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

General Information of Drug (ID: DMPIDXT)

Drug Name

Rosiglitazone + metformin Drug Info

Synonyms

Orantinib; TSU-68; 252916-29-3; SU-6668; SU6668; SU 6668; 210644-62-5; UNII-9RL37ZZ665; Orantinib (TSU-68); NSC 702827; TSU68; CHEMBL274654; 9RL37ZZ665; TSU 68; PDGFR Tyrosine Kinase Inhibitor VI, SU6668; 2,4-Dimethyl-5-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-pyrrole-3-propanoic acid; J-502593; Orantinibum; 3-(2,4-dimethyl-5-{[(3Z)-2-oxo-1H-indol-3-ylidene]methyl}-1H-pyrrol-3-yl)propanoic acid; 3-[2,4-dimethyl-5-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid; Orantinib [INN]

Indication

Disease Entry	ICD 11	Status	REF
Diabetic complication	5A2Y	Phase 3	[1]
Advanced solid tumour	2A00-2F9Z	Phase 1	[2] , [3]

Cross-matching ID

PubChem CID: 5329099
CAS Number: CAS 210644-62-5
TTD Drug ID: DMPIDXT

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Aurora kinase A (AURKA)	TTPS3C0	AURKA_HUMAN	Inhibitor	[4] , [5]
Aurora kinase B (AURKB)	TT5LS6T	AURKB_HUMAN	Inhibitor	[4] , [5]
Fibroblast growth factor receptor 1 (FGFR1)	TTRLW2X	FGFR1_HUMAN	Inhibitor	[4] , [5]
Peroxisome proliferator-activated receptor gamma (PPAR-gamma)	TTZMAO3	PPARG_HUMAN	Agonist	[6]
Platelet-derived growth factor receptor (PDGFR)	TTI2WET	NOUNIPROTAC	Inhibitor	[4] , [5]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[4] , [5]

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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
Peroxisome proliferator-activated receptor gamma (PPAR-gamma)	DTT	PPARG	5.576	6.977	5.736	5.758
Fibroblast growth factor receptor 1 (FGFR1)	DTT	FGFR1	5.32	6.548	5.908	6.126
Aurora kinase A (AURKA)	DTT	AURKA	4.479	5.036	4.392	4.505
Aurora kinase B (AURKB)	DTT	AURKB	2.104	2.536	1.766	5.423

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

Diabetic complication

ICD Disease Classification

5A2Y

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Peroxisome proliferator-activated receptor gamma (PPAR-gamma)	DTT	PPARG	2.41E-01	-0.06	-0.25
Vascular endothelial growth factor receptor 2 (KDR)	DTT	KDR	1.98E-01	0.11	0.2
Fibroblast growth factor receptor 1 (FGFR1)	DTT	FGFR1	4.79E-02	-0.03	-0.15

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	ClinicalTrials.gov (NCT00499707) Efficacy and Safety Study of Rosiglitazone/Metformin Therapy vs Rosiglitazone and Metformin in Type 2 Diabetes Subjects. U.S. National Institutes of Health.
2	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: 7816).
3	A phase I surrogate endpoint study of SU6668 in patients with solid tumors. Invest New Drugs. 2004 Nov;22(4):459-66.
4	A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
5	Dose-finding study of the multitargeted tyrosine kinase inhibitor SU6668 in patients with advanced malignancies. Clin Cancer Res. 2005 Sep 1;11(17):6240-6.
6	Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).