TAK-778, a novel synthetic 3-benzothiepin derivative, promotes chondrogenesis in vitro and in vivo

TAK-778, a novel synthetic 3-benzothiepin derivative, stimulates the format ion of cartilaginous nodules in mouse chondroprogenitor-like ATDC5 cells in vitro in association with upregulation of the gene expression of transform ing growth factor-beta(2), but not bone morphogenetic protein-4 and insulin -like growth factor-I. One-shot injection of the TAK-778-containing sustain ed-release microcapsules accelerated the repair process of the full thickne ss defects of articular cartilage in rabbit knees. Our in vitro and in vivo results indicate that TAK-778 may be a therapeutically useful synthetic ag ent for articular cartilage repair. (C) 1999 Academic Press.