Antagonists of pcsk9
OwnerCarl P. Sparrow, Ayesha Sitlani +3inventors
InventorsCarl P. Sparrow, Ayesha Sitlani, Shilpa Pandit, Jon H. Condra, Holly A. Hammond
Life of this patent
Estimating the term…
Abstract
Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.
Claims26
An isolated PCSK9-specific antagonist that antagonizes PCSK9's inhibition of cellular LDL uptake and comprises:
- (a) a heavy chain variable region comprising a CDR3 domain comprising SEQ ID NO:
- 17 or an equivalent thereof characterized as having one or more conservative amino acid substitutions in the CDR3 domain;
- and/or
- (b) a light chain variable region comprising a CDR3 domain comprising SEQ ID NO:
- 7 or an equivalent thereof characterized as having one or more conservative amino acid substitutions in the CDR3 domain.
An isolated PCSK9-specific antagonist that antagonizes PCSK9's inhibition of cellular uptake and comprises:
- (a) a heavy chain variable region comprising a CDR3 domain comprising SEQ ID NO:
- 17 or an equivalent thereof characterized as having one or more conservative amino acid substitutions in the CDR3 domain;
- and/or
- (b) a light chain variable region comprising a CDR3 domain comprising SEQ ID NO:
- 7 or an equivalent thereof characterized as having one or more conservative amino acid substitutions in the CDR3 domain;
- wherein said PCSK9-specific antagonist is an antibody molecule;
- and
- wherein said PCSK9-specific antagonist antagonizes PCSK9's inhibition of cellular uptake by at least 20%.
Dependencies are inferred from the claim text.