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

General Information of Drug (ID: DM7A8TW)

Drug Name
Ezetimibe Drug Info
Synonyms
Ezedoc; Ezetimib; Ezetrol; Zetia; Zient; Essex brand of ezetimibe; MSD brand of ezetimibe; Merck brand of ezetimibe; SCH58235; Sch 58235; Ezetimibe [USAN:INN]; Inegy (TN); MK-0653; SCH-58235; Schering-Plough brand of ezetimibe; Vytorin (TN); Zetia (TN); Zetia , Ezetrol, Ezetimibe; Ezetimibe (JAN/USAN/INN); (-)-Sch 58235; (1-(4-fluorophenyl)-(3R)-(3-(4-fluorophenyl)-(3S)-hydroxypropyl)-(4S)-(4-hydroxyphenyl)-2-azetidinone); (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one; (3R,4S)-1-(p-Fluorophenyl)-3-((3S)-3-(p-fluorophenyl)-3-hydroxypropyl)-4-(p-hydroxyphenyl)-2-azetidinone; 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-(4-hydroxyphenyl)-2-azetidione; 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone
Indication
Disease Entry ICD 11 Status REF
Atherosclerosis BD40 Approved [1]
Hypercholesterolaemia 5C80.0 Approved [2]
Hyperlipidemia 5C80.Z Approved [1]
Hyperlipidemia, familial combined, LPL related Approved [1]
Non-alcoholic fatty liver disease DB92 Approved [1]
Type-1/2 diabetes 5A10-5A11 Approved [1]
Therapeutic Class
Anticholesteremic Agents
Cross-matching ID
PubChem CID
150311
ChEBI ID
CHEBI:49040
CAS Number
CAS 163222-33-1
TTD Drug ID
DM7A8TW
VARIDT Drug ID
DR00140
INTEDE Drug ID
DR0677
ACDINA Drug ID
D00262

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Niemann-Pick C1-like protein 1 (NPC1L1) TTPD1CN NPCL1_HUMAN Inhibitor [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Bile salt export pump (ABCB11) DTJ0EW4 ABCBB_HUMAN Approved [4]
Multidrug resistance-associated protein 3 (ABCC3) DTQ3ZHF MRP3_HUMAN Approved [5]
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Approved [6]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Approved [5]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Approved [7]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [9]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Approved [9]
UDP-glucuronosyltransferase 2B7 (UGT2B7) DEB3CV1 UD2B7_HUMAN Approved [9]
UDP-glucuronosyltransferase 1A3 (UGT1A3) DEF2WXN UD13_HUMAN Approved [10]
UDP-glucuronosyltransferase 2B15 (UGT2B15) DENZ6B1 UDB15_HUMAN Approved [9]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Niemann-Pick C1-like protein 1 (NPC1L1) DTT NPC1L1 7.112 3.536 3.655 8.459
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Multidrug resistance-associated protein 3 (ABCC3) DTP MRP3 7.688 7.801 5.548 6.957
Bile salt export pump (ABCB11) DTP BSEP 6.055 5.066 4.456 4.797
Breast cancer resistance protein (ABCG2) DTP BCRP 6.732 7.513 6.326 9.277
Multidrug resistance-associated protein 2 (ABCC2) DTP MRP2 7.751 4.17 6.425 6.282
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 9.79 0.485 3.511 2.07
UDP-glucuronosyltransferase 2B15 (UGT2B15) DME UGT2B15 9.165 4.684 3.036 5.897
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 Atherosclerosis
ICD Disease Classification BD40
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Niemann-Pick C1-like protein 1 (NPC1L1) DTT NPC1L1 1.75E-01 -0.05 -0.27
P-glycoprotein 1 (ABCB1) DTP P-GP 3.29E-14 -7.08E-01 -1.99E+00
Multidrug resistance-associated protein 3 (ABCC3) DTP MRP3 5.09E-05 4.90E-01 1.66E+00
Bile salt export pump (ABCB11) DTP BSEP 2.41E-01 -3.08E-02 -2.35E-01
Breast cancer resistance protein (ABCG2) DTP BCRP 2.28E-08 -3.66E-01 -8.07E-01
Multidrug resistance-associated protein 2 (ABCC2) DTP MRP2 4.30E-02 -2.29E-01 -9.10E-01
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 3.27E-01 -5.78E-02 -3.84E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 2.00E-01 5.79E-02 3.00E-01
UDP-glucuronosyltransferase 2B15 (UGT2B15) DME UGT2B15 1.87E-01 -5.07E-03 -2.38E-02
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 Ezetimibe FDA Label
2 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).
3 Update on patented cholesterol absorption inhibitors. Expert Opin Ther Pat. 2009 Aug;19(8):1083-107.
4 Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43.
5 Complex pharmacokinetic behavior of ezetimibe depends on abcc2, abcc3, and abcg2. Drug Metab Dispos. 2009 Aug;37(8):1698-702.
6 Intestinal expression of P-glycoprotein (ABCB1), multidrug resistance associated protein 2 (ABCC2), and uridine diphosphate-glucuronosyltransferase 1A1 predicts the disposition and modulates the effects of the cholesterol absorption inhibitor ezetimibe in humans. Clin Pharmacol Ther. 2006 Mar;79(3):206-17.
7 A LC-MS/MS method to quantify the novel cholesterol lowering drug ezetimibe in human serum, urine and feces in healthy subjects genotyped for SLCO1B1. J Chromatogr B Analyt Technol Biomed Life Sci. 2006 Jan 2;830(1):143-50.
8 Pharmacokinetic and pharmacodynamic interactions between the immunosuppressant sirolimus and the lipid-lowering drug ezetimibe in healthy volunteers. Clin Pharmacol Ther. 2010 Jun;87(6):663-7.
9 Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet. 2005;44(5):467-94.
10 Drug interactions between the immunosuppressant tacrolimus and the cholesterol absorption inhibitor ezetimibe in healthy volunteers. Clin Pharmacol Ther. 2011 Apr;89(4):524-8.