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

General Information of Drug (ID: DMZMSCT)

Drug Name

Cilostazol Drug Info

Synonyms

cilostazol; 73963-72-1; Pletal; Cilostazole; Pletaal; Cilostazolum; OPC-13013; Cilostazolum [INN-Latin]; OPC-21; OPC 13013; OPC 21; UNII-N7Z035406B; CHEBI:31401; C20H27N5O2; 6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydro-2(1H)-quinolinone; BRN 3632107; 6-[4-(1-cyclohexyltetrazol-5-yl)butoxy]-3,4-dihydro-1H-quinolin-2-one; 6-(4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydroquinolin-2(1H)-one; 3,4-Dihydro-6-(4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy)-2(1H)-quinolinone; MLS000028470; Cilostazole; Otsuka brand of cilostazol; C 0737; CL23867; Cilostazol [INN:JAN]; Pleta (TN); Pletal (TN); Pletal, Cilostazol; Cilostazol (JP15/USAN/INN); 6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydrocarbostyril; 6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxyl)-3,4-dihydrocarobostyril; 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)-butoxy]-3,4-dihydro-2(1H)-quinolinone; 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydroquinolin-2(1H)-one

Indication

Disease Entry	ICD 11	Status	REF
Intermittent claudication	BD40.00	Approved	[1]

Therapeutic Class

Vasodilator Agents

Cross-matching ID

PubChem CID: 2754
ChEBI ID: CHEBI:31401
CAS Number: CAS 73963-72-1
TTD Drug ID: DMZMSCT
VARIDT Drug ID: DR01322
INTEDE Drug ID: DR0324
ACDINA Drug ID: D00129

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Phosphodiesterase 3 (PDE3)	TTZCG4L	NOUNIPROTAC	Modulator	[2]
Phosphodiesterase 3A (PDE3A)	TT06AWU	PDE3A_HUMAN	Inhibitor	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DT3D8F0	SO1B1_HUMAN	Approved	[4]
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DT9C1TS	SO1B3_HUMAN	Approved	[4]
Organic anion transporter 3 (SLC22A8)	DTVP67E	S22A8_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	[6]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Approved	[6]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Approved	[6]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Approved	[6]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Approved	[6]
Cytochrome P450 3A7 (CYP3A7)	DERD86B	CP3A7_HUMAN	Approved	[6]

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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
Phosphodiesterase 3A (PDE3A)	DTT	PDE3A	4.717	6.087	5.051	5.051
Organic anion transporter 3 (SLC22A8)	DTP	OAT3	2.722	2.07	8.103	3.597
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
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	10.036	5.779	6.508	6.481
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	10.08	7.207	5.403	9.211
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	7.867	5.142	5.52	7.08
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	3.307	5.005	3.921	5.327
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

Intermittent claudication

ICD Disease Classification

BD40.00

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Phosphodiesterase 3A (PDE3A)	DTT	PDE3A	3.33E-01	1.35E-02	0.14
Organic anion transporter 3 (SLC22A8)	DTP	OAT3	3.89E-02	6.02E-02	4.19E-01
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DTP	OATP1B3	4.64E-01	3.84E-02	2.91E-01
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DTP	OATP1B1	2.66E-02	2.54E-02	2.28E-01
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	6.75E-01	4.94E-02	4.06E-01
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	1.38E-02	1.07E-01	8.83E-01
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	6.62E-01	1.75E-02	1.07E-01
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	6.76E-03	-1.19E-01	-1.54E+00
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	4.50E-03	-5.35E-02	-4.77E-01

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: 7148).
2	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
3	A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity. J Med Chem. 1985 May;28(5):537-45.
4	Organic Anion-Transporting Polypeptide and Efflux Transporter-Mediated Hepatic Uptake and Biliary Excretion of Cilostazol and Its Metabolites in Rats and Humans. J Pharm Sci. 2017 Sep;106(9):2515-2523.
5	Aspirin and probenecid inhibit organic anion transporter 3-mediated renal uptake of cilostazol and probenecid induces metabolism of cilostazol in the rat. Drug Metab Dispos. 2014 Jun;42(6):996-1007.
6	Effects of CYP3A inhibition on the metabolism of cilostazol. Clin Pharmacokinet. 1999;37 Suppl 2:61-8.