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

General Information of Drug (ID: DM1UJO0)

Drug Name
PITAVASTATIN CALCIUM Drug Info
Synonyms
Livalo; Pitavastatin calcium; 147526-32-7; Pitavastatin hemicalcium; NK-104; Nisvastatin; UNII-IYD54XEG3W; Flovas; IYD54XEG3W; 2C25H23FNO4Ca; CHEBI:71258; NK 104 (acid); Calcium (3R,5S,E)-7-(2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-3,5-dihydroxyhept-6-enoate; AK-50694; Itavastatin calcium; Bis((3R,5S,6E)-7-(2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl)-3,5-dihydroxy-6-heptenoate), monocalcium salt; Pitavastatin calcium (JAN); Alipza; Livazo; P-872441; P 872441; 6-Heptenoic acid,
Indication
Disease Entry ICD 11 Status REF
Dyslipidemia 5C80-5C81 Approved [1]
Cross-matching ID
PubChem CID
5282451
ChEBI ID
CHEBI:71258
CAS Number
CAS 147526-32-7
TTD Drug ID
DM1UJO0
VARIDT Drug ID
DR00206
INTEDE Drug ID
DR1306

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 [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Sodium/taurocholate cotransporting polypeptide (SLC10A1) DT56EKP NTCP_HUMAN Approved [3]
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Approved [4]
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Approved [5]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Approved [3]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Approved [6]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Approved [7]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Approved [8]
Organic anion transporter 3 (SLC22A8) DTVP67E S22A8_HUMAN Approved [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Approved [9]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Approved [10]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Approved [11]
UDP-glucuronosyltransferase 2B7 (UGT2B7) DEB3CV1 UD2B7_HUMAN Approved [9]
UDP-glucuronosyltransferase 1A3 (UGT1A3) DEF2WXN UD13_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
HMG-CoA reductase (HMGCR) DTT HMGCR 6.357 6.256 5.17 6.85
Organic anion transporter 3 (SLC22A8) DTP OAT3 2.722 2.07 8.103 3.597
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 8.165 6.597 6.591 6.397
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 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
Sodium/taurocholate cotransporting polypeptide (SLC10A1) DTP NTCP 10.34 6.714 6.815 6.055
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 9.79 0.485 3.511 2.07
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 9.791 3.744 3.413 1.609
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 11.76 5.931 6.164 9.423
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 Dyslipidemia
ICD Disease Classification 5C80-5C81
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
Organic anion transporter 3 (SLC22A8) DTP OAT3 1.54E-03 -5.09E-01 -1.49E+00
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 3.80E-01 -1.23E-02 -5.33E-02
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 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
Sodium/taurocholate cotransporting polypeptide (SLC10A1) DTP NTCP 7.48E-02 -5.70E-02 -2.14E-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
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 1.47E-02 -1.13E-01 -1.13E+00
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 2.63E-03 -1.18E-01 -3.80E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2 Cholesterol-lowering effect of NK-104, a 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor, in guinea pig model of hyperlipidemia. Arzneimittelforschung. 2001;51(3):197-203.
3 Transporter-mediated influx and efflux mechanisms of pitavastatin, a new inhibitor of HMG-CoA reductase. J Pharm Pharmacol. 2005 Oct;57(10):1305-11.
4 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
5 Drug-drug interaction between pitavastatin and various drugs via OATP1B1. Drug Metab Dispos. 2006 Jul;34(7):1229-36.
6 Involvement of BCRP (ABCG2) in the biliary excretion of pitavastatin. Mol Pharmacol. 2005 Sep;68(3):800-7.
7 The effect of SLCO1B1*15 on the disposition of pravastatin and pitavastatin is substrate dependent: the contribution of transporting activity changes by SLCO1B1*15. Pharmacogenet Genomics. 2008 May;18(5):424-33.
8 Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther. 2004 Oct;311(1):139-46.
9 Pitavastatin: a review in hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168.
10 Metabolic fate of pitavastatin, a new inhibitor of HMG-CoA reductase: human UDP-glucuronosyltransferase enzymes involved in lactonization. Xenobiotica. 2003 Jan;33(1):27-41.
11 Comparison of the safety, tolerability, and pharmacokinetic profile of a single oral dose of pitavastatin 4 mg in adult subjects with severe renal impairment not on hemodialysis versus healthy adult subjects. J Cardiovasc Pharmacol. 2012 Jul;60(1):42-8.