"目錄號: HY-14799
Palovarotene 是一種核視網(wǎng)膜酸受體γ (RAR-γ) 激動劑水评。
相關(guān)產(chǎn)品
Retinoic acid-Tamibarotene-AM580-Bexarotene-Fenretinide-AGN 194310-Tazarotene-Isotretinoin-TTNPB-Acitretin-Adapalene-AGN 195183-Magnolol-(R)-Flurbiprofen-AR7-
生物活性
Description
Palovarotene is a nuclear retinoic acid receptor γ (RAR-γ) agonist.
IC50& Target
RAR-γ[1]
In Vivo
Palovarotene suppresses post-traumatic chondrogenesis and osteogenesis and mitigated trauma-induced ectopic bone formation. Palovarotene inhibits subcutaneous and intramuscular heterotopic ossification (HO) in mice. Palovarotene is given orally for 14 days at 1 mg/kg/day starting on post-operative day (POD) 1 or POD-5, and HO amount, wound dehiscence and related processes are monitored for up to 84 days post injury. Compared to vehicle-control animals, Palovarotene significantly decreases HO by 50 to 60% regardless of when the treatment started and if infection is present[1]. Starting from day 1 of injury, half of the Acvr1cR206H/+mice are treated with Palovarotene by daily gavage for 14 days and the other half received vehicle as control. Analysis by mCT and 3D image reconstruction at day 14 shows that large HO tissue masses have formed in the targeted leg of Acvr1cR206H/+mutant mice receiving vehicle, but HO formation is greatly diminished in Palovarotene-treated companions by more than 80% based on bone volume/total volume quantification[2].
Clinical Trial
Clementia Pharmaceuticals Inc.
Fibrodysplasia Ossificans Progressiva
January 2016
Phase 2
Clementia Pharmaceuticals Inc.
Fibrodysplasia Ossificans Progressiva
November 2016
Phase 2
Clementia Pharmaceuticals Inc.
Fibrodysplasia Ossificans Progressiva
October 2014
Phase 2
Clementia Pharmaceuticals Inc.
Fibrodysplasia Ossificans Progressiva
July 2014
Phase 2
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References
