Anti-PCSK9 antibodies
AssigneeRegeneron Pharmaceuticals, Inc.
InventorsMark W. Sleeman, Joel H. Martin, Tammy T. Huang, Douglas MacDonald
Life of this patent
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Abstract
An human antibody or antigen-binding fragment of a human antibody that specifically binds and inhibits human proprotein convertase subtilisin/kexin type 9 (hPCSK9) characterized by the ability to reduce serum LDL cholesterol by 40-80% over a 24, 60 or 90 day period relative to predose levels, with little or no reduction in serum HDL cholesterol and/or with little or no measurable effect on liver function, as determined by ALT and AST measurements.
Claims12
A nucleic acid molecule encoding a heavy chain variable region (HCVR) and a light chain variable region (LCVR) of an anti-human proprotein convertase subtilisin/kexin type 9 (PCSK9) PCSK9 antibody or antigen-binding fragment thereof,
- wherein the HCVR comprises a heavy chain complementarity determining region (HCDR) 1 comprising the amino acid sequence of SEQ ID NO:220, an HCDR2 comprising the amino acid sequence of SEQ ID NO:222, and an HCDR3 comprising the amino acid sequence of SEQ ID NO:224;
- and
- wherein the LCVR comprises a light chain complementarity determining region (LCDR) 1 comprising the amino acid sequence of SEQ ID NO:228, an LCDR2 comprising the amino acid sequence LGS, and an LCDR3 comprising the amino acid sequence of SEQ ID NO:
- 232.
A method of producing an anti-human PCSK9 antibody or antigen-binding fragment thereof, the method comprising:
- culturing a host cell under conditions permitting production of the antibody or antigen-binding fragment thereof,
- wherein the host cell comprises:
- (i) a first recombinant expression vector comprising a nucleic acid molecule encoding an HCVR of the anti-human PCSK9 antibody,
- wherein the HCVR comprises an HCDR1 having the amino acid sequence of SEQ ID NO:220, an HCDR2 having the amino acid sequence of SEQ ID NO:222, and an HCDR3 having the amino acid sequence of SEQ ID NO:224;
- and
- (ii) a second recombinant expression vector comprising a nucleic acid molecule encoding a LCVR of the anti-human PCSK9 antibody,
- wherein the LCVR comprises an LCDR1 having the amino acid sequence of SEQ ID NO:228, an LCDR2 having the amino acid sequence LGS, and an LCDR3 having the amino acid sequence of SEQ ID NO:232;
- and
- recovering the antibody or antigen-binding fragment produced.
Dependencies are inferred from the claim text.