Palovarotene an orally bioavailable retinoic acid receptor γ (RARγ) agonist.
1 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.
2 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).
3 It inhibits heterotopic ossification and preserves limb movement and growth in a
ACVR1R206H fibrodysplasia ossificans progressiva (FOP) mouse model.
4 Palovarotene (1 mg/kg per day for 14 days) decreases heterotopic ossification by 50 to 60% in a rat model of traumatic blast injury.
5 
