Seladelpar

Seladelpar is a peroxisome proliferator-activated receptor (PPAR)-delta (δ) agonist. However, the mechanism by which seladelpar exerts its therapeutic effects in patients with PBC is not well understood.

• LIVDELZI is indicated for the treatment of primary biliary cholangitis (PBC) in combination with ursodeoxycholic acid (UDCA) in adults who have had an inadequate response to UDCA, or as monotherapy in patients unable to tolerate UDCA. This indication is approved under accelerated approval based on a reduction of alkaline phosphatase (ALP) [see Clinical Studies (14) ] .

• None. None.contraindicated

The recommended dosage of LIVDELZI is 10 mg orally once daily. Administer LIVDELZI with or without food. ( 2.1 ) 2.1 Recommended Dosage and Administration The recommended dosage of LIVDELZI is 10 mg orally once daily. Administer LIVDELZI with or without food [see Clinical Pharmacology (12.3) ] . 2.2 Administration Modification for Bile Acid Sequestrants Administer LIVDELZI at least 4 hours before or 4 hours after taking bile acid sequestrants, or at as great an interval as possible [see Drug Interactions (7.1) ] .

Fractures : Consider the risk of fracture in patients treated with LIVDELZI. Monitor bone health according to current standards of care. ( 5.1 ) Liver Test Abnormalities : Obtain baseline clinical and laboratory liver assessments prior to starting LIVDELZI and monitor during treatment. Interrupt or discontinue LIVDELZI if the liver tests worsen. ( 5.2 ) Biliary Obstruction : Avoid use in patients with complete biliary obstruction. If biliary obstruction is suspected, interrupt LIVDELZI and treat as clinically indicated. ( 5.3 ) 5.1 Fractures Fractures occurred in 4% of LIVDELZI-treated patients compared to no placebo-treated patients [see Adverse Reactions (6.1) ] . Consider the risk of fracture in the care of patients treated with LIVDELZI and monitor bone health according to current standards of care. 5.2 Liver Test Abnormalities LIVDELZI has been associated with dose-related increases in serum transaminase (aspartate aminotransferase [AST] and alanine aminotransferase [ALT]) levels greater than 3-times upper limit of normal (ULN) in PBC patients receiving 50 mg once daily (5-times higher than the recommended dosage) and 200 mg (20-times higher than the recommended dosage) once daily. Transaminase levels returned to pretreatment levels upon LIVDELZI discontinuation. LIVDELZI 10 mg once daily did not show a similar pattern for increases in transaminase levels [see Overdosage (10) ] . Obtain baseline clinical and laboratory assessments at treatment initiation with LIVDELZI and monitor thereafter according to routine patient management.

The following clinically significant adverse reactions are described elsewhere in labeling: Fractures [see Warnings and Precautions (5.1) ] Liver Test Abnormalities [see Warnings and Precautions (5.2) ] Most common adverse reactions (reported in ≥5% and higher compared to placebo) are headache, abdominal pain, nausea, abdominal distension, and dizziness. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Gilead Sciences, Inc. at 1-800-GILEAD-5 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. In Trial 1, 193 patients were randomized to receive either LIVDELZI 10 mg (N=128) or placebo (N=65) once daily for 12 months [see Clinical Studies (14) ] . LIVDELZI or placebo was administered in combination with UDCA in 94% of patients and as monotherapy in 6% of patients who were unable to tolerate UDCA. Common Adverse Reactions Table 1 presents common adverse reactions that occurred in Trial 1. Table 1: Common Adverse Reactions Occurring Through Week 52 in Adult Patients with PBC (Trial 1) Included 12 patients (6%) who were intolerant to UDCA and initiated treatment as monotherapy: 8 patients (6%) in the LIVDELZI 10 mg arm and 4 patients (6%) in the placebo arm.

Hepatic Impairment: Monitor patients with cirrhosis for evidence of decompensation. Consider discontinuation if patient progresses to moderate or severe hepatic impairment (Child-Pugh B or C). ( 8.7 ) 8.1 Pregnancy Risk Summary There are insufficient data from human pregnancies exposed to LIVDELZI to allow an assessment of a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. In animal reproduction studies, no malformations or effects on embryo-fetal survival occurred in pregnant rats or rabbits after seladelpar treatment at exposures of up to 176-times and 49-times the recommended dose based on AUC (area under the plasma concentration-time curve), respectively. Reduction of fetal growth associated with maternal toxicity occurred in pregnant rabbits at 49-times the recommended dose based on AUC, but not at 3-times the recommended dose. In a pre- and postnatal development study in rats with maternal dosing of seladelpar during organogenesis through lactation, postnatal growth and pre-weaning survival of offspring was reduced at 115-times the recommended dose based on AUC, but not at the lower exposure of 16-times the recommended dose (see Data ) . The background risks of major birth defects and miscarriage for the indicated population are unknown.

Metabolism

Following a single dose administration, seladelpar systemic exposure increased dose-proportionally from 2 mg (0.2 times the recommended dosage) to 15 mg (1.5 times the recommended dosage) and greater than dose proportionally at higher doses. For a dose increase from 10 mg to 200 mg (20 times the recommended dosage), mean C max and mean AUC for seladelpar increased 70-fold and 27-fold, respectively.

PBC patients who received 5-times the recommended dosage or 20-times the recommended dosage of LIVDELZI experienced an increase in liver transaminases, muscle pain, and/or elevations in creatine phosphokinase, which resolved upon LIVDELZI discontinuation [see Warnings and Precautions (5.2) ] . There is no specific treatment for overdose with LIVDELZI. General supportive care of the patient is indicated, as appropriate. If indicated, elimination of unabsorbed drug should be achieved by emesis or gastric lavage; usual precautions should be observed to maintain the airway. Because seladelpar is highly bound to plasma proteins, hemodialysis should not be considered.

• Aug 14, 2024NDANDA217899Gilead Sciences Inc

1. 1Drug Ineffective2111%
2. 2Blood Alkaline Phosphatase Increased168.0%
3. 3Headache147.0%
4. 4Aspartate Aminotransferase Increased136.5%
5. 5Dizziness136.5%
6. 6Pruritus136.5%
7. 7Alanine Aminotransferase Increased126.0%
8. 8Hepatic Enzyme Increased105.0%
9. 9Diarrhoea94.5%
10. 10Abdominal Distension84.0%
11. 11Abdominal Pain73.5%
12. 12Nausea73.5%
13. 13Fatigue63.0%
14. 14Vomiting63.0%
15. 15Abdominal Pain Upper52.5%

The 10 most recently updated of 15 ClinicalTrials.gov registrations naming Seladelpar as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Patients With Primary Biliary Cholangitis(PBC)
  Active not recruiting · Observational · 30 enrolled · Fondazione Policlinico Universitario Agostino Gemelli IRCCS
  NCT07629128updated 2026-06-05
• Intended to Determine the Effects of Seladelpar on Normalization of Alkaline Phosphatase Levels in Subjects With Primary Biliary Cholangitis (PBC)
  Completed · Phase 3 · Interventional · 96 enrolled · Gilead Sciences
  NCT06060665updated 2026-06-04
• Seladelpar in Subjects With Primary Biliary Cholangitis (PBC) and Compensated Cirrhosis
  Recruiting · Phase 3 · Interventional · 318 enrolled · Gilead Sciences
  NCT06051617updated 2026-05-26
• An Open-Label Study Following Oral Dosing of Seladelpar to Participants With Primary Biliary Cholangitis (PBC) and Hepatic Impairment (HI)
  Completed · Phase 1 · Interventional · 24 enrolled · Gilead Sciences
  NCT04950764updated 2026-05-04
• Study of Seladelpar in Participants With Primary Biliary Cholangitis (PBC)
  Active not recruiting · Phase 3 · Interventional · 340 enrolled · Gilead Sciences
  NCT03301506updated 2026-05-04
• Clinical Characterization of Patients With Primary Biliary Cirrhosis Treated With Seladelpar in the Real-life Setting
  Not yet recruiting · Observational · 100 enrolled · University of Leipzig
  NCT07549607updated 2026-04-24
• Seladelpar in Adult Liver Transplant Recipients With Ischemic Cholangiopathy (SELIC).
  Not yet recruiting · Phase 2 · Interventional · 10 enrolled · University of California, San Diego
  NCT07305363updated 2026-04-09
• Monitoring the Response of Combination Ursodiol and Seladelpar Treatment
  Not yet recruiting · Observational · 100 enrolled · Methodist Health System
  NCT07122206updated 2025-08-14
• Study to Evaluate the Effects of Two Doses of Seladelpar (MBX-8025) in Subjects With Primary Biliary Cirrhosis (PBC)
  Terminated · Phase 2 · Interventional · 41 enrolled · Gilead Sciences
  NCT02609048updated 2025-02-25
• A Study to Evaluate the Safety, and Tolerability, and Efficacy of Seladelpar in Patients With PSC
  Terminated · Phase 2 · Interventional · 1 enrolled · Gilead Sciences
  NCT04024813updated 2025-01-16

Frequently asked questions

How does Seladelpar work?

Seladelpar is a peroxisome proliferator-activated receptor (PPAR)-delta (δ) agonist. However, the mechanism by which seladelpar exerts its therapeutic effects in patients with PBC is not well understood.

What is Seladelpar used for?

According to FDA labeling, Seladelpar carries indications including: LIVDELZI is indicated for the treatment of primary biliary cholangitis (PBC) in combination with ursodeoxycholic acid (UDCA) in adults who have had an inadequate response to UDCA, or as monotherapy in patients unable to tolerate UDCA. This indication is approved under accelerated approval based on a reduction of alkaline phosphatase (ALP) [see Clinical Studies (14) ] .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Seladelpar?

Seladelpar is classified as Other drugs for bile therapy, Peroxisome Proliferator-activated Receptor delta Agonists, Bile Secretion Alteration.

What are the brand names for Seladelpar?

Seladelpar is marketed under brand names including Livdelzi.

What are the contraindications for Seladelpar?

Seladelpar labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.