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MK-0767

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Also known as MK 0767Mk0767

Summary

Mk-0767 (CHEMBL4297404) is a phase-3 clinical-stage small molecule targeting PPARA and PPARG; indicated across 3 conditions including diabetes mellitus and type 2 diabetes mellitus.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 2 (PPARA, PPARG)
  • Indications: 3 conditions
  • Clinical trials: 10
  • Chemistry: 422.4 Da · C20H17F3N2O5

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL4297404
NameMK-0767
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID56842109
Molecular formulaC20H17F3N2O5
Molecular weight422.4
InChIKeyORZMUVMQJPGFOM-UHFFFAOYSA-N

SMILES: COC1=C(C=C(C=C1)CC2C(=O)NC(=O)O2)C(=O)NCC3=CC=C(C=C3)C(F)(F)F

IUPAC name: 5-[(2,4-dioxo-1,3-oxazolidin-5-yl)methyl]-2-methoxy-N-[[4-(trifluoromethyl)phenyl]methyl]benzamide

Also known as: MK 0767, Mk-0767, Mk0767, MK-0767

Patent coverage: 82 distinct patent families (212 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-αAgonist7.640.7%Q07869
PPARGPeroxisome proliferator-activated receptor-γFull agonist6.492.6%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

3 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
diabetes mellitus3MONDO:0005015EFO:0000400
type 2 diabetes mellitus3MONDO:0005148MONDO:0005148
metabolic syndrome X2MONDO:0011565EFO:0000195

Clinical trials

Total trials: 10.

Phase distribution

PhaseTrials
PHASE38
PHASE22

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00543010PHASE3TERMINATEDMK0767 Glipizide Comparator Cardiac Safety Study (0767-018)
NCT00543361PHASE3TERMINATEDStudy MK0767 and Metformin in Type 2 Diabetic Patients (0767-020)
NCT00543491PHASE3TERMINATEDMK0767 and Sulfonylurea Combination Study (0767-027)
NCT00543517PHASE3TERMINATEDStudy A - MK0767 Monotherapy Study
NCT00543738PHASE3TERMINATEDMK0767 and Metformin Combination Study (0767-028)
NCT00543751PHASE3TERMINATEDPlacebo Controlled Metformin and Sulfonylurea Combination Study in Patients With Type 2 Diabetes (0767-025)
NCT00543816PHASE3TERMINATEDMK0767 Added to Insulin Therapy in Patients With Type 2 Diabetes (0767-030)
NCT00547274PHASE3TERMINATEDDyslipidemia in Type 2 Diabetes (0767-034)
NCT00543556PHASE2TERMINATEDMK0767 in Type 2 Diabetes (0767-012)
NCT00703690PHASE2TERMINATEDMK0767 in Metabolic Syndrome-Dyslipidemia (0767-016)

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