U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C15H22O3
Molecular Weight 250.3334
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GEMFIBROZIL

SMILES

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

InChI

InChIKey=HEMJJKBWTPKOJG-UHFFFAOYSA-N
InChI=1S/C15H22O3/c1-11-6-7-12(2)13(10-11)18-9-5-8-15(3,4)14(16)17/h6-7,10H,5,8-9H2,1-4H3,(H,16,17)

HIDE SMILES / InChI

Molecular Formula C15H22O3
Molecular Weight 250.3334
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018422s055lbl.pdf

Gemfibrozil, a fibric acid antilipemic agent similar to clofibrate, is used to treat hyperlipoproteinemia and as a second-line therapy for type IIb hypercholesterolemia. It acts to reduce triglyceride levels, reduce VLDL levels, reduce LDL levels (moderately), and increase HDL levels (moderately). Gemfibrozil increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. It does so by activating Peroxisome proliferator-activated receptor-alpha (PPARα) 'transcription factor ligand', a receptor that is involved in metabolism of carbohydrates and fats, as well as adipose tissue differentiation. This increase in the synthesis of lipoprotein lipase thereby increases the clearance of triglycerides. Chylomicrons are degraded, VLDLs are converted to LDLs, and LDLs are converted to HDL. This is accompanied by a slight increase in secretion of lipids into the bile and ultimately the intestine. Gemfibrozil also inhibits the synthesis and increases the clearance of apolipoprotein B, a carrier molecule for VLDL. Gemfibrozil is most commonly sold as the brand name, Lopid. Other brand names include Jezil and Gen-Fibro.

CNS Activity

Curator's Comment: gemfibrozil was shown to cross the blood brain barrier in mice

Approval Year

Targets

Targets

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
LOPID

Approved Use

LOPID (gemfibrozil tablets, USP) is indicated as adjunctive therapy to diet for: 1. Treatment of adult patients with very high elevations of serum triglyceride levels (Types IV and V hyperlipidemia) who present a risk of pancreatitis and who do not respond adequately to a determined dietary effort to control them. 2. Reducing the risk of developing coronary heart disease only in Type IIb patients without history of or symptoms of existing coronary heart disease who have had an inadequate response to weight loss, dietary therapy, exercise, and other pharmacologic agents (such as bile acid sequestrants and nicotinic acid, known to reduce LDL- and raise HDL-cholesterol) and who have the following triad of lipid abnormalities: low HDL-cholesterol levels in addition to elevated LDL-cholesterol and elevated triglycerides

Launch Date

3.77654411E11
Preventing
LOPID

Approved Use

LOPID (gemfibrozil tablets, USP) is indicated as adjunctive therapy to diet for: 1. Treatment of adult patients with very high elevations of serum triglyceride levels (Types IV and V hyperlipidemia) who present a risk of pancreatitis and who do not respond adequately to a determined dietary effort to control them. 2. Reducing the risk of developing coronary heart disease only in Type IIb patients without history of or symptoms of existing coronary heart disease who have had an inadequate response to weight loss, dietary therapy, exercise, and other pharmacologic agents (such as bile acid sequestrants and nicotinic acid, known to reduce LDL- and raise HDL-cholesterol) and who have the following triad of lipid abnormalities: low HDL-cholesterol levels in addition to elevated LDL-cholesterol and elevated triglycerides

Launch Date

3.77654411E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
28 μg/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GEMFIBROZIL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
17400 ng/mL
600 mg single, oral
dose: 600 mg
route of administration: oral
experiment type: single
co-administered:
GEMFIBROZIL plasma
Homo sapiens
population: healthy
age:
sex:
food status:
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
104 μg × h/mL
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GEMFIBROZIL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
4.4 h
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GEMFIBROZIL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
600 mg 2 times / day multiple, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p.198
unhealthy, 59
n = 87
Health Status: unhealthy
Condition: Non-insulin-dependent diabetes mellitus
Age Group: 59
Sex: M+F
Population Size: 87
Sources: Page: p.198
Disc. AE: Depression, Flushing...
AEs leading to
discontinuation/dose reduction:
Depression (1.1%)
Flushing (1.1%)
Nausea (2.2%)
Vomiting (1.1%)
Rash (1.1%)
Sources: Page: p.198
9 g single, oral
Overdose
Dose: 9 g
Route: oral
Route: single
Dose: 9 g
Sources: Page: p.13
healthy, 7
n = 1
Health Status: healthy
Age Group: 7
Population Size: 1
Sources: Page: p.13
Disc. AE: Abdominal cramps, Abnormal liver function tests...
AEs leading to
discontinuation/dose reduction:
Abdominal cramps
Abnormal liver function tests
Diarrhea
CPK increased
Joint pain
Muscle pain
Nausea
Vomiting
Sources: Page: p.13
AEs

AEs

AESignificanceDosePopulation
Depression 1.1%
Disc. AE
600 mg 2 times / day multiple, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p.198
unhealthy, 59
n = 87
Health Status: unhealthy
Condition: Non-insulin-dependent diabetes mellitus
Age Group: 59
Sex: M+F
Population Size: 87
Sources: Page: p.198
Flushing 1.1%
Disc. AE
600 mg 2 times / day multiple, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p.198
unhealthy, 59
n = 87
Health Status: unhealthy
Condition: Non-insulin-dependent diabetes mellitus
Age Group: 59
Sex: M+F
Population Size: 87
Sources: Page: p.198
Rash 1.1%
Disc. AE
600 mg 2 times / day multiple, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p.198
unhealthy, 59
n = 87
Health Status: unhealthy
Condition: Non-insulin-dependent diabetes mellitus
Age Group: 59
Sex: M+F
Population Size: 87
Sources: Page: p.198
Vomiting 1.1%
Disc. AE
600 mg 2 times / day multiple, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p.198
unhealthy, 59
n = 87
Health Status: unhealthy
Condition: Non-insulin-dependent diabetes mellitus
Age Group: 59
Sex: M+F
Population Size: 87
Sources: Page: p.198
Nausea 2.2%
Disc. AE
600 mg 2 times / day multiple, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p.198
unhealthy, 59
n = 87
Health Status: unhealthy
Condition: Non-insulin-dependent diabetes mellitus
Age Group: 59
Sex: M+F
Population Size: 87
Sources: Page: p.198
Abdominal cramps Disc. AE
9 g single, oral
Overdose
Dose: 9 g
Route: oral
Route: single
Dose: 9 g
Sources: Page: p.13
healthy, 7
n = 1
Health Status: healthy
Age Group: 7
Population Size: 1
Sources: Page: p.13
Abnormal liver function tests Disc. AE
9 g single, oral
Overdose
Dose: 9 g
Route: oral
Route: single
Dose: 9 g
Sources: Page: p.13
healthy, 7
n = 1
Health Status: healthy
Age Group: 7
Population Size: 1
Sources: Page: p.13
CPK increased Disc. AE
9 g single, oral
Overdose
Dose: 9 g
Route: oral
Route: single
Dose: 9 g
Sources: Page: p.13
healthy, 7
n = 1
Health Status: healthy
Age Group: 7
Population Size: 1
Sources: Page: p.13
Diarrhea Disc. AE
9 g single, oral
Overdose
Dose: 9 g
Route: oral
Route: single
Dose: 9 g
Sources: Page: p.13
healthy, 7
n = 1
Health Status: healthy
Age Group: 7
Population Size: 1
Sources: Page: p.13
Joint pain Disc. AE
9 g single, oral
Overdose
Dose: 9 g
Route: oral
Route: single
Dose: 9 g
Sources: Page: p.13
healthy, 7
n = 1
Health Status: healthy
Age Group: 7
Population Size: 1
Sources: Page: p.13
Muscle pain Disc. AE
9 g single, oral
Overdose
Dose: 9 g
Route: oral
Route: single
Dose: 9 g
Sources: Page: p.13
healthy, 7
n = 1
Health Status: healthy
Age Group: 7
Population Size: 1
Sources: Page: p.13
Nausea Disc. AE
9 g single, oral
Overdose
Dose: 9 g
Route: oral
Route: single
Dose: 9 g
Sources: Page: p.13
healthy, 7
n = 1
Health Status: healthy
Age Group: 7
Population Size: 1
Sources: Page: p.13
Vomiting Disc. AE
9 g single, oral
Overdose
Dose: 9 g
Route: oral
Route: single
Dose: 9 g
Sources: Page: p.13
healthy, 7
n = 1
Health Status: healthy
Age Group: 7
Population Size: 1
Sources: Page: p.13
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG



Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
yes [Ki 1.5 uM]
yes [Ki 14.2 uM]
yes [Ki 5.8 uM]
yes (co-administration study)
Comment: [PMID:11719730]:Gemfibrozil modestly increases the plasma concentrations of glimepiride. This may be caused by inhibition of CYP2C9.
yes
yes
yes
yes
yes
yes (co-administration study)
Comment: [PMID:22472994]: CYP2C8 inactivation by gemfibrozil caused dose-dependent increases in AUC of repaglinide
Drug as victim
PubMed

PubMed

TitleDatePubMed
Rhabdomyolysis and renal failure associated with cerivastatin-gemfibrozil combination therapy.
1999 Apr 1
Effects of fibrate compounds on expression of plasminogen activator inhibitor-1 by cultured endothelial cells.
1999 Jun
Rhabdomyolysis and acute renal failure after changing statin-fibrate combinations.
2000
A risk factor for atherosclerosis: triglyceride-rich lipoproteins.
2001
Hypertriglyceridemia: a review of clinical relevance and treatment options: focus on cerivastatin.
2001
Treatment of dyslipoproteinemia in the metabolic syndrome.
2001
Effect of a six month gemfibrozil treatment and dietary recommendations on the metabolic risk profile of visceral obese men.
2001 Aug
Bayer decides to withdraw cholesterol lowering drug.
2001 Aug 18
Altered expression of the carboxylesterases ES-4 and ES-10 by peroxisome proliferator chemicals.
2001 Aug 28
Treatment for the procoagulant state in type 2 diabetes.
2001 Dec
Rhabdomyolysis with HMG CoA reductase inhibitors: a class effect?
2001 Dec
Determination of drugs in surface water and wastewater samples by liquid chromatography-mass spectrometry: methods and preliminary results including toxicity studies with Vibrio fischeri.
2001 Dec 14
Evidence for significant differences in microsomal drug glucuronidation by canine and human liver and kidney.
2001 Feb
The effects of gemfibrozil upon the metabolism of chylomicron-like emulsions in patients with endogenous hypertriglyceridemia.
2001 Feb 1
Short-term gemfibrozil treatment reverses lipid profile and peroxidation but does not alter blood glucose and tissue antioxidant enzymes in chronically diabetic rats.
2001 Jan
Stimulatory effect of clofibrate and gemfibrozil administration on the formation of fatty acid esters of estradiol by rat liver microsomes.
2001 Jan
Normocholesterolaemic dyslipidaemia: is there a role for fibrates?
2001 Jan 15
Gemfibrozil prevents major coronary events by increasing HDL-cholesterol and more.
2001 Jul
Effect of gemfibrozil on the composition and oxidation properties of very-low-density lipoprotein and high-density lipoprotein in patients with hypertriglyceridemia.
2001 Jun
Effect of statin versus fibrate on postprandial endothelial dysfunction: role of remnant-like particles.
2001 Jun
[Helsinki Heart Study].
2001 Mar
Relation of gemfibrozil treatment and lipid levels with major coronary events: VA-HIT: a randomized controlled trial.
2001 Mar 28
Choice of lipid-regulating drugs.
2001 May 28
Attenuation by fibrates of plasminogen activator inhibitor type-1 expression in human arterial smooth muscle cells.
2001 Nov
Effect of trans-dehydrocrotonin, a 19-nor-clerodane diterpene from Croton cajucara on experimental hypertriglyceridaemia and hypercholesterolaemia induced by Triton WR 1339 (tyloxapol) in mice.
2001 Nov
Effect of gemfibrozil on the pharmacokinetics and pharmacodynamics of glimepiride.
2001 Nov
Ciprofibrate versus gemfibrozil in the treatment of mixed hyperlipidemias: an open-label, multicenter study.
2001 Nov
Clinical inquiries. What laboratory monitoring is appropriate to detect adverse drug reactions in patients on cholesterol-lowering agents?
2001 Nov
Gemfibrozil increases paraoxonase activity in type 2 diabetic patients. A new hypothesis of the beneficial action of fibrates?
2001 Nov
Effects of fenofibrate and gemfibrozil on plasma homocysteine.
2001 Nov 24
Cyclic nucleotides in platelets of genetically hypertriglyceridemic and hypertensive rats. Thrombin and nitric oxide responses are unrelated to plasma triglyceride levels.
2001 Oct 1
[Cholestatic hepatitis caused by gemfibrozil].
2001 Sep
Cerivastatin and gemfibrozil-associated rhabdomyolysis.
2001 Sep
Bayer pulls cerivastatin (Baycol) from market.
2001 Sep 4
Sexual dysfunction secondary to gemfibrozil.
2002 Jan
Cost-effectiveness of gemfibrozil for coronary heart disease patients with low levels of high-density lipoprotein cholesterol: the Department of Veterans Affairs High-Density Lipoprotein Cholesterol Intervention Trial.
2002 Jan 28
Patents

Sample Use Guides

The recommended dose for adults is 1200 mg administered in two divided doses 30 minutes before the morning and evening meals
Route of Administration: Oral
Sustained potent reduction of [Ca²⁺]i in cultured rat VSMCs was observed with Gemfibrozil 50mg/L
Substance Class Chemical
Created
by admin
on Wed Jul 05 22:50:46 UTC 2023
Edited
by admin
on Wed Jul 05 22:50:46 UTC 2023
Record UNII
Q8X02027X3
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GEMFIBROZIL
EP   HSDB   INN   JAN   MART.   MI   ORANGE BOOK   USAN   USP   USP-RS   VANDF   WHO-DD  
USAN   INN  
Official Name English
GEMFIBROZIL [IARC]
Common Name English
Gemfibrozil [WHO-DD]
Common Name English
GEMFIBROZIL [HSDB]
Common Name English
2,2-DIMETHYL-5-(2,5-XYLYLOXY) VALERIC ACID
Systematic Name English
gemfibrozil [INN]
Common Name English
GEMFIBROZIL [EP MONOGRAPH]
Common Name English
GEMFIBROZIL [MART.]
Common Name English
GEMFIBROZIL [USAN]
Common Name English
GEMFIBROZIL [USP-RS]
Common Name English
GEMFIBROZIL [JAN]
Common Name English
NSC-757024
Code English
GEMFIBROZIL [ORANGE BOOK]
Common Name English
GEMFIBROZIL [MI]
Common Name English
GEMFIBROZIL [INCI]
Common Name English
CI-719
Code English
GEMFIBROZIL [USP MONOGRAPH]
Common Name English
PENTANOIC ACID, 5-(2,5-DIMETHYLPHENOXY)-2,2-DIMETHYL-
Common Name English
LOPID
Brand Name English
GEMFIBROZIL [VANDF]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 834821
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
FDA ORPHAN DRUG 591917
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
EU-Orphan Drug EU/3/18/1993
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
NCI_THESAURUS C98150
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
WHO-VATC QC10AB04
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
FDA ORPHAN DRUG 591917
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
FDA ORPHAN DRUG 546216
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
NDF-RT N0000170118
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
NDF-RT N0000175375
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
NDF-RT N0000175596
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
WHO-ATC C10AB04
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
NDF-RT N0000170118
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
LIVERTOX NBK547926
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
FDA ORPHAN DRUG 834921
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
Code System Code Type Description
CAS
25812-30-0
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
HSDB
7735
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
DRUG BANK
DB01241
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
DAILYMED
Q8X02027X3
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
ECHA (EC/EINECS)
247-280-2
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
INN
3899
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
SMS_ID
100000092643
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
EPA CompTox
DTXSID0020652
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
EVMPD
SUB07894MIG
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
FDA UNII
Q8X02027X3
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
DRUG CENTRAL
1285
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
NSC
757024
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
IUPHAR
3439
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
RXCUI
4719
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY RxNorm
MESH
D015248
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
RS_ITEM_NUM
1288500
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
LACTMED
Gemfibrozil
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
NCI_THESAURUS
C29071
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
MERCK INDEX
M5692
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY Merck Index
ChEMBL
CHEMBL457
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
WIKIPEDIA
GEMFIBROZIL
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
CHEBI
5296
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
PUBCHEM
3463
Created by admin on Wed Jul 05 22:50:46 UTC 2023 , Edited by admin on Wed Jul 05 22:50:46 UTC 2023
PRIMARY
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