Gemfibrozil

Peroxisome Proliferator Receptor alpha Agonist — CARDIOVASCULAR SYSTEM

Key facts

Gemfibrozil is an ofp drug in the Peroxisome Proliferator Receptor alpha Agonist class catalogued in DrugCentral. It was first approved by the FDA in 1981. Its mechanism of action is classified as Peroxisome Proliferator-activated Receptor alpha Agonists. DrugCentral lists 8 molecular targets, including TTR, CYP2C8 and Fabp1. Recorded indications include Hypertriglyceridemia and Primary Prevention of Coronary Heart Disease.

• Approval status: ofp (first approved 1981 by the FDA).
• Drug class: Peroxisome Proliferator Receptor alpha Agonist.
• Mechanism of action: Peroxisome Proliferator-activated Receptor alpha Agonists.
• Molecular targets: TTR, CYP2C8, Fabp1 and CISD1 (8 listed in DrugCentral).
• Indications: Hypertriglyceridemia and Primary Prevention of Coronary Heart Disease.
• ATC code: C10AB04 (Fibrates).
• Molecular formula: C15H22O3; molecular weight 250.34 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Hypertriglyceridemia
• Primary Prevention of Coronary Heart Disease

Off-label uses (1)

• Hypoalphalipoproteinemia

Contraindications (10)

• Acute nephropathy
• Anemia
• Breastfeeding (mother)
• Calculus in biliary tract
• Disease of liver
• Disorder of gallbladder
• Impaired renal function disorder
• Leukopenia
• Primary biliary cirrhosis
• Thrombocytopenic disorder

Mechanism & targets

• Mechanism of action (MoA): Peroxisome Proliferator-activated Receptor alpha Agonists
• Established pharmacologic class: Peroxisome Proliferator Receptor alpha Agonist

Molecular targets (8)

Target	Gene	Action	Activity
Transthyretin	TTR	unknown	Kd 7.00
Cytochrome P450 2C8	CYP2C8	unknown	Ki 5.74
Fatty acid-binding protein, liver	Fabp1	unknown	Ki 5.73
CDGSH iron-sulfur domain-containing protein 1	CISD1	unknown	Ki 5.14
Cytochrome P450 2C9	CYP2C9	unknown	Ki 4.52
Peroxisome proliferator-activated receptor alpha	PPARA	agonist	EC50 4.23
Peroxisome proliferator-activated receptor gamma	PPARG	unknown	EC50 4.17
Lipoprotein lipase	LPL	unknown	—

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1981-12-21	FDA	—	PFIZER PHARMS

ATC classification

ATC code	Therapeutic hierarchy
C10AB04	CARDIOVASCULAR SYSTEM › LIPID MODIFYING AGENTS › LIPID MODIFYING AGENTS, PLAIN › Fibrates

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Rhabdomyolysis	1066.4
Blood creatine phosphokinase increased	225.3
Blood triglycerides increased	217.0
Acute kidney injury	207.4
Myocardial infarction	176.4
Coronary artery disease	175.6
Myalgia	166.7
Drug interaction	145.3
Cardiac failure congestive	131.5
Off label use	118.9
Pancreatitis	86.7
Drug hypersensitivity	83.6

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Gemfibrozil is on its molecule page.

• Molecular formula: C₁₅H₂₂O₃
• Molecular weight: 250.34 g/mol
• CAS number: 25812-30-0
• InChIKey: HEMJJKBWTPKOJG-UHFFFAOYSA-N
• PubChem CID: 3463

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

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Gemfibrozil used for?

DrugCentral lists the following indications for Gemfibrozil: Hypertriglyceridemia and Primary Prevention of Coronary Heart Disease.

How does Gemfibrozil work?

Gemfibrozil is classified as Peroxisome Proliferator-activated Receptor alpha Agonists; its molecular targets in DrugCentral include TTR, CYP2C8, Fabp1 and CISD1.

When was Gemfibrozil first approved?

Gemfibrozil was first approved by the FDA in 1981.

What drug class does Gemfibrozil belong to?

Gemfibrozil is in the Peroxisome Proliferator Receptor alpha Agonist class.

What is the chemical formula of Gemfibrozil?

Gemfibrozil has the molecular formula C15H22O3 and a molecular weight of 250.34 g/mol.

Sources

• DrugCentral drug card 1285 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL457 — compound record and bioactivity
• PubChem CID 3463 — chemical identifiers
• DrugBank DB01241 — drug record
• FDA UNII Q8X02027X3 — substance identity
• DailyMed: FDA labels for Gemfibrozil — current prescribing information (label search)
• UniProt P02766 (TTR) — target protein
• UniProt P10632 (CYP2C8) — target protein
• UniProt Q9NZ45 (CISD1) — target protein
• UniProt P11712 (CYP2C9) — target protein
• UniProt Q07869 (PPARA) — target protein
• UniProt P37231 (PPARG) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.