Neridronic acid is an amino bisphosphonate that inhibits farnesyl pyrophosphate (FPP) synthase (IC50 = 388.2 nM in a cell-free assay).1 It decreases the differentiation of RAW 264.7 cells into osteoclasts in a CRL-12257 co-culture model of osteoclastogenesis when used at concentrations ranging from 0.001 to 100 ?M.2 Neridronic acid (30 ?M) inhibits FGF2-induced proliferation and tube formation in human umbilical vein endothelial cells (HUVECs).3 It reduces the loss of trabeculae and increases bone density in the tibial metaphysis of growing rats when administered subcutaneously at a dose of 0.1 mg/kg per day.4
1.Dunford, J.E., Kwaasi, A.A., Rogers, M.J., et al.Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: Time-dependent inhibition of human farnesyl pyrophosphate synthaseJ. Med. Chem.51(7)2187-2195(2008) 2.Nicolin, V., Bareggi, R., Baldini, G., et al.Effects of neridronic acid on osteoclasts derived by physiological dual-cell culturesActa Histochem.109(5)397-402(2007) 3.Ribatti, D., Nico, B., Mangieri, D., et al.Neridronate inhibits angiogenesis in vitro and in vivoClin. Rheumatol.26(7)1094-1098(2007) 4.Schenk, R., Eggli, P., Fleisch, H., et al.Quantitative morphometric evaluation of the inhibitory activity of new aminobisphosphonates on bone resorption in the ratCalcif. Tissue Int.38(6)342-349(1986)