Gemfibrozil

drug
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Also known as CI-719EmfibGemfibroziloLopidNSC-757024SID11112705SID17389870SID26751515SID855780SID49718189SID144204164SID174007259SID144209195SID144213101SID170464998C0164788

Summary

Gemfibrozil (CHEMBL457) is an approved small-molecule antilipemic drug (ATC C10AB04) targeting SLCO1B1, SLCO1B3, and SLCO2B1; indicated across 15 conditions including coronary artery disorder and cardiovascular disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C10AB04
  • Targets: 4 (SLCO1B1, SLCO1B3, SLCO2B1…)
  • Indications: 15 conditions
  • Clinical trials: 35
  • Chemistry: 250.33 Da · C15H22O3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL457
NameGemfibrozil
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID3463
ChEBICHEBI:5296
ATCC10AB04
Molecular formulaC15H22O3
Molecular weight250.33
InChIKeyHEMJJKBWTPKOJG-UHFFFAOYSA-N

SMILES: CC1=CC(=C(C=C1)C)OCCCC(C)(C)C(=O)O

IUPAC name: 5-(2,5-dimethylphenoxy)-2,2-dimethylpentanoic acid

Pharmacological roles (ChEBI): antilipemic drug.

Also known as: CI-719, Emfib, Gemfibrozil, Gemfibrozilo, Lopid, NSC-757024, gemfibrozil, SID11112705, SID17389870, SID26751515, SID855780, GEMFIBROZIL

Patent coverage: 9,271 distinct patent families (35,238 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 35,152 (100%) 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
SLCO1B1OATP1B1Inhibition0%Q9Y6L6
SLCO1B3OATP1B3Inhibition0%Q9NPD5
SLCO2B1OATP2B1Inhibition0%O94956
PPARAPeroxisome proliferator-activated receptor-αAgonist4.230.7%Q07869

Broader ChEMBL bioactivity targets: 18 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Nuclear receptor ROR-gamma, Survival motor neuron protein, 4’-phosphopantetheinyl transferase ffp, Solute carrier organic anion transporter family member 1B1, Solute carrier organic anion transporter family member 1B3, CDGSH iron-sulfur domain-containing protein 1, 5-hydroxytryptamine receptor 2B, Thyrotropin receptor, Muscarinic acetylcholine receptor M1, Alpha-1A adrenergic receptor, Peroxisome proliferator-activated receptor gamma, Peroxisome proliferator-activated receptor alpha, Transthyretin, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2C8, Fatty acid-binding protein, liver.

Bioactivity

ChEMBL activities: 11 potent at pChembl ≥ 5 of 28 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
TTR7Kd100nMCHEMBL_ACT_15670985
P026925.73Ki1860nMCHEMBL_ACT_2445226
CYP2C85.39IC504100nMCHEMBL_ACT_12163618
SLCO1B15.39IC504074nMCHEMBL_ACT_13800618
HTR2B5.36AC504400nMCHEMBL_ACT_25228002
SMN15.35Potency4467nMCHEMBL_ACT_3867033
CYP2C95.2Potency6310nMCHEMBL_ACT_5033439
CYP2C95.2AC506310nMCHEMBL_ACT_6071368
SLCO1B35.15IC507079nMCHEMBL_ACT_13798619
CISD15.14Ki7291nMCHEMBL_ACT_16766257
CYP2C95.02IC509600nMCHEMBL_ACT_12163620

Target pathways

Aggregated over 4 target gene(s): SLCO1B1, SLCO1B3, SLCO2B1, PPARA.

Top Reactome pathways

32 total, by targets touching each:

PathwayTargetsGenes
Heme degradation3SLCO1B1, SLCO1B3, SLCO2B1
Transport of small molecules3SLCO1B1, SLCO1B3, SLCO2B1
Transport of vitamins, nucleosides, and related molecules3SLCO1B1, SLCO1B3, SLCO2B1
SLC-mediated transmembrane transport3SLCO1B1, SLCO1B3, SLCO2B1
Organic anion transport by SLCO transporters3SLCO1B1, SLCO1B3, SLCO2B1
Atorvastatin ADME3SLCO1B1, SLCO1B3, SLCO2B1
Metabolism2SLCO1B1, SLCO1B3
Recycling of bile acids and salts2SLCO1B1, SLCO1B3
Disease2SLCO1B1, SLCO1B3
Metabolism of porphyrins2SLCO1B1, SLCO1B3
Bile acid and bile salt metabolism2SLCO1B1, SLCO1B3
Metabolism of lipids2SLCO1B1, SLCO1B3
SLC transporter disorders2SLCO1B1, SLCO1B3
Disorders of transmembrane transporters2SLCO1B1, SLCO1B3
Metabolism of steroids2SLCO1B1, SLCO1B3
Drug ADME2SLCO1B1, SLCO1B3
BMAL1:CLOCK,NPAS2 activates circadian expression1PPARA
PPARA activates gene expression1PPARA
Transcriptional activation of mitochondrial biogenesis1PPARA
Activation of gene expression by SREBF (SREBP)1PPARA
Transcriptional regulation of white adipocyte differentiation1PPARA
Nuclear Receptor transcription pathway1PPARA
Regulation of lipid metabolism by PPARalpha1PPARA
SUMOylation of intracellular receptors1PPARA
Defective SLCO1B3 causes hyperbilirubinemia, Rotor type (HBLRR)1SLCO1B3
Defective SLCO1B1 causes hyperbilirubinemia, Rotor type (HBLRR)1SLCO1B1
Cytoprotection by HMOX11PPARA
Heme signaling1PPARA
Aspirin ADME1SLCO2B1
Transcriptional regulation of brown and beige adipocyte differentiation by EBF21PPARA
Expression of BMAL (ARNTL), CLOCK, and NPAS21PPARA
RORA,B,C and NR1D1 (REV-ERBA) regulate gene expression1PPARA

Dominant GO biological processes

GO termTargets
xenobiotic metabolic process3
monoatomic ion transport3
obsolete organic anion transport3
bile acid and bile salt transport3
heme catabolic process3
sodium-independent organic anion transport3
transmembrane transport3
lipid transport2
prostaglandin transport2
thyroid hormone transport1
transport across blood-brain barrier1
negative regulation of transcription by RNA polymerase II1
response to hypoxia1
gluconeogenesis1
fatty acid metabolic process1

Indications & clinical

Indications

2 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

IndicationPhaseMONDOEFO
coronary artery disorder4MONDO:0005010EFO:0001645
cardiovascular disorder4MONDO:0004995EFO:0000319

10 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)PhaseMONDOEFO
nicotine dependence2MONDO:0008575EFO:0003768
myocardial ischemia2MONDO:0024644EFO:1001375
alcohol abuse2MONDO:0002046MONDO:0007079
Parkinson disease2MONDO:0005180MONDO:0005180
anemia1MONDO:0002280EFO:0004272
HIV infectious disease1MONDO:0005109EFO:0000764
hypertriglyceridemia1MONDO:0005347EFO:0004211
type 2 diabetes mellitus1MONDO:0005148MONDO:0005148
neoplasm1MONDO:0005070MONDO:0004992
multiple sclerosis1MONDO:0005301MONDO:0005301

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

Clinical trials

Total trials: 35.

Phase distribution

PhaseTrials
PHASE125
PHASE25
PHASE42
PHASE31
EARLY_PHASE11
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00243672PHASE4WITHDRAWNEarly Therapeutic Effects of Statins and Fibrates on Unstable Atherosclerotic Plaques
NCT01385020PHASE4COMPLETEDEffect of Gemfibrozil on the Safety and Pharmacokinetics of Red Yeast Rice in Healthy Subjects
NCT00283335PHASE3COMPLETEDThe VA HDL Intervention Trial (HIT): Secondary Prevention of Coronary Heart Disease in Men With Low HDL-Cholesterol and Desirable LDL-Cholesterol
NCT05931484PHASE2NOT_YET_RECRUITINGStudy to Evaluate the Safety, Tolerability, Efficacy, and PK of FHL-301 in Parkinson’s Disease Patients.
NCT00000461PHASE2COMPLETEDHarvard Atherosclerosis Reversibility Project (HARP)
NCT01876810PHASE2COMPLETEDInitial Screening of Gemfibrozil as a Novel Treatment for Tobacco Addiction
NCT02638597PHASE2COMPLETEDGemfibrozil for Nicotine Smoking Cessation
NCT03539432PHASE2TERMINATEDExploration of Gemfibrozil as a Treatment for AUD
NCT00039663PHASE1COMPLETEDEndothelial Dysfunction as a Risk Factor in HIV Study
NCT00108511PHASE1COMPLETEDEffect of Gemfibrozil on Serum Glycosylphosphatidylinositol (GPI) Phospholipase D and Triglycerides
NCT00566865PHASE1COMPLETEDDrug-Drug Interaction Study of Mitiglinide and Gemfibrozil
NCT00800475PHASE1COMPLETEDBioequivalence Study Between Two Oral Formulations of Gemfibrozil Tablets
NCT00966966PHASE1COMPLETEDStudy Evaluating Potential Interaction Between SAM-531 And Gemfibrozil When Co-Administered
NCT01083212PHASE1COMPLETEDTo Evaluate the Effect of Gemfibrozil on the Pharmacokinetics and Pharmacodynamics of a Single Dose of AZD1656
NCT01301742PHASE1COMPLETEDRelative Bioavailability of Single Dose Empagliflozin (BI 10773) When Co-administered With Multiple Doses of 600 mg Gemfibrozil Compared to Single Dose Treatment With Empagliflozin (BI 10773) When Given Alone in Healthy Volunteers
NCT01340846PHASE1COMPLETEDA Pharmacokinetics Study of the Effects of GSK2118436 on Warfarin, the Effects of Ketoconazole and Gemfibrozil on GSK2118436, and the Effects of Repeat Doses of GSK2118436 in Subjects With BRAF Mutant Solid Tumors
NCT01376232PHASE1COMPLETEDStudy to Assess the Pharmacokinetics of GSK1278863A Coadministered With a High Fat Meal or an Inhibitor of CYP2C8 (Gemfibrozil)
NCT01736254PHASE1COMPLETEDA Study of Evacetrapib in Healthy Participants
NCT01797198PHASE1COMPLETEDA Study to Assess the Effect of Multiple Doses of Gemfribozil on a Single Dose of ASP3652, and to Assess the Effects of Multiple Doses of ASP3652 on a Single Dose of Repaglinide in the Body of Healthy Subjects
NCT01836198PHASE1COMPLETEDThe Effect of Gemfibrozil, Ketoconazole and Clarithromycin on the Amount of LY2409021 in the Bloodstream
NCT01913379PHASE1COMPLETEDDrug-drug Interaction Study With MDV3100 (ASP9785) and Gemfibrozil and Itraconazole
NCT02230033PHASE1COMPLETEDStudy to Assess Drug-Drug Interaction Between Itraconazole or Gemfibrozil and JNJ-56021927
NCT02770222PHASE1COMPLETEDA Clinical Study to Investigate the Effect of Gemfibrozil or Rifampicin on Blood Concentrations of Selexipag in Healthy Subjects
NCT03624959PHASE1COMPLETEDDrug-drug Interaction Study of Ozanimod With Inhibitor or Inducer of CYP2C8 and/or CYP3A
NCT03723395PHASE1COMPLETEDA Drug-Drug Interaction Study in Healthy Volunteers of the Effects of Tucatinib
NCT04008186PHASE1COMPLETEDA Clinical Drug-Drug Interaction (DDI) Study With Omaveloxolone
NCT04956627PHASE1COMPLETEDA Study to Assess the Effect of Itraconazole, Phenytoin and Gemfibrozil on the Drug Levels of BMS-986166 in Healthy Participants
NCT05069870PHASE1UNKNOWNA Study to Investigate the Drug-drug Interactions (DDIs) of SKLB1028 With Itraconazole, Gemfibrozil or Rifampicin in Healthy Subjects
NCT05932303PHASE1COMPLETEDA Study to Assess the Effect of Multiple Doses of Itraconazole, Gemfibrozil, or Carbamazepine on BMS-986278 in Healthy Participants
NCT05959447PHASE1COMPLETEDEvaluation of the Potential Drug-drug Interactions Between Gemfibrozil or Dabigatran Etexilate and Camlipixant
NCT06064539PHASE1COMPLETEDStudy of Drug-drug Interaction of the Effects of Gemfibrozil and Rifampicin on SAR442168 in Healthy Adult Subjects
NCT06392659PHASE1COMPLETEDA Phase 1, Open-label Study Evaluating the Pharmacokinetics and Drug-drug Interaction of VX-993 in Healthy Adults
NCT06809608PHASE1COMPLETEDA Study Investigating the Effect of Different Approved Medications on How the Body Processes the Study Compound RO7795081
NCT02045056EARLY_PHASE1COMPLETEDModulation of Micro-RNA Pathways by Gemfibrozil in Predementia Alzheimer Disease
NCT00474201Not specifiedCOMPLETEDDrug Interaction Study of Lopinavir/Ritonavir and Gemfibrozil

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.

336 molecules share ≥1 primary target. Top 100 by shared-target count:

MoleculeSourceStatusShared targets
CYCLOSPORINEChEMBL + PubChemPhase 4 (approved)PPARA, SLCO1B1, SLCO1B3, SLCO2B1
ATAZANAVIRChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
ATORVASTATINChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
CLARITHROMYCINChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
DIGOXINChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
ERLOTINIBChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
INDOMETHACINChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
OLMESARTAN MEDOXOMILChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
PACLITAXELChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
PRAVASTATINChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
RIFAMPINChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
RIFAMYCINChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
RITONAVIRChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
TELMISARTANChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
VERAPAMILChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
VINBLASTINEChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
VINCRISTINEChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
ELTROMBOPAGChEMBLPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
SULFASALAZINEChEMBLPhase 4 (approved)SLCO1B1, SLCO1B3, SLCO2B1
SILYBIN AChEMBLPhase 3SLCO1B1, SLCO1B3, SLCO2B1
GENISTEINChEMBL + PubChemPhase 2 (approved)SLCO1B1, SLCO1B3, SLCO2B1
GLYCYRRHIZINChEMBL + PubChemPhase 2 (approved)SLCO1B1, SLCO1B3, SLCO2B1
SILICRISTINChEMBLPhase 2SLCO1B1, SLCO1B3, SLCO2B1
URSOLIC ACIDChEMBLPhase 2PPARA, SLCO1B1, SLCO1B3
AcyclovirPubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
AllopurinolPubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
AmantadinePubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
aminohippuric acidPubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
AmitriptylinePubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
AtenololPubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
Cholic AcidPubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
DexamethasonePubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
ErythromycinPubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
EzetimibePubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
MetforminPubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
MethotrexatePubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
PhenytoinPubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
SildenafilPubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
theophyllinePubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
ValacyclovirPubChemApprovedSLCO1B1, SLCO1B3, SLCO2B1
CANDESARTAN CILEXETILChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3
DOXORUBICINChEMBL + PubChemPhase 4 (approved)SLCO1B3, SLCO2B1
ETOPOSIDEChEMBL + PubChemPhase 4 (approved)SLCO1B3, SLCO2B1
FenofibrateChEMBL + PubChemPhase 4 (approved)PPARA, SLCO2B1
GLYBURIDEChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO2B1
HYDROXYZINE PAMOATEChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3
LOVASTATINChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO2B1
MITOXANTRONEChEMBL + PubChemPhase 4 (approved)SLCO1B3, SLCO2B1
PioglitazoneChEMBL + PubChemPhase 4 (approved)PPARA, SLCO2B1
RosiglitazoneChEMBL + PubChemPhase 4 (approved)PPARA, SLCO2B1
SIMVASTATINChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO2B1
TANNIC ACIDChEMBL + PubChemPhase 4 (approved)SLCO1B1, SLCO1B3
BETA CAROTENEChEMBLPhase 4 (approved)SLCO1B1, SLCO1B3
CARBENOXOLONEChEMBLPhase 4 (approved)SLCO1B1, SLCO1B3
DICLOXACILLINChEMBLPhase 4 (approved)SLCO1B1, SLCO1B3
ERYTHROMYCIN ESTOLATEChEMBLPhase 4 (approved)SLCO1B1, SLCO1B3
ERYTHROMYCIN ETHYLSUCCINATEChEMBLPhase 4 (approved)SLCO1B1, SLCO1B3
LOSARTANChEMBLPhase 4 (approved)SLCO1B1, SLCO1B3
MOMETASONE FUROATEChEMBLPhase 4 (approved)SLCO1B1, SLCO1B3
NONOXYNOL 9ChEMBLPhase 4 (approved)SLCO1B1, SLCO1B3
TELITHROMYCINChEMBLPhase 4 (approved)SLCO1B1, SLCO1B3
ADMILPARANTChEMBLPhase 3SLCO1B1, SLCO1B3
ALISPORIVIRChEMBLPhase 3SLCO1B1, SLCO1B3
FASIGLIFAMChEMBLPhase 3SLCO1B1, SLCO1B3
GOSSYPOLChEMBLPhase 3SLCO1B1, SLCO1B3
PAMIPARIBChEMBLPhase 3SLCO1B1, SLCO1B3
SILIBININChEMBLPhase 3SLCO1B1, SLCO1B3
BMS-986020ChEMBLPhase 2SLCO1B1, SLCO1B3
ENOXOLONEChEMBLPhase 2SLCO1B1, SLCO1B3
.gamma.-aminobutyric acidPubChemApprovedSLCO1B1, SLCO1B3
AcetaminophenPubChemApprovedSLCO1B1, SLCO1B3
AcetazolamidePubChemApprovedSLCO1B1, SLCO1B3
Acetohydroxamic AcidPubChemApprovedSLCO1B1, SLCO1B3
acetylcysteinePubChemApprovedSLCO1B1, SLCO1B3
Acetylsalicylsalicylic acidPubChemApprovedSLCO1B1, SLCO1B3
AdeninePubChemApprovedSLCO1B1, SLCO1B3
AlbendazolePubChemApprovedSLCO1B1, SLCO1B3
AllantoinPubChemApprovedSLCO1B1, SLCO1B3
AlmotriptanPubChemApprovedSLCO1B1, SLCO1B3
Aminolevulinic AcidPubChemApprovedSLCO1B1, SLCO1B3
AmoxapinePubChemApprovedSLCO1B1, SLCO1B3
AmpicillinPubChemApprovedSLCO1B1, SLCO1B3
Amprolium ionPubChemApprovedSLCO1B1, SLCO1B3
AnthralinPubChemApprovedSLCO1B1, SLCO1B3
AntipyrinePubChemApprovedSLCO1B1, SLCO1B3
apiole (parsley)PubChemApprovedSLCO1B1, SLCO1B3
ApomorphinePubChemApprovedSLCO1B1, SLCO1B3
AzaperonePubChemApprovedSLCO1B1, SLCO1B3
AzathioprinePubChemApprovedSLCO1B1, SLCO1B3
Azelaic AcidPubChemApprovedSLCO1B1, SLCO1B3
BacitracinPubChemApprovedSLCO1B1, SLCO1B3
BaclofenPubChemApprovedSLCO1B1, SLCO1B3
Beclomethasone DipropionatePubChemApprovedSLCO1B1, SLCO1B3
BenzocainePubChemApprovedSLCO1B1, SLCO1B3
Berberine ChloridePubChemApprovedSLCO1B1, SLCO1B3
Betamethasone ValeratePubChemApprovedSLCO1B1, SLCO1B3
Bethanechol ChloridePubChemApprovedSLCO1B1, SLCO1B3
BiotinPubChemApprovedSLCO1B1, SLCO1B3
BisacodylPubChemApprovedSLCO1B1, SLCO1B3
BumetanidePubChemApprovedSLCO1B1, SLCO1B3