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

General Information of Drug (ID: DMMIQ7G)

Drug Name

Rosuvastatin Drug Info

Synonyms

Astende; Cirantan; Cresadex; Creston; Crestor; Provisacor; Razel; Rosedex; Rosimol; Rosumed; Rosustatin; Rosuvas; Rosuvast; Rosvel; Rovartal; Simestat; Sinlip; Vivacor; Rosuvastatin [INN]; Rosuvastatin calcium; Rosuvastatin calcium [USAN]; Rosuvastatin hemicalcium; S 4522; ZD 4522; ZD4522; AZD-4522; Creston (TN);Crestor (TN); Pyrimidine Compound, 26; Rosuvastatin (INN); S-4522; ZD 4522, calcium salt; ZD-4522; Rosuvastatin calcium (JAN/USAN); Bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino] pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhelpt-6-enoic acid] calcium salt; Calcium (E,3R,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoate; (3R,5S,6E)-7-(4-(4-fluorophenyl)-6-(1-methylethyl)-2-(ethyl(methylsulfonyl)amino)-5-pyrimidinyl)-3,5-dihydroxy-6-heptenoic acid; (3R,5S,6E)-7-{4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-(propan-2-yl)pyrimidin-5-yl}-3,5-dihydroxyhept-6-enoic acid; (3R,5S,6E)-7-{4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl}-3,5-dihydroxyhept-6-enoic acid; (E,3R,5R)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid; (E,3R,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid; (S-((R*,S*-(E)))-7-(4-(4-fluorophenyl)-6-(1-methylethyl)-2-(methyl(methylsulfonyl) amino)-5-pyrimidinyl)-3,5-dihydroxy-6-heptenoic acid, calcium salt (2:1); (S-(R*,S*-(E)))-7-(4-(4-Fluorophenyl)-6-(1-methylethyl)-2-(methyl(methylsulfonyl)amino)-5-pyrimidinyl)-3,5-dihydroxy-6-heptenoic acid, calcium salt (2:1); 6-Heptenoic acid, 7-(4-(4-fluorophenyl)-6-(1-methylethyl)-2-(ethyl(methylsulfonyl)amino)-5-pyrimidinyl)-3,5-dihydroxy-, (3R,5S,6E); 6-Heptenoic acid, 7-(4-(4-fluorophenyl)-6-(1-methylethyl)-2-(methyl(methylsulfonyl)amino)-5-pyrimidinyl)-3,5-dihydroxy-, calcium salt (2:1), (3R,5S,6E)

Indication

Disease Entry	ICD 11	Status	REF
Arteriosclerosis	BD40	Approved	[1]
Hypercholesterolaemia	5C80.0	Approved	[2]
Hyperlipidemia, familial combined, LPL related		Approved	[1]
Hypertriglyceridemia	5C80.1	Approved	[1]
Elevated C-reactive protein	MA14.15	Phase 3	[2]
Colon cancer	2B90.Z	Investigative	[1]
Precancerous condition		Investigative	[1]
Stroke	8B20	Investigative	[1]

Therapeutic Class

Anticholesteremic Agents

Cross-matching ID

PubChem CID: 446157
ChEBI ID: CHEBI:38545
CAS Number: CAS 287714-41-4
TTD Drug ID: DMMIQ7G
VARIDT Drug ID: DR00223
INTEDE Drug ID: DR1445
ACDINA Drug ID: D00608

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	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
Sodium/taurocholate cotransporting polypeptide (SLC10A1)	DT56EKP	NTCP_HUMAN	Approved	[4]
Multidrug resistance-associated protein 2 (ABCC2)	DTFI42L	MRP2_HUMAN	Approved	[5]
Organic anion transporting polypeptide 2B1 (SLCO2B1)	DTPFTEQ	SO2B1_HUMAN	Approved	[5]
Organic anion transporting polypeptide 1A2 (SLCO1A2)	DTE2B1D	SO1A2_HUMAN	Approved	[4]
Breast cancer resistance protein (ABCG2)	DTI7UX6	ABCG2_HUMAN	Approved	[5]
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DT3D8F0	SO1B1_HUMAN	Approved	[5]
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DT9C1TS	SO1B3_HUMAN	Approved	[5]
Organic anion transporter 3 (SLC22A8)	DTVP67E	S22A8_HUMAN	Approved	[6]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[5]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Approved	[7]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Approved	[7]
Cytochrome P450 1B1 (CYP1B1)	DE9QHP6	CP1B1_HUMAN	Approved	[8]

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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
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
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 1B1 (CYP1B1)	DME	CYP1B1	5.098	5.256	8.133	6.2
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	11.76	5.931	6.164	9.423
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

Arteriosclerosis

ICD Disease Classification

BD40

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
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
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
Cytochrome P450 1B1 (CYP1B1)	DME	CYP1B1	1.27E-09	2.24E+00	2.07E+00
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	2.63E-03	-1.18E-01	-3.80E-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	Rosuvastatin 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: 2954).
3	New dimension of statin action on ApoB atherogenicity. Clin Cardiol. 2003 Jan;26(1 Suppl 1):I7-10.
4	Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology. 2006 May;130(6):1793-806.
5	Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos. 2008 Oct;36(10):2014-23.
6	The contribution of organic anion transporters OAT1 and OAT3 to the renal uptake of rosuvastatin. J Pharmacol Exp Ther. 2007 Sep;322(3):1221-7.
7	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.
8	Pharmacokinetics of rosuvastatin when coadministered with rifampicin in healthy males: a randomized, single-blind, placebo-controlled, crossover study. Clin Ther. 2008 Jul;30(7):1283-9.