elafibranor   Click here for help

GtoPdb Ligand ID: 11135

Synonyms: GFT-505 | GFT505
PDB Ligand
Compound class: Synthetic organic
Comment: Elafibranor (GFT-505) is a PPARα/δ agonist. It was taken into clinical development by Genfit, as a therapuetic for nonalcoholic steatohepatitis (NASH) [3]. Genfit terminated development at Phase 3 in mid-2020 following futility analysis. Dual PPARα/δ agonists are also referred to as 'glitazars'.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
2D Structure
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2D Structure

An image of the ligand's 2D structure. For small molecules with SMILES these are drawn using the NCI/CADD Chemical Identifier Resolver. Click on the image to access the chemical structure search tool with the ligand pre-loaded in the structure editor. For other types of ligands, e.g. longer nucleotides and peptides, a manually drawn representation of the molecule may be provided.

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Physico-chemical Properties
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Physico-chemical Properties

Calculated molecular properties are available for small molecules and natural products (not peptides). Properties were generated using the CDK toolkit. All properties were selected to enable the prediction of the Lipinski Rule-of-Five profile or ‘druglikeness’ for each ligand. For more info on each category see the help pages.

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Hydrogen bond acceptors 3
Hydrogen bond donors 1
Rotatable bonds 7
Topological polar surface area 88.9
Molecular weight 384.14
XLogP 4.97
No. Lipinski's rules broken 0
SMILES / InChI / InChIKey
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SMILES / InChI / InChIKey

SMILES (Simplified Molecular Input Line Entry Specification) A specification for unambiguously describing the structure of chemical molecules using short ASCII strings. Canonical SMILES specify a unique representation of the 2D structure without chiral or isotopic specifications. Isomeric SMILES include chiral specification and isotopes.

Standard InChI (IUPAC International Chemical Identifier) and InChIKey InChI is a non-proprietary, standard, textual identifier for chemical substances designed to facilitate linking of information and database searching. An InChIKey is a simplified version of a full InChI, designed for easier web searching.

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Canonical SMILES CSc1ccc(cc1)C(=O)/C=C/c1cc(C)c(c(c1)C)OC(C(=O)O)(C)C
Isomeric SMILES CSc1ccc(cc1)C(=O)/C=C/c1cc(C)c(c(c1)C)OC(C(=O)O)(C)C
InChI 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+
InChI Key AFLFKFHDSCQHOL-IZZDOVSWSA-N
No information available.
Summary of Clinical Use Click here for help
Phase 1/2 trials confirmed the potential efficacy of elafibranor, and specific adverse safety signals were not detected in these studies [1-2]. However, interim analysis of Phase 3 trial data, concluded that elafibranor was not better than placebo at improving NASH symptoms without worsening fibrosis.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT01261494 Study With GFT505 (80mg) Versus Placebo in Patients With Type 2 Diabetes Mellitus Phase 2 Interventional Genfit
NCT00001693 Phase I-II Multiple-Dose Safety and Efficacy Study of a Selective Inhibitor of Cyclooxygenase - 2 (SC-58635) in Hereditary Non-Polyposis Colorectal Cancer (HNPCC) Patients and Carriers Phase 1 Interventional National Institutes of Health Clinical Center (CC) 2
NCT01271751 Pilot Study With GFT505 (80mg) in Atherogenic Dyslipidaemic Patients With Abdominal Obesity Phase 2 Interventional Genfit 2
NCT02704403 Phase 3 Study to Evaluate the Efficacy and Safety of Elafibranor Versus Placebo in Patients With Nonalcoholic Steatohepatitis (NASH) Phase 3 Interventional Genfit As of July 2020 this trial was being closed down, as the drug was unlikely to show efficacy.