Pemafibrate

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

Fibrates are considered as the preferred treatment for reducing TG. They act primarily by binding to and activating peroxisome proliferator activated receptor alpha (PPARα), a nuclear receptor. But conventional fibrates have low selectivity and potency for binding to PPARα. As a result, sometimes they fail to achieve desired TG level and often associated with various side effects.

Pemafibrate, a new selective PPARα modulator, is strongly effective in treating hypertriglyceridemia and low HDL-C levels. Its unique Y-shaped structure allows it to bind tightly to the PPARα receptor.

Pemafibrate structure contains benzoxazole and phenoxyalkyl side-chains along with common fibric acid group, which ensures-

• High selectivity for PPARα
• Strong interaction with the receptor
• Maximum activation of the receptor

Thus, Pemafibrate shows over 2,500-fold greater potency for PPARα compared to conventional fibrates and provides better therapeutic outcome.

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: The risk or severity of adverse effects can be increased when Pemafibrate is combined with other fibrates.

HMG CoA reductase inhibitors: Concurrent use with statins, which are commonly prescribed for lipid management, may increase the risk of muscle-related side effects such as myopathy or rhabdomyolysis.

Oral anticoagulant therapy: Patients taking anticoagulants such as warfarin should also be cautious, as Pemafibrate can potentiate the effects of these medications, increasing the risk of bleeding. Regular monitoring of coagulation parameters is recommended to adjust the anticoagulant dose as needed.

Pemafibrate is contraindicated in-

• patients with known hypersensitivity to Pemafibrate or to any of the excipients.
• patients with severe hepatic disorder, Child-Pugh grade B or C cirrhosis, or biliary obstruction
• patients with cholelithiasis
• pregnant or possibly pregnant women
• patients receiving concomitant
• cyclosporine or rifampicin

Gastro-intestinal disorder (e.g. nausea, diarrhoea, abdominal pain), jaundice, skin rashes, gallstones, myotoxicity.

Pregnancy: Pemafibrate is contraindicated in pregnant or possibly pregnant women. The safety of Pemafibrate has not
been established for use during pregnancy.

Breast-feeding: The use of Pemafibrate should be avoided in beast-feeding women. If the administration of Pemafibrate is unavoidable, breast-feeding should be discontinued.

An increased risk of rhabdomyolysis has been reported with other fibrates when co-administered with an HMG-CoA reductase inhibitor (statin), especially in case of pre-existing muscular disease. Pemafibrate should be used with caution in patients receiving statins. Muscle toxicity should be suspected in patients presenting diffuse myalgia, myositis, muscle cramps and weakness and/or marked increase in (CK>5 times the upper limit of normal range). In such cases, treatment with Pemafibrate should be stopped. Pemafibrate should be used with caution in patients with hepatic disorder or those with history of hepatic disorder. Abnormal liver function tests may occur. The plasma concentration of Pemafibrate may increase in patients with hepatic disorder (Child-Pugh grade A cirrhosis, etc). Liver function should be monitored periodically during treatment. Since cholelithiasis has been reported, Pemafibrate should be used with caution in patients with a history of cholelithiasis. Since increase in LDL-cholesterol levels may occur, LDL-cholesterol levels should be monitored periodically during treatment.

Do not store above 30°C. Keep away from light and out of the reach of children.