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Table 1 Characteristics of Lipid-lowering drug target genes

From: Correlations between genetically predicted lipid-lowering drug targets and inflammatory bowel disease

Drug class

Related Drugs

Drug targets

Primary pharmacological action

Target genes

Gene region (GRCh3.p13 by NCBI Gene)

Key regulator

RGX-501a

LDL Receptor

Reduced

LDL-C

LDLR

chr19: 11200139–11244496

HMG-CoA reductase inhibitors

Lovastatin Simvastatin

Atorvastatin

Rosuvastatin Pravastatin Fluvastatin

HMG-CoA reductase

HMGCR

chr5: 74632993–74657941

Cholesterol absorption inhibitors

Ezetimibe

Niemann-Pick C1-like protein 1

NPC1L1

chr7: 44552134–4458092

Proprotein convertase subtilisin/kexin type 9 inhibitors

Alirocumab Evolocumab

Proprotein convertase subtilisin/kexin type 9

PCSK9

chr1: 55505221–55530525

Antisense oligonucleotide targeting ApoB-100 mRNA

Mipomersen

Apolipoprotein B-100

APOB

chr2: 21224301–21266945

Bile acid sequestrants

Colesevelam Colestipol Cholestyramine

ATP Binding Cassette Subfamily G Member 5/ATP Binding Cassette Subfamily G Member 8

ABCG5/ ABCG8b

chr2: 44039611–44065978/44066110–44110127

Key regulator

 

Lipoprotein Lipasea

Reduced

TG

LPL

chr8: 19796764–19824770

peroxisome proliferator receptor alpha activators

Fenofibrate Gemfibrozil Bezafibrate Clofibrate

Peroxisome proliferator-activated receptor-a

PPARA

chr22:46546429–46639653

Angiopoietin-like 3 Inhibitor

Evinacumab

Angiopoietin-related protein 3

ANGPTL3

chr1: 63063191–63071984

Antisense oligonucleotide targeting ApoC-III mRNA

Volanesorsen

Apolipoprotein C-III

APOC3

chr11: 116700623–116703788

  1. Abbreviation: chr chromosome, mRNA messenger ribonucleic acid, LDL-C low-density lipoprotein cholesterol, TG triglyceride
  2. aRGX-501 is not yet approved for marketing and is being studied for the treatment of homozygous familial hypercholesterolemia
  3. bDrug targets of bile acid sequestrants were not specified in the DrugBank. They were identified from a previous study [20]