Generic
Pemafibrate
2 brands available in the market
At a glance
Pemafibrate is a selective PPARα modulator used as adjunctive therapy to diet to reduce TG in patients with dyslipidemia, including familial hyperlipidemia.
Description
Hypertriglyceridemia along with reduced HDL-C are risk factors of Atherosclerotic Cardiovascular Disease (ASCVD). Fibrates are considered the preferred treatment for reducing TG, acting by binding to and activating PPARα. Pemafibrate is a new selective PPARα modulator that is over 2,500-fold more potent than conventional fibrates, with high selectivity and strong receptor interaction.
Indications
- Dyslipidemia (hypertriglyceridemia)
- Familial hyperlipidemia
Therapeutic class
Anti-anginal & lipid lowering drugs
Pharmacological class
PPARα Modulator (Fibrate)
Pharmacology
Pemafibrate is a selective PPARα modulator containing benzoxazole and phenoxyalkyl side-chains along with a fibric acid group. It binds tightly to the PPARα receptor and provides maximum activation. It is over 2,500-fold more potent than conventional fibrates with high selectivity.
Mechanism of action
Binds to and activates PPARα receptors, reducing triglyceride levels and increasing HDL-C.
Dosage
Adult Dose (Oral):
- Usual dose: 0.1 mg twice daily
- Dose may be individualized according to patient's age and symptoms
- Renal impairment (eGFR <30 mL/min/1.73m²): Lower starting dose or prolonged dosing intervals; max 0.2 mg/day
Pediatric Dose: Safety not established.
Administration
- May be taken with or without food
- Take at the same time each day
- Follow the prescribed dose
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Side Effects:
- Gastro-intestinal disorders (nausea, diarrhea, abdominal pain)
- Jaundice
- Skin rashes
- Gallstones
- Myotoxicity
Precautions & warnings
- Rhabdomyolysis risk (with statins); suspect muscle toxicity if myalgia, myositis, muscle cramps, weakness, or CK >5 x ULN; discontinue treatment
- Caution in hepatic disorders; monitor liver function
- Caution in history of cholelithiasis
- Monitor LDL-cholesterol levels
Contraindications
- Hypersensitivity to pemafibrate or any excipients
- Severe hepatic disorder (Child-Pugh grade B or C cirrhosis, biliary obstruction)
- Cholelithiasis
- Pregnant or possibly pregnant women
- Concomitant treatment with cyclosporine or rifampicin
Drug interactions
- Other fibrates: Increased risk/severity of adverse effects
- Statins: Increased risk of myopathy or rhabdomyolysis
- Oral anticoagulants (warfarin): Pemafibrate may potentiate effects; increased bleeding risk; monitor coagulation parameters
Food interactions
Take with food for better absorption.
Use in pregnancy
Use in Pregnancy: Contraindicated in pregnant or possibly pregnant women; safety not established.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Should be avoided in breastfeeding women; if unavoidable, discontinue breastfeeding.
Pediatric use
Safety not established in children.
Geriatric use
Caution required in elderly patients; dose adjustment may be needed.
Renal / hepatic impairment
Renal Impairment: Caution with eGFR <30 mL/min/1.73m²; lower starting dose or prolonged intervals; max 0.2 mg/day.
Hepatic Impairment: Caution in severe hepatic disorder; plasma concentration may increase in Child-Pugh grade A cirrhosis.
Overdose effects
No overdose information available; consult your doctor if taken in excess.
Storage conditions
Do not store above 30°C; keep away from light; keep out of reach of children.
Chemical structure
Pemafibrate