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

General Information of Drug (ID: DM1SLJ9)

• Drug Name: AD-5075 Drug Info
• Synonyms: 2,4-Thiazolidinedione, 5-((4-(2-hydroxy-2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy)phenyl)methyl)-; AD 5075; 103788-05-2; 5-[[4-[2-hydroxy-2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione; 2,4-Thiazolidinedione,5-[[4-[2-hydroxy-2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]-; YVQKIDLSVHRBGZ-UHFFFAOYSA-N; [3H]AD5075; [3H]-AD5075; ACMC-20m6lh; AC1L2TSO; CHEMBL88496; SCHEMBL131888; GTPL2702; GTPL2701; CTK4A2384; AD5075; 5-(4-(2-(5-Methyl-2-phenyl-4-oxazolyl)-2-hydroxyethoxy)benzyl)-2,4-thiazolidinedione; [3H]AD-5075

Indication

Disease Entry	ICD 11	Status	REF
Type-2 diabetes	5A11	Terminated	[1]

• Cross-matching ID:
  PubChem CID: 128440
  CAS Number: CAS 103788-05-2
  TTD Drug ID: DM1SLJ9

Molecule-Related Drug Atlas

Drug(s) Targeting PPAR-gamma messenger RNA (PPARG mRNA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Bardoxolone methyl	DMODA2X	Mixed connective tissue disease	4A43.3	Phase 3	[3]
2-chloro-5-nitro-N-phenylbenzamide	DMUGQIV	Discovery agent	N.A.	Investigative	[4]
L-783483	DM6OTGE	Discovery agent	N.A.	Investigative	[5]
LG100754	DMEK4FY	Discovery agent	N.A.	Investigative	[6]
L-796449	DMWTGQM	Discovery agent	N.A.	Investigative	[7]
L-165461	DMKBSGN	Discovery agent	N.A.	Investigative	[7]
AD-5061	DM5WV13	Discovery agent	N.A.	Investigative	[8]
TZD18	DMVCHOX	Discovery agent	N.A.	Investigative	[9]
(9Z,12E)-12-nitrooctadeca-9,12-dienoic acid	DM2REIN	Discovery agent	N.A.	Investigative	[10]
reglitazar	DMQ3ER0	Discovery agent	N.A.	Investigative	[11]

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	[12]
Pioglitazone	DMKJ485	Amyotrophic lateral sclerosis	8B60.0	Approved	[13]
Lobeglitazone	DMHY3IP	Type-2 diabetes	5A11	Approved	[14]
Rosiglitazone XR	DMT45MU	Type-2 diabetes	5A11	Approved	[15]
Thiazolidinedione	DMC1NBW	Alzheimer disease	8A20	Approved	[13]
Glitazone	DMDN4A1	N. A.	N. A.	Phase 4	[16]
MURAGLITAZAR	DMG3NFZ	N. A.	N. A.	Phase 3	[17]
Rivoglitazone	DMBY31K	Ocular inflammation	9C61.24	Phase 3	[18]
Balaglitazone	DMXBHR6	Type-1 diabetes	5A10	Phase 3	[19]
Ragaglitazar	DMFSHEM	Type-1 diabetes	5A10	Phase 3	[20]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Peroxisome proliferator-activated receptor gamma (PPAR-gamma)	TTZMAO3	PPARG_HUMAN	Modulator	[2]
PPAR-gamma messenger RNA (PPARG mRNA)	TTT2SVW	PPARG_HUMAN	Agonist	[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: 2701).
• [2] 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.
• [3] A synthetic triterpenoid, 2-cyano-3,12-dioxooleana-1,9-dien-28-oic acid (CDDO), is a ligand for the peroxisome proliferator-activated receptor gamma. Mol Endocrinol. 2000 Oct;14(10):1550-6.
• [4] Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling. Eur J Med Chem. 2008 Dec;43(12):2699-716.
• [5] Novel peroxisome proliferator-activated receptor (PPAR) gamma and PPARdelta ligands produce distinct biological effects. J Biol Chem. 1999 Mar 5;274(10):6718-25.
• [6] The antidiabetic agent LG100754 sensitizes cells to low concentrations of peroxisome proliferator-activated receptor gamma ligands. J Biol Chem. 2002 Apr 12;277(15):12503-6.
• [7] Phenylacetic acid derivatives as hPPAR agonists. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1277-80.
• [8] A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes. Eur J Pharmacol. 2004 Jul 8;495(1):17-26.
• [9] A novel peroxisome proliferator-activated receptor alpha/gamma dual agonist demonstrates favorable effects on lipid homeostasis. Endocrinology. 2004 Apr;145(4):1640-8.
• [10] Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree ... J Med Chem. 2009 Aug 13;52(15):4631-9.
• [11] Pharmacological profiles of a novel oral antidiabetic agent, JTT-501, an isoxazolidinedione derivative. Eur J Pharmacol. 1999 Jan 8;364(2-3):211-9.
• [12] 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.
• [13] Functional PPAR-gamma receptor is a novel therapeutic target for ACTH-secreting pituitary adenomas. Nat Med. 2002 Nov;8(11):1281-7.
• [14] 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.
• [15] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [16] Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity. J Biol Chem. 2000 Jun 2;275(22):16638-42.
• [17] 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.
• [18] 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.
• [19] Balaglitazone: a second generation peroxisome proliferator-activated receptor (PPAR) gamma () agonist.Mini Rev Med Chem.2012 Feb;12(2):87-97.
• [20] 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.