DGIdb - GEMFIBROZIL Drug Record

GEMFIBROZIL chembl:CHEMBL457 Approved

Alternate Names:

LOPID
CI-719
GEMFIBROZIL
EMFIB
GEMFIBROZILUM
GEMFIBROZILO
2,2-DIMETHYL-5-(2,5-DIMETHYLPHENOXY)VALERIANSAEURE
2,2-DIMETHYL-5-(2,5-XYLYLOXY)VALERIANSAEURE
2,2-DIMETHYL-5-(2,5-XYLYLOXY)VALERIC ACID
JEZIL®
GEN-FIBRO®
chembl:CHEMBL457
pubchem.compound:3463
chemidplus:25812-30-0
drugbank:01241
rxcui:4719

Drug Info:

Drug Class	antilipemic agents
Year of Approval	1981
FDA Approval	1981
Drug Class	small molecule
Drug Indications	Antilipemic Agents
Drug Categories	valerates
Drug Categories	pentanoic acids
Drug Categories	agents causing muscle toxicity
Drug Categories	cytochrome p-450 cyp1a2 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2c8 inducers (strength unknown)
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 enzyme inducers
Drug Categories	cytochrome p-450 substrates
Drug Categories	drugs causing inadvertant photosensitivity
Drug Categories	drugs that are mainly renally excreted
Drug Categories	fribic acid derivatives
Drug Categories	hypolipidemic agents indicated for hyperlipidemia
Drug Categories	oat3/slc22a8 inhibitors
Drug Categories	oatp1b1/slco1b1 inhibitors
Drug Categories	oatp1b3 inhibitors
Drug Categories	peroxisome proliferator receptor alpha agonist
Drug Categories	peroxisome proliferator-activated receptor alpha agonists
Drug Categories	photosensitizing agents
Drug Categories	ugt1a1 inhibitors
Drug Categories	ugt1a1 substrates
Drug Categories	ugt1a3 inhibitors
Drug Categories	ugt1a3 substrates
Drug Categories	ugt1a9 substrates
Drug Categories	ugt2b7 substrates

(6 More Sources)

Publications:

Goto et al., 1997, Upregulation of low density lipoprotein receptor by gemfibrozil, a hypolipidemic agent, in human hepatoma cells through stabilization of mRNA transcripts., Arterioscler. Thromb. Vasc. Biol.
Yamazaki et al., 2005, Effects of fibrates on human organic anion-transporting polypeptide 1B1-, multidrug resistance protein 2- and P-glycoprotein-mediated transport., Xenobiotica
Varma MV et al., 2015, Quantitative Rationalization of Gemfibrozil Drug Interactions: Consideration of Transporters-Enzyme Interplay and the Role of Circulating Metabolite Gemfibrozil 1-O-β-Glucuronide., Drug Metab Dispos
Sharma P et al., 2010, Validation of cell-based OATP1B1 assays to assess drug transport and the potential for drug-drug interaction to support regulatory submissions., Xenobiotica
Roy et al., 2007, Myelin basic protein-primed T cells induce neurotrophins in glial cells via alphavbeta3 [corrected] integrin., J. Biol. Chem.
Pahan et al., 2002, Gemfibrozil, a lipid-lowering drug, inhibits the induction of nitric-oxide synthase in human astrocytes., J. Biol. Chem.
Shoji et al., 2003, Preparation of antiserum against rat delta6-desaturase and its use to evaluate the desaturase protein levels in rats treated with gemfibrozil, a ligand for peroxisome proliferator-activated receptor alpha., Biosci. Biotechnol. Biochem.
Clavey et al., 1999, Cell culture conditions determine apolipoprotein CIII secretion and regulation by fibrates in human hepatoma HepG2 cells., Cell. Physiol. Biochem.
Bossé et al., Influences of the PPAR alpha-L162V polymorphism on plasma HDL(2)-cholesterol response of abdominally obese men treated with gemfibrozil., Genet. Med.
Rizvi et al., 2003, Beneficial effects of fish liver preparations of sea bass (Lates calcarifer) versus gemfibrozil in high fat diet-induced lipid-intolerant rats., J Med Food
De Filippis et al., 2011, Discovery of gemfibrozil analogues that activate PPARα and enhance the expression of gene CPT1A involved in fatty acids catabolism., Eur J Med Chem
Törüner et al., 2004, Effects of PPARgamma and PPARalpha agonists on serum leptin levels in diet-induced obese rats., Horm. Metab. Res.
Hung et al., 1999, Effects of lovastatin and gemfibrozil in subjects with high ratios of total cholesterol to high-density lipoprotein cholesterol., J. Formos. Med. Assoc.
MacDonald ML et al., 2006, Identifying off-target effects and hidden phenotypes of drugs in human cells., Nat Chem Biol
Irish et al., 1996, The effects of gemfibrozil upon the hypercoagulable state in dyslipidaemic patients with chronic renal failure., Nephrol. Dial. Transplant.
Noé et al., 2007, Substrate-dependent drug-drug interactions between gemfibrozil, fluvastatin and other organic anion-transporting peptide (OATP) substrates on OATP1B1, OATP2B1, and OATP1B3., Drug Metab. Dispos.
Bossé Y et al., 2002, Influence of the angiotensin-converting enzyme gene insertion/deletion polymorphism on lipoprotein/lipid response to gemfibrozil., Clin Genet

GEMFIBROZIL LEP

Interaction Score: 0.87

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15114521 10083765

Sources:
NCI
GEMFIBROZIL PPARA

Interaction Score: 0.57

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

Direct Interaction? True

PMIDs:
12244038 12834305 10494028 12172398 12935323 21889235

Sources:
DTC DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
GEMFIBROZIL SLC22A8

Interaction Score: 0.55

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
25941268

Sources:
DrugBank
GEMFIBROZIL SLCO2B1

Interaction Score: 0.55

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
17470528

Sources:
DrugBank GuideToPharmacology
GEMFIBROZIL SLCO1B3

Interaction Score: 0.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
17470528

Sources:
DrugBank GuideToPharmacology
GEMFIBROZIL SLCO1B1

Interaction Score: 0.48

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
16316932 25941268 19919292

Sources:
DrugBank NCI GuideToPharmacology
GEMFIBROZIL LDLR

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9409246

Sources:
NCI
GEMFIBROZIL IL6

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8941582

Sources:
NCI
GEMFIBROZIL LPL

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
GEMFIBROZIL JUN

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16680159

Sources:
DTC
GEMFIBROZIL BDNF

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17823123

Sources:
NCI
GEMFIBROZIL ACE

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12123487

Sources:
PharmGKB
GEMFIBROZIL CYP2C9

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

DrugBank: DB01241

Version: 5.1.7

Alternate Names:

GEMFIBROZIL DrugBank Drug Name

25812-30-0 CAS Number

Apo-gemfibrozil Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories acids, acyclic

Publications:

Varma MV et al., 2015, Quantitative Rationalization of Gemfibrozil Drug Interactions: Consideration of Transporters-Enzyme Interplay and the Role of Circulating Metabolite Gemfibrozil 1-O-β-Glucuronide., Drug Metab Dispos

Sharma P et al., 2010, Validation of cell-based OATP1B1 assays to assess drug transport and the potential for drug-drug interaction to support regulatory submissions., Xenobiotica

Noé et al., 2007, Substrate-dependent drug-drug interactions between gemfibrozil, fluvastatin and other organic anion-transporting peptide (OATP) substrates on OATP1B1, OATP2B1, and OATP1B3., Drug Metab. Dispos.

TEND: GEMFIBROZIL
- Version: 01-August-2011
Alternate Names:

GEMFIBROZIL Primary Drug Name

Drug Info:

Year of Approval 1981

Drug Class antilipemic agents

Publications:
TdgClinicalTrial: GEMFIBROZIL
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications Antilipemic Agents

Drug Class small molecule

FDA Approval 1981

Publications:

NCI: GEMFIBROZIL

Version: 14-September-2017

Alternate Names:

C29071 NCI drug code

Drug Info:

Publications:

Irish et al., 1996, The effects of gemfibrozil upon the hypercoagulable state in dyslipidaemic patients with chronic renal failure., Nephrol. Dial. Transplant.

Goto et al., 1997, Upregulation of low density lipoprotein receptor by gemfibrozil, a hypolipidemic agent, in human hepatoma cells through stabilization of mRNA transcripts., Arterioscler. Thromb. Vasc. Biol.

Hung et al., 1999, Effects of lovastatin and gemfibrozil in subjects with high ratios of total cholesterol to high-density lipoprotein cholesterol., J. Formos. Med. Assoc.

DTC: GEMFIBROZIL

Version: 02-September-2020

Alternate Names:

CHEMBL457 ChEMBL Drug ID

Drug Info:

Publications:

MacDonald ML et al., 2006, Identifying off-target effects and hidden phenotypes of drugs in human cells., Nat Chem Biol

De Filippis et al., 2011, Discovery of gemfibrozil analogues that activate PPARα and enhance the expression of gene CPT1A involved in fatty acids catabolism., Eur J Med Chem

PharmGKB: gemfibrozil
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Bossé Y et al., 2002, Influence of the angiotensin-converting enzyme gene insertion/deletion polymorphism on lipoprotein/lipid response to gemfibrozil., Clin Genet
GuideToPharmacology: 178100439
- Version: 29-September-2020
Alternate Names:

GEMFIBROZIL GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Gemfibrozil
- Version: 2020.06.01
Alternate Names:

D05VIX TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL457
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL457
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Mechanism of Interaction	Peroxisome proliferator-activated receptor alpha agonist
Direct Interaction	yes
Direct Interaction?	True

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

GEMFIBROZIL	DrugBank Drug Name
25812-30-0	CAS Number
Apo-gemfibrozil	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Categories	acids, acyclic

GEMFIBROZIL Drug Record

GEMFIBROZIL chembl:CHEMBL457 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15114521 10083765

Sources: NCI

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist Direct Interaction yes Direct Interaction? True

PMIDs: 12244038 12834305 10494028 12172398 12935323 21889235

Sources: DTC DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 25941268

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: 17470528

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: 17470528

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: 16316932 25941268 19919292

Sources: DrugBank NCI GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9409246

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8941582

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16680159

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17823123

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12123487

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

DrugBank: DB01241

Alternate Names: GEMFIBROZIL DrugBank Drug Name 25812-30-0 CAS Number Apo-gemfibrozil Drug Brand

Drug Info: Drug Type small molecule Drug Groups approved Drug Categories acids, acyclic

TEND: GEMFIBROZIL

Alternate Names: GEMFIBROZIL Primary Drug Name

Drug Info: Year of Approval 1981 Drug Class antilipemic agents

Publications:

TdgClinicalTrial: GEMFIBROZIL

Alternate Names:

Drug Info: Drug Indications Antilipemic Agents Drug Class small molecule FDA Approval 1981

Publications:

NCI: GEMFIBROZIL

Alternate Names: C29071 NCI drug code

Drug Info:

DTC: GEMFIBROZIL

Alternate Names: CHEMBL457 ChEMBL Drug ID

Drug Info:

PharmGKB: gemfibrozil

Alternate Names:

Drug Info:

Publications: Bossé Y et al., 2002, Influence of the angiotensin-converting enzyme gene insertion/deletion polymorphism on lipoprotein/lipid response to gemfibrozil., Clin Genet

GuideToPharmacology: 178100439

Alternate Names: GEMFIBROZIL GuideToPharmacology Ligand Name

Interaction Types & Directionality:

n/a

PMIDs:
15114521 10083765

Sources:
NCI

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Peroxisome proliferator-activated receptor alpha agonist

Direct Interaction yes

Direct Interaction? True

PMIDs:
12244038 12834305 10494028 12172398 12935323 21889235

Sources:
DTC DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
25941268

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
17470528

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
17470528

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
16316932 25941268 19919292

Sources:
DrugBank NCI GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
9409246

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
8941582

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
16680159

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
17823123

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
12123487

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

GEMFIBROZIL DrugBank Drug Name

25812-30-0 CAS Number

Apo-gemfibrozil Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories acids, acyclic

Alternate Names:

GEMFIBROZIL Primary Drug Name

Drug Info:

Year of Approval 1981

Drug Class antilipemic agents

Drug Info:

Drug Indications Antilipemic Agents

Drug Class small molecule

FDA Approval 1981

Alternate Names:

C29071 NCI drug code

Alternate Names:

CHEMBL457 ChEMBL Drug ID

Publications:

Bossé Y et al., 2002, Influence of the angiotensin-converting enzyme gene insertion/deletion polymorphism on lipoprotein/lipid response to gemfibrozil., Clin Genet

Alternate Names:

GEMFIBROZIL GuideToPharmacology Ligand Name

Alternate Names:

D05VIX TTD Drug ID