Drug intelligence / Profile preview

peretinoin

Development stage
Phase 3
Lead developer
Kowa
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Peretinoin is an orally available small molecule classified as an acyclic retinoid. It acts primarily by binding to and activating nuclear retinoic acid receptor (RAR) and retinoid X receptor (RXR), which leads to the recruitment of coactivator proteins and the promotion of transcription of target genes involved in cell differentiation and apoptosis[1][2][5]. Peretinoin has demonstrated potential antineoplastic and chemopreventive activities. It is being developed mainly for the prevention of recurrence in hepatocellular carcinoma (HCC) after curative therapy[5]. Additional research suggests it may suppress hepatitis B virus replication by modulating sphingosine metabolic pathways and enhance autophagy via increased Atg16L1 expression[6][8].

Brand names
peretinoin
Other names
acyclic retinoid(2E,4E,6E,10E)-3,7,11,15-tetramethylhexadeca-2,4,6,10,14-pentaenoic acid
02

Targets

RAR (Retinoic acid receptor)RXRA (Retinoid X receptor alpha)

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