MAGNESIUM CLOFIBRATE

US Previously Marketed

Details

Stereochemistry	ACHIRAL
Molecular Formula	2C10H10ClO3.Mg
Molecular Weight	451.58
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[Mg++].CC(C)(OC1=CC=C(Cl)C=C1)C([O-])=O.CC(C)(OC2=CC=C(Cl)C=C2)C([O-])=O

InChI

InChIKey=SYMULEBHDFQHNX-UHFFFAOYSA-L

InChI=1S/2C10H11ClO3.Mg/c2*1-10(2,9(12)13)14-8-5-3-7(11)4-6-8;/h2*3-6H,1-2H3,(H,12,13);/q;;+2/p-2

HIDE SMILES / InChI

Molecular Formula	C10H10ClO3
Molecular Weight	213.638
Charge	-1
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	Mg
Molecular Weight	24.305
Charge	2
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7853724 | https://www.ncbi.nlm.nih.gov/pubmed/27354598

Clofibrate is a fibric acid derivative used to lower cholesterol and triglyceride (fat-like substances) levels in the blood. This may help prevent medical problems caused by such substances clogging the blood vessels. However, this treatment was discontinued in 2002 due to adverse effects. Clofibrate is an agonist of the PPAR-α receptor in muscle, liver, and other tissues. This agonism ultimately leads to modification in gene expression resulting in increased beta-oxidation, decreased triglyceride secretion, increased HDL, and increased lipoprotein lipase activity. Clofibrate increased the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis, inhibited the synthesis, and increases the clearance of apolipoprotein B, a carrier molecule for VLDL. In addition, clofibrate was investigated as a novel therapy agent in multiple myeloma and it shown the promising results.

Approval Year

Targets

Primary Target	Pharmacology	Potency
Peroxisome proliferator-activated receptor alpha 62 Target ID: CHEMBL239 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19817384	Agonist 2752	50.0 µM [EC50]
Taste receptor type 1 member 3 14 Target ID: Q7RTX0 Gene ID: 83756.0 Gene Symbol: TAS1R3 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/19817384	Inhibitor 8504	28.0 µM [IC50]
Peroxisome proliferator-activated receptor alpha 62 Target ID: CHEMBL239 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10922459	Agonist 2752

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hyperlipoproteinemia 9 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7853724	Primary		Approved 8583	ATROMID-S Approved Use Unknown Launch Date 1967
Multiple myeloma 159 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27354598	Primary		Basic research	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
216 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7550835/	100 mg/kg single, oral dose: 100 mg/kg route of administration: Oral experiment type: SINGLE co-administered:		CLOFIBRIC ACID plasma	Homo sapiens population: UNHEALTHY age: NEWBORN sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
30649 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7550835/	100 mg/kg single, oral dose: 100 mg/kg route of administration: Oral experiment type: SINGLE co-administered:		CLOFIBRIC ACID plasma	Homo sapiens population: UNHEALTHY age: NEWBORN sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
103.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7550835/	100 mg/kg single, oral dose: 100 mg/kg route of administration: Oral experiment type: SINGLE co-administered:		CLOFIBRIC ACID plasma	Homo sapiens population: UNHEALTHY age: NEWBORN sex: FEMALE / MALE food status: UNKNOWN

Overview

CYP3A4	CYP2C9	CYP2D6	hERG

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OATP1B1 1079 MRP2 499 P-gp 1741		CYP4A1 17 CYP2B1 26 UGT 32

Drug as perpetrator

Target	Modality	Activity
OATP1B1 1095	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/16316932/ Page: 6.0	moderate [Inhibition 100 uM]
P-gp 1932	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/16316932/	no
MRP2 625	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/16316932/	not significant
CYP2B1 41	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/7685601/	yes
CYP4A1 25	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/7685601/	yes
UGT 70	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/11033061/	yes

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:34648	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:34648
ChemicalBook	CB1282957	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB1282957
eMolecules	487665	https://www.emolecules.com/cgi-bin/more?vid=487665
MolPort	MolPort-000-146-057	https://www.molport.com/shop/molecule-link/MolPort-000-146-057
ZINC	ZINC000000001187	http://zinc15.docking.org/substances/ZINC000000001187

PubMed

Title	Date	PubMed
Glucagon secretion in primary endogenous hypertriglyceridemia before and after clofibrate treatment.	1975 Aug	1143089
[A 50-year history of new drugs in Japan: the developments and trends of antihyperlipidemic drugs].	2001	11968219
Tg.AC genetically altered mouse: assay working group overview of available data.	2001	11695563
Neonatal mouse model: review of methods and results.	2001	11695548
Use of real-time gene-specific polymerase chain reaction to measure RNA expression of three family members of rat cytochrome P450 4A.	2001	11424223
WY-14,643 and other agonists of the peroxisome proliferator-activated receptor reveal a new mode of action for salicylic acid in soybean disease resistance.	2001 Apr	11346966
The peroxisomal proliferator clofibrate enhances the hepatic cytoplasmic movement of fatty acids in rats.	2001 Feb	11172343
Tocopherols are metabolized in HepG2 cells by side chain omega-oxidation and consecutive beta-oxidation.	2001 Jul 15	11440834
Unique gene expression patterns in liver and kidney associated with exposure to chemical toxicants.	2001 Jun	11356909
Comparison of various characteristics of women who do and do not attend for breast cancer screening.	2002	11879559
Characterization of catechol glucuronidation in rat liver.	2002 Feb	11792691
Synergistic effect of 4-hydroxynonenal and PPAR ligands in controlling human leukemic cell growth and differentiation.	2002 Feb 1	11827749
Peroxisome proliferator-activated receptor ligands as antiatherogenic agents: panacea or another Pandora's box?	2002 Jan	12000972
Fibrate and statin synergistically increase the transcriptional activities of PPARalpha/RXRalpha and decrease the transactivation of NFkappaB.	2002 Jan 11	11779144
Gene expression analysis reveals chemical-specific profiles.	2002 Jun	12011481
Clofibrate-induced relocation of phosphatidylcholine transfer protein to mitochondria in endothelial cells.	2002 Mar 10	11855861
Lipid-lowering drug use and cardiovascular events after myocardial infarction.	2002 May	11978147

Patents

Sample Use Guides

In Vivo Use Guide

For oral dosage form (capsules): for high cholesterol: adults—1.5 to 2 grams a day. This is divided into two to four doses. Children—Dose must be determined by doctor.

Route of Administration: Oral

In Vitro Use Guide

The antitumor apoptotic effect of clofibrate at doses ranging from 0.1-600 μM was investigated on four human and one murine myeloma cell lines, as well as in two human lymphoma cell lines, using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium-bromide assay. Clofibrate significantly reduced cell viability in all tested myeloma and lymphoma cell lines in a dose-dependent manner, while healthy cells were hardly affected.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:00:01 GMT 2025` Edited by `admin` on `Mon Mar 31 18:00:01 GMT 2025`
Record UNII	Y11SP157PJ
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

CLOFIBRIC ACID MAGNESIUM SALT

Preferred Name

English

MAGNESIUM CLOFIBRATE

Official Name

English

MAGNESIUM CLOFIBRATE [MART.]

Common Name

English

Magnesium clofibrate [WHO-DD]

Common Name

English

magnesium clofibrate [INN]

Common Name

English

CLOFIBRIC ACID MAGNESIUM SALT [MI]

Common Name

English

CLOFIBRATE MAGNESICO CHOBET

Brand Name

English

BIS(2-(P-CHLOROPHENOXY)-2-METHYLPROPIONATO)MAGNESIUM

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C98150