CIPROFIBRATE

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C13H14Cl2O3
Molecular Weight	289.154
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC(C)(OC1=CC=C(C=C1)C2CC2(Cl)Cl)C(O)=O

InChI

InChIKey=KPSRODZRAIWAKH-UHFFFAOYSA-N

InChI=1S/C13H14Cl2O3/c1-12(2,11(16)17)18-9-5-3-8(4-6-9)10-7-13(10,14)15/h3-6,10H,7H2,1-2H3,(H,16,17)

HIDE SMILES / InChI

Molecular Formula	C13H14Cl2O3
Molecular Weight	289.154
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description

Ciprofibrate is an orally active phenoxyisobutyrate hypolipidemic compound. It acts by activating peroxisome proliferator activated receptor alpha. Ciprofibrate is efficacious for the correction of hyperlipidaemias.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Peroxisome proliferator-activated receptor alpha 62	Agonist 2,678		58.0 µM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hyperlipidemia 80	Primary		Approved 8,429	CIPROFIBRATE

C_max

Value	Dose	Analyte	Population
66 μg/mL	100 mg 1 times / day steady-state, oral	CIPROFIBRATE plasma	Homo sapiens
111 μg/mL	200 mg 1 times / day steady-state, oral	CIPROFIBRATE plasma	Homo sapiens
20.93 μg/mL	100 mg single, oral	CIPROFIBRATE plasma	Homo sapiens
24 μg/mL	100 mg single, oral	CIPROFIBRATE plasma	Homo sapiens
22 μg/mL	100 mg single, oral	CIPROFIBRATE plasma	Homo sapiens
17 μg/mL	100 mg single, oral	CIPROFIBRATE plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
1666 μg × h/mL	100 mg 1 times / day steady-state, oral	CIPROFIBRATE plasma	Homo sapiens
2832 μg × h/mL	200 mg 1 times / day steady-state, oral	CIPROFIBRATE plasma	Homo sapiens
818.58 μg × h/mL	100 mg single, oral	CIPROFIBRATE plasma	Homo sapiens
1370 μg × h/mL	100 mg single, oral	CIPROFIBRATE plasma	Homo sapiens
1759 μg × h/mL	100 mg single, oral	CIPROFIBRATE plasma	Homo sapiens
2445 μg × h/mL	100 mg single, oral	CIPROFIBRATE plasma	Homo sapiens
2431 μg × h/mL	100 mg single, oral	CIPROFIBRATE plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
104 h	100 mg 1 times / day steady-state, oral	CIPROFIBRATE plasma	Homo sapiens
96 h	200 mg 1 times / day steady-state, oral	CIPROFIBRATE plasma	Homo sapiens
81 h	100 mg single, oral	CIPROFIBRATE plasma	Homo sapiens
117 h	100 mg single, oral	CIPROFIBRATE plasma	Homo sapiens
172 h	100 mg single, oral	CIPROFIBRATE plasma	Homo sapiens
154 h	100 mg single, oral	CIPROFIBRATE plasma	Homo sapiens

F_unbound

Value	Dose	Co-administered	Analyte	Population
2%			CIPROFIBRATE plasma	Homo sapiens

Doses

Show entries

Dose	Population	Adverse events
100 mg 1 times / day multiple, oral Recommended	unhealthy, ADULT	Disc. AE: Alopecia, Somnolence...

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AEs

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AE	Significance	Dose	Population
Alopecia	1.2% Disc. AE	100 mg 1 times / day multiple, oral Recommended	unhealthy, ADULT
Fever	1.2% Disc. AE	100 mg 1 times / day multiple, oral Recommended	unhealthy, ADULT
Somnolence	1.2% Disc. AE	100 mg 1 times / day multiple, oral Recommended	unhealthy, ADULT

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PubMed

Show entries

Title	Date	PubMed
Use of dominant negative nuclear receptors to study xenobiotic-inducible gene expression in primary cultured hepatocytes.	2002 May-Jun	12628309
[Conjugation reactions of ciprofibrate with human and laboratory animals].	2003	12785120
[Long-term hypolipidemic treatment of mixed hyperlipidemia with a combination of statins and fibrates].	2003 Aug	14626567
Action of ciprofibrate in type IIb hyperlipoproteinemia: modulation of the atherogenic lipoprotein phenotype and stimulation of high-density lipoprotein-mediated cellular cholesterol efflux.	2003 Aug	12915663
Lipid-lowering drugs and serum liver enzymes: the effects of body weight and baseline enzyme levels.	2003 Aug	12914553