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Pamidronate

帕米膦酸
Mechanism of action:
Pamidronate 是一種含氮雙磷酸鹽(nitrogen-containing bisphosphonate)衍生物。Pamidronate 會選擇性結合於骨表面的羥磷灰石,特別集中在骨吸收活躍的部位。當破骨細胞(osteoclast)進行骨吸收時,pamidronate 會隨骨基質被破骨細胞吞入細胞內。Pamidronate 在破骨細胞內會抑制法尼基焦磷酸合酶(farnesyl pyrophosphate synthase),阻斷異戊二烯化(prenylation)所需的中間產物生成。當小型 GTP 結合蛋白(如 Ras、Rho、Rab)無法進行異戊二烯化(prenylation)時,破骨細胞的多種代謝會受到抑制,最終導致破骨細胞凋亡。
Reference(s):
1. Zarychanski R et al. (2006). Osteonecrosis of the jaw associated with pamidronate therapy. Am J Hematol.
2. Cremers S et al. (2019). Pharmacology of bisphosphonates. Br J Clin Pharmacol.
3. Russell RG et al. (2008). Mechanisms of action of bisphosphonates: similarities and differences and their potential influence on clinical efficacy. Osteoporos Int.
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