TAK-778, a derivative of ipriflavone, demonstrates the ability to stimulate bone growth in both in vitro and in vivo models.

In both in vitro and in vivo studies, TAK-778, a derivative of ipriflavone, effectively promotes bone growth. Continuous administration of TAK-778 (10 μM) from 1 to 21 days enhances the formation of mineralized nodules and markedly increases the activity of cellular Alkaline Phosphatase (ALP) at concentrations of 1 μM and above. It also modestly, yet significantly, elevates the DNA content at the cellular confluence stage. Additionally, TAK-778 treatment from days 5 to 7 leads to dose-dependent augmentations in soluble collagen and osteocalcin levels in the culture medium, as well as stimulates TGF-β and IGF-I secretion throughout the 21-day culture period. Although TAK-778 does not enhance ALP activity, it significantly boosts the saturated cell density in a concentration-dependent manner, with a noteworthy reduction observed at 10 μM[2].

TAK-778/PLGA-MC (a single local application,0.2 to 5 mg/site) results in a dose-dependent increase in the radio-opaque area formed in the defect. Histological studies show the defect area is occupied by a bony bridge and the newly-formed radio-opaque area corresponds to a calcified bone containing bone marrow cavities surrounded by thick osteoid seams with cuboidal osteoblasts. Two months after the operation, the TAK-778/PLGA-MC pellets induce radiological osseous union across the defects[2]. TAK-778 (Oral treatment of OVX rats)causes a more pronounced increase in bone mineral density (BMD) of the lumbar vertebrae compare to vehicle controls[3].