Seladelpar is a novel peroxisome proliferator-activated receptor delta (PPAR-δ) agonist, which was approved in the United States in 2024 for the treatment of primary biliary cholangitis (PBC).
Indications for Seladelpar
Primary Biliary Cholangitis (PBC)
Seladelpar is indicated for use in combination with ursodeoxycholic acid (UDCA) for the treatment of adult patients with PBC who have an inadequate response to UDCA, or as monotherapy for patients who are intolerant to UDCA.
Its indication is based on the accelerated approval process, supported by the reduction in alkaline phosphatase (ALP) levels; however, its efficacy in improving survival or reducing hepatic decompensation events has not been confirmed.
Key Limitations
Contraindicated Populations: It is not recommended for patients with decompensated cirrhosis (e.g., ascites, variceal bleeding, hepatic encephalopathy).
Special Warnings: Vigilance is required regarding the risk of fractures (occurring in 4% of patients in clinical trials) and abnormal liver enzymes (transaminase elevation may occur at high doses).
Specifications and Properties of Seladelpar
Dosage Form Characteristics
Specification: Hard gelatin capsules containing 10mg of active ingredient per capsule, with an opaque light gray body and a dark blue cap. The cap is imprinted with "CBAY" and the body with "10".
Composition: The active ingredient is seladelpar lysine dihydrate, and the excipients include butylated hydroxytoluene, microcrystalline cellulose, etc. The capsule shell contains gelatin, titanium dioxide, and iron oxide colorants.
Pharmacological Properties
Pharmacological Action: It inhibits CYP7A1, a key enzyme in bile acid synthesis, by activating PPAR-δ, thereby reducing bile acid accumulation.
Metabolic Characteristics: It is mainly metabolized by CYP2C9, with a half-life of approximately 6 hours. 73.4% of the drug is excreted in urine (almost entirely as metabolites).
Storage Methods for Seladelpar
Routine Storage Conditions
Temperature: Store at 20°C to 25°C (68°F to 77°F); short-term storage at 15°C to 30°C (59°F to 86°F) is permitted.
Packaging: Supplied in original high-density polyethylene bottles with child-resistant caps, containing 30 capsules per bottle.
Usage Precautions
Light and Moisture Protection: Keep the bottle cap tightly sealed to prevent the capsules from absorbing moisture or being exposed to direct sunlight.
Expiration Management: It is recommended to use the capsules within 6 months after opening the bottle. If the capsules are deformed or leaking, they should be discarded immediately.
