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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

Molecular Formula C22H24O4S
Molecular Weight 384.489
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 1
Optical Activity NONE

Description

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.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
45.0 nM [EC50]
175.0 nM [EC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
385.216 ng/mL
80 mg 1 times / day multiple, oral
ELAFIBRANOR plasma
Homo sapiens
658.054 ng/mL
120 mg 1 times / day multiple, oral
ELAFIBRANOR plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
973.301 ng × h/mL
80 mg 1 times / day multiple, oral
ELAFIBRANOR plasma
Homo sapiens
1457.728 ng × h/mL
120 mg 1 times / day multiple, oral
ELAFIBRANOR plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
34.17 h
80 mg 1 times / day multiple, oral
ELAFIBRANOR plasma
Homo sapiens
37.62 h
120 mg 1 times / day multiple, oral
ELAFIBRANOR plasma
Homo sapiens

Doses

AEs

PubMed

Sample Use Guides

In Vivo Use Guide
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
In Vitro Use Guide
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).
Substance Class Chemical
Record UNII
2J3H5C81A5
Record Status Validated (UNII)
Record Version