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

General Information of Drug (ID: DM02AWV)

Drug Name

Tolbutamide Drug Info

Synonyms

Aglicid; Arcosal; Arkozal; Artosin; Artozin; Beglucin; Butamid; Butamide; Butamidum; Diaben; Diabesan; Diabetamid; Diabetol; Diabuton; Diasulfon; Diaval; Dirastan; Dolipol; Drabet; Glyconon; Ipoglicone; Mobenol; Orabet; Oralin; Oramide; Orezan; Orinase; Orinaz; Oterben; Pramidex; Rastinon; Restinon; Tarasina; Tolbet;Tolbusal; Tolbutamid; Tolbutamida; Tolbutamidum; Tolbutone; Toluina; Tolumid; Toluran; Toluvan; Tolylsulfonylbutylurea; Willbutamide; Apotex Brand of Tolbutamide; Aventis Brand of Tolbutamide; BerlinChemie Brand of Tolbutamide; Butamide Brand of Tolbutamide; Hoechst Brand of Tolbutamide; Pfizer Brand of Tolbutamide; TOLBUTAMIDE USP; Tolbutamide Aventis Brand; Tolbutamide Butamide Brand; Tolbutamide Hoechst Brand; Tolbutamide Pfizer Brand; Valdecasas Brand of Tolbutamide; Yamanouchi Brand of Tolbutamide; D 860; HLS 831; T 0891; U 2043; Apo-Tolbutamide; Berlin-Chemie Brand of Tolbutamide; Novo-Butamide; Orinase (TN); Sk-tolbutamide; Tol-Tab; Tolbutamida [INN-Spanish]; Tolbutamidum [INN-Latin]; Tolbutamide [INN:BAN:JAN]; R.A.N. Brand of Tolbutamide; Tolbutamid R.A.N.; Tolbutamide (JP15/USP/INN); N-4-Methylbenzolsulfonyl-N-butylurea; N-4-(Methylbenzolsulfonyl)-n-butylurea; N-Butyl-N'-p-toluenesulfonylurea; N-n-Butyl-N'-tosylurea; N-(4-Methylbenzenesulfonyl)-N'-butylurea; N-(4-Methylphenylsulfonyl)-N'-butylurea; N-(p-Tolylsulfonyl)-N'-butylcarbamide; N-Butyl-N'-(4-methylphenylsulfonyl)urea; N-Butyl-N'-(p-tolylsulfonyl)urea; N-Butyl-N'-toluene-p-sulfonylurea; N-(p-tolylsulfonyl)-N'-n-butylurea; 1-Butyl-3-(4-methylphenylsulfonyl)urea; 1-Butyl-3-(p-methylphenylsulfonyl)urea; 1-Butyl-3-(p-tolylsulfonyl)urea; 1-Butyl-3-(para-tolylsulfonyl) urea; 1-Butyl-3-tosylurea; 1-butyl-3-(4-methylphenyl)sulfonylurea; 1-p-Toluenesulfonyl-3-butylurea; 3-(p-Tolyl-4-sulfonyl)-1-butylurea; 3-(p-tolylsulfonyl)-1-butylurea; 3-[p-Tolyl-4-sulfonyl]-1-butylurea

Indication

Disease Entry	ICD 11	Status	REF
Advanced cancer	2A00-2F9Z	Approved	[1]
Non-insulin dependent diabetes	5A11	Approved	[2]

Therapeutic Class

Hypoglycemic Agents

Cross-matching ID

PubChem CID: 5505
ChEBI ID: CHEBI:27999
CAS Number: CAS 64-77-7
TTD Drug ID: DM02AWV
VARIDT Drug ID: DR00104
INTEDE Drug ID: DR1612
ACDINA Drug ID: D00685

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
ATP-binding cassette transporter C8 (ABCC8)	TTP835K	ABCC8_HUMAN	Blocker	[3]
ATP-binding cassette transporter C9 (ABCC9)	TTEF5MJ	ABCC9_HUMAN	Blocker	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
Sulfonylurea receptor 1 (ABCC8)	DTI58LU	ABCC8_HUMAN	Approved	[4]
Sulfonylurea receptor 2 (ABCC9)	DT3JCE6	ABCC9_HUMAN	Approved	[4]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Approved	[5]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Approved	[6]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Approved	[7]
Cytochrome P450 2C18 (CYP2C18)	DEZMWRE	CP2CI_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
ATP-binding cassette transporter C9 (ABCC9)	DTT	ABCC9	6.009	4.315	3.524	5.588
Sulfonylurea receptor 1 (ABCC8)	DTP	SUR1	2.916	3.17	2.678	2.573
Sulfonylurea receptor 2 (ABCC9)	DTP	SUR2	6.009	4.315	3.524	5.588
Cytochrome P450 2C18 (CYP2C18)	DME	CYP2C18	8.485	5.28	4.621	8.889
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	9.791	3.744	3.413	1.609
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	7.867	5.142	5.52	7.08
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

Advanced cancer

ICD Disease Classification

2A00-2F9Z

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
ATP-binding cassette transporter C9 (ABCC9)	DTT	ABCC9	6.51E-01	0.02	0.06
ATP-binding cassette transporter C9 (ABCC9)	DTT	ABCC9	8.46E-01	0.02	0.22
Sulfonylurea receptor 1 (ABCC8)	DTP	SUR1	2.48E-02	1.04E-01	3.79E-01
Sulfonylurea receptor 1 (ABCC8)	DTP	SUR1	6.55E-02	1.00E-01	4.41E-01
Sulfonylurea receptor 2 (ABCC9)	DTP	SUR2	6.51E-01	2.26E-02	6.23E-02
Sulfonylurea receptor 2 (ABCC9)	DTP	SUR2	8.46E-01	2.42E-02	2.17E-01
Cytochrome P450 2C18 (CYP2C18)	DME	CYP2C18	8.28E-05	1.33E-01	1.20E+00
Cytochrome P450 2C18 (CYP2C18)	DME	CYP2C18	1.51E-03	-1.83E-01	-2.01E-01
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	2.41E-01	3.17E-02	2.29E-01
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	5.67E-01	5.11E-02	1.35E-01
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	4.79E-03	1.32E-01	7.85E-01
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	1.82E-01	-1.71E-02	-9.86E-02
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	7.33E-02	5.59E-02	2.99E-01
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	5.65E-03	-7.28E-02	-1.24E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Tolbutamide FDA Label
2	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
3	Expression of an activating mutation in the gene encoding the KATP channel subunit Kir6.2 in mouse pancreatic beta cells recapitulates neonatal diabetes. J Clin Invest. 2009 Jan;119(1):80-90.
4	ABCC8 and ABCC9: ABC transporters that regulate K+ channels. Pflugers Arch. 2007 Feb;453(5):703-18.
5	Effects of organic solvents on the activities of cytochrome P450 isoforms, UDP-dependent glucuronyl transferase, and phenol sulfotransferase in human hepatocytes. Drug Metab Dispos. 2001 Feb;29(2):141-4.
6	CYP2C19 participates in tolbutamide hydroxylation by human liver microsomes. Drug Metab Dispos. 2000 Mar;28(3):354-9.
7	Prediction of in vivo drug-drug interactions between tolbutamide and various sulfonamides in humans based on in vitro experiments. Drug Metab Dispos. 2000 Apr;28(4):475-81.
8	Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.