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PCSK9

Brief Information

Name:Proprotein convertase subtilisin kexin type 9
Target Synonym:EC 3.4.21,Neural apoptosis-regulated convertase 1,Proprotein convertase 9,NARC1,PSEC0052,PCSK9,NARC-1,EC:3.4.21.-,Proprotein Convertase Subtilisin/Kexin Type 9,Subtilisin/Kexin-Like Protease PC9,PC9,Convertase Subtilisin/Kexin Type 9 Preproprotein,Hypercholesterolemia, Autosomal Dominant 3,EC 3.4.21.-,HCHOLA3,LDLCQ1,FH3,EC 3.4.21.111,Neural Apoptosis Regulated Convertase 1,FHCL3
Number of Launched Drugs:4
Number of Drugs in Clinical Trials:26
Lastest Research Phase:Approved

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Part of Bioactivity data

PCY-H5225-Cell-based assay
 PCSK9 FACS

FACS analysis shows that Human PCSK9 (D374Y), His Tag (Cat. No. PCY-H5225) inhibits LDL uptake in HepG2 cells. The EC50 for this effect is 0.0689-0.3049 μg/mL.

PCY-H5225-Cell-based assay
 PCSK9 FACS

FACS analysis shows that the effect of Human PCSK9 (D374Y), His Tag (Cat. No. PCY-H5225) inhibiting LDL uptake in HepG2 cells was neutralized by Anti-Human PCSK9 antibody. The concentration of PCSK9 used is 5 μg/mL. The EC50 for Anti-Human PCSK9 antibody is 6.816-12.67 μg/mL.

PC9-H5256-BLI
 PCSK9 BLI

Loaded Human PCSK9, Fc Tag (Cat. No. PC9-H5256) on Protein A Biosensor, can bind Human LDL R, His Tag (Cat. No. LDR-H5224) with an affinity constant of 12.7 nM as determined in BLI assay (ForteBio Octet Red96e) (Routinely tested).

PC9-H52E4-BLI
 PCSK9 BLI

Loaded Human LDL R, Fc Tag (Cat. No. LDR-H5254) on Protein A Biosensor, can bind Hamster PCSK9, His Tag (Cat. No. PC9-H52E4) with an affinity constant of 4.09 nM as determined in BLI assay (ForteBio Octet Red96e) (Routinely tested).

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Synonym Name

PCSK9,FH3,HCHOLA3,LDLCQ1,NARC1,PC9

Background

Proprotein convertase subtilisin/kexin type 9 (PCSK9), is an enzyme which in humans is encoded by the PCSK9 gene.This gene encodes a proprotein convertase belonging to the proteinase K subfamily of the secretory subtilase family. This protein plays a major regulatory role in cholesterol homeostasis. PCSK9 binds to the epidermal growth factor-like repeat A (EGF-A) domain of the low-density lipoprotein receptor (LDLR), inducing LDLR degradation. PCSK9 may also have a role in the differentiation of cortical neurons. Mutations in this gene have been associated with a rare form of autosomal dominant familial hypercholesterolemia (HCHOLA3).

Clinical and Translational Updates

Related Molecule

Public Drug Information

Name Research Code Research Phase Company First Brand Name First Approved Country First Indication First Approved Company First Approved Date Indications Clinical Trials
Evolocumab AMG-145 Approved Amgen Inc, Astellas Pharma Inc 瑞百安, Repatha EU Dyslipidemias; Hypercholesterolemia Amgen Europe Bv 2015-07-17 Acute Coronary Syndrome; Aortic Aneurysm, Abdominal; Diabetes Mellitus; Hyperlipoproteinemia Type II; Hyperlipidemias; Glioma; Rejection in heart transplantation; Cardiovascular Diseases; Coronary Disease; Heterozygous familial hypercholesterolemia; Dyslipidemias; Stroke; HIV Infections; Sepsis; Glioblastoma; Coronary Artery Disease; Hypercholesterolemia; Heart Failure; Atherosclerosis; Myocardial Infarction; Diabetes Mellitus, Type 2; ST Elevation Myocardial Infarction; Homozygous familial hypercholesterolemia Details
Tafolecimab IBI-306 Approved Innovent Biologics(Suzhou) Co Ltd 信必乐 Mainland China Dyslipidemias; Hypercholesterolemia Innovent Biologics(Suzhou) Co Ltd 2023-08-15 Homozygous familial hypercholesterolemia; Drug-Related Side Effects and Adverse Reactions; Hypercholesterolemia; Dyslipidemias; Heterozygous familial hypercholesterolemia Details
Inclisiran sodium ALN-60212; PCSK9si; ALN-PCSsc; KJX839; KJX-839 Approved Alnylam Pharmaceuticals Inc Leqvio, 乐可为 EU Dyslipidemias; Hypercholesterolemia Novartis Europharm Ltd 2020-12-09 Acute Coronary Syndrome; Diabetes Mellitus; Hyperlipidemias; Hyperlipoproteinemia Type II; Cardiovascular Diseases; Dyslipidemias; Coronary Disease; Heterozygous familial hypercholesterolemia; Hypolipoproteinemias; Stroke; Homozygous familial hypercholesterolemia; Kidney Diseases; Coronary Artery Disease; Hypercholesterolemia; Carotid Artery Diseases; Diabetes Mellitus, Type 2; Myocardial Infarction; Atherosclerosis; Plaque, Atherosclerotic Details
Alirocumab 316P; REGN-727; SAR-236553 Approved Sanofi, Regeneron Pharmaceuticals Inc 波立达, Praluent United States Hypercholesterolemia Regeneron Pharmaceuticals Inc 2015-07-24 Stroke; Hyperlipidemias; Drinking Behavior; Cardiovascular Diseases; Coronary Disease; Vascular Diseases; Heterozygous familial hypercholesterolemia; Dyslipidemias; Acute Coronary Syndrome; Hemorrhage; Intracranial Arteriosclerosis; Angina Pectoris; Shock, Septic; Hypercholesterolemia; Sepsis; ST Elevation Myocardial Infarction; Diabetes Mellitus, Type 2; Atherosclerosis; Myocardial Infarction; Liver Diseases, Alcoholic; HIV Infections; Plaque, Atherosclerotic; Homozygous familial hypercholesterolemia Details

Clinical Drug Information

Name Research Code Research Phase Company Indications Clinical Trials
AZD-0780 AZD0780; AZD-0780 Phase 2 Clinical Astrazeneca Plc Dyslipidemias; Cardiovascular Diseases Details
Recombinant human anti-PCSK9 monoclonal antibody (Salubris) SAL003 Phase 3 Clinical Shenzhen Salubris Pharmaceuticals Co Ltd Hypercholesterolemia; Dyslipidemias; Hyperlipidemias; Hyperlipidemia, Familial Combined Details
VERVE-101 VERVE-101 Phase 1 Clinical Broad Institute, Harvard University Plaque, Atherosclerotic; Hypercholesterolemia; Heterozygous familial hypercholesterolemia Details
CVI-LM-001 CVI-LM-001; CVI-LM001; C-8304 Phase 2 Clinical Xiwei'Ai Medicine Technology (Shanghai) Co Ltd Hypercholesterolemia; Hyperlipidemias Details
RBD-7022 RBD-7022; RBD7022 Phase 1 Clinical Suzhou Ribo Life Science Co Ltd Hypercholesterolemia; Hyperlipidemias; Hyperlipidemia, Familial Combined Details
ATX-304 O-304; ATX-304; O-304X Phase 2 Clinical Betagenon Ab Mitochondrial Diseases; Diabetes Mellitus, Type 2; Peripheral Arterial Disease Details
NN-6434 NN-6434 Phase 1 Clinical Novo Nordisk A/S Details
CiVi-007 CiVi-007; LNA-PCSK -9; LNA-PCSK9-GalNac Phase 2 Clinical F. Hoffmann-La Roche Ltd Hypercholesterolemia Details
Recombinant human anti-PCSK9 monoclonal antibody (Tasly Pharm) B1655; B-1655 Phase 1 Clinical Tianjin Tasly Pharmaceutical Co Ltd Hypercholesterolemia Details
RN-0191 RN0191 Phase 1 Clinical Rona Therapeutics Inc Atherosclerosis; Hypercholesterolemia; Dyslipidemias Details
PCSK9 modulator (Genekey Biotech) Phase 1 Clinical Shenzhen Salubris Pharmaceuticals Co Ltd Metabolic Diseases; Inflammation Details
Lerodalcibep LIB-003 Phase 3 Clinical Lib Therapeutics Llc Atherosclerosis; Hypercholesterolemia; Stroke; Heterozygous familial hypercholesterolemia; Cardiovascular Diseases; Arteriosclerosis; Hyperlipoproteinemia Type II Details
ATH-04 ATH-04; Affitope AT04A Phase 1 Clinical Affiris Ag Atherosclerosis Details
MK-0616 MK-0616 Phase 3 Clinical Merck Sharp & Dohme Corp Atherosclerosis; Hypercholesterolemia; Kidney Diseases; Cardiovascular Diseases; Arteriosclerosis; Hyperlipoproteinemia Type II Details
DC-371739 JYP-0739; DC-371739 Phase 1 Clinical Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Hypercholesterolemia; Dyslipidemias; Hyperlipidemias Details
SAL-092 SAL092; SAL-092 Phase 1 Clinical Shenzhen Salubris Pharmaceuticals Co Ltd Hypercholesterolemia; Dyslipidemias Details
Anti-PCSK9 monoclonal antibody (Biocad) Phase 1 Clinical Biocad Cardiovascular Diseases Details
VERVE-102 VERVE-102 Phase 1 Clinical Verve Therapeutics Inc Atherosclerosis; Coronary Disease; Heterozygous familial hypercholesterolemia Details
AZD-8233 AZD-8233; IONIS-AZ4-2.5-LRx; ION-449 Phase 2 Clinical Ionis Pharmaceuticals Inc Hypercholesterolemia; Dyslipidemias; Hyperlipidemias; Kidney Failure, Chronic Details
NNC0385-0434 NNC0385-0434 Phase 2 Clinical Novo Nordisk A/S Plaque, Atherosclerotic; Diabetes Mellitus, Type 2; Hypercholesterolemia; Cardiovascular Diseases; Renal Insufficiency, Chronic; Arteriosclerosis Details
MIL-86 MIL-86 Phase 2 Clinical Beijing Mabworks Biotech Co Ltd Hypercholesterolemia; Heterozygous familial hypercholesterolemia; Cardiovascular Diseases; Hyperlipidemias; Hyperlipoproteinemia Type II Details
SGB-3403 SGB-3403 Phase 1 Clinical Suzhou Sanegene Biopharmaceuticals Ltd Atherosclerosis; Hypercholesterolemia; Heterozygous familial hypercholesterolemia Details
JX-7002 JX7002; JX-7002 Phase 1 Clinical Zhejiang Jingxin Pharmaceutical Co Ltd Hypercholesterolemia; Hyperlipidemias Details

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