Table 2: Approaches and Mechanism of PCSK9 Inhibition.

Approaches to PCSK9 Inhibition	Mechanism	Example	Phase
Gene Silencing	Antisense oligonucleotide Small interfering RNA (siRNA)	ISIS pharmaceutical[1a] Santaris pharma[2a] Alnylam Pharmaceuticals[3a]	Preclinical Phase I
Mimetic Peptides	Peptide that mimics EGFA domain of LDLR and binds PCSK9[4a,5a] Peptide that mimics PCSK9 and binds LDLR[6a]	Genentech, Inc	Preclinical Preclinical
Small molecule inhibitors	Target binds of PCSK9	Natural inhibitor Annexin[7a,8a] Berberine[9a,10a] BMS-962476[11a]	Preclinical
Monoclonal antibodies	Targeting catalytic domain of PCSK9	Amgen AMG145 (evolocumab) Regeneron SAR236553/REGN7270 Pfizer RN316 (bococizumab) Novartis LGT209 Genentech MPSK3169A	Phase I - III

LDLR = LDL receptor