Drug intelligence / Profile preview

polyprenoic acid

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

E-5166 is a **synthetic polyprenoic acid** compound and a member of the retinoid class. It has been shown to **inhibit the proliferation of keratinocytes** and various tumor cells in vitro, with effects superior to some aromatic retinoids. Mechanistically, E-5166 modulates epidermal differentiation by **augmenting beta-adrenergic adenylate cyclase response** (increasing epinephrine-induced cyclic AMP accumulation) while **decreasing histamine-induced cyclic AMP accumulation** in the skin, likely through a pathway similar to other retinoids. Its antiproliferative and differentiating activity has led to evaluated efficacy in experimental skin tumors and clinical studies in psoriasis. Unique among some retinoids, E-5166 required a higher dose for effect and was noted for a distinct safety profile where typical mucocutaneous side effects (like scaling and cheilitis) were less pronounced. E-5166 has also been observed to inhibit hydroxyl radical generation at therapeutic concentrations, suggesting antioxidant potential[1][2][3][5][11].

Other names
3,7,11,15-tetramethyl-2,4,6,10,14-hexadecapentaenoic acid
02

Targets

RARA (Retinoic acid receptor alpha)CRABP2 (Cellular retinoic acid-binding protein 2)

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