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peretinoin

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

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

Targets

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

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