Choline Fenofibrate

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Cat Number

API856676238

CAS Number

856676-23-8

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Product Detail Description Scientific Support Customer Q&A

CAS Number

856676-23-8

EINECS

629-768-0

Storage

Store at room temperature

Synonyms

UNII-4BMH7IZT98; Fenofibrate de choline; 2-Hydroxy-N,N,N-trimethylethanaminium 2-(4-(4-chlorobenzoyl)phenoxy)-2-methylpropanoate; Fenofibric acid choline salt; 4BMH7IZT98

Molecular Formula

C22H28ClNO5

Molecular Weight

421.9

Smiles

CC(C)(C(=O)[O-])OC1=CC=C(C=C1)C(=O)C2=CC=C(C=C2)Cl.C[N+](C)(C)CCO

Appearance

White to light yellow solid powder

Melting Point

210-212°C

Boiling Point

486.5°C at 760 mmHg

General Description

Choline fenofibrate is a choline salt of fenofibric acid, designed to enhance the aqueous solubility of the parent lipid‑lowering agent. The molecule dissociates in the gastrointestinal tract to release fenofibric acid, the active metabolite, and choline. The choline moiety acts as an essential nutrient and improves dissolution compared to conventional fenofibrate formulations that require micronization.

Mechanism of Action

Fenofibric acid activates peroxisome proliferator‑activated receptor alpha (PPAR‑α), which regulates genes involved in lipoprotein metabolism. Activation of PPAR‑α increases lipoprotein lipase activity, reduces apolipoprotein C‑III synthesis, and enhances fatty acid beta‑oxidation. These actions lower triglycerides, increase high‑density lipoprotein (HDL) cholesterol, and reduce small dense low‑density lipoprotein (LDL) particles.

Application

Choline fenofibrate is indicated as adjunctive therapy to diet for the treatment of severe hypertriglyceridemia and for mixed dyslipidemia (elevated triglycerides and LDL) in combination with a statin. It is particularly useful in patients who cannot achieve target lipid levels with statin monotherapy.

In male and female C57BL/6J mice with paclitaxel‑induced peripheral neuropathy (PIPN), fenofibrate (150 mg/kg i.p.) partially reversed and prevented mechanical hypersensitivity, while choline‑fenofibrate (60 mg/kg p.o.) completely reversed and prevented it. Both fibrates fully reversed and prevented cold hypersensitivity and restored sensory nerve action potential amplitude. The mechanism involved upregulation of PPAR‑α and decreased neuroinflammation in dorsal root ganglia. Co‑treatment with fenofibric acid did not reduce paclitaxel’s antitumor effect on cancer cell lines. Fibrates show therapeutic potential for PIPN repurposing.

Fig. 1 PPAR-α mRNA expression in DRG and spinal after paclitaxel injection. (Caillaud M, et al., 2021)

References

Caillaud M, et al. Targeting Peroxisome Proliferator-Activated Receptor-α (PPAR- α) to reduce paclitaxel-induced peripheral neuropathy. Brain Behav Immun. 2021;93:172-185.

Does Choline Fenofibrate require protection from moisture during storage?

Yes, it is moderately hygroscopic. Under high humidity, it may absorb moisture and clump, affecting flowability. Store in tightly sealed containers with desiccant.

What is the recommended storage temperature for Choline Fenofibrate?

Store at controlled room temperature (15-25°C). Avoid excessive heat above 30°C, which can accelerate hydrolysis of the choline salt to fenofibric acid.

Is Choline Fenofibrate stable in tablet formulations with standard excipients?

Yes, when formulated with moisture-protective packaging.

How is the impurity fenofibric acid (free acid from salt dissociation) monitored?

This degradation product is quantified using a stability-indicating HPLC method, ensuring it remains within ICH qualification thresholds.