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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:6
Number of Drugs in Clinical Trials:28
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 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
Inclisiran sodium KJX-839; ALN-60212; PCSK9si; ALN-PCSsc; KJX839 Approved Alnylam Pharmaceuticals Inc Leqvio, 乐可为 EU Dyslipidemias; Hypercholesterolemia Novartis Europharm Ltd 2020-12-09 Hypolipoproteinemias; Diabetes Mellitus; Hyperlipidemias; Hyperlipoproteinemia Type II; Cardiovascular Diseases; Dyslipidemias; Heterozygous familial hypercholesterolemia; Coronary Disease; Acute Coronary Syndrome; Stroke; Plaque, Atherosclerotic; Coronary Artery Disease; Hypercholesterolemia; Renal Insufficiency; Myocardial Infarction; Diabetes Mellitus, Type 2; Carotid Artery Diseases; Atherosclerosis; Homozygous familial hypercholesterolemia Details
Ongericimab JS-002 Approved Shanghai Junshi Biosciences Co Ltd 君适达 Mainland China Hypercholesterolemia; Dyslipidemias Shanghai Junshi Biosciences Co Ltd 2024-10-09 Hypertriglyceridemia; Atherosclerosis; Hypercholesterolemia; Neoplasms; Heterozygous familial hypercholesterolemia; Dyslipidemias; Hyperlipidemias; Hyperlipidemia, Familial Combined Details
Ebronucimab AK-102 Approved Zhongshan Akeso Biopharma Co Ltd, Yabao Us Pharmaceutical Co Ltd 伊喜宁 Mainland China Hypercholesterolemia; Dyslipidemias Kang Rong Dongfang (Guangdong) Pharmaceutical Co Ltd 2024-09-26 Homozygous familial hypercholesterolemia; Hypercholesterolemia; Dyslipidemias; Heterozygous familial hypercholesterolemia; Hyperlipidemias; Hyperlipidemia, Familial Combined; Hyperlipoproteinemia Type II Details
Recaticimab SHR-1209 Approved Jiangsu Hengrui Medicine Co Ltd 艾心安 Mainland China Hypercholesterolemia; Dyslipidemias Guangdong Hengrui Pharmaceutical Co Ltd 2025-01-08 Hypercholesterolemia; Dyslipidemias; Hyperlipidemias; Hyperlipidemia, Familial Combined; Hyperlipoproteinemia Type II Details
Evolocumab AMG-145 Approved Amgen Inc, Astellas Pharma Inc 瑞百安, Repatha EU Dyslipidemias; Hypercholesterolemia Amgen Europe Bv 2015-07-17 Stroke; Heart Failure, Systolic; Aortic Aneurysm, Abdominal; Diabetes Mellitus; Hyperlipidemias; Hyperlipoproteinemia Type II; Glioma; Rejection in heart transplantation; Cardiovascular Diseases; Coronary Disease; Dyslipidemias; Heterozygous familial hypercholesterolemia; HIV Infections; Acute Coronary Syndrome; Glioblastoma; Coronary Artery Disease; Sepsis; Hypercholesterolemia; ST Elevation Myocardial Infarction; Atherosclerosis; Diabetes Mellitus, Type 2; 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; Hypercholesterolemia; Heterozygous familial hypercholesterolemia; Dyslipidemias 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 Hemorrhage; Hyperlipidemias; Drinking Behavior; Cardiovascular Diseases; Ischemic Stroke; Vascular Diseases; Coronary Disease; Heterozygous familial hypercholesterolemia; Dyslipidemias; Angina Pectoris; Intracranial Arteriosclerosis; Stroke; Shock, Septic; Acute Coronary Syndrome; Hypercholesterolemia; Sepsis; Myocardial Infarction; Diabetes Mellitus, Type 2; ST Elevation Myocardial Infarction; Atherosclerosis; Homozygous familial hypercholesterolemia; Plaque, Atherosclerotic; Liver Diseases, Alcoholic; HIV Infections Details

Clinical Drug Information

Name Research Code Research Phase Company Indications Clinical Trials
Recombinant human anti-PCSK9 monoclonal antibody (Salubris) SAL003 Phase 3 Clinical Shenzhen Salubris Pharmaceuticals Co Ltd Hypercholesterolemia; Dyslipidemias; Hyperlipidemia, Familial Combined; Hyperlipidemias Details
AZD-0780 AZD0780; AZD-0780 Phase 3 Clinical Dogma Therapeutics Plaque, Atherosclerotic; Renal Insufficiency; Dyslipidemias; Hepatic Insufficiency; Cardiovascular Diseases Details
Enlicitide Decanoate MK-0616 Phase 3 Clinical Merck Sharp & Dohme Corp Atherosclerosis; Renal Insufficiency; Hypercholesterolemia; Kidney Diseases; Cardiovascular Diseases; Hepatic Insufficiency; Arteriosclerosis; Hyperlipoproteinemia Type II 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
CiVi-007 CiVi-007; LNA-PCSK -9; LNA-PCSK9-GalNac Phase 2 Clinical F. Hoffmann-La Roche Ltd 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
ATX-304 O-304; ATX-304; O-304X Phase 2 Clinical Betagenon Ab Mitochondrial Diseases; Diabetes Mellitus, Type 2; Peripheral Arterial Disease Details
MIL-86 MIL-86 Phase 2 Clinical Beijing Mabworks Biotech Co Ltd Hypercholesterolemia; Heterozygous familial hypercholesterolemia; Cardiovascular Diseases; Hyperlipidemias; Hyperlipoproteinemia Type II Details
NNC0385-0434 NNC0385-0434; NN-6435; NNC 0385 0434 Phase 2 Clinical Novo Nordisk A/S Plaque, Atherosclerotic; Diabetes Mellitus, Type 2; Hypercholesterolemia; Cardiovascular Diseases; Arteriosclerosis; Renal Insufficiency, Chronic Details
PCSK9 Inhibitors therapy(Guangdong Provincial People'S Hospital) Phase 2 Clinical Guangdong Provincial People'S Hospital Colorectal Neoplasms Details
SYH-2053 SYH2053; SYH-2053 Phase 2 Clinical CSPC Pharmaceutical Group Ltd Hypercholesterolemia; Dyslipidemias; Hyperlipidemia, Familial Combined; Hyperlipidemias Details
RBD-7022 RBD7022; RBD-7022; SR043; SR-043; QLC-7401 Phase 2 Clinical Suzhou Ribo Life Science Co Ltd Hypercholesterolemia; Hyperlipidemias; Hyperlipidemia, Familial Combined Details
Recombinant human anti-PCSK9 monoclonal antibody (Tasly Pharm) B1655; B-1655 Phase 1 Clinical Tianjin Tasly Pharmaceutical Co Ltd Hypercholesterolemia Details
DC-371739 JYP-0739; DC-371739 Phase 1 Clinical Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Hypercholesterolemia; Dyslipidemias; Hyperlipidemias Details
Anti-PCSK9 monoclonal antibody (Biocad) Phase 1 Clinical BIOCAD JSC Cardiovascular Diseases Details
ATH-04 ATH-04; Affitope AT04A Phase 1 Clinical Affiris Ag Atherosclerosis Details
VERVE-101 VERVE-101 Phase 1 Clinical Broad Institute, Harvard University Plaque, Atherosclerotic; Hypercholesterolemia; Heterozygous familial hypercholesterolemia Details
SAL-092 SAL092; SAL-092 Phase 1 Clinical Shenzhen Salubris Pharmaceuticals Co Ltd Hypercholesterolemia; Dyslipidemias Details
VERVE-102 VERVE-102 Phase 1 Clinical Verve Therapeutics Inc Atherosclerosis; Heterozygous familial hypercholesterolemia; Coronary Disease Details
SGB-3403 SGB-3403 Phase 1 Clinical Suzhou Sanegene Biopharmaceuticals Ltd Atherosclerosis; Hypercholesterolemia; Heterozygous familial hypercholesterolemia; Cardiovascular Diseases; Hyperlipidemias Details
RN-0191 RN0191 Phase 1 Clinical Darui Biomedical Technology (Shanghai) Co Ltd Atherosclerosis; Hypercholesterolemia; Dyslipidemias Details
RP-910 RP910; RP-910 Phase 1 Clinical Runjia (Shanghai) Pharmaceutical Technology Co Ltd Metabolic Diseases; Hyperlipidemias Details
YOLT-101 YOLT-101 Phase 1 Clinical Yoltech Therapeutics Co Ltd Hyperlipoproteinemia Type II Details
JX-7002 JX7002; JX-7002 Phase 1 Clinical Zhejiang Jingxin Pharmaceutical Co Ltd Hypercholesterolemia; Hyperlipidemias Details
NN-6434 NN-6434 Phase 1 Clinical Novo Nordisk A/S Details
PCSK9 modulator (Genekey Biotech) Phase 1 Clinical Shenzhen Salubris Pharmaceuticals Co Ltd Metabolic Diseases; Inflammation Details

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