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Alendronate is an amino bisphosphonate that inhibits farnesyl pyrophosphate (FPP) synthase (IC50 = 50 nM for the recombinant human enzyme).1 It inhibits bone resorption in a pit formation assay using isolated rat osteoclasts (IC50 = 2 nM).2 Alendronate (3 and 10 µM) reduces angiotensin II-induced collagen I synthesis in isolated rat cardiac fibroblasts.3 It prevents femoral bone mineral density loss in ovariectomized rats when administered at a dose of 5 mg/kg.4 Formulations containing alendronate have been used in the treatment of osteoporosis and Paget's disease.
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1. Structure-
2. Bisphosphonates act on rat bone resorption through the mediation of osteoblasts. J. Clin. Invest. 91(5), 2004-2011 (1993).
3. Alendronate prevents angiotensin II-
4. Effects of continuous alendronate treatment on bone mass and mechanical properties in ovariectomized rats: Comparison with pamidronate and etidronate in growing rats. J. Pharmacol. Exp. Ther. 286(1), 128-135 (1998).