Pemafibrate

Chemical formula: C₂₈H₃₀N₂O₆ Molecular mass: 490.21 g/mol PubChem compound: 11526038

Interactions

Pemafibrate interacts in the following cases:

Strong CYP3A inducers

Drug	Clinical symptoms/Treatment	Mechanism/Risk factors
Strong CYP3A inducers Carbamazepine Phenobarbital Phenytoin Foods containing hypericum perforatum (St. John’s wort), etc.	The plasma concentration of pemafibrate may be decreased, which may reduce the efficacy of pemafibrate.	The strong induction of CYP3A by these drugs may accelerate the metabolism of pemafibrate.

Mild renal impairment, moderate renal impairment

In patients with renal impairment, renal function should be monitored periodically during treatment with pemafibrate.

Severe renal impairment

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

Mild hepatic disorder, history of hepatic disorder

Pemafibrate should be used with caution in patients with hepatic disorder (Child-Pugh grade A cirrhosis, etc.) or a history of hepatic disorder. Dose reduction should be considered as necessary.

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.

Statins

An increased risk of rhabdomyolysis has been reported with other fibrates when co-administered with an HMG-CoA reductase inhibitor (statin), especially in cases of pre-existing muscular disease. Pemafibrate should be used with caution in patients receiving statins.

Anion exchange resins

Drug	Clinical symptoms/Treatment	Mechanism/Risk factors
Anion exchange resins Cholestyramine Colestimide	Pemafibrate should be administered with the longest interval possible after the intake of anion exchange resins because the plasma concentration of pemafibrate may be decreased.	Pemafibrate may be absorbed onto anion exchange resins, and the absorption of pemafibrate may be reduced.

Clarithromycin, HIV protease inhibitors

Drug	Clinical symptoms/Treatment	Mechanism/Risk factors
Clarithromycin HIV protease inhibitors Ritonavir, etc.	Presumably due to inhibition of CYP3A, OATP1B1 and OATP1B3 by clarithromycin (or HIV protease inhibitors).

Clopidogrel sulfate

Drug	Clinical symptoms/Treatment	Mechanism/Risk factors
Clopidogrel sulfate	Concomitant administration of clopidogrel sulfate with pemafibrate resulted in an increase in the plasma concentration of pemafibrate Dose reduction of pemafibrate should be considered as necessary when used concomitantly with pemafibrate.	Presumably due to inhibition of CYP2C8 and OATP1B1 by clopidogrel sulfate.

Fluconazole

Drug	Clinical symptoms/Treatment	Mechanism/Risk factors
Fluconazole	Concomitant administration of fluconazole with pemafibrate resulted in an increase in the plasma concentration of pemafibrate	Presumably due to inhibition of CYP2C9 and CYP3A by fluconazole.

History of cholelithiasis

Since cholelithiasis has been reported, pemafibrate should be used with caution in patients with a history of cholelithiasis.

Pregnancy

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

Nursing mothers

The use of pemafibrate should be avoided in breast-feeding women. If the administration of pemafibrate is unavoidable, breast-feeding should be discontinued. An animal study (rat) has shown that pemafibrate is excreted in rat milk.

Carcinogenesis, mutagenesis and fertility

Fertility

No current data.

Effects on ability to drive and use machines

No studies of the effects of pemafibrate on a patient’s ability to drive, or to measure a reduced capacity to safely use machines have been performed.

Adverse reactions

Summary of the safety profile

In clinical studies conducted by the time of approval in Japan, adverse reactions were observed in 206 of 1,418 patients (14.5%). The most commonly reported adverse reactions included cholelithiasis observed in 20 patients (1.4%), diabetes mellitus in 20 patients (1.4%), and blood creatine phosphokinase increased in 12 patients (0.8%).

Summary of adverse reactions

Adverse reactions and frequencies observed in clinical studies conducted by the time of approval in Japan are listed below. If any of the following adverse reactions or similar is observed, the patients should be treated appropriately according to the symptoms.

	≥1%	≥0.1% to <1%
Liver	Cholelithiasis	Hepatic function abnormal, Aspartate aminotransferase increased, Alanine aminotransferase increased
Muscle		Blood creatine phosphokinase increased, Myoglobin blood increased, Myalgia
Skin		Rash, Itching
Others	Diabetes mellitus (including Diabetes mellitus aggravated)	Glycosylated haemoglobin increased, Low density lipoprotein increased, Blood uric acid increased

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