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

General Information of Drug (ID: DMOE5SZ)

• Drug Name: GW-409544 Drug Info
• Synonyms: GW-409544X; GW-544; GW-6471; Lipid regulators, Ligand/Glaxo

Indication

Disease Entry	ICD 11	Status	REF
Hyperlipidaemia	5C80	Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 446642
  ChEBI ID: CHEBI:79990
  CAS Number: CAS 258345-41-4
  TTD Drug ID: DMOE5SZ

Molecule-Related Drug Atlas

Drug(s) Targeting Peroxisome proliferator-activated receptor gamma (PPAR-gamma)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[3]
Pioglitazone	DMKJ485	Amyotrophic lateral sclerosis	8B60.0	Approved	[4]
Lobeglitazone	DMHY3IP	Type-2 diabetes	5A11	Approved	[5]
Rosiglitazone XR	DMT45MU	Type-2 diabetes	5A11	Approved	[6]
Thiazolidinedione	DMC1NBW	Alzheimer disease	8A20	Approved	[4]
Glitazone	DMDN4A1	N. A.	N. A.	Phase 4	[7]
MURAGLITAZAR	DMG3NFZ	N. A.	N. A.	Phase 3	[8]
Rivoglitazone	DMBY31K	Ocular inflammation	9C61.24	Phase 3	[9]
Balaglitazone	DMXBHR6	Type-1 diabetes	5A10	Phase 3	[10]
Ragaglitazar	DMFSHEM	Type-1 diabetes	5A10	Phase 3	[11]

Drug(s) Targeting Peroxisome proliferator-activated receptor alpha (PPARA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lobeglitazone	DMHY3IP	Type-2 diabetes	5A11	Approved	[5]
Fenofibrate	DMFKXDY	Coronary atherosclerosis		Approved	[7]
Bezafibrate	DMZDCS0	Hypercholesterolaemia	5C80.0	Approved	[12]
Ciprofibrate	DMGC5DB	Hyperlipoproteinemia	5C80	Approved	[7]
Pemafibrate	DMD1VZL	Hyperlipidemia	5C80.Z	Approved	[13]
MURAGLITAZAR	DMG3NFZ	N. A.	N. A.	Phase 3	[8]
Ragaglitazar	DMFSHEM	Type-1 diabetes	5A10	Phase 3	[11]
CS-038	DM67P0F	Type-2 diabetes	5A11	Phase 3	[14]
TESAGLITAZAR	DMGRBN5	Type-1 diabetes	5A10	Phase 3	[15]
GFT-505	DM7ZOAE	Non-alcoholic steatohepatitis	DB92.1	Phase 3	[16]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Peroxisome proliferator-activated receptor alpha (PPARA)	TTJ584C	PPARA_HUMAN	Modulator	[2]
Peroxisome proliferator-activated receptor gamma (PPAR-gamma)	TTZMAO3	PPARG_HUMAN	Modulator	[2]

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: 3440).
• [2] 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.
• [3] 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.
• [4] Functional PPAR-gamma receptor is a novel therapeutic target for ACTH-secreting pituitary adenomas. Nat Med. 2002 Nov;8(11):1281-7.
• [5] 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.
• [6] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [7] Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity. J Biol Chem. 2000 Jun 2;275(22):16638-42.
• [8] 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.
• [9] 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.
• [10] Balaglitazone: a second generation peroxisome proliferator-activated receptor (PPAR) gamma () agonist.Mini Rev Med Chem.2012 Feb;12(2):87-97.
• [11] 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.
• [12] Bezafibrate at clinically relevant doses decreases serum/liver triglycerides via down-regulation of sterol regulatory element-binding protein-1c in... Mol Pharmacol. 2009 Apr;75(4):782-92.
• [13] Pemafibrate: First Global Approval. Drugs. 2017 Oct;77(16):1805-1810.
• [14] 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.
• [15] Tesaglitazar, a dual PPAR-/ agonist, hamster carcinogenicity, investigative animal and clinical studies.Toxicol Pathol.2012;40(1):18-32.
• [16] Dual peroxisome proliferator-activated receptor / agonist GFT505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects.Diabetes Care.2013 Oct;36(10):2923-30.