REVIEW Risedronic acid monohydrate is a bisphosphonate used to strengthen bone, treat or prevent osteoporosis, and treat Paget's disease of bone. Its mode of action on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. It also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates such as risedronic acid appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover.
REFERENCES
[1]
Wieczorek, Maciej; Stawinski, Tomasz; Chrulski, Krzysztof Preparation of risedronic acid Eur. Pat. Appl. (2002), EP 1243592 A2 20020925.
[2]
Dembkowski, Leszek; Rynkiewicz, Robert; Rachon, Janusz; Makowiec, Stawomir; Przychodzen, Witold; Witt, Dariusz Process for the preparation of [1-hydroxy-2-(3-pyridinyl)ethylidene]bisphosphonic acid and hemi-pentahydrate monosodium salt thereof PCT Int. Appl. (2006), WO 2006071128 A1 20060706.
[3]
Adiyaman, Mustafa; Keskin, Huelya; Karliga, Bekir Process for the preparation of 3-pyridyl-1-hydroxyethylidene-1,1-biphosphonic acid and hydrated forms thereof PCT Int. Appl. (2007), WO 2007068678 A1 20070621.
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