Palovarotene an orally bioavailable retinoic acid receptor γ (RARγ) agonist. It increases retinoic acid response element (RARE) activity and decreases NF-κB activity induced by IL-1β in primary mouse stromal cells in reporter assays when used at a concentration of 60 nM. Palovarotene (10 nM) inhibits activin A-induced chondrogenic and osteogenic differentiation of mouse fibro/adipogenic progenitors (FAPs) expressing a mutated form of human activin A receptor type I (ACVR1R206H). It inhibits heterotopic ossification and preserves limb movement and growth in a ACVR1R206H fibrodysplasia ossificans progressiva (FOP) mouse model. Palovarotene (1 mg/kg per day for 14 days) decreases heterotopic ossification by 50 to 60% in a rat model of traumatic blast injury.
Palovarotene, is a highly selective retinoic acid receptor gamma (RAR-γ) agonist that is under investigation as a potential treatment for emphysema.
ChEBI: Palovarotene is a stilbenoid.
