Drug intelligence / Profile preview

palmitoylethanolamide (Epitech Group)

Development stage
Unknown
Lead developer
Epitech
Modality
Small Molecules
Administration
Oral
01

Overview

Palmitoylethanolamide (PEA) is an endogenous fatty acid amide belonging to the class of N-acylethanolamines. The ultra-micronized formulation (um-PEA) is specifically engineered with a particle size distribution between 0.8 and 6.0 micrometers to overcome the poor water solubility and low bioavailability of the native compound. um-PEA acts primarily as a selective agonist of the peroxisome proliferator-activated receptor-alpha (PPAR-α). Activation of PPAR-α leads to the downregulation of pro-inflammatory genes and the reduction of mast cell degranulation, a process known as Autacoid Local Inflammation Antagonism (ALIA). Additionally, PEA exerts an entourage effect by inhibiting the degradation of the endocannabinoid anandamide via competition for fatty acid amide hydrolase (FAAH), thereby indirectly activating cannabinoid receptors (CB1, CB2) and TRPV1 channels. It is widely used as a medical food or nutraceutical for the management of chronic and neuropathic pain conditions, including sciatica, diabetic neuropathy, and pelvic pain.

Brand names
Normast
Other names
ultra-micronized palmitoylethanolamidepalmidrolN-palmitoylethanolaminePEA
02

Targets

CNR1 (Cannabinoid receptor 1)FAAHGPR119 (Glucose-dependent insulinotropic receptor)GPR55 (G protein-coupled receptor 55)PPARA (Peroxisome proliferator-activated receptor alpha)TRPV1 (Transient receptor potential cation channel subfamily V member 1)

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