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Details

Stereochemistry ACHIRAL
Molecular Formula C22H24O4S
Molecular Weight 384.489
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of ELAFIBRANOR

SMILES

CSC1=CC=C(C=C1)C(=O)\C=C\C2=CC(C)=C(OC(C)(C)C(O)=O)C(C)=C2

InChI

InChIKey=AFLFKFHDSCQHOL-IZZDOVSWSA-N
InChI=1S/C22H24O4S/c1-14-12-16(13-15(2)20(14)26-22(3,4)21(24)25)6-11-19(23)17-7-9-18(27-5)10-8-17/h6-13H,1-5H3,(H,24,25)/b11-6+

HIDE SMILES / InChI
Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α and peroxisome proliferator-activated receptor-δ. GFT505 has an active metabolite, GFT1007, and both have potent agonist activity for PPAR-a and to a lesser extent for PPAR-d. Elafibranor improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation. Elafibranor (GFT505) reverses nonalcoholic steatohepatitis (NASH) to prevent fibrosis progression. With an outstanding safety and tolerance profile, elafibranor provides NASH patients with needed cardio-protective benefits. Elafibranor is currently being evaluated in the clinical Phase 3 study RESOLVE-IT. The safety profile of GFT505 from the completed clinical trials appears satisfactory with no indication of PPAR-g agonist effects such as edema or body weight gain.

Approval Year

Doses

Doses

DosePopulationAdverse events​
120 mg 1 times / day multiple, oral
Highest studied dose
Dose: 120 mg, 1 times / day
Route: oral
Route: multiple
Dose: 120 mg, 1 times / day
Sources: Page: p.1155
unhealthy, ADULT
n = 89
Health Status: unhealthy
Condition: non-alcoholic steatohepatitis
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 89
Sources: Page: p.1155
Other AEs: Renal impairment, Renal failure unspecified...
Other AEs:
Renal impairment (2.25%)
Renal failure unspecified (4.49%)
Sources: Page: p.1155
AEs

AEs

AESignificanceDosePopulation
Renal impairment 2.25%
120 mg 1 times / day multiple, oral
Highest studied dose
Dose: 120 mg, 1 times / day
Route: oral
Route: multiple
Dose: 120 mg, 1 times / day
Sources: Page: p.1155
unhealthy, ADULT
n = 89
Health Status: unhealthy
Condition: non-alcoholic steatohepatitis
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 89
Sources: Page: p.1155
Renal failure unspecified 4.49%
120 mg 1 times / day multiple, oral
Highest studied dose
Dose: 120 mg, 1 times / day
Route: oral
Route: multiple
Dose: 120 mg, 1 times / day
Sources: Page: p.1155
unhealthy, ADULT
n = 89
Health Status: unhealthy
Condition: non-alcoholic steatohepatitis
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 89
Sources: Page: p.1155
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Activation of intestinal peroxisome proliferator-activated receptor-α increases high-density lipoprotein production.
2013 Aug
Early investigational drugs targeting PPAR-α for the treatment of metabolic disease.
2015 May
Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening.
2016 May
Patents

Sample Use Guides

Nonalcoholic Steatohepatitis (NASH) With Fibrosis :Coated tablets dosed at 120mg Elafibranor; oral administration; one tablet per day before breakfast with a glass of water.
Route of Administration: Oral
Human jejunal biopsies were treated with Elafibranor (1uM) for 18h. Elafibranor (1uM) increased mRNA levels of fatty-acid-oxidation genes including Carnitine-Palmitoyl-Transferase-1 (CPT-1A), ACOX1 and long-chain Acyl-CoA synthetase family member 5 (ACSL5).
Name Type Language
ELAFIBRANOR
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
Elafibranor [WHO-DD]
Common Name English
elafibranor [INN]
Common Name English
ELAFIBRANOR [USAN]
Common Name English
GFT505
Code English
PROPANOIC ACID, 2-(2,6-DIMETHYL-4-((1E)-3-(4-(METHYLTHIO)PHENYL)-3-OXO-1-PROPEN-1-YL)PHENOXY)-
Systematic Name English
PROPANOIC ACID, 2-(2,6-DIMETHYL-4-(3-(4-(METHYLTHIO)PHENYL)-3-OXO-1-PROPEN-1-YL)PHENOXY)-2-METHYL-
Systematic Name English
GFT-505
Code English
Classification Tree Code System Code
FDA ORPHAN DRUG 693919
Created by admin on Fri Dec 15 16:42:44 GMT 2023 , Edited by admin on Fri Dec 15 16:42:44 GMT 2023
Code System Code Type Description
USAN
CD-135
Created by admin on Fri Dec 15 16:42:44 GMT 2023 , Edited by admin on Fri Dec 15 16:42:44 GMT 2023
PRIMARY
DRUG BANK
DB05187
Created by admin on Fri Dec 15 16:42:44 GMT 2023 , Edited by admin on Fri Dec 15 16:42:44 GMT 2023
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NCI_THESAURUS
C166574
Created by admin on Fri Dec 15 16:42:44 GMT 2023 , Edited by admin on Fri Dec 15 16:42:44 GMT 2023
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CAS
923978-27-2
Created by admin on Fri Dec 15 16:42:44 GMT 2023 , Edited by admin on Fri Dec 15 16:42:44 GMT 2023
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ChEMBL
CHEMBL3707395
Created by admin on Fri Dec 15 16:42:44 GMT 2023 , Edited by admin on Fri Dec 15 16:42:44 GMT 2023
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CAS
824932-88-9
Created by admin on Fri Dec 15 16:42:44 GMT 2023 , Edited by admin on Fri Dec 15 16:42:44 GMT 2023
NON-SPECIFIC STEREOCHEMISTRY
SMS_ID
100000174091
Created by admin on Fri Dec 15 16:42:44 GMT 2023 , Edited by admin on Fri Dec 15 16:42:44 GMT 2023
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PUBCHEM
9864881
Created by admin on Fri Dec 15 16:42:44 GMT 2023 , Edited by admin on Fri Dec 15 16:42:44 GMT 2023
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FDA UNII
2J3H5C81A5
Created by admin on Fri Dec 15 16:42:44 GMT 2023 , Edited by admin on Fri Dec 15 16:42:44 GMT 2023
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WIKIPEDIA
Elafibranor
Created by admin on Fri Dec 15 16:42:44 GMT 2023 , Edited by admin on Fri Dec 15 16:42:44 GMT 2023
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EPA CompTox
DTXSID601045330
Created by admin on Fri Dec 15 16:42:44 GMT 2023 , Edited by admin on Fri Dec 15 16:42:44 GMT 2023
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INN
9973
Created by admin on Fri Dec 15 16:42:44 GMT 2023 , Edited by admin on Fri Dec 15 16:42:44 GMT 2023
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