Nitroflurbiprofen inhibits bone resorption through a novel mechanism
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Inpharma 1315 - 24 Nov 2001 ■ Nitroflurbiprofen * inhibits bone resorption in mice, apparently by a novel mechanism that is distinct from its prostaglandin-inhibitory effects, say researchers from the UK and France. In an in vitro murine osteoblast/osteoclast coculture system, nitroflurbiprofen [HCT1026] was significantly more active than flurbiprofen in inhibiting osteoclast formation and bone resorption, with half-maximal effects on osteoclast formation in interleukin-1-stimulated cultures at approximately 20 µmol/L. ** However, the 2 drugs had similar inhibitory effects on prostaglandin production. When it was administered to ovariectomised mice, nitroflurbiprofen 12.5 mg/kg/day abolished the reduction in bone mineral content induced by ovariectomy, whereas flurbiprofen 7.5 mg/kg/day had no significant effect. * NicOx; phase II for treatment of postmenopausal osteoporosis, neurogenic bladder, Paget’s disease, skin disorders, urinary incontinence and urticaria ** The study was supported by NicOx SA. Armour KJ, et al. Inhibition of bone resorption in vitro and prevention of ovariectomy-induced bone loss in vivo by flurbiprofen nitroxybutylester (HCT1026). Arthritis and Rheumatism 44: 2185-2192, Sep 2001 800886210 1 Inpharma 24 Nov 2001 No. 1315 1173-8324/10/1315-0001/$14.95 Adis © 2010 Springer International Publishing AG. All rights reserved
Transcript of Nitroflurbiprofen inhibits bone resorption through a novel mechanism
Inpharma 1315 - 24 Nov 2001
■ Nitroflurbiprofen* inhibits bone resorption inmice, apparently by a novel mechanism that is distinctfrom its prostaglandin-inhibitory effects, sayresearchers from the UK and France. In an in vitromurine osteoblast/osteoclast coculture system,nitroflurbiprofen [HCT1026] was significantly moreactive than flurbiprofen in inhibiting osteoclastformation and bone resorption, with half-maximaleffects on osteoclast formation ininterleukin-1-stimulated cultures at approximately 20µmol/L.** However, the 2 drugs had similar inhibitoryeffects on prostaglandin production. When it wasadministered to ovariectomised mice, nitroflurbiprofen12.5 mg/kg/day abolished the reduction in bonemineral content induced by ovariectomy, whereasflurbiprofen 7.5 mg/kg/day had no significant effect.* NicOx; phase II for treatment of postmenopausal osteoporosis,neurogenic bladder, Paget’s disease, skin disorders, urinaryincontinence and urticaria** The study was supported by NicOx SA.
Armour KJ, et al. Inhibition of bone resorption in vitro and prevention ofovariectomy-induced bone loss in vivo by flurbiprofen nitroxybutylester(HCT1026). Arthritis and Rheumatism 44: 2185-2192, Sep 2001 800886210
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Inpharma 24 Nov 2001 No. 13151173-8324/10/1315-0001/$14.95 Adis © 2010 Springer International Publishing AG. All rights reserved
