Details of Disease

General Information of Disease (ID: DIS9U23P)

• Disease Name: Hypercholesterolaemia
• Disease Class: 5C80: Hyper-lipoproteinaemia
• Disease Hierarchy:
  DIS01GPL: Grass pollen hypersensitivity
  DIS9U23P: Hypercholesterolaemia
• ICD Code:
  ICD-11: ICD-11: 5C80.0
  ICD-9: ICD-9: 272
  Expand ICD-9: 272

Drug-Interaction Atlas (DIA) of This Disease

This Disease is Treated as An Indication in 23 Approved Drug(s)

Drug Name	Drug ID	Highest Status	Drug Type	REF
Atorvastatin	DMF28YC	Approved	Small molecular drug	[1]
Bezafibrate	DMZDCS0	Approved	Small molecular drug	[2]
Cholestyramine	DM3370M	Approved	NA	[3]
Colesevelam	DMMUFKM	Approved	Small molecular drug	[4]
Colestipol	DMIRPD8	Approved	Small molecular drug	[5]
Evinacumab	DMBLX7U	Approved	NA	[6]
Evolocumab	DMNSAND	Approved	Monoclonal antibody	[7]
Ezetimibe	DM7A8TW	Approved	Small molecular drug	[8]
Fenofibrate	DMFKXDY	Approved	Small molecular drug	[9]
Fluvastatin	DM4MDJY	Approved	Small molecular drug	[10]
Guar gum	DMDSD5T	Approved	NA	[4]
Hydroxypropyl methylcellulose	DMVJSU6	Approved	NA	[4]
Inclisiran	DMP3YTE	Approved	NA	[11]
Lovastatin	DM9OZWQ	Approved	Small molecular drug	[12]
Pitavastatin	DMJH792	Approved	NA	[13]
Pravastatin	DM6A0X7	Approved	Small molecular drug	[14]
Probucol	DMVZQ2M	Approved	Small molecular drug	[15]
REGN-727	DM87XSN	Approved	Antibody	[11]
Rosuvastatin	DMMIQ7G	Approved	Small molecular drug	[16]
Simvastatin	DM30SGU	Approved	Small molecular drug	[17]
Vitamin B3	DMQVRZH	Approved	Small molecular drug	[18]
Vitamin E	DMZC90K	Approved	Small molecular drug	[19]
TKM-ApoB	DM2M47Y	Phase 4	siRNA drug	[20]

This Disease is Treated as An Indication in 12 Clinical Trial Drug(s)

Drug Name	Drug ID	Highest Status	Drug Type	REF
AMG 145	DMG324Y	Phase 3	NA	[21]
LIB003	DMVP8WU	Phase 3	Fusion protein	[22]
PF-04950615	DM0TWCY	Phase 3	Antibody	[23]
AZD8233	DMBT2D2	Phase 2	Antisense oligonucleotide	[24]
BMS-770767	DMTVGY7	Phase 2	NA	[25]
BMS-823778	DMTQLAR	Phase 2	NA	[26]
KT6-971	DM08F12	Phase 2	NA	[27]
MD-0727	DM5DSGJ	Phase 2	NA	[28]
MGL-3196	DM1HC9R	Phase 2	NA	[29]
MK-0616	DMVGMNC	Phase 2	Peptide	[30]
VK-2809	DMY5NUR	Phase 2	NA	[11]
NNC-0385-0434	DMBII8C	Phase 1	Small molecule	[31]

This Disease is Treated as An Indication in 7 Discontinued Drug(s)

Drug Name	Drug ID	Highest Status	Drug Type	REF
GT102-279	DMZDZAV	Discontinued in Phase 2	NA	[32]
PF-05335810	DM5KX69	Discontinued in Phase 1	NA	[33]
QRX-401	DMEUVB0	Discontinued in Phase 1	NA	[34]
CEB-925	DMNJXRG	Terminated	NA	[36]
CVT-1	DMPWZCI	Terminated	NA	[37]
DuP-129	DMJGCYO	Terminated	NA	[38]
FR-194738	DMNACIV	Terminated	Small molecular drug	[39]

This Disease is Treated as An Indication in 1 Preclinical Drug(s)

Drug Name	Drug ID	Highest Status	Drug Type	REF
ALN-PCS	DMCJMOS	Preclinical	RNAi therapeutics	[35]

This Disease is Treated as An Indication in 14 Investigative Drug(s)

Drug Name	Drug ID	Highest Status	Drug Type	REF
AAV-miApoB	DM67ILO	Investigative	NA	[40]
AD10-1025	DMYLA29	Investigative	NA	[41]
BPH-652	DMX4WI7	Investigative	Small molecular drug	[42]
Brutieridin	DMKZM1L	Investigative	NA	[43]
DYB-186	DMFPLNA	Investigative	NA	[40]
ER-21036	DMSHUX7	Investigative	NA	[40]
KP-9928	DM2JJ6B	Investigative	NA	[40]
LP-1810	DM3PYF7	Investigative	NA	[40]
LPD-608	DMSJPLM	Investigative	NA	[40]
MT-001	DM7KIVX	Investigative	NA	[43]
SC-435	DMYR21Q	Investigative	Small molecular drug	[44]
SP-1000	DM5GHUX	Investigative	NA	[40]
Statin	DM4WQHU	Investigative	Small molecular drug	[43]
SX-PCK9	DMGRCID	Investigative	NA	[40]

Molecular Interaction Atlas (MIA) of This Disease

References

• [1] Atorvastatin FDA Label
• [2] Simvastatin and bezafibrate: effects on serum lipoproteins and lecithin: cholesterol acyltransferase activity in familial hypercholesterolaemia. Eur J Clin Pharmacol. 1988;35(6):579-83.
• [3] Cholestyramine FDA Label
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [5] Colestipol FDA Label
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
• [7] Impact of alirocumab/evolocumab on lipoprotein (a) concentrations in patients with familial hypercholesterolaemia: a systematic review and meta-analysis of randomized controlled trials. Endokrynol Pol. 2023;74(3):234-242.
• [8] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6816).
• [9] Fenofibrate FDA Label
• [10] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2951).
• [11] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [12] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2739).
• [13] Pitavastatin FDA Label
• [14] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2953).
• [15] Probucol FDA Label
• [16] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2954).
• [17] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2955).
• [18] Vitamin B3 impairs reverse cholesterol transport in Apolipoprotein E-deficient mice. Clin Investig Arterioscler. 2019 Nov-Dec;31(6):251-260.
• [19] Riboflavin FDA Label
• [20] ClinicalTrials.gov (NCT00348686) Candesartan Effectiveness Study in Pro-B Type Natriuretic Peptides (BNP). U.S. National Institutes of Health.
• [21] ClinicalTrials.gov (NCT01854918) Open Label Study of Long Term Evaluation Against LDL-C Trial-2. U.S. National Institutes of Health.
• [22] ClinicalTrials.gov (NCT05234775) Cross-Over Study to Compare the Pharmacokinetics and Pharmacodynamics of LIB003 Process 1 and Process 2 Drug Product in Subjects With or Without Statin Therapy. U.S.National Institutes of Health.
• [23] ClinicalTrials.gov (NCT01975376) The Evaluation of Bococizumab (PF-04950615;RN316) in Reducing the Occurrence of Major Cardiovascular Events in High Risk Subjects. U.S. National Institutes of Health.
• [24] ClinicalTrials.gov (NCT04964557) A Randomised, Parallel, Double-Blind, Placebo-Controlled Phase 2b Study to Assess the Safety, Tolerability and Efficacy of AZD8233 Treatment in Participants With Hyperlipidaemia. U.S.National Institutes of Health.
• [25] ClinicalTrials.gov (NCT01058083) Safety Study of BMS-770767 in Subjects With Hypercholesterolemia. U.S. National Institutes of Health.
• [26] ClinicalTrials.gov (NCT01602367) Safety and Efficacy Study of BMS-823778 to Treat Uncontrolled High Blood Pressure in Overweight and Obese Patients. U.S. National Institutes of Health.
• [27] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032919)
• [28] ClinicalTrials.gov (NCT00404001) Study of Oral MD-0727 Administered to Patients With Primary Hypercholesterolemia. U.S. National Institutes of Health.
• [29] ClinicalTrials.gov (NCT01367873) Ascending Single-Dose Study to Evaluate VIA-3196 in Healthy Subjects. U.S. National Institutes of Health.
• [30] ClinicalTrials.gov (NCT05261126) A Phase 2b, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of MK-0616 in Adults With Hypercholesterolemia. U.S.National Institutes of Health.
• [31] ClinicalTrials.gov (NCT04058834) A First Human Dose Trial Investigating Safety, Tolerability and Pharmacokinetics of Single Doses of NNC0385-0434 in Healthy Subjects and Patients With Hypercholesterolaemia. U.S.National Institutes of Health.
• [32] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011481)
• [33] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036584)
• [34] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017830)
• [35] Clinical pipeline report, company report or official report of Alnylam Pharmaceuticals, Inc (2011).
• [36] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010079)
• [37] Lack of effect of cholesterol esterase inhibitor CVT-1 on cholesterol absorption and LDL cholesterol in humans. Cardiovasc Drugs Ther. 1999 Sep;13(5):449-54.
• [38] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003587)
• [39] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009590)
• [40] The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
• [41] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1800).
• [42] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 645).
• [43] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 639).
• [44] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6530).
• [45] Efficacy and safety of fenofibric acid in combination with atorvastatin and ezetimibe in patients with mixed dyslipidemia. Am Heart J. 2010 Oct;160(4):759-66.