Overview
Pemafibrate is a novel selective PPARα modulator developed to address hypertriglyceridemia, a condition characterized by elevated triglyceride levels in the blood. Unlike traditional fibrates, pemafibrate exhibits higher selectivity for PPARα receptors, reducing off-target effects such as liver toxicity or muscle-related adverse events. It was first approved in Japan in 2017 under the brand name Praluent® and is increasingly used in global markets due to its improved safety profile. As a B2B pharmaceutical raw material, pemafibrate is typically supplied as a tosilate salt (pemafibrate tosilate) to enhance stability and bioavailability. Its targeted mechanism of action makes it a preferred choice for patients with residual cardiovascular risk despite statin therapy.
Physical and Chemical Properties
Pemafibrate is a white to off-white crystalline powder with a molecular weight of 427.88 g/mol. It is soluble in dimethyl sulfoxide (DMSO) and other polar organic solvents but exhibits limited solubility in water, which influences its formulation as an oral tablet. The compound’s melting point ranges between 160-165°C, indicating moderate thermal stability. Key chemical features include a chlorophenoxy moiety and a carboxylic acid group, which contribute to its PPARα binding affinity. The tosilate salt form (CAS: 1240836-25-2) improves pharmacokinetic properties, ensuring consistent absorption in the gastrointestinal tract. Analytical methods like HPLC and mass spectrometry are commonly used for quality control during production.
Main Applications
Pemafibrate is primarily prescribed for patients with severe hypertriglyceridemia (triglyceride levels ≥500 mg/dL) to prevent pancreatitis. It is also used off-label for mixed dyslipidemia, often in combination with statins, to address residual cardiovascular risk. Clinical trials demonstrate its ability to reduce triglycerides by 45-60% while increasing HDL cholesterol. In research settings, pemafibrate serves as a tool compound to study PPARα-mediated pathways in metabolic diseases. Its selectivity minimizes confounding effects from PPARγ or PPARδ activation, making it valuable for mechanistic studies. Pharmaceutical manufacturers prioritize pemafibrate in fixed-dose combinations for metabolic syndrome management.
Safety and Storage
Pemafibrate should be stored in a cool (2-8°C), dry environment, protected from light and humidity to prevent degradation. Bulk quantities require airtight containers with desiccants to maintain stability. Handling precautions include using personal protective equipment (PPE) to avoid inhalation or skin contact, though its acute toxicity is low. Safety data sheets (SDS) highlight potential risks such as mild gastrointestinal disturbances or elevated liver enzymes in clinical use. Contraindications include severe hepatic impairment and pregnancy (Category X). Drug interactions are rare due to its low cytochrome P450 inhibition, but concomitant use with warfarin requires monitoring.
B2B Procurement Guide
When sourcing pemafibrate, B2B buyers should prioritize suppliers with GMP (Good Manufacturing Practice) certification to ensure pharmaceutical-grade quality. Key specifications include purity (≥98% by HPLC), residual solvent levels (e.g., <500 ppm for DMSO), and endotoxin testing for injectable formulations. Procurement contracts should clarify batch-specific COA (Certificate of Analysis) requirements and stability data. Prices vary by order volume; bulk purchases (1 kg+) may reduce costs by 20-30%. Due to patent restrictions in some regions, verify regulatory status to avoid legal complications. Preferred suppliers include specialized fine chemical manufacturers in Japan, India, and Europe.
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