Details of the Drug

General Information of Drug (ID: DMILWZR)

Drug Name

Rosiglitazone

Indication

Disease Entry	ICD 11	Status	REF
Chronic kidney disease	GB61	Terminated	[]
------------------------------------------------------------------------------------

ADMET Property

Clearance: The apparent oral clearance of drug is 3.03 +/- 0.87 L/h []
Half-life: The concentration or amount of drug in body reduced by one-half in 3 - 4 hours [1]
Metabolism: The drug is metabolized via the hepatic []
Vd: The volume of distribution (Vd) of drug is 17.6 L []

Chemical Identifiers

Formula: C18H19N3O3S
IUPAC Name: 5-[[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
Canonical SMILES: CN(CCOC1=CC=C(C=C1)CC2C(=O)NC(=O)S2)C3=CC=CC=N3
InChI: InChI=1S/C18H19N3O3S/c1-21(16-4-2-3-9-19-16)10-11-24-14-7-5-13(6-8-14)12-15-17(22)20-18(23)25-15/h2-9,15H,10-12H2,1H3,(H,20,22,23)
InChIKey: YASAKCUCGLMORW-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 77999
ChEBI ID: CHEBI:50122
CAS Number: 122320-73-4
DrugBank ID: DB00412
VARIDT ID: DR01221

Combinatorial Drugs (CBD)

Click to Jump to the Detailed CBD Information of This Drug

Molecular Interaction Atlas of This Drug

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Breast cancer resistance protein (ABCG2)	DTI7UX6	ABCG2_HUMAN	Substrate	[2]

------------------------------------------------------------------------------------

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[3]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Substrate	[4]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Substrate	[4]
Prostaglandin G/H synthase 1 (COX-1)	DE073H6	PGH1_HUMAN	Substrate	[5]

------------------------------------------------------------------------------------

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
1-acyl-sn-glycerol-3-phosphate acyltransferase delta (AGPAT4)	OT5CTQKO	PLCD_HUMAN	Gene/Protein Processing	[6]
11-beta-hydroxysteroid dehydrogenase 1 (HSD11B1)	OTO7FJA9	DHI1_HUMAN	Gene/Protein Processing	[7]
11-beta-hydroxysteroid dehydrogenase type 2 (HSD11B2)	OTHF4H9U	DHI2_HUMAN	Gene/Protein Processing	[8]
2-acylglycerol O-acyltransferase 3 (MOGAT3)	OTPGLUBS	MOGT3_HUMAN	Gene/Protein Processing	[9]
2-aminomuconic semialdehyde dehydrogenase (ALDH8A1)	OTINY3MW	AL8A1_HUMAN	Gene/Protein Processing	[9]
3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 2 (HSD3B2)	OT02MSKN	3BHS2_HUMAN	Gene/Protein Processing	[10]
4-aminobutyrate aminotransferase, mitochondrial (ABAT)	OTXAGR7J	GABT_HUMAN	Gene/Protein Processing	[9]
5'-nucleotidase (NT5E)	OT7J5LT6	5NTD_HUMAN	Gene/Protein Processing	[9]
5-aminolevulinate synthase, non-specific, mitochondrial (ALAS1)	OTQY6ZSF	HEM1_HUMAN	Gene/Protein Processing	[9]
5-hydroxytryptamine receptor 3A (HTR3A)	OTAIV1AK	5HT3A_HUMAN	Gene/Protein Processing	[9]

------------------------------------------------------------------------------------

Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

References

1	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
2	ATP-binding cassette transporters in human heart failure. Naunyn Schmiedebergs Arch Pharmacol. 2008 May;377(3):231-43.
3	Effects of gemfibrozil, itraconazole, and their combination on the pharmacokinetics of pioglitazone. Clin Pharmacol Ther. 2005 May;77(5):404-14.
4	Characterization of the cytochrome P450 enzymes involved in the in vitro metabolism of rosiglitazone. Br J Clin Pharmacol. 1999 Sep;48(3):424-32.
5	Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
6	PPARgamma controls CD1d expression by turning on retinoic acid synthesis in developing human dendritic cells. J Exp Med. 2006 Oct 2;203(10):2351-62.
7	Effects of chronic rosiglitazone therapy on gene expression in human adipose tissue in vivo in patients with type 2 diabetes. J Clin Endocrinol Metab. 2007 Feb;92(2):720-4.
8	Tributyltin and triphenyltin induce 11-hydroxysteroid dehydrogenase 2 expression and activity through activation of retinoid X receptor . Toxicol Lett. 2020 Apr 1;322:39-49. doi: 10.1016/j.toxlet.2020.01.001. Epub 2020 Jan 9.
9	Transcriptomic analysis of untreated and drug-treated differentiated HepaRG cells over a 2-week period. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):27-35.
10	Cinnamic acid based thiazolidinediones inhibit human P450c17 and 3beta-hydroxysteroid dehydrogenase and improve insulin sensitivity independent of PPARgamma agonist activity. J Mol Endocrinol. 2004 Apr;32(2):425-36.