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

General Information of Drug (ID: DM5SXUV)

Drug Name

Repaglinide Drug Info

Synonyms

Actulin; GlucoNorm; NovoNorm; Prandin; Repaglinida; Repaglinidum; Glaxo Wellcome brand of replaginide; Novo Nordisk brand of repaglinide; Repaglinide [USAN]; Novo Nordisk brand 2 of repaglinide; AG-EE 388; AG-EE 388 ZW; AG-EE 623 ZW; AGEE-623ZW; GlucoNorm (TN); NN-623; NovoNorm (TN); Prandin (TN); Repa-glinide; Repaglinida [INN-Spanish]; Repaglinidum [INN-Latin]; SMP-508; AG-EE-388; AG-EE-623 ZW; Prandin, GlucoNorm, NovoNorm, Repaglinide; Repaglinide (JAN/USP/INN); Repaglinide, (+-)-isomer; (+)-2-Ethoxy-alpha-(((S)-alpha-isobutyl-o-piperidinobenzyl)carbamoyl)-p-toluic acid; (S)-(+)-2-Ethoxy-4-[N-[1-(2-piperidinophenyl)-3-methyl-1-butyl]aminocarbonylmethyl]benzoic acid; (S)-2-Ethoxy-4-(2-((methyl-1-(2-(1-piperidinyl)phenyl)butyl)amino)-2-oxoethyl)-benzoic acid; (S)-2-ethoxy-4-(2-((3-methyl-1-(2-(1-piperidinyl)-phenyl)butyl)amino)-2-oxoethyl)-benzoic acid; 111GE012; 2-ethoxy-4-(2-((3-methyl-1-(2-(1-piperidinyl)phenyl)butyl)amino)-2-oxoethyl)benzoic acid; 2-ethoxy-4-(2-{[(1S)-3-methyl-1-(2-piperidin-1-ylphenyl)butyl]amino}-2-oxoethyl)benzoic acid; 2-ethoxy-4-[2-({(1S)-3-methyl-1-[2-(piperidin-1-yl)phenyl]butyl}amino)-2-oxoethyl]benzoic acid; 2-ethoxy-4-[2-[[(1S)-3-methyl-1-(2-piperidin-1-ylphenyl)butyl]amino]-2-oxoethyl]benzoic acid; 2-ethoxy-N-(alpha-(2-methyl-1-propyl)-2-piperidinobenzyl)-4-carbamoylmethylbenzoic acid

Indication

Disease Entry	ICD 11	Status	REF
Diabetic complication	5A2Y	Approved	[1]

Therapeutic Class

Hypoglycemic Agents

Cross-matching ID

PubChem CID: 65981
ChEBI ID: CHEBI:8805
CAS Number: CAS 135062-02-1
TTD Drug ID: DM5SXUV
VARIDT Drug ID: DR00446
INTEDE Drug ID: DR1404
ACDINA Drug ID: D00587

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	[2]
ATP-binding cassette transporter C9 (ABCC9)	TTEF5MJ	ABCC9_HUMAN	Blocker	[2]

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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	[3]

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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	[4]
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DEYGVN4	UD11_HUMAN	Approved	[5]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Approved	[4]

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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
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 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

Diabetic complication

ICD Disease Classification

5A2Y

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
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DTP	OATP1B1	2.41E-01	-2.63E-02	-8.50E-02
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DTP	OATP1B1	5.54E-01	-1.65E-02	-1.24E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	8.29E-01	-5.44E-03	-2.25E-02
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	4.23E-03	9.31E-02	4.30E-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
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	2.13E-01	4.03E-02	2.50E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	8.21E-02	8.17E-02	4.35E-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: 6841).
2	Metformin/Repaglinide (PrandiMet) for type 2 diabetes. Med Lett Drugs Ther. 2009 Jun 1;51(1313):41-3.
3	Disease-Associated Changes in Drug Transporters May Impact the Pharmacokinetics and/or Toxicity of Drugs: A White Paper From the International Transporter Consortium. Clin Pharmacol Ther. 2018 Nov;104(5):900-915.
4	Drug-drug and food-drug pharmacokinetic interactions with new insulinotropic agents repaglinide and nateglinide. Clin Pharmacokinet. 2007;46(2):93-108.
5	Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism. Br J Clin Pharmacol. 2010 Dec;70(6):870-80.