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Chemical Compound Review:

Tiludronate [(4-chlorophenyl)sulfanyl- phosphono...

Synonyms: acpmd, CHEMBL1350, AC1Q3OOE, SR-41319, BIDD:GT0814, ...

Barbier, A. et al., Emonds-Alt, X. et al., Schwietert, H.R. et al., Lafuma, A. et al., Chesnut, C.H., et al.

Lafuma, Fagnani, Meunier,

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Disease relevance of C08141

The clinical development of tiludronate (tiludronic acid, disodium salt) for the treatment of Paget's disease of bone is now being complemented by another clinical trials program to investigate its use in osteoporosis [1].
We conclude that SR 41319 may be a potentially useful drug for the treatment of rheumatoid arthritis [2].
Effect of (chloro-4-phenyl) thiomethylene bisphosphonic acid (SR 41319) on the autoimmune disease activity in MRL/l mice [3].

High impact information on C08141

Studies on the chronic phase of adjuvant arthritis: effect of SR 41319, a new diphosphonate [2].
Collagenase, neutral casein and proteoglycan-degrading proteinase secretion was inhibited by SR 41319, a new bisphosphonate, in a concentration-dependent manner [4].
The results suggest that the ability of SR 41319 to inhibit the MCF-mediated secretion of neutral enzymes involved in cartilage destruction could be valuable in the management of connective tissue damage in rheumatoid arthritis [4].
OBJECTIVES: A double-blind, placebo-controlled study was conducted to assess the pharmacokinetics and pharmacodynamics of the bisphosphonate tiludronic acid, administered once daily as sodium tiludronate 200, 400, 600 and 800 mg for 12 days [5].
Comparative study of etidronate and SR 41319, a new diphosphonate, on passive cutaneous anaphylaxis and phospholipase A2 activity [6].

Chemical compound and disease context of C08141

The objective of this study was to evaluate the long term comparative outcome of intermittent courses of therapy with low-dosage tiludronic acid (400 mg/day) versus etidronic acid in patients with Paget's disease of bone [7].

Biological context of C08141

Decrease in Ca entry into mast cells and anti-PLA2 activity of SR 41319 might partly explain the SR 41319 inhibition of PCA [6].

Associations of C08141 with other chemical compounds

Results showed that: (1) intravenously, SR 41319 induced a dose-dependent inhibition of PCA more pronounced than the EHDP one; (2) in PLA2 assay, marked inhibition was obtained with SR 41319 whereas EHDP was slightly active [6].

References

Tiludronate: development as an osteoporosis therapy. Chesnut, C.H. Bone (1995) [Pubmed]
Studies on the chronic phase of adjuvant arthritis: effect of SR 41319, a new diphosphonate. Barbier, A., Breliére, J.C., Remandet, B., Roncucci, R. Ann. Rheum. Dis. (1986) [Pubmed]
Effect of (chloro-4-phenyl) thiomethylene bisphosphonic acid (SR 41319) on the autoimmune disease activity in MRL/l mice. Barbier, A., Planchenault, C., Breliere, J.C. Agents Actions (1986) [Pubmed]
Effects of 1-hydroxyethylidene-1,1 bisphosphonate and (chloro-4 phenyl) thiomethylene bisphosphonic acid (SR 41319) on the mononuclear cell factor-mediated release of neutral proteinases by articular chondrocytes and synovial cells. Emonds-Alt, X., Brelière, J.C., Roncucci, R. Biochem. Pharmacol. (1985) [Pubmed]
Multiple dose pharmacokinetics of tiludronate in healthy volunteers. Schwietert, H.R., Peeters, P.A., Dingemanse, J., Thiercelin, J.F., Necciari, J., de Bruin, H., Jonkman, J.H. Eur. J. Clin. Pharmacol. (1996) [Pubmed]
Comparative study of etidronate and SR 41319, a new diphosphonate, on passive cutaneous anaphylaxis and phospholipase A2 activity. Barbier, A., Breliere, J.C., Paul, R., Roncucci, R. Agents Actions (1985) [Pubmed]
An economic evaluation of tiludronic acid treatment in Paget's disease of bone. Lafuma, A., Fagnani, F., Meunier, P.J. PharmacoEconomics. (1997) [Pubmed]

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