Comparative Safety of Bone Remodeling Agents with a Focus on Osteoporosis Therapies

Kleerekoper, Michael; Schein, Jeffrey

doi:10.1177/00912700122010050

Cited by 18 publications

(9 citation statements)

References 97 publications

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“…For example, tamoxifen and raloxifene are selective estrogen receptor modulators that work, at least in part, by antagonizing estrogen binding [1,2]. In addition to their use in the treatment of cancer, such estrogen receptor antagonists are beginning to be used for the treatment of cardiovascular diseases and osteoporosis [3,4].…”

Section: Introductionmentioning

confidence: 99%

Combination of receptor-binding assays and designed mutant receptors for discerning agonists and antagonists

Matsui¹

2007

Journal of Pharmaceutical and Biomedical Analysis

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Section: Introductionmentioning

confidence: 99%

Combination of receptor-binding assays and designed mutant receptors for discerning agonists and antagonists

Matsui¹

2007

Journal of Pharmaceutical and Biomedical Analysis

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“…Exposure to fluoride in drinking water has been shown to be beneficial for oral and general health, [1][2][3][4][5] especially in relation to dental caries and osteoporosis. In a study carried out in 21 cities in four states in the US, Dean et al 1 showed that exposure to water containing about 1 ppm fluoride in drinking water reduced caries experience by 50%.…”

mentioning

confidence: 99%

Fluoride Levels in Drinking Water in the Central Province of Saudi Arabia

et al. 2003

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Background: This study was designed to assess the fluoride levels in drinking water in the Central Province of Saudi Arabia. Materials and Methods: A total of 817 water samples were collected from 260 locations in Central Saudi Arabia. An atomic absorption spectrophotometer [HACH instrument, model DR 3000] was used in the analyses of water samples for fluoride levels. Results:The results showed that fluoride levels vary between 0.00 and 6.20 ppm. About 75% and 6% of the population in Riyadh and Qassim regions, respectively, were exposed to very low fluoride levels (0.00-0.30 ppm), while less than 3% of the population in both regions were exposed to fluoride levels ranging from 0.61 to 0.80 ppm. A higher percentage of the population in Qassim than Riyadh region were exposed to high fluoride levels (>0.81 ppm); 28.63% than in Riyadh with 9.24%. Conclusions: The findings of this study can serve as a baseline data for water fluoridation and other dental preventive programs in the area.

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“…Salmon calcitonin (sCT), a polypeptide hormone composed of 32 amino acids, is a potent inhibitor of osteoclastic resorption and is therapeutically efficacious when used in the treatments of metabolic bone-related diseases such as postmenopausal osteoporosis, Paget's disease, and hypercalcemia [Rodan and Martin, 2000;Kleerekoper and Schein, 2001]. Like other therapeutic peptides, sCT can only be administered by parenteral or nasal route because of its physicochemical instability, susceptibility to proteolysis, large molecular weight, and limited ability to traverse biological barriers [Wearley, 2001;Banga and Chien, 1988].…”

Section: Introductionmentioning

confidence: 99%

Enhancing effect of chemically conjugated deoxycholic acid on permeability of calcitonin in Caco-2 cells

Kim

Lee

et al. 2005

Drug Dev. Res.

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One approach for enhancing intestinal absorption of therapeutic peptides is chemical conjugation to bile acids. In this study, recombinant salmon calcitonin (sCT) was chemically modified by covalent attachment of deoxycholic acid (DOCA). Three different sCT-DOCA conjugates, namely, sCTmono-DOCA, sCT-di-DOCA, and sCT-tri-DOCA, were prepared and characterized for their structural and biological properties. The permeability of these conjugates in the gastrointestinal tract was evaluated using Caco-2 cell monolayers to determine their potential as an oral dosage form. The conjugates were isolated by reversed-phase fast protein liquid chromatography (FPLC) and confirmed by matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry. Circular dichroism spectra in 50% trifluoroethanol aqueous condition showed the ordered secondary structure of sCT-DOCA. The biological activities of sCT-DOCA conjugates were evaluated by cyclic AMP assay using T-47D cells, and the mean EC 50 values of sCT, sCT-mono-DOCA, and sCT-di-DOCA were 0.034, 0.076, and 0.46 nM, respectively. The transport experiments using the Caco-2 cell monolayer showed that the permeability of sCT-DOCA conjugates in buffer was not altered from the native sCT. However, the permeability of sCT-DOCA conjugates was increased up to 2.5 times that of the native sCT when sCT-DOCA was formulated in 1% dimethylsulfoxide (DMSO) solution. The conjugated DOCA of sCT-DOCA significantly enhanced the absorption of sCT-DOCA in the intestinal membrane when sCT-DOCA conjugates were completely solubilized by DMSO. In conclusion, this study proposes that therapeutic peptides that have poor absorption profiles could potentially be developed into orally active drugs by conjugation with DOCA in the formulation with appropriate solubilizing agents. Drug Dev. Res. 64:129-135, 2005.

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Comparative Safety of Bone Remodeling Agents with a Focus on Osteoporosis Therapies

Cited by 18 publications

References 97 publications

Combination of receptor-binding assays and designed mutant receptors for discerning agonists and antagonists

Combination of receptor-binding assays and designed mutant receptors for discerning agonists and antagonists

Fluoride Levels in Drinking Water in the Central Province of Saudi Arabia

Enhancing effect of chemically conjugated deoxycholic acid on permeability of calcitonin in Caco-2 cells

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