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

General Information of Drug (ID: DMXCM7H)

Drug Name

Cerivastatin Drug Info

Synonyms

cerivastatin; Baycol; cerivastatin acid; Lipobay; 145599-86-6; Cerivastatin [INN:BAN]; UNII-AM91H2KS67; CHEBI:3558; AM91H2KS67; HSDB 7357; (3R,5S,6E)-7-(4-(p-Fluorophenyl)-2,6-diisopropyl-5-(methoxymethyl)-3-pyridyl)-3,5-dihydroxy-6-heptenoic acid; (3R,5S,6E)-7-(4-(4-Fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl)-3,5-dihydroxy-6-heptenoic acid; 143201-11-0; 6-Heptenoic acid, 7-(4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl)-3,5-dihydroxy-, (3R,5S,6E)-; Statins

Indication

Disease Entry	ICD 11	Status	REF
Hyperlipidaemia	5C80	Approved	[1]
Multiple myeloma	2A83	Phase 1/2	[2]

Cross-matching ID

PubChem CID: 446156
ChEBI ID: CHEBI:3558
CAS Number: CAS 145599-86-6
TTD Drug ID: DMXCM7H
VARIDT Drug ID: DR00391
INTEDE Drug ID: DR0290

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]

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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	[3]
Multidrug resistance-associated protein 2 (ABCC2)	DTFI42L	MRP2_HUMAN	Approved	[4]
Organic anion transporting polypeptide 2B1 (SLCO2B1)	DTPFTEQ	SO2B1_HUMAN	Approved	[5]
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	[7]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[4]

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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	[8]
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DEYGVN4	UD11_HUMAN	Approved	[9]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Approved	[10]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Approved	[11]
Cytochrome P450 3A7 (CYP3A7)	DERD86B	CP3A7_HUMAN	Approved	[10]
UDP-glucuronosyltransferase 1A3 (UGT1A3)	DEF2WXN	UD13_HUMAN	Approved	[9]

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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
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 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 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

ICD Disease Classification

02 Neoplasm

Disease Class

ICD-11: 2C82 Prostate cancer

The Studied Tissue

Bone marrow

The Studied Disease

Multiple myeloma [ICD-11:2C82]

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
HMG-CoA reductase (HMGCR)	DTT	HMGCR	1.48E-06	1.01	4.34
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.42E-01	-4.36E-02	-2.21E-01
P-glycoprotein 1 (ABCB1)	DTP	P-GP	6.80E-01	2.46E-01	2.41E-01
Organic anion transporting polypeptide 2B1 (SLCO2B1)	DTP	OATP2B1	1.70E-02	-1.23E+00	-1.37E+00
Organic anion transporting polypeptide 2B1 (SLCO2B1)	DTP	OATP2B1	4.78E-01	9.86E-02	7.44E-01
Breast cancer resistance protein (ABCG2)	DTP	BCRP	3.08E-02	-4.06E-01	-8.83E-01
Breast cancer resistance protein (ABCG2)	DTP	BCRP	7.10E-01	5.87E-03	1.61E-02
Multidrug resistance-associated protein 2 (ABCC2)	DTP	MRP2	2.22E-01	-1.68E-01	-6.27E-01
Multidrug resistance-associated protein 2 (ABCC2)	DTP	MRP2	2.44E-01	6.35E-02	3.90E-01
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DTP	OATP1B3	2.19E-02	4.44E-02	4.09E-01
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DTP	OATP1B3	6.12E-01	1.16E-01	7.74E-01
Sodium/taurocholate cotransporting polypeptide (SLC10A1)	DTP	NTCP	1.21E-03	-4.83E-01	-2.00E+00
Sodium/taurocholate cotransporting polypeptide (SLC10A1)	DTP	NTCP	2.13E-01	1.57E-01	7.50E-01
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DTP	OATP1B1	1.50E-04	1.94E-01	2.06E+00
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DTP	OATP1B1	6.86E-01	3.72E-02	2.86E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	6.60E-01	2.51E-02	8.26E-02
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	8.62E-03	1.37E-01	8.67E-01
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	7.83E-01	2.87E-03	6.52E-02
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	5.86E-02	-1.69E-01	-8.79E-01
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	2.26E-02	7.10E-02	1.00E+00
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	7.23E-01	-2.28E-02	-3.11E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	2.51E-01	8.39E-02	5.00E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	1.93E-04	-6.16E-01	-2.64E+00

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	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: 2950).
2	Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
3	Differential effect of genetic variants of Na(+)-taurocholate co-transporting polypeptide (NTCP) and organic anion-transporting polypeptide 1B1 (OATP1B1) on the uptake of HMG-CoA reductase inhibitors. Xenobiotica. 2011 Jan;41(1):24-34.
4	Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67.
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10	Drug Interactions Flockhart Table
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