Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMF28YC)

Drug Name
Atorvastatin Drug Info
Synonyms
Atogal; Atorlip; Atorpic; Atorvastatina; Atorvastatine; Atorvastatinium; Atrovastin; Cardyl; Faboxim; Lipotropic; Lipovastatinklonal; Liprimar; Lowden; Sincol; Sortis; Sotis; Torvacard; Torvast; Totalip; Tozalip; Tulip; Vastina; Xanator; Xarator; Xavator; Zurinel; Atorvastatin (INN); Atorvastatin [INN:BAN]; Lipitor (TN); Lipitor(TM); Sortis (TN); (3R,5R)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-propan-2-ylpyrrol-1-yl]-3,5-dihydroxyheptanoic acid; (3R,5R)-7-[3-(anilinocarbonyl)-5-(4-fluorophenyl)-2-isopropyl-4-phenyl-1H-pyrrol-1-yl]-3,5-dihydroxyheptanoic acid; (R-(R*,R*))-2-(4-Fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-((phenylamino)carbonyl)-1H-pyrrole-1-heptanoic acid; (betaR,deltaR)-2-(p-Fluorophenyl)-beta,delta-dihydroxy-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)pyrrole-1-heptanoic acid; 7-[2-(4-FLUORO-PHENYL)-5-ISOPROPYL-3-PHENYL-4-PHENYLCARBAMOYL-PYRROL-1-YL]-3,5-DIHYDROXY-HEPTANOIC ACID
Indication
Disease Entry ICD 11 Status REF
Acute coronary syndrome BA41 Approved [1]
Angina pectoris BA40 Approved [1]
Arteriosclerosis BD40 Approved [1]
Cardiovascular disease BA00-BE2Z Approved [2]
Coronary atherosclerosis Approved [1]
Hypercholesterolaemia 5C80.0 Approved [1]
Hyperlipidemia 5C80.Z Approved [3]
Hyperlipidemia, familial combined, LPL related Approved [1]
Hypertriglyceridemia 5C80.1 Approved [1]
Inflammation 1A00-CA43.1 Approved [1]
Non-insulin dependent diabetes 5A11 Approved [1]
Psoriasis EA90 Approved [1]
Type-1/2 diabetes 5A10-5A11 Approved [1]
Coronavirus Disease 2019 (COVID-19) 1D6Y Phase 2 [4]
Stroke 8B20 Investigative [1]
Venous thromboembolism BD72 Investigative [1]
Therapeutic Class
Anticholesteremic Agents
Cross-matching ID
PubChem CID
60823
ChEBI ID
CHEBI:39548
CAS Number
CAS 134523-00-5
TTD Drug ID
DMF28YC
VARIDT Drug ID
DR00030
INTEDE Drug ID
DR0155
ACDINA Drug ID
D00050

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
HMG-CoA reductase (HMGCR) TTPADOQ HMDH_HUMAN Inhibitor [5]
HUMAN MYD88NF-kappa-B proinflammatory pathway (MYD88-NFKB pathway) TTDJB68 . Inhibitor [6]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Monocarboxylate transporter 2 (SLC16A7) DTLT3UG MOT2_HUMAN Approved [7]
Monocarboxylate transporter 1 (SLC16A1) DT342ZG MOT1_HUMAN Approved [8]
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Approved [9]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Approved [10]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Approved [11]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Approved [12]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [13]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [14]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Approved [15]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Approved [16]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Approved [17]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Approved [18]
UDP-glucuronosyltransferase 1A3 (UGT1A3) DEF2WXN UD13_HUMAN Approved [19]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
HMG-CoA reductase (HMGCR) DTT HMGCR 6.357 6.256 5.17 6.85
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 8.165 6.597 6.591 6.397
Monocarboxylate transporter 2 (SLC16A7) DTP MCT2 5.184 4.991 6.519 5.361
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTP OATP1A2 4.365 4.466 3.248 2.632
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 8.873 2.17 2.485 3.322
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 9.79 0.485 3.511 2.07
Monocarboxylate transporter 1 (SLC16A1) DTP MCT1 5.809 6.193 5.485 5.825
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 9.791 3.744 3.413 1.609
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Acute coronary syndrome
ICD Disease Classification BA41
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
HMG-CoA reductase (HMGCR) DTT HMGCR 1.01E-05 0.65 1.53
P-glycoprotein 1 (ABCB1) DTP P-GP 3.29E-14 -7.08E-01 -1.99E+00
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 3.80E-01 -1.23E-02 -5.33E-02
Monocarboxylate transporter 2 (SLC16A7) DTP MCT2 4.57E-02 2.44E-01 5.98E-01
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTP OATP1A2 7.28E-02 -7.13E-02 -4.55E-01
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 1.65E-01 -6.07E-02 -3.77E-01
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 3.27E-01 -5.78E-02 -3.84E-01
Monocarboxylate transporter 1 (SLC16A1) DTP MCT1 1.39E-04 6.49E-01 2.64E+00
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 2.00E-01 5.79E-02 3.00E-01
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 1.47E-02 -1.13E-01 -1.13E+00
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 3.65E-02 -8.90E-02 -5.58E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 3.24E-05 -3.48E-01 -1.34E+00
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Atorvastatin FDA Label
2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
3 FDA Approved Drug Products from FDA Official Website. 2019. Application Number: (ANDA) 205945.
4 ClinicalTrials.gov (NCT04380402) Atorvastatin in COVID-19. U.S. National Institutes of Health.
5 Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64.
6 Statin therapy in COVID-19 infection. Eur Heart J Cardiovasc Pharmacother. 2020 Apr 29. pii: pvaa042.
7 Monocarboxylate Transporters in Drug Disposition: Role in the Toxicokinetics and Toxicodynamics of the Drug of Abuse GHB.
8 H+-coupled nutrient, micronutrient and drug transporters in the mammalian small intestine. Exp Physiol. 2007 Jul;92(4):603-19.
9 Human platelets express organic anion-transporting peptide 2B1, an uptake transporter for atorvastatin. Drug Metab Dispos. 2009 May;37(5):1129-37.
10 Influence of the flavonoids apigenin, kaempferol, and quercetin on the function of organic anion transporting polypeptides 1A2 and 2B1. Biochem Pharmacol. 2010 Dec 1;80(11):1746-53.
11 Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
12 FDA Drug Development and Drug Interactions
13 Tarascon Pocket Pharmacopoeia 2018 Classic Shirt-Pocket Edition.
14 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
15 Atorvastatin glucuronidation is minimally and nonselectively inhibited by the fibrates gemfibrozil, fenofibrate, and fenofibric acid. Drug Metab Dispos. 2007 Aug;35(8):1315-24.
16 Effects of acid and lactone forms of eight HMG-CoA reductase inhibitors on CYP-mediated metabolism and MDR1-mediated transport. Pharm Res. 2006 Mar;23(3):506-12.
17 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
18 Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers.
19 UGT1A1*28 is associated with decreased systemic exposure of atorvastatin lactone. Mol Diagn Ther. 2013 Aug;17(4):233-7.