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Ipriflavone
Author(s): Kitatani K, Morii H
Source: Nippon Rinsho. 1998; 56(6):1537-1543.

Abstract:

[Article in Japanese]

Ipriflavone (7-isopropoxyisoflavone), a non-hormonal isoflavone derivative, is currently used in several countries for prevention and treatment of postmenopausal osteoporosis. This compound is devoid of estrogenic activity in humans, but increases the activity of estrogens. Ipriflavone has been shown to be effective in reducing bone turnover rate mainly through an inhibition of bone resorption and stimulating of bone formation. Inhibitory effect of ipriflavone on bone resorption has been demonstrated both directly by the activation of mature osteoclast and the formation of new osteoclasts by stimulating estrogen-induced calcitonin secretion by thyroids in vivo. There is some evidence that ipriflavone has direct effect on bone formation. Several clinical studies have demonstrated that bone mineral density (BMD) was increased or maintained in patients treated with ipriflavone.

Effect of Chronic Treatment with Ipriflavone in Postmenopausal Women with Low Bone Mass

Author(s): Gennari C, Adami S, Agnusdei D, Bufal'ino L, Cervetti R, Crepaldi G, Di Marco C, Di Munno O, Fantasia L, Isaia GC, Mazzuoli GF, Ortolani S, Passeri M, Serni U, Vecchiet L
Source: Calcif Tissue Int. 1997; 61:Sl9-S22.

Abstract:

We present the results of two multicenter, double-blind, placebo-controlled, 2-year studies to evaluate the efficacy and tolerability of ipriflavone in postmenopausal women (PMW) with low bone mass. 453 PMW (aged 50-65 years) with a vertebral (VMD) or radial (RMD) mineral density value 1 SD lower compared with age-matched controls, were randomly selected to receive oral ipriflavone (200 mg T.I.D. at meals) or matching placebo, plus 1 g oral calcium daily. Vertebral (study A, by dual X-ray absorptiometry-DXA) and radial (study B, by dual photon absorptiometry-DPA) bone density, serum bone Gla-protein (BGP), and urinary hydroxyproline/creatinine (HOP/Cr) were measured every 6 months. In both studies, the Valid Completers (VC) analysis showed a maintenance of bone mass in ipriflavone-treated women, whereas in the placebo group, bone mineral density (BMD) was significantly decreased. The final outcome was a bone-sparing effect of 1.6% in study A, and of 3.5% in study B after 2 years. The Intention to Treat (ITT) analysis confirmed the decrease in the placebo group, with no changes in ipriflavone-treated women. A significant (P < 0.05) between-treatment difference was found in both studies.

Biochemical markers of bone turnover decreased in patients treated with ipriflavone, thus suggesting a reduction of bone turnover rate. Twenty-six women treated with ipriflavone and 28 receiving the placebo dropped out because of side effects, mainly gastrointestinal. The compliance to the oral long-term treatment was good. The results of these studies show that ipriflavone is able to prevent both axial and peripheral bone loss in PMW with low bone mass, and is well tolerated.

A Double Blind, Placebo-Controlled Trial of Ipriflavone for Prevention of Postmenopausal Spinal Bone Loss

Author(s): Agnusdei D, Crepaldi G, Isaia G, Mazzuoli G, Ortolani S, Passeri M, Bufalino L, Gennari

Source: Calcification Tissue International. 1997; 61(2):142-147.

Abstract:

One hundred ninety-eight postmenopausal women (aged 50-65 years) with vertebral bone density (VBD) 1 SD below the mean value for normal, age-matched, postmenopausal subjects were enrolled in six Italian centers and 134 completed 2 years of treatment. All subjects were randomly allocated to a 2-year treatment with oral ipriflavone (200 mg t.i.d.) or a matching placebo, according to a double-blind, parallel group design. All patients also received an oral daily calcium supplement of 1 g as calcium carbonate. VBD and markers of bone turnover were measured at baseline, and every 6 months. A complete routine analysis of liver and kidney functions along with hematological parameters were measured before and at the end of treatment period. The valid completers analysis showed a significant increase of VBD in ipriflavone-treated women with average percent changes of +1.4 after 1 year, and +1% at the end of treatment period (P < 0.05). The placebo group presented a significant decrease of VBD after 2 years of treatment (P < 0.05). The difference between treatments was significant (P < 0.01).

The intention to treat analysis confirmed the significant decrease of VBD in the placebo group, with no changes in ipriflavone-treated women. Skeletal ALP significantly decreased in ipriflavone-treated women (P < 0.05). Serum BGP and urine HOP/Cr showed a significant decrease only in ipriflavone-treated women, suggesting an inhibitory effect on bone turnover rate. Adverse reactions, mainly gastrointestinal, occurred to a similar extent in the two treatment groups. The evaluation of patients' compliance, assessed by residual tablets count, revealed a drug intake of more than 80% after 2 years in 92.5% and 92.8% of patients treated with ipriflavone or placebo, respectively. This study demonstrates that ipriflavone can prevent bone loss in postmenopausal women with low bone mass.

Effects of Combined Low Dose of the Isoflavone Derivative Ipriflavone and Estrogen Replacement on Bone Mineral Density and Metabolism in Postmenopausal Women

Author(s): Gambacciani M, Ciaponi M, Cappagli B, Piaggesi L, Genazzani AR

Source: Maturitas. 1997; 28(1):75-81.

Abstract:

OBJECTIVES: To assess the pattern of biochemical markers of bone metabolism and vertebral bone mineral density in early postmenopausal women treated with combined ipriflavone and low dose conjugated estrogens.

METHODS: Bone biochemical markers and vertebral bone density were evaluated in a longitudinal, comparative, 2 year study conducted in postmenopausal women treated with sole calcium supplementation (500 mg/day), or with either ipriflavone (IP) at the standard dose (600 mg/day) plus the same calcium dose, low dose conjugated estrogens (CE) (0.3 mg/day) plus calcium, or low dose IP (400 mg/day) plus low dose CE (0.3 mg/day) plus calcium. The results were analyzed by repeated measures analysis of variance, as appropriate.

RESULTS: No modifications of both urinary excretion of hydroxyproline and plasma osteocalcin levels were observed in calcium and in CE-treated women, while vertebral bone density significantly decreased (P < 0.0001) in both groups. In IP or IP + CE-treated women, plasma osteocalcin did not show any modification, while urinary hydroxyproline showed a significant (P < 0.05) decrease, that paralleled a significant (P < 0.05) increase in vertebral bone density.

CONCLUSION: Postmenopausal IP administration, at the standard dose of 600 mg/day, can prevent the increase in bone turnover and the decrease in bone density that follow ovarian failure. The same effect can be obtained with the combined administration of low dose (400 mg/day) IP with low dose (0.3 mg/day) CE.

These statements have not been evaluated by the Food and Drug Administration. These products are not intended to diagnose, treat, cure or prevent any disease.