General Information of DTT (ID: TTZMAO3)

DTT Name Peroxisome proliferator-activated receptor gamma (PPAR-gamma) DTT Info
Gene Name PPARG

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Preclinical Drug(s)
Patented Agent(s)
Investigative Drug(s)
6 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lobeglitazone DMHY3IP Type-2 diabetes 5A11 Approved [1]
Pioglitazone DMKJ485 Amyotrophic lateral sclerosis 8B60.0 Approved [2]
Rosiglitazone XR DMT45MU Type-2 diabetes 5A11 Approved [3]
Thiazolidinedione DMC1NBW Alzheimer disease 8A20 Approved [2]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [4]
Glitazone DMDN4A1 N. A. N. A. Phase 4 [5]
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⏷ Show the Full List of 6 Approved Drug(s)
25 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Balaglitazone DMXBHR6 Type-1 diabetes 5A10 Phase 3 [6]
CS-038 DM67P0F Type-2 diabetes 5A11 Phase 3 [7]
FARGLITAZAR DMOKT7Y Type-1 diabetes 5A10 Phase 3 [8]
Imiglitazar DM7BCWT Type-2 diabetes 5A11 Phase 3 [9]
Leriglitazone DMQFD42 Cerebral X-linked adrenoleukodystrophy 5C57.1 Phase 3 [10]
MURAGLITAZAR DMG3NFZ N. A. N. A. Phase 3 [11]
Ragaglitazar DMFSHEM Type-1 diabetes 5A10 Phase 3 [12]
Rivoglitazone DMBY31K Ocular inflammation 9C61.24 Phase 3 [13]
TESAGLITAZAR DMGRBN5 Type-1 diabetes 5A10 Phase 3 [14]
ZYH-1 DMMBJYC Lipid metabolism disorder 5C52.Z Phase 3 [15]
MBX-102 DMONYS9 Gout FA25 Phase 2/3 [16]
CHS-131 DMMRKPF Multiple sclerosis 8A40 Phase 2 [17]
FK-614 DMY61TJ Type-2 diabetes 5A11 Phase 2 [18]
GED-0507-34-Levo DMMQY0O Inflammatory bowel disease DD72 Phase 2 [19]
MBX-2044 DMQMTO1 Type-2 diabetes 5A11 Phase 2 [16]
Naveglitazar DMD0E8U Diabetic complication 5A2Y Phase 2 [20]
Netoglitazone DM8H7OA Non-alcoholic fatty liver disease DB92 Phase 2 [21]
OMS405 DMWC36Y Nicotine dependence 6C4A.2 Phase 2 [22]
ONO-5129 DMFX3P1 Diabetic complication 5A2Y Phase 2 [23]
T3D-959 DMR3245 Alzheimer disease 8A20 Phase 2 [24]
CLX-0921 DMJQG25 Type-2 diabetes 5A11 Phase 1 [25]
DSP-8658 DM2PYE0 Alzheimer disease 8A20 Phase 1 [26]
Englitazone sodium DMKPBVX Type-2 diabetes 5A11 Phase 1 [27]
GW-409544 DMOE5SZ Hyperlipidaemia 5C80 Phase 1 [28]
Oxeglitazar DMN4LMT Gout FA25 Phase 1 [29]
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⏷ Show the Full List of 25 Clinical Trial Drug(s)
24 Patented Agent(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
1-(biphenyl-4-yl-methyl)-1H-imidazole derivative 1 DMGYZQ2 N. A. N. A. Patented [30]
3-phenyl acrylic acid derivative 1 DMXMV6N N. A. N. A. Patented [30]
A-substituted phenylpropionic acid derivative 1 DMGM72Q N. A. N. A. Patented [30]
A-substituted phenylpropionic acid derivative 2 DMH5FEO N. A. N. A. Patented [30]
Biaromatic compound 1 DMJG1ZS N. A. N. A. Patented [30]
Cannabinoid quinone derivative 1 DM81SYN N. A. N. A. Patented [30]
Crystalline anhydrous toluene derivative 1 DM76Q10 N. A. N. A. Patented [30]
Flavonoid derivative 8 DM4O9T3 N. A. N. A. Patented [30]
Fused aromatic compound 1 DM4EUFL N. A. N. A. Patented [30]
Fused ring compound 1 DMPHL3J N. A. N. A. Patented [30]
MRL20 DMNGQ3I Discovery agent N.A. Patented [30]
MRL24 DM8NS7U Discovery agent N.A. Patented [30]
Phenylpropionic acid derivative 1 DMTEJRB N. A. N. A. Patented [30]
Phenylpyridine derivative 3 DMDT5JI N. A. N. A. Patented [30]
PMID25416646-Compound-Figure2-J DMJETVH N. A. N. A. Patented [30]
PMID25416646-Compound-Figure2-K DMNTAYK N. A. N. A. Patented [30]
PMID25416646-Compound-Figure2-N DMLDPGY N. A. N. A. Patented [30]
PMID25416646-Compound-Figure5-A DM9OHAN N. A. N. A. Patented [30]
PMID25416646-Compound-Figure5-C DM17FKL N. A. N. A. Patented [30]
PMID25416646-Compound-Figure5-E DMYO7VH N. A. N. A. Patented [30]
PMID25416646-Compound-Figure5-H DMCJTU1 N. A. N. A. Patented [30]
Spirolaxine derivative 1 DMK5G7D N. A. N. A. Patented [30]
Sulfonamide derivative 18 DMHTJ7N N. A. N. A. Patented [30]
Thiazolidine dione crystalline derivative 1 DMLBA4D N. A. N. A. Patented [30]
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⏷ Show the Full List of 24 Patented Agent(s)
18 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
AVE-0847 DMRYK1C Hyperlipidaemia 5C80 Discontinued in Phase 2 [31]
GSK-677954 DM5WRJX Non-alcoholic fatty liver disease DB92 Discontinued in Phase 2 [32]
Indeglitazar DMS56UD Type-2 diabetes 5A11 Discontinued in Phase 2 [33]
KRP-297 DM9VHZC Type-2 diabetes 5A11 Discontinued in Phase 2 [34]
Reglixane DMIN73Y Diabetic complication 5A2Y Discontinued in Phase 2 [23]
Sodelglitazar DMJ816F Hyperlipidaemia 5C80 Discontinued in Phase 2 [35]
YM-440 DM7OHR6 Type-1 diabetes 5A10 Discontinued in Phase 2 [36]
DS-6930 DMDAO8E Diabetic complication 5A2Y Discontinued in Phase 1 [37]
E-3030 DMJWR1I Hyperlipidaemia 5C80 Discontinued in Phase 1 [38]
LY-929 DMVYG5X Lipid metabolism disorder 5C52.Z Discontinued in Phase 1 [39]
AD-5075 DM1SLJ9 Type-2 diabetes 5A11 Terminated [41]
AKP-320 DMMTZXV Type-2 diabetes 5A11 Terminated [42]
BVT-142 DMIYPLU Type-2 diabetes 5A11 Terminated [43]
CS-204 DM1E7H3 Metabolic disorder 5C50-5D2Z Terminated [44]
DARGLITAZONE DM6IGRL Diabetic complication 5A2Y Terminated [45]
Edaglitazone DMIC460 Type-2 diabetes 5A11 Terminated [46]
SB-219994 DMCZDE9 Diabetic complication 5A2Y Terminated [47]
Sipoglitazar DM5SBUJ Diabetic complication 5A2Y Terminated [15]
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⏷ Show the Full List of 18 Discontinued Drug(s)
2 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ciglitazone DMAPO0T Pulmonary fibrosis CB03.4 Preclinical [40]
MC-3002 DM7UGY9 Metabolic disorder 5C50-5D2Z Preclinical [23]
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12 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(2S)-2-(4-chlorophenoxy)-3-phenylpropanoic acid DMNKEUG Discovery agent N.A. Investigative [48]
(2S)-2-(4-ethylphenoxy)-3-phenylpropanoic acid DMYBXHF Discovery agent N.A. Investigative [48]
(2S)-2-(biphenyl-4-yloxy)-3-phenylpropanoic acid DM73TPQ Discovery agent N.A. Investigative [48]
(9Z,11E,13S)-13-hydroxyoctadeca-9,11-dienoic acid DM12GHQ Discovery agent N.A. Investigative [48]
15-deoxy-Delta(12, 14)-prostaglandin J(2) DM8VUX3 Discovery agent N.A. Investigative [4]
2-chloro-5-nitro-N-phenylbenzamide DMUGQIV Discovery agent N.A. Investigative [48]
3-(5-methoxy-1H-indol-3-yl)propanoic acid DMXLVG6 Discovery agent N.A. Investigative [48]
9-hydroxyoctadecadienoic acid DM0FWNJ Discovery agent N.A. Investigative [48]
DB-900 DMGRUN1 Type-2 diabetes 5A11 Investigative [49]
GW-2331 DMM8V9E Discovery agent N.A. Investigative [50]
GW7845 DMEK2I4 Discovery agent N.A. Investigative [51]
ZY H2 DMN9UCI Discovery agent N.A. Investigative [52]
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⏷ Show the Full List of 12 Investigative Drug(s)
Molecule Interaction Atlas

References

1 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.
2 Functional PPAR-gamma receptor is a novel therapeutic target for ACTH-secreting pituitary adenomas. Nat Med. 2002 Nov;8(11):1281-7.
3 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
4 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.
5 Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity. J Biol Chem. 2000 Jun 2;275(22):16638-42.
6 Balaglitazone: a second generation peroxisome proliferator-activated receptor (PPAR) gamma () agonist.Mini Rev Med Chem.2012 Feb;12(2):87-97.
7 Determination of chiglitazar, a dual alpha/gamma peroxisome proliferator-activated receptor (PPAR) agonist, in human plasma by liquid chromatograph... Pharmazie. 2007 Nov;62(11):825-9.
8 Rosiglitazone (BRL49653), a PPARgamma-selective agonist, causes peroxisome proliferator-like liver effects in obese mice. J Lipid Res. 1999 Jul;40(7):1177-84.
9 A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes. Eur J Pharmacol. 2004 Jul 8;495(1):17-26.
10 Clinical pipeline report, company report or official report of Minoryx Therapeutics
11 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.
12 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.
13 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.
14 Tesaglitazar, a dual PPAR-/ agonist, hamster carcinogenicity, investigative animal and clinical studies.Toxicol Pathol.2012;40(1):18-32.
15 Pharmacokinetics, safety, and tolerability of saroglitazar (ZYH1), a predominantly PPARalpha agonist with moderate PPARgamma agonist activity in healthy human subjects. Clin Drug Investig. 2013 Nov;33(11):809-16.
16 MBX-102/JNJ39659100, a novel peroxisome proliferator-activated receptor-ligand with weak transactivation activity retains antidiabetic properties in the absence of weight gain and edema. Mol Endocrinol. 2009 Jul;23(7):975-88.
17 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
18 FK-614, a selective peroxisome proliferator-activated receptor gamma agonist, improves peripheral glucose utilization while decreasing hepatic insulin extraction in alloxan-induced diabetic dogs. Metabolism. 2005 Sep;54(9):1250-8.
19 PPAR-gamma in ulcerative colitis: a novel target for intervention. Curr Drug Targets. 2013 Nov;14(12):1501-7.
20 The disposition and metabolism of naveglitazar, a peroxisome proliferator-activated receptor alpha-gamma dual, gamma-dominant agonist in mice, rats... Drug Metab Dispos. 2007 Jan;35(1):51-61.
21 Netoglitazone is a PPAR-gamma ligand with selective effects on bone and fat. Bone. 2006 Jan;38(1):74-84.
22 Clinical pipeline report, company report or official report of Avarx.
23 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
24 Phrma report (2013 Alzheimers disease)
25 A novel peroxisome proliferator-activated gamma (PPAR gamma) agonist, CLX-0921, has potent antihyperglycemic activity with low adipogenic potential. Metabolism. 2003 Aug;52(8):1012-8.
26 Effects of DSP-8658, a Novel Selective Peroxisome Proliferator-activated Receptors a/gamma Modulator, on Adipogenesis and Glucose Metabolism in Diabetic Obese Mice. Exp Clin Endocrinol Diabetes. 2015Sep;123(8):492-9.
27 PPARgamma agonists in the treatment of type II diabetes: is increased fatness commensurate with long-term efficacy. Int J Obes Relat Metab Disord. 2003 Feb;27(2):147-61.
28 Design novel dual agonists for treating type-2 diabetes by targeting peroxisome proliferator-activated receptors with core hopping approach. PLoS One. 2012;7(6):e38546.
29 Therapeutic potential of aleglitazar, a new dual PPAR-alpha/gamma agonist: implications for cardiovascular disease in patients with diabetes mellitus. Am J Cardiovasc Drugs. 2010;10(4):209-16.
30 PPAR ligands and their therapeutic applications: a patent review (2008 - 2014).Expert Opin Ther Pat. 2015 Feb;25(2):175-91.
31 DOI: 10.1038/scibx.2012.669
32 Emerging drugs for non-alcoholic fatty liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):145-58.
33 Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent. Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7.
34 KRP-297, MCC-555. Nihon Rinsho. 2001 Nov;59(11):2200-6.
35 Docking and molecular dynamics simulations of peroxisome proliferator activated receptors interacting with pan agonist sodelglitazar. Protein Pept Lett. 2011 Oct;18(10):1021-7.
36 The novel hypoglycemic agent YM440 improves hepatic insulin resistance in obese Zucker fatty rats. J Pharmacol Sci. 2006 Aug;101(4):311-7.
37 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036558)
38 Antidiabetic and hypolipidemic effects of a novel dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist, E3030, in db/db mice and beagle dogs.J Pharmacol Sci.2008 Sep;108(1):40-8.
39 CN patent application no. 1882326, Ppar agonists for the treatment of hcv infection.
40 New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202.
41 Thiazolidinediones produce a conformational change in peroxisomal proliferator-activated receptor-gamma: binding and activation correlate with antidiabetic actions in db/db mice. Endocrinology. 1996 Oct;137(10):4189-95.
42 Chronic glucose-lowering effects of rosiglitazone and bis(ethylmaltolato) oxovanadium(IV) in ZDF rats. Canadian Journal of Physiology and Pharmacology. 12/2003; 81(11):1049-55.
43 A new class of peroxisome proliferator-activated receptor agonists with a novel binding epitope shows antidiabetic effects. J Biol Chem. 2004 Sep 24;279(39):41124-30.
44 Peroxisome Proliferators-Activated Receptor (PPAR) Modulators and Metabolic Disorders. PPAR Res. 2008; 2008: 679137.
45 The PPAR-gamma agonist, darglitazone, restores acute inflammatory responses to cerebral hypoxia-ischemia in the diabetic ob/ob mouse. J Cereb Blood Flow Metab. 2010 February; 30(2): 352-360.
46 A specific peroxisome proliferator-activated receptor-gamma (PPAR-gamma) ligand, pioglitazone, ameliorates gastric mucosal damage induced by ischemia and reperfusion in rats. Redox Rep. 2002;7(5):343-6.
47 PPAR-gamma agonists as therapy for diseases involving airway neutrophilia. Eur Respir J. 2004 Jul;24(1):18-23.
48 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
49 CN patent application no. 102459215, 3-(4-aminophenyl)-2-furancarboxylic acid derivative and pharmaceutically acceptable salt thereof.
50 PPAR-alpha and -gamma but not -delta agonists inhibit airway inflammation in a murine model of asthma: in vitro evidence for an NF-kappaB-independe... Br J Pharmacol. 2003 May;139(1):163-71.
51 A new ligand for the peroxisome proliferator-activated receptor-gamma (PPAR-gamma), GW7845, inhibits rat mammary carcinogenesis. Cancer Res. 1999 Nov 15;59(22):5671-3.
52 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.