◎ Sugi Atlas

Atlas / Drug / Seladelpar

Seladelpar

drug
On this page

Also known as (+)-MBX-8025Mbx-8025RWJ-800025SELADELPAR LYSINE

Summary

Seladelpar (CHEMBL230158) is an approved small molecule (ATC A05AX07) targeting PPARA, PPARD, and PPARG; indicated across 6 conditions including primary biliary cholangitis and sclerosing cholangitis.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: A05AX07
  • Targets: 3 (PPARA, PPARD, PPARG)
  • Indications: 6 conditions
  • Clinical trials: 11
  • Chemistry: 444.5 Da · C21H23F3O5S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL230158
NameSeladelpar
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID11236126
ATCA05AX07
Molecular formulaC21H23F3O5S
Molecular weight444.5
InChIKeyJWHYSEDOYMYMNM-QGZVFWFLSA-N

SMILES: CCO[C@H](COC1=CC=C(C=C1)C(F)(F)F)CSC2=CC(=C(C=C2)OCC(=O)O)C

IUPAC name: 2-[4-[(2R)-2-ethoxy-3-[4-(trifluoromethyl)phenoxy]propyl]sulfanyl-2-methylphenoxy]acetic acid

Also known as: (+)-MBX-8025, Mbx-8025, MBX-8025, RWJ-800025, Seladelpar, SELADELPAR, SELADELPAR LYSINE

Parent form; salt/anhydrous children: CHEMBL3989960, CHEMBL5303479

Patent coverage: 241 distinct patent families (854 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 615 (72%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
PPARAPeroxisome proliferator-activated receptor-αAgonist60.7%Q07869
PPARDPeroxisome proliferator-activated receptor-β/δAgonist8.720.6%Q03181
PPARGPeroxisome proliferator-activated receptor-γAgonist62.6%P37231

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Peroxisome proliferator-activated receptor alpha, Peroxisome proliferator-activated receptor delta.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PPARD8.72EC501.9nMCHEMBL_ACT_1900874
PPARD8.7EC502nMCHEMBL_ACT_19005348
PPARD8.7EC502nMCHEMBL_ACT_25110730
PPARA5.82EC501500nMCHEMBL_ACT_19005346

Target pathways

Aggregated over 3 target gene(s): PPARA, PPARD, PPARG.

Top Reactome pathways

18 total, by targets touching each:

PathwayTargetsGenes
Nuclear Receptor transcription pathway3PPARA, PPARD, PPARG
PPARA activates gene expression2PPARA, PPARG
Transcriptional regulation of white adipocyte differentiation2PPARA, PPARG
SUMOylation of intracellular receptors2PPARA, PPARG
Transcriptional regulation of brown and beige adipocyte differentiation by EBF22PPARA, PPARG
BMAL1:CLOCK,NPAS2 activates circadian expression1PPARA
Carnitine shuttle1PPARD
Transcriptional activation of mitochondrial biogenesis1PPARA
Activation of gene expression by SREBF (SREBP)1PPARA
Regulation of lipid metabolism by PPARalpha1PPARA
Signaling by Retinoic Acid1PPARD
Regulation of PTEN gene transcription1PPARG
MECP2 regulates transcription factors1PPARG
Cytoprotection by HMOX11PPARA
Heme signaling1PPARA
MLL4 and MLL3 complexes regulate expression of PPARG target genes in adipogenesis and hepatic steatosis1PPARG
Expression of BMAL (ARNTL), CLOCK, and NPAS21PPARA
RORA,B,C and NR1D1 (REV-ERBA) regulate gene expression1PPARA

Dominant GO biological processes

GO termTargets
negative regulation of transcription by RNA polymerase II3
fatty acid metabolic process3
heart development3
hormone-mediated signaling pathway3
negative regulation of cholesterol storage3
cell differentiation3
intracellular receptor signaling pathway3
positive regulation of DNA-templated transcription3
positive regulation of fatty acid metabolic process3
positive regulation of transcription by RNA polymerase II3
positive regulation of fatty acid oxidation3
negative regulation of inflammatory response3
negative regulation of miRNA transcription3
regulation of DNA-templated transcription3
response to nutrient2

Indications & clinical

Indications

6 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
primary biliary cholangitis3MONDO:0005388EFO:1001486
sclerosing cholangitis2MONDO:0018646EFO:0004268
metabolic dysfunction-associated steatohepatitis2MONDO:0007027EFO:1001249
hyperlipidemia2MONDO:0021187MONDO:0021187
liver disorder1MONDO:0005154EFO:0001421

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 11.

Phase distribution

PhaseTrials
PHASE25
PHASE34
PHASE12

Top trials by phase / activity

NCTPhaseStatusTitle
NCT06051617PHASE3RECRUITINGSeladelpar in Subjects With Primary Biliary Cholangitis (PBC) and Compensated Cirrhosis
NCT06060665PHASE3ACTIVE_NOT_RECRUITINGIntended to Determine the Effects of Seladelpar on Normalization of Alkaline Phosphatase Levels in Subjects With Primary Biliary Cholangitis (PBC)
NCT03602560PHASE3COMPLETEDENHANCE: Seladelpar in Subjects With Primary Biliary Cholangitis (PBC) and an Inadequate Response to or an Intolerance to Ursodeoxycholic Acid (UDCA)
NCT04620733PHASE3COMPLETEDRESPONSE: Response to Seladelpar in Subjects With Primary Biliary Cholangitis (PBC) and an Inadequate Control to or an Intolerance to Ursodeoxycholic Acid (UDCA)
NCT07305363PHASE2NOT_YET_RECRUITINGSeladelpar in Adult Liver Transplant Recipients With Ischemic Cholangiopathy (SELIC).
NCT00701883PHASE2COMPLETEDSafety and Benefit of MBX-8025 With and Without Commonly Used Statins in Moderately Overweight Patients With High Cholesterol
NCT02609048PHASE2TERMINATEDStudy to Evaluate the Effects of Two Doses of Seladelpar (MBX-8025) in Subjects With Primary Biliary Cirrhosis (PBC)
NCT03551522PHASE2TERMINATEDA Study to Evaluate Seladelpar in Subjects With Nonalcoholic Steatohepatitis (NASH)
NCT04024813PHASE2TERMINATEDA Study to Evaluate the Safety, and Tolerability, and Efficacy of Seladelpar in Patients With PSC
NCT03369002PHASE1COMPLETEDStudy to Evaluate the Pharmacokinetics, Safety, and Tolerability of Seladelpar in Subjects With Hepatic Impairment and Healthy Subjects
NCT04950764PHASE1COMPLETEDAn Open-Label Study Following Oral Dosing of Seladelpar to Participants With Primary Biliary Cholangitis (PBC) and Hepatic Impairment (HI)

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

93 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
ELAFIBRANORChEMBLPhase 4 (approved)PPARA, PPARD, PPARG
PEMAFIBRATEChEMBLPhase 4 (approved)PPARA, PPARD, PPARG
PIOGLITAZONEChEMBLPhase 4 (approved)PPARA, PPARD, PPARG
ROSIGLITAZONEChEMBLPhase 4 (approved)PPARA, PPARD, PPARG
ALEGLITAZARChEMBLPhase 3PPARA, PPARD, PPARG
BEZAFIBRATEChEMBLPhase 3PPARA, PPARD, PPARG
GAMOLENIC ACIDChEMBLPhase 3PPARA, PPARD, PPARG
ICOSAPENTChEMBLPhase 3PPARA, PPARD, PPARG
LANIFIBRANORChEMBLPhase 3PPARA, PPARD, PPARG
DIHOMO-GAMMA-LINOLENIC ACIDChEMBLPhase 2PPARA, PPARD, PPARG
FARGLITAZARChEMBLPhase 2PPARA, PPARD, PPARG
GW501516ChEMBLPhase 2PPARA, PPARD, PPARG
GW590735ChEMBLPhase 2PPARA, PPARD, PPARG
INDEGLITAZARChEMBLPhase 2PPARA, PPARD, PPARG
LINOLEIC ACIDChEMBLPhase 2PPARA, PPARD, PPARG
LY-518674ChEMBLPhase 2PPARA, PPARD, PPARG
NAVEGLITAZARChEMBLPhase 2PPARA, PPARD, PPARG
OLEIC ACIDChEMBLPhase 2PPARA, PPARD, PPARG
PIRINIXIC ACIDChEMBLPhase 2PPARA, PPARD, PPARG
BERBERINEChEMBLPhase 4 (approved)PPARA, PPARD
FENOFIBRATEChEMBLPhase 4 (approved)PPARA, PPARG
FENOFIBRIC ACIDChEMBLPhase 4 (approved)PPARA, PPARG
GEMFIBROZILChEMBLPhase 4 (approved)PPARA, PPARG
IMIGLITAZARChEMBLPhase 3PPARA, PPARG
LOBEGLITAZONEChEMBLPhase 3PPARA, PPARG
MURAGLITAZARChEMBLPhase 3PPARA, PPARG
NAMODENOSONChEMBLPhase 3PPARD, PPARG
TESAGLITAZARChEMBLPhase 3PPARA, PPARG
RAGAGLITAZARChEMBLPhase 2PPARA, PPARG
REGLITAZARChEMBLPhase 2PPARA, PPARG
FULVESTRANTChEMBL + PubChemPhase 4 (approved)PPARG
BENZBROMARONEChEMBLPhase 4 (approved)PPARG
BEXAROTENEChEMBLPhase 4 (approved)PPARG
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)PPARG
CANNABIDIOLChEMBLPhase 4 (approved)PPARG
CARVEDILOLChEMBLPhase 4 (approved)PPARG
CEFAMANDOLEChEMBLPhase 4 (approved)PPARG
CEFOTAXIMEChEMBLPhase 4 (approved)PPARG
CEFOXITINChEMBLPhase 4 (approved)PPARG
CEFTAZIDIMEChEMBLPhase 4 (approved)PPARG
CEFTRIAXONEChEMBLPhase 4 (approved)PPARG
CIPROFIBRATEChEMBLPhase 4 (approved)PPARA
CLOBETASOL PROPIONATEChEMBLPhase 4 (approved)PPARG
CLOFIBRATEChEMBLPhase 4 (approved)PPARA
CYCLOSPORINEChEMBLPhase 4 (approved)PPARA
EFAVIRENZChEMBLPhase 4 (approved)PPARG
GLYBURIDEChEMBLPhase 4 (approved)PPARG
INDOMETHACINChEMBLPhase 4 (approved)PPARG
LASOFOXIFENEChEMBLPhase 4 (approved)PPARG
LEVOTHYROXINEChEMBLPhase 4 (approved)PPARG
LIOTHYRONINEChEMBLPhase 4 (approved)PPARG
LUMIRACOXIBChEMBLPhase 4 (approved)PPARG
MASOPROCOLChEMBLPhase 4 (approved)PPARG
METHYLENE BLUEChEMBLPhase 4 (approved)PPARG
MONTELUKASTChEMBLPhase 4 (approved)PPARG
NINTEDANIBChEMBLPhase 4 (approved)PPARG
RACECADOTRILChEMBLPhase 4 (approved)PPARA
RIMONABANTChEMBLPhase 4 (approved)PPARG
SULINDACChEMBLPhase 4 (approved)PPARG
TELMISARTANChEMBLPhase 4 (approved)PPARG

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot