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Chiglitazar

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Also known as Carfloglitazar, (s)-CS 038CS-038

Summary

Chiglitazar (CHEMBL4650349) is a phase-3 clinical-stage small molecule targeting PPARA and PPARG; indicated across 5 conditions including type 2 diabetes mellitus and metabolic dysfunction-associated steatohepatitis.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 2 (PPARA, PPARG)
  • Indications: 5 conditions
  • Clinical trials: 17
  • Chemistry: 572.6 Da · C36H29FN2O4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL4650349
NameChiglitazar
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID71402018
Molecular formulaC36H29FN2O4
Molecular weight572.6
InChIKeyQNLWMPLUWMWDMQ-YTTGMZPUSA-N

SMILES: C1=CC=C2C(=C1)C3=CC=CC=C3N2CCOC4=CC=C(C=C4)C[C@@H](C(=O)O)NC5=CC=CC=C5C(=O)C6=CC=C(C=C6)F

IUPAC name: (2S)-3-[4-(2-carbazol-9-ylethoxy)phenyl]-2-[2-(4-fluorobenzoyl)anilino]propanoic acid

Also known as: Carfloglitazar, (s)-, Chiglitazar, CS 038, CS-038, CHIGLITAZAR

Patent coverage: 163 distinct patent families (443 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 439 (99%) 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-αAgonist5.920.7%Q07869
PPARGPeroxisome proliferator-activated receptor-γAgonist7.12.6%P37231

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

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

5 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
type 2 diabetes mellitus3MONDO:0005148MONDO:0005148
metabolic dysfunction-associated steatohepatitis2MONDO:0007027EFO:1001249
polycystic ovary syndrome2MONDO:0008487EFO:0000660
liver disorder1MONDO:0005154EFO:0001421
kidney disorder1MONDO:0005240EFO:0003086

Clinical trials

Total trials: 17.

Phase distribution

PhaseTrials
Not specified6
PHASE15
PHASE33
PHASE22
PHASE2/PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT02121717PHASE3COMPLETEDStudy of Chiglitazar Compare With Placebo in Type 2 Diabetes Patients
NCT02173457PHASE3COMPLETEDStudy of Chiglitazar Compare With Sitagliptin in Type 2 Diabetes Patients
NCT04807348PHASE3COMPLETEDChiglitazar Added to Metformin for Type 2 Diabetes
NCT06125587PHASE2/PHASE3COMPLETEDChiglitazar/Metformin in Non-obese Women With PCOS
NCT07303803PHASE2NOT_YET_RECRUITINGA Study of Chiglitazar in Patients With Metabolic Dysfunction-associated Steatohepatitis and Type 2 Diabetes Mellitus
NCT05193916PHASE2COMPLETEDA Phase II Clinical Trial of Chiglitazar for NASH
NCT07511010PHASE1NOT_YET_RECRUITINGFood Effect and Multiple-Dose Study of Chiglitazar/Metformin Extended-Release Tablets
NCT05515445PHASE1COMPLETEDPharmacokinetics of Chiglitazar in Subjects With Hepatic Impairment and Normal Hepatic Function
NCT05515458PHASE1COMPLETEDPharmacokinetics of Chiglitazar in Subjects With Renal Impairment and Normal Renal Function
NCT05681273PHASE1COMPLETEDDrug-Drug Interaction Study of Chiglitazar in Healthy Subjects.
NCT05760677PHASE1UNKNOWNStudy on the Efficacy and Safety of Chiglitazar Sodium in PCOS With T2DM
NCT06773221Not specifiedNOT_YET_RECRUITINGThe Efficacy and Safety of Chiglitazar in Patients with MAFLD-related Cirrhosis
NCT07519265Not specifiedNOT_YET_RECRUITINGBioequivalence Study of Chiglitazar/Metformin Extended-Release Tablets
NCT07558525Not specifiedNOT_YET_RECRUITINGEvaluation of Chiglitazar Sodium With Lifestyle Intervention for Reversing Prediabetes
NCT07580638Not specifiedNOT_YET_RECRUITINGChiglitazar Added to SGLT-2 Inhibitors for Type 2 Diabetes
NCT06007014Not specifiedUNKNOWNEfficacy and Safety of Chiglitazar Added to Glargine in Patients With Type 2 Diabetes
NCT06191328Not specifiedUNKNOWNA Prospective, Open, Self-controlled Study of the Effects of Chiglitazar Sodium on Glucose and Lipid Metabolism in Patients With Type 2 Diabetes Mellitus (T2DM)

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 1 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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