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

General Information of Drug (ID: DM7ZOAE)

• Drug Name: GFT-505 Drug Info
• Synonyms: GFT-1007; PPAR activator (dyslipidemia/type 2 diabetes), Genfit

Indication

Disease Entry	ICD 11	Status	REF
Non-alcoholic steatohepatitis	DB92.1	Phase 3	[1]
Type-2 diabetes	5A11	Phase 2	[2]

• Cross-matching ID:
  PubChem CID: 9864881
  CAS Number: CAS 923978-27-2
  TTD Drug ID: DM7ZOAE

Molecule-Related Drug Atlas

Drug(s) Targeting Peroxisome proliferator-activated receptor delta (PPARD)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MBX-8025	DMNTCV4	Obesity	5B81	Phase 2/3	[4]
T3D-959	DMR3245	Alzheimer disease	8A20	Phase 2	[5]
T3D-959	DMR3245	Alzheimer disease	8A20	Phase 2	[6]
KD3010	DMNFDYE	Metabolic disorder	5C50-5D2Z	Phase 1	[7]
SAR351034	DM15PG9	Dyslipidemia	5C80-5C81	Phase 1	[8]
CER-002	DMLBKZV	Dyslipidemia	5C80-5C81	Phase 1	[9]
PMID25416646-Compound-Figure5-C	DM17FKL	N. A.	N. A.	Patented	[10]
GW-501516	DMPL2KM	Type-1 diabetes	5A10	Discontinued in Phase 4	[11]
Sodelglitazar	DMJ816F	Hyperlipidaemia	5C80	Discontinued in Phase 2	[12]
Indeglitazar	DMS56UD	Type-2 diabetes	5A11	Discontinued in Phase 2	[13]

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	[14]
Fenofibrate	DMFKXDY	Coronary atherosclerosis		Approved	[15]
Bezafibrate	DMZDCS0	Hypercholesterolaemia	5C80.0	Approved	[16]
Ciprofibrate	DMGC5DB	Hyperlipoproteinemia	5C80	Approved	[15]
Pemafibrate	DMD1VZL	Hyperlipidemia	5C80.Z	Approved	[17]
MURAGLITAZAR	DMG3NFZ	N. A.	N. A.	Phase 3	[18]
Ragaglitazar	DMFSHEM	Type-1 diabetes	5A10	Phase 3	[19]
CS-038	DM67P0F	Type-2 diabetes	5A11	Phase 3	[20]
TESAGLITAZAR	DMGRBN5	Type-1 diabetes	5A10	Phase 3	[21]
ZYH-1	DMMBJYC	Lipid metabolism disorder	5C52.Z	Phase 3	[22]

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	[3]
Peroxisome proliferator-activated receptor delta (PPARD)	TT2JWF6	PPARD_HUMAN	Modulator	[3]

References

• [1] ClinicalTrials.gov (NCT02704403) Phase 3 Study to Evaluate the Efficacy and Safety of Elafibranor Versus Placebo in Patients With Nonalcoholic Steatohepatitis (NASH) (RESOLVE-IT). U.S. National Institutes of Health.
• [2] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025107)
• [3] 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.
• [4] ClinicalTrials.gov (NCT00701883) Safety and Benefit of MBX-8025 With and Without Commonly Used Statins in Moderately Overweight Patients With High Cholesterol. U. S. National Institute of Health. 2008.
• [5] Phrma report (2013 Alzheimers disease)
• [6] T3D-959: A Multi-Faceted Disease Remedial Drug Candidate for the Treatment of Alzheimer's Disease. J Alzheimers Dis. 2016;51(1):123-38.
• [7] Kalypsys nearing completion of phase Ia study of KD3010 for metabolic disorders. Kalypsys. 2007.
• [8] Addressing Unmet Medical Needs in Type 2 Diabetes: A Narrative Review of Drugs under Development. Curr Diabetes Rev. 2015 March; 11(1): 17-31.
• [9] Fibrates, glitazones, and peroxisome proliferator-activated receptors. Arterioscler Thromb Vasc Biol. 2010 May; 30(5): 894-899.
• [10] PPAR ligands and their therapeutic applications: a patent review (2008 - 2014).Expert Opin Ther Pat. 2015 Feb;25(2):175-91.
• [11] Lipid effects of peroxisome proliferator-activated receptor- agonist GW501516 in subjects with low high-density lipoprotein cholesterol: characteristics of metabolic syndrome.Arterioscler Thromb Vasc Biol.2012 Sep;32(9):2289-94.
• [12] Docking and molecular dynamics simulations of peroxisome proliferator activated receptors interacting with pan agonist sodelglitazar. Protein Pept Lett. 2011 Oct;18(10):1021-7.
• [13] 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.
• [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] Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity. J Biol Chem. 2000 Jun 2;275(22):16638-42.
• [16] 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.
• [17] Pemafibrate: First Global Approval. Drugs. 2017 Oct;77(16):1805-1810.
• [18] 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.
• [19] 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.
• [20] 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.
• [21] Tesaglitazar, a dual PPAR-/ agonist, hamster carcinogenicity, investigative animal and clinical studies.Toxicol Pathol.2012;40(1):18-32.
• [22] 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.