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Saroglitazar

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Summary

Saroglitazar (CHEMBL4297530) is a phase-3 clinical-stage small-molecule PPARγ agonist targeting PPARA and PPARG; indicated across 8 conditions including fatty liver disease and primary biliary cholangitis.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 2 (PPARA, PPARG)
  • Indications: 8 conditions
  • Clinical trials: 20
  • Chemistry: 439.6 Da · C25H29NO4S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL4297530
NameSaroglitazar
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID60151560
ChEBICHEBI:134708
Molecular formulaC25H29NO4S
Molecular weight439.6
InChIKeyMRWFZSLZNUJVQW-DEOSSOPVSA-N

SMILES: CCO[C@@H](CC1=CC=C(C=C1)OCCN2C(=CC=C2C3=CC=C(C=C3)SC)C)C(=O)O

IUPAC name: (2S)-2-ethoxy-3-[4-[2-[2-methyl-5-(4-methylsulfanylphenyl)pyrrol-1-yl]ethoxy]phenyl]propanoic acid

ChEBI definition: A monocarboxylic acid that is (2S)-2-ethoxy-3-(p-ethoxyphenyl)propanoic acid in which one of the methyl hydrogens of the p-ethoxy substituent has been replaced by the nitrogen of 2-methyl-5-[4-(methylthio)phenyl]-1H-pyrrole. An agonist at the subtypes α and γ of the peroxisome proliferator-activated receptor (PPAR) with predominant PPARα activity, it is used in the treatment of type 2 diabetes.

Pharmacological roles (ChEBI): PPARγ agonist, hypoglycemic agent, PPARα agonist.

Also known as: Saroglitazar, SAROGLITAZAR, saroglitazar

Patent coverage: 451 distinct patent families (1,320 SureChEMBL compound mentions), from 1 matched compound structure(s). 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-αAgonist13.190.7%Q07869
PPARGPeroxisome proliferator-activated receptor-γAgonist8.522.6%P37231

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: Thromboxane A2 receptor, Progesterone receptor, Muscarinic acetylcholine receptor M1, Prostaglandin G/H synthase 1, Sodium-dependent noradrenaline transporter, Alpha-1A adrenergic receptor, D(3) dopamine receptor, 3’,5’-cyclic-AMP phosphodiesterase 4A, Adenosine receptor A3.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 9 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PGR5.07AC508570nMCHEMBL_ACT_25204917
PTGS15.02AC509494nMCHEMBL_ACT_25205850

Target pathways

Aggregated over 2 target gene(s): PPARA, PPARG.

Top Reactome pathways

16 total, by targets touching each:

PathwayTargetsGenes
PPARA activates gene expression2PPARA, PPARG
Transcriptional regulation of white adipocyte differentiation2PPARA, PPARG
Nuclear Receptor transcription pathway2PPARA, PPARG
SUMOylation of intracellular receptors2PPARA, PPARG
Transcriptional regulation of brown and beige adipocyte differentiation by EBF22PPARA, PPARG
BMAL1:CLOCK,NPAS2 activates circadian expression1PPARA
Transcriptional activation of mitochondrial biogenesis1PPARA
Activation of gene expression by SREBF (SREBP)1PPARA
Regulation of lipid metabolism by PPARalpha1PPARA
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 II2
fatty acid metabolic process2
heart development2
response to nutrient2
hormone-mediated signaling pathway2
negative regulation of macrophage derived foam cell differentiation2
negative regulation of cholesterol storage2
cell differentiation2
negative regulation of transforming growth factor beta receptor signaling pathway2
intracellular receptor signaling pathway2
peroxisome proliferator activated receptor signaling pathway2
regulation of circadian rhythm2
positive regulation of DNA-templated transcription2
positive regulation of fatty acid metabolic process2
positive regulation of transcription by RNA polymerase II2

Indications & clinical

Indications

8 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
fatty liver disease3MONDO:0004790HP:0001397
primary biliary cholangitis3MONDO:0005388EFO:1001486
metabolic dysfunction-associated steatotic liver disease2MONDO:0013209EFO:0003095
metabolic dysfunction-associated steatohepatitis2MONDO:0007027EFO:1001249
liver disorder1MONDO:0005154EFO:0001421
kidney disorder1MONDO:0005240EFO:0003086
cirrhosis of liver1MONDO:0005155EFO:0001422

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

Clinical trials

Total trials: 20.

Phase distribution

PhaseTrials
PHASE27
PHASE16
PHASE35
PHASE41
PHASE2/PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05872269PHASE4UNKNOWNA Study to Evaluate the Safety and Effectiveness of Saroglitazar 4 mg in Patients With NAFLD With Comorbidities
NCT06427395PHASE3ACTIVE_NOT_RECRUITINGOpen-Label Extension Study of Saroglitazar Magnesium in Participants With Primary Biliary Cholangitis
NCT07216235PHASE3NOT_YET_RECRUITINGLong-Term Study to Evaluate the Safety and Efficacy in Participants With Primary Biliary Cholangitis of Saroglitazar Magnesium-V on Clinical Outcomes
NCT07424677PHASE3NOT_YET_RECRUITINGStudy of Saroglitazar Magnesium for PBC Patients With Incomplete Response or Intolerant to UDCA Therapy
NCT02265276PHASE3UNKNOWNA Prospective, Randomized Trial to Compare saroGLitazar With pioglitAZone in Nonalcoholic Fatty livEr Disease
NCT04193982PHASE3UNKNOWNAn Investigator Initiated Prospective, Four Arms Randomized Comparative Study of Efficacy and Safety of Saroglitazar, Vitamin E and Life Style Modification in Patients With Nonalcoholic Fatty Liver Disease (NAFLD)/ Non-alcoholic Steatohepatitis (NASH)
NCT05133336PHASE2/PHASE3COMPLETEDSaroglitazar Magnesium for Treatment of Primary Biliary Cholangitis
NCT03061721PHASE2COMPLETEDSaroglitazar Magnesium in Patients With Nonalcoholic Fatty Liver Disease and/or Nonalcoholic Steatohepatitis
NCT03097107PHASE2SUSPENDEDEvaluate the Safety and Efficacy of Saroglitazar Mg in Patients With Fasting Triglyceride ≥500 mg/dL and ≤1500 mg/dL
NCT03112681PHASE2COMPLETEDStudy to Evaluate Safety, Tolerability and Efficacy of Saroglitazar Mg in Patients With Primary Biliary Cholangitis
NCT03639623PHASE2COMPLETEDSafety, Tolerability, and Efficacy of Saroglitazar Mg 4 mg in Liver Transplant Recipients With Nonalcoholic Fatty Liver Disease (NAFLD)
NCT03863574PHASE2COMPLETEDSaroglitazar Magnesium in the Treatment of Non-Alcoholic Steatohepatitis
NCT05011305PHASE2COMPLETEDSaroglitazar Magnesium for the Treatment of Nonalcoholic Steatohepatitis With Fibrosis
NCT05211284PHASE2TERMINATEDSaroglitazar Magnesium 4 mg for Nonalcoholic Fatty Liver Disease (NAFLD) in People Living With HIV in the US
NCT05045482PHASE1RECRUITINGHepatic Impairment With Cirrhosis Due to Cholestatic Liver Disease
NCT06825559PHASE1RECRUITINGEvaluate PK & Safety of Saroglitazar in Subjects With Moderate Hepatic Impairment Due to Cholestatic Liver Disease
NCT04045769PHASE1COMPLETEDA Study to Evaluate the Effect of Saroglitazar Magnesium on the QTc Interval in Healthy Volunteers
NCT04112446PHASE1COMPLETEDStudy to Evaluate Absorption, Metabolism and Excretion of Single-dose [14C]-Saroglitazar in Healthy Male Subjects
NCT04446507PHASE1COMPLETEDA Pharmacokinetic Study of Saroglitazar Magnesium in Subjects with Severe Renal Impairment and Normal Renal Function
NCT04469920PHASE1COMPLETEDHepatic Impairment, Cholestatic Liver Disease, & NASH with Advanced Fibrosis & Normal Hepatic Function

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

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

MoleculeSourceStatusShared targets
ELAFIBRANORChEMBLPhase 4 (approved)PPARA, PPARG
FENOFIBRATEChEMBLPhase 4 (approved)PPARA, PPARG
FENOFIBRIC ACIDChEMBLPhase 4 (approved)PPARA, PPARG
GEMFIBROZILChEMBLPhase 4 (approved)PPARA, PPARG
PEMAFIBRATEChEMBLPhase 4 (approved)PPARA, PPARG
PIOGLITAZONEChEMBLPhase 4 (approved)PPARA, PPARG
ROSIGLITAZONEChEMBLPhase 4 (approved)PPARA, PPARG
ALEGLITAZARChEMBLPhase 3PPARA, PPARG
BEZAFIBRATEChEMBLPhase 3PPARA, PPARG
GAMOLENIC ACIDChEMBLPhase 3PPARA, PPARG
ICOSAPENTChEMBLPhase 3PPARA, PPARG
IMIGLITAZARChEMBLPhase 3PPARA, PPARG
LANIFIBRANORChEMBLPhase 3PPARA, PPARG
LOBEGLITAZONEChEMBLPhase 3PPARA, PPARG
MURAGLITAZARChEMBLPhase 3PPARA, PPARG
TESAGLITAZARChEMBLPhase 3PPARA, PPARG
DIHOMO-GAMMA-LINOLENIC ACIDChEMBLPhase 2PPARA, PPARG
FARGLITAZARChEMBLPhase 2PPARA, PPARG
GW501516ChEMBLPhase 2PPARA, PPARG
GW590735ChEMBLPhase 2PPARA, PPARG
INDEGLITAZARChEMBLPhase 2PPARA, PPARG
LINOLEIC ACIDChEMBLPhase 2PPARA, PPARG
LY-518674ChEMBLPhase 2PPARA, PPARG
NAVEGLITAZARChEMBLPhase 2PPARA, PPARG
OLEIC ACIDChEMBLPhase 2PPARA, PPARG
PIRINIXIC ACIDChEMBLPhase 2PPARA, PPARG
RAGAGLITAZARChEMBLPhase 2PPARA, PPARG
REGLITAZARChEMBLPhase 2PPARA, PPARG
FULVESTRANTChEMBL + PubChemPhase 4 (approved)PPARG
SELADELPARChEMBL + PubChemPhase 4 (approved)PPARA
BENZBROMARONEChEMBLPhase 4 (approved)PPARG
BERBERINEChEMBLPhase 4 (approved)PPARA
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