Seladelpar Lysine
[CAS# 928821-40-3]

Identification

• Classification: Biochemical >> Inhibitor >> Metabolism >> PPAR agonist
• Name: Seladelpar Lysine
• Synonyms: (2S)-2,6-diaminohexanoic acid;2-[4-[(2R)-2-ethoxy-3-[4-(trifluoromethyl)phenoxy]propyl]sulfanyl-2-methylphenoxy]acetic acid;dihydrate
• Molecular Formula: C₂₇H₄₁F₃N₂O₉S
• Molecular Weight: 626.68
• CAS Registry Number: 928821-40-3
• SMILES: CCO[C@H](COC1=CC=C(C=C1)C(F)(F)F)CSC2=CC(=C(C=C2)OCC(=O)O)C.C(CCN)C[C@@H](C(=O)O)N.O.O

Discovory and Applicatios

Seladelpar lysine is a novel compound derived from seladelpar, a selective peroxisome proliferator-activated receptor delta (PPAR-δ) agonist. Seladelpar has shown significant potential in treating metabolic and liver disorders, particularly primary biliary cholangitis (PBC). However, optimizing its pharmacokinetic properties and stability posed a challenge. The introduction of seladelpar lysine addresses these issues by conjugating seladelpar with the amino acid lysine, which enhances solubility, bioavailability, and therapeutic consistency.

The mechanism of action of seladelpar lysine relies on its selective activation of PPAR-δ. This receptor is involved in regulating lipid metabolism, inflammation, and bile acid homeostasis. By activating PPAR-δ, seladelpar lysine reduces hepatic inflammation, promotes bile flow, and mitigates cholestasis. These effects are crucial for patients with PBC, a progressive autoimmune liver disease that damages bile ducts and leads to fibrosis and cirrhosis if left untreated. Clinical trials have demonstrated that seladelpar lysine effectively reduces alkaline phosphatase (ALP) levels, a key biomarker of liver function, and alleviates symptoms such as pruritus and fatigue.

Seladelpar lysine has also shown potential in treating nonalcoholic steatohepatitis (NASH), a severe form of nonalcoholic fatty liver disease (NAFLD). NASH is characterized by inflammation, steatosis, and fibrosis caused by excessive fat accumulation in the liver. The compound's ability to modulate lipid metabolism and reduce hepatic inflammation makes it a promising candidate for managing NASH. Early-phase clinical trials indicate that seladelpar lysine improves liver enzyme levels, reduces steatosis, and decreases inflammatory markers, positioning it as a potential therapeutic option for this growing health concern.

The development of seladelpar lysine underscores the importance of optimizing drug formulations to overcome pharmacokinetic limitations. By conjugating seladelpar with lysine, researchers have created a compound with enhanced stability and absorption, facilitating more consistent dosing and improved patient outcomes. This innovation not only benefits patients with PBC and NASH but also opens avenues for exploring the compound's efficacy in other metabolic and inflammatory diseases.

Further research is ongoing to fully understand the long-term safety and efficacy of seladelpar lysine. The compound's favorable profile in clinical studies thus far highlights its potential to become a standard treatment option for liver diseases characterized by inflammation and impaired bile acid metabolism. The continued development of seladelpar lysine reflects a broader trend in pharmaceutical research aimed at refining existing therapeutics to address unmet medical needs and improve clinical outcomes.