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-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Approved Drug(s)
Patented Agent(s)
Drug(s) Targeting Aurora kinase B (AURKB)
Drug Name Drug ID Indication ICD 11 Highest Status REF
AT9283 DMQ94CT Solid tumour/cancer 2A00-2F9Z Phase 3 [7]
PHA-739358 DMGYBZI Prostate cancer 2C82.0 Phase 2 [8]
VX-680 DM93YKJ Solid tumour/cancer 2A00-2F9Z Phase 2 [4]
ABT-348 DMMZOYN Haematological malignancy 2B33.Y Phase 2 [9]
HPP-607 DM5VSZR Solid tumour/cancer 2A00-2F9Z Phase 1 [10]
CYC116 DMUMHXT Solid tumour/cancer 2A00-2F9Z Phase 1 [11]
AMG 900 DMASGXJ Solid tumour/cancer 2A00-2F9Z Phase 1 [12]
SNS-314 DMAC5F2 Solid tumour/cancer 2A00-2F9Z Phase 1 [13]
BI-847325 DMY4B6J Solid tumour/cancer 2A00-2F9Z Phase 1 [14]
R763 DME0CJ9 Haematological malignancy 2B33.Y Phase 1 [15]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [16]
Intedanib DMSTA36 Colorectal cancer 2B91.Z Approved [17]
Pemigatinib DM819JF Cholangiocarcinoma 2C12.10 Approved [18]
E-3810 DM42PFT Solid tumour/cancer 2A00-2F9Z Phase 3 [19]
Sulfatinib DMPOTM4 Neuroendocrine cancer 2B72.1 Phase 3 [20]
BGJ398 DMNKBEC Cholangiocarcinoma 2C12.10 Phase 3 [21]
ARQ-087 DM02BVQ Intrahepatic cholangiocarcinoma 2C12.10 Phase 3 [22]
AZD4547 DM3827C Solid tumour/cancer 2A00-2F9Z Phase 2/3 [23]
Debio 1347 DMZW50O Solid tumour/cancer 2A00-2F9Z Phase 2 [24]
AM-001 DMGVQI8 Actinic keratosis EK90.0 Phase 2 [25]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [4]
Pazopanib HCl DM6U9CQ Renal cell carcinoma 2C90 Approved [26]
Intedanib DMSTA36 Colorectal cancer 2B91.Z Approved [17]
CT-102 DMB8PF3 Diabetic foot ulcer BD54 Approved [27]
Trapidil DMY67U8 Acute coronary syndrome BA41 Phase 4 [28]
TKI258 DMYLT67 Renal cell carcinoma 2C90 Phase 3 [4]
BAY-57-9352 DMVA5NS Gastric adenocarcinoma 2B72 Phase 2 [4]
X-82 DMW1NKO Age-related macular degeneration 9B75.0 Phase 2 [29]
Vorolanib DMIM1U9 Non-small cell lung cancer 2C25 Phase 2 [30]
PMID25623274-Compound-WO2014132220C2 DMXEZWP Pulmonary arterial hypertension BB01.0 Patented [31]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [32]
Pioglitazone DMKJ485 Diabetic complication 5A2Y Approved [33]
Lobeglitazone DMHY3IP Type-2 diabetes 5A11 Approved [34]
Rosiglitazone XR DMT45MU Type-2 diabetes 5A11 Approved [6]
Thiazolidinedione DMC1NBW Alzheimer disease 8A20 Approved [33]
Glitazone DMDN4A1 N. A. N. A. Phase 4 [35]
Muraglitazar DMG3NFZ N. A. N. A. Phase 3 [36]
Rivoglitazone DMBY31K Ocular inflammation 9C61.24 Phase 3 [37]
Balaglitazone DMXBHR6 Type-1 diabetes 5A10 Phase 3 [38]
Ragaglitazar DMFSHEM Type-1 diabetes 5A10 Phase 3 [39]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sorafenib DMS8IFC Hepatocellular carcinoma 2C12.02 Approved [40]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [16]
Regorafenib DMHSY1I Metastatic colorectal cancer 2B91 Approved [41]
Sunitinib DMCBJSR Gastrointestinal cancer 2C11 Approved [42]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [43]
Vandetanib DMRICNP Solid tumour/cancer 2A00-2F9Z Approved [4]
Pazopanib HCl DM6U9CQ Renal cell carcinoma 2C90 Approved [26]
Cabozantinib DMIYDT4 Thyroid cancer 2D10 Approved [44]
Tivozanib DMUKC5L Renal cell carcinoma 2C90 Approved [45]
Lenvatinib DMB1IU4 Thyroid cancer 2D10 Approved [46]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Aurora kinase A (AURKA)
Drug Name Drug ID Indication ICD 11 Highest Status REF
AT9283 DMQ94CT Solid tumour/cancer 2A00-2F9Z Phase 3 [7]
MLN8237 DMO8PT9 Solid tumour/cancer 2A00-2F9Z Phase 3 [47]
PHA-739358 DMGYBZI Prostate cancer 2C82.0 Phase 2 [8]
VX-680 DM93YKJ Solid tumour/cancer 2A00-2F9Z Phase 2 [4]
ABT-348 DMMZOYN Haematological malignancy 2B33.Y Phase 2 [9]
ENMD-2076 DMJZVPB Acute myeloid leukaemia 2A60 Phase 2 [8]
LY3295668 DM8RJTB Solid tumour/cancer 2A00-2F9Z Phase 1/2 [48]
HPP-607 DM5VSZR Solid tumour/cancer 2A00-2F9Z Phase 1 [10]
MLN8054 DMUANF3 Solid tumour/cancer 2A00-2F9Z Phase 1 [4]
CYC116 DMUMHXT Solid tumour/cancer 2A00-2F9Z Phase 1 [11]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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]

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).
7 A phase I trial of AT9283 (a selective inhibitor of aurora kinases) in children and adolescents with solid tumors: a Cancer Research UK study. Clin Cancer Res. 2015 Jan 15;21(2):267-73.
8 Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
9 Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J Pharmacol Exp Ther. 2012 Dec;343(3):617-27.
10 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. (Target id: 1936).
11 Clinical pipeline report, company report or official report of Cyclacel.
12 Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res. 2010 Dec 1;70(23):9846-54.
13 SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer Chemother Pharmacol. 2010 Mar;65(4):707-17.
14 doi: 10.1158/1535-7163.TARG-13-B281
15 Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen. J Cancer Res Clin Oncol. 2010 Jan;136(1):99-113.
16 Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
17 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
18 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
19 E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405.
20 Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
21 Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res. 2013 Apr;28(4):899-911.
22 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. (Target id: 1808).
23 AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012 Apr 15;72(8):2045-56.
24 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
25 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029917)
26 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
27 Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
28 Osteitis fibrosa is mediated by Platelet-Derived Growth Factor-A via a phosphoinositide 3-kinase-dependent signaling pathway in a rat model for chr... Endocrinology. 2008 Nov;149(11):5735-46.
29 National Cancer Institute Drug Dictionary (drug id 695817).
30 Vorolanib, an oral VEGFR/PDGFR dual tyrosine kinase inhibitor for treatment of patients with advanced solid tumors: An open-label, phase I dose escalation and dose expansion trial. Chin J Cancer Res. 2021 Feb 28;33(1):103-114.
31 Evaluation of WO-2014132220, selective PDGFR inhibitors for the treatment of pulmonary arterial hypertension.Expert Opin Ther Pat. 2015 Apr;25(4):493-9.
32 Expression of peroxisome proliferator-activated receptors (PPARs) in human urinary bladder carcinoma and growth inhibition by its agonists. Int J Cancer. 2003 May 1;104(5):597-602.
33 Functional PPAR-gamma receptor is a novel therapeutic target for ACTH-secreting pituitary adenomas. Nat Med. 2002 Nov;8(11):1281-7.
34 Tolerability and pharmacokinetics of lobeglitazone, a novel peroxisome proliferator-activated receptor-gamma agonist, after a single oral administration in healthy female subjects. Clin Drug Investig. 2014 Jul;34(7):467-74.
35 Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity. J Biol Chem. 2000 Jun 2;275(22):16638-42.
36 Muraglitazar, a dual (alpha/gamma) PPAR activator: a randomized, double-blind, placebo-controlled, 24-week monotherapy trial in adult patients with... Clin Ther. 2005 Aug;27(8):1181-95.
37 A randomized-controlled trial to investigate the effects of rivoglitazone, a novel PPAR gamma agonist on glucose-lipid control in type 2 diabetes. Diabetes Obes Metab. 2011 Sep;13(9):806-13.
38 Balaglitazone: a second generation peroxisome proliferator-activated receptor (PPAR) gamma () agonist.Mini Rev Med Chem.2012 Feb;12(2):87-97.
39 Ragaglitazar: the pharmacokinetics, pharmacodynamics, and tolerability of a novel dual PPAR alpha and gamma agonist in healthy subjects and patients with type 2 diabetes. J Clin Pharmacol. 2003 Nov;43(11):1244-56.
40 Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40.
41 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
42 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
43 Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
44 Clinical pipeline report, company report or official report of Exelixis (2011).
45 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
46 Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.
47 Effect of Aurora A kinase inhibitor MLN8237 combined with rituximab on antitumor activity in preclinical B-cell non-Hodgkin's lymphoma models. Journal of Clinical Oncology, 2009:8553.
48 Aurora A-Selective Inhibitor LY3295668 Leads to Dominant Mitotic Arrest, Apoptosis in Cancer Cells, and Shows Potent Preclinical Antitumor Efficacy. Mol Cancer Ther. 2019 Dec;18(12):2207-2219.