seladelpar   Click here for help

GtoPdb Ligand ID: 11137

Synonyms: compound 3r [PMID: 17524639] | MBX-8025 | MBX8025
Compound class: Synthetic organic
Comment: Seladelpar (MBX-8025) is a clinical stage, selective PPARδ agonist [3] that was initially developed as a therapy for atherogenic dyslipidemia and nonalcoholic steatohepatitis (NASH).
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 3
Hydrogen bond donors 1
Rotatable bonds 12
Topological polar surface area 90.29
Molecular weight 444.12
XLogP 5.14
No. Lipinski's rules broken 2
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Canonical SMILES CCO[C@H](COc1ccc(cc1)C(F)(F)F)CSc1ccc(c(c1)C)OCC(=O)O
Isomeric SMILES CCO[C@H](COc1ccc(cc1)C(F)(F)F)CSc1ccc(c(c1)C)OCC(=O)O
InChI InChI=1S/C21H23F3O5S/c1-3-27-17(11-28-16-6-4-15(5-7-16)21(22,23)24)13-30-18-8-9-19(14(2)10-18)29-12-20(25)26/h4-10,17H,3,11-13H2,1-2H3,(H,25,26)/t17-/m1/s1
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Summary of Clinical Use Click here for help
Phase 2 studies were suspended when histological tests detected signs of liver damage in some NASH trial subjects. However, other measures of liver injury (e.g. liver enzyme levels) did not point to liver damage. Following a review, and lifting of the FDA's clinical hold for all three seladelpar indications, the drug's developer (CymaBay) have made the decision to re-initiate studies (as of July 2020), beginning with primary biliary cholangitis (PBC).
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT02609048 Study to Evaluate the Effects of Two Doses of MBX-8025 in Subjects With Primary Biliary Cirrhosis (PBC) Phase 2 Interventional CymaBay Therapeutics, Inc. 2
NCT00701883 Safety and Benefit of MBX-8025 With and Without Commonly Used Statins in Moderately Overweight Patients With High Cholesterol Phase 2 Interventional CymaBay Therapeutics, Inc. 1
NCT03301506 Seladelpar in Subjects With Primary Biliary Cholangitis (PBC) Phase 2/Phase 3 Interventional CymaBay Therapeutics, Inc.