In vivo study and thermodynamic investigation of two lanthanum complexes, La(dpp)3 and La(XT), for the treatment of bone resorption disorders

摘要: Bone density diseases such as osteoporosis affect a significant number of people worldwide. Lanthanide ions are functional mimics calcium ions, able to substitute for Ca2+ in the bone mineral component, hydroxyapatite (HAP). undergoes continuous remodelling cycle and lanthanides can this cycle, exerting positive influence on mineral. We have been engaged efforts find new lanthanide containing complexes active agents treatment these identified two lead compounds, 3-hydroxy-1,2-dimethylpyridin-4(1H)-one (Hdpp) phosphinate-EDTA derivative, bis[[bis(carboxymethyl)amino]-methyl]phosphinate (H5XT). In paper, we report vivo data first time compounds. The pharmacokinetics La(dpp)3 suggest complex is rapidly cleared from plasma. demonstrate that La3+ accumulates following IV dose either or La(XT) investigated each chelating ligand incorporation into HAP using ITC HAP-binding studies.