Seladelpar is a peroxisome proliferator-activated receptor (PPAR)-δ agonist, which was approved in the United States in 2024 for the treatment of primary biliary cholangitis (PBC).
How to Use Seladelpar
Standard Dosage Regimen
Adults and adolescent patients with body weight ≥ 40 kg: 10 mg orally, once daily.
Administration method: May be taken with food or on an empty stomach.
Dosage form and specification: 10 mg opaque hard gelatin capsules (light gray capsule body and dark blue capsule cap).
Specific Administration Requirements
Combination therapy: Should be used in combination with ursodeoxycholic acid (UDCA) for adult PBC patients with an inadequate response to UDCA, or as monotherapy for patients intolerant to UDCA.
Contraindications: There are no absolute contraindications, but it is not recommended for patients with decompensated cirrhosis.
Baseline examination: Clinical and laboratory liver assessment results must be obtained before treatment.
Dosage Adjustment of Seladelpar
Principles for Managing Adverse Reactions
Fracture risk: The incidence during treatment is 4%, and bone health should be monitored in accordance with current standards.
Hepatic dysfunction: Treatment should be interrupted if ALT/AST > 3 × upper limit of normal (ULN); permanent discontinuation is required if hepatic function deteriorates again after treatment resumption.
Biliary obstruction: Treatment should be interrupted and clinical evaluation conducted if biliary obstruction is suspected.
Adjustments for Drug Interactions
Bile acid sequestrants: Administration should be separated by at least 4 hours.
OAT3 inhibitors: Concomitant use is prohibited (e.g., probenecid).
Strong CYP2C9 inhibitors: Concomitant use is prohibited.
Rifampicin: Biochemical indicators such as ALP and bilirubin should be monitored.
Seladelpar Administration in Special Populations
Patients with Hepatic Impairment
Child-Pugh Class A: No dosage adjustment is required.
Decompensated cirrhosis: Use is not recommended.
Monitoring requirements: Patients with cirrhosis need to be monitored for signs of decompensation; consideration should be given to discontinuing the drug if the condition progresses to Child-Pugh Class B/C.
Patients with Renal Impairment
Mild to moderate impairment (eGFR ≥ 30 mL/min/1.73m²): No dosage adjustment is required.
End-stage renal disease: Not yet studied; use with caution.
Geriatric Use
Aged 65–75 years: No dosage adjustment is required.
Aged > 75 years: Limited clinical experience; enhanced monitoring for adverse events is recommended.
Pregnancy and Lactation
Pregnancy risk: Animal studies have shown that high doses can affect fetal development; use is prohibited during pregnancy.
Contraception requirement: Effective contraception is required during treatment and for 5 months after the last dose.
Lactation: Breastfeeding is prohibited during treatment and for 5 months after discontinuing the drug.
Pediatric Use
Aged ≥ 12 years and body weight ≥ 40 kg: Adult dosage can be used.
Aged < 12 years or body weight < 40 kg: Efficacy has not been established.
