US 12,281,173 B2
Methods for treating patients with hyperlipidemia by administering a PCSK9 inhibitor in combination with an ANGPTL3 inhibitor
Viktoria Gusarova, Pleasantville, NY (US); Jesper Gromada, Scarsdale, NY (US); and Andrew J. Murphy, Croton-on-Hudson, NY (US)
Assigned to Regeneron Pharmaceuticals, Inc., Tarrytown, NY (US)
Filed by Regeneron Pharmaceuticals, Inc., Tarrytown, NY (US)
Filed on Mar. 3, 2020, as Appl. No. 16/808,058.
Application 16/808,058 is a continuation of application No. 15/446,720, filed on Mar. 1, 2017, abandoned.
Claims priority of provisional application 62/302,907, filed on Mar. 3, 2016.
Prior Publication US 2020/0199253 A1, Jun. 25, 2020
Int. Cl. C07K 16/40 (2006.01); A61K 9/00 (2006.01); C07K 16/22 (2006.01); A61K 39/00 (2006.01)
CPC C07K 16/40 (2013.01) [A61K 9/0019 (2013.01); C07K 16/22 (2013.01); A61K 2039/505 (2013.01); A61K 2039/507 (2013.01); A61K 2039/545 (2013.01); C07K 2317/21 (2013.01); C07K 2317/56 (2013.01); C07K 2317/565 (2013.01); C07K 2317/76 (2013.01)] 25 Claims
 
1. A method of treating a patient suffering from familial hypercholesterolemia (FH), wherein the patient is non-responsive to, inadequately controlled by, or intolerant to treatment with a standard lipid modifying therapy, the method comprising treating the patient with a combination of a proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor and an inhibitor of angiopoietin-like protein 3 (ANGPTL3), wherein the PSCK9 inhibitor is an antibody, or an antigen-binding fragment thereof, that binds specifically to PCSK9, wherein the antibody or antigen-binding fragment thereof that binds specifically to PCSK9 comprises the complementary determining regions (CDRs) of a heavy chain variable (HCVR) having the amino acid sequence of SEQ ID NO: 12 and the CDRs of a light chain variable region (LCVR) of SEQ ID NO: 17, wherein the ANGPTL3 inhibitor is an antibody, or an antigen-binding fragment thereof, that binds specifically to ANGPTL3, wherein the antibody or antigen-binding fragment thereof that binds specifically to ANGPTL3 comprises the complementary determining regions (CDRs) of a heavy chain variable (HCVR) having the amino acid sequence of SEQ ID NO: 2 and the CDRs of a light chain variable region (LCVR) of SEQ ID NO: 3, wherein the patient who is non-responsive to, inadequately controlled by, or intolerant to treatment with a standard lipid modifying therapy exhibits (i) an LDL-C level of greater than or equal to 100 mg/dL despite undergoing the standard lipid modifying therapy or (ii) a reduction in LDL-C or non-HDL-C of less than 50% from baseline despite undergoing the standard lipid modifying therapy.