Pemafibrate tablet is indicated as an adjunctive therapy to diet to reduce triglyceride (TG) levels in patients with dyslipidemia, including familial hyperlipidemia.

Hypertriglyceridemia, particularly when associated with low HDL-C levels, is an important risk factor for atherosclerotic cardiovascular disease (ASCVD). Lifestyle factors such as physical inactivity and high-fat diets contribute to elevated triglyceride (TG) levels and make their control more challenging.

Fibrates are commonly used for lowering triglycerides and exert their effect mainly by activating peroxisome proliferator-activated receptor alpha (PPARα), a nuclear receptor. However, traditional fibrates have relatively low selectivity and binding strength for PPARα, which may limit their effectiveness and lead to undesirable side effects in some patients.

Pemafibrate is a newer, selective PPARα modulator that demonstrates high efficacy in reducing triglycerides and improving HDL-C levels. Its distinct Y-shaped molecular structure enables strong and selective binding to the PPARα receptor.

The molecular structure of pemafibrate includes benzoxazole and phenoxyalkyl side chains along with a fibric acid moiety, resulting in:

• High selectivity for PPARα
• Strong receptor binding affinity
• Enhanced activation of the receptor

As a result, pemafibrate exhibits over 2,500-fold greater potency for PPARα compared to conventional fibrates and offers improved therapeutic outcomes.

Adult dose: The usual adult dosage is 0.1 mg of pemafibrate orally administered twice daily. The dose may be individualized according to the patient’s age and symtoms. Pemafibrate can be taken with or without food.

Use in children: The safety of Pemafibrate in children has not been established.

Renal impairment: Pemafibrate should be used with caution in patients with renal impairment defined as estimated glomerular filtration rate (eGFR) less than 30 mg/min/1.73 m2. A lower starting dose or prolong dosing intervals should be considered. The maximum dose is 0.2 mg daily.

Hepatic impairment: Pemafibrate should be used with caution in patients with severe hepatic disorder

Other fibrates: Concomitant use of Pemafibrate with other fibrates may increase the likelihood or severity of adverse reactions.

HMG-CoA reductase inhibitors (statins): Combined use with statins may elevate the risk of muscle-related adverse effects, including myopathy and rhabdomyolysis.

Oral anticoagulants: Pemafibrate may enhance the effects of anticoagulants such as warfarin, increasing bleeding risk. Monitoring of coagulation parameters is advised, and dose adjustments may be required.

Pemafibrate is contraindicated in:

• Patients with known hypersensitivity to Pemafibrate or any of its excipients
• Patients with severe hepatic impairment (Child-Pugh class B or C) or biliary obstruction
• Patients with cholelithiasis
• Pregnant or potentially pregnant women
• Patients receiving concomitant cyclosporine or rifampicin

Adverse effects may include gastrointestinal disturbances (such as nausea, diarrhea, abdominal discomfort), jaundice, skin rashes, gallstones, and muscle toxicity.

Pregnancy: Pemafibrate is contraindicated in pregnant or potentially pregnant women, and its safety during pregnancy has not been established.

Breast-feeding: Use of Pemafibrate is not recommended during breastfeeding. If treatment is necessary, breastfeeding should be discontinued.

There is an increased risk of rhabdomyolysis when Pemafibrate is used with statins, especially in patients with pre-existing muscle disorders. Patients presenting with muscle pain, weakness, or elevated creatine kinase (CK) levels should be evaluated, and treatment should be discontinued if necessary. Pemafibrate should be used cautiously in patients with liver disease or a history of hepatic dysfunction. Liver function tests may become abnormal, so periodic monitoring is recommended. Plasma concentrations of Pemafibrate may be elevated in patients with hepatic impairment. Since gallstones have been reported, caution is advised in patients with a history of cholelithiasis. LDL-cholesterol levels may increase during therapy; therefore, regular monitoring is necessary.

Anti-anginal & lipid-lowering drugs

Store below 30°C, protected from light, and keep out of reach of children.