Hanotin (Paris, FR); Robert C. Pordy (Tarrytown, NY); William J. Sasiela (Tarrytown, NY); Jacques Rey (Paris, FR)

Assignees: SANOFI BIOTECHNOLOGY; REGENERON PHARAMACEUTICALS, INC.

C07K16/40A61K2039/505A61K2039/545C07K2317/21C07K2317/56C07K2317/565C07K2317/76

Abstract

Claims (20)

1 . A method for reducing low-density lipoprotein cholesterol (LDL-C) in a subject in need thereof, the method comprising:

(a) selecting a subject with primary hypercholesterolemia who is not taking a statin; and

(b) administering to the subject a pharmaceutical composition comprising an anti-proprotein convertase subtilisin/kexin type 9 (anti-PCSK9) antibody or antigen-binding fragment thereof at a dose of about 300 mg every 4 weeks for at least 3 doses in the absence of a concomitant statin therapy, wherein the antibody or antigen-binding fragment thereof comprises the heavy and light chain complementarity determining regions (CDRs) of a heavy chain variable region/light chain variable region (HCVR/LCVR) amino acid sequence pair of SEQ ID NOs: 1/6,

thereby reducing the LDL-C in the subject.

2 . The method of claim 1 , wherein the antibody or antigen-binding fragment thereof comprises heavy and light chain CDR amino acid sequences having SEQ ID NOs: 2, 3, 4, 7, 8, and 10.

3 . The method of claim 2 , wherein the antibody or antigen-binding fragment thereof comprises an HCVR having the amino acid sequence of SEQ ID NO:1 and an LCVR having the amino acid sequence of SEQ ID NO:6.

4 . The method of claim 1 , wherein the subject is on a non-statin lipid-lowering agent before and/or during administration of the antibody or antigen-binding protein.

5 . The method of claim 4 , wherein the non-statin lipid-lowering agent is selected from the group consisting of: ezetimibe, a fibrate, fenofibrate, niacin, an omega-3 fatty acid, and a bile acid resin.

6 . The method of claim 5 , wherein the non-statin lipid-lowering agent is ezetimibe or fenofibrate.

7 . The method of claim 1 , wherein the antibody or antigen binding protein is administered subcutaneously.

8 . The method of claim 1 , wherein the subject is not on a non-statin lipid-lowering agent before and/or during administration of the antibody or antigen-binding fragment thereof.

9 . The method of claim 1 , wherein the subject has a form of hypercholesterolemia that is not Familial Hypercholesterolemia (nonFH).

10 . The method of claim 1 , wherein the subject has heterozygous Familial Hypercholesterolemia (heFH).

11 . The method of claim 10 , wherein the diagnosis of heFH is made either by genotyping or clinical criteria.

12 . The method of claim 11 , wherein the clinical criteria is either the Simon Broome Register Diagnostic Criteria for Heterozygous Familial Hypercholesterolemia, or the WHO/Dutch Lipid Network criteria with a score >8.

13 . The method of claim 1 , further comprising the step of (c) administering to the subject one or more following doses of 300 mg of the antibody or antigen-binding fragment thereof about every four weeks if the LDL-C level in the subject after step (b) is lower than 70 mg/dL, or administering one or more following doses of 150 mg of the antibody or antigen-binding fragment thereof about every two weeks if the LDL-C level in the subject after step (b) is greater than or equal to 70 mg/dL.

14 . The method of claim 1 , further comprising the step of measuring the LDL-C of the subject after step (a) and before step (b).

15 . The method of claim 14 , wherein the LDL-C of the subject is measured just prior to the next scheduled dose of the antibody or antigen-binding fragment thereof.

16 . The method of claim 13 , further comprising the step of measuring the LDL-C of the subject after step (b) and before step (c).

17 . The method of claim 16 , wherein the LDL-C of the subject is measured just prior to the next scheduled dose of the antibody or antigen-binding fragment thereof.

Assignments (3)

Priority Claims (1)

Continuity (5)

References Cited (400)