Risedronate sodium was launched as Actonel in the US for treatment of
Paget's disease. Risedronic acid is readily obtained by condensation of 2-(3-
pyridyl)acetic acid with phosphorous acid in presence of phosphorus
oxychloride. Risedronate sodium is an orally active bisphosphonate of third
generation, showing more potent bone antiresorptive properties than most of
prior bisphosphonates like etidronate which has been used for the same
indication since 1978. The biological mechanism by which Risedronate, and
generally bisphosphonates, act is not quite clear presently ; recent advances
have suggested that aminobisphosphonates interfere with the HMG-CoA
pathway and inhibit protein prenylation, causing apoptosis of osteoclasts and
macrophages. These apoptotic effects are correlated to the anti-resorptive
properties of this class of compounds. In a 2 month clinical trial involving
patients with Paget's desease, 30 mg risedronate daily achieved an appreciable
reduction of serum alkaline phosphatase levels, an indicator of bone
stabilization, in 77% of patients, compared with 11% on etidronate at 400 mg
daily for 6 months. Risedronate is also in development for the treatment and
prevention of various bone diseases, particularly post-menopausal and
corticosteroid-induced osteoporosis.
화학적 성질
Fine White to Off-White Crystalline Powder
용도
Risedronic Acid is a pyridinyl biphosphonate bone resorption inhibitor.
위험도
Human systemic effects.
생물학적 활성
Orally active biphosphonate that inhibits farnesyl diphosphate (FPP) synthase. Exhibits antiproliferative and proapoptotic activity in numerous tumor cell lines and inhibits osteoclast-mediated bone reabsorption in vivo .
