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Research

Bisphosphonates in development for metabolic bone disease

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Pages 1255-1276 | Published online: 03 Mar 2008

References

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  • FLEISCH H: Diphosphonates: History and mechanisms of action. Metab Bone Dis. Rel. Res. (1981) 3:279-287.Good overview of history and early work on bisphosphonates.
  • FLEISCH H, RUSSELL RGG, BISAZ S, CASEY PA, MUHL-BAUER RC: The influence of pyrophosphate analogs (diphosphonates) on the precipitation and dissolution of calcium phosphate in vitro and in vivo. Calcif. Tissue Res. (1968) 2 (sup pl.) :10-10A.
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  • BRELIERE JC, EMONDS-ALT X, GARCIA G: Anti-inflamma-tory products derived from methylene diphosphonic acid and process for their preparation. United States Patent No. 4,876,248; (October 24) 1989.
  • ANONYMOUS: US launch for Ticlid soon. Scrip (1991)1675: 23.
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  • A very good review of the varying bone affinities in the phosphonoal-kyl phosphinate class of analogues.
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  • This is one of the best papers on the effects of a bisphosphonate in experimental arthritis. It includes colour pictures of histological sections.
  • ANONYMOUS: YM-175. Drugs Future (1992) 17:293–296.
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  • IBBOTSON KJ, D'SOUZA SM, BAYLESS A, EBRAHIMPOURA, EBETINO FH, WOODIEL FN, FALL PE, RAISZ LG: The phosphonate moieties of bisphosphonates are more than just a targeting function: evidence from the study of bisphosphonates analogues in vitro. Bone and Miner. (suppl. 1), S1-S92, S66
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  • Landmark paper examining the histologic response to antiresorptive bisphosphonates.
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  • This paper outlines structure-activity discoveries and how they were made temporally.
  • TAKEUCHI M, SAKAMOTO S, YOSHIDA M, ABE T, AND ISOMURA Y: Studies on novel bone resorption inhibi-tors. L Synthesis and pharmacological activities of aminomethylenebisphosphonate derivatives. Chem. Pharm. Bulk (1993) 41:688–693.
  • The best review, to date, of YM175 chemistry and its analogues.
  • MUHLBAUER RC, BAUSS F, SCHENK R, ETAL.: BM-21.0955,a potent new bisphosphonate to inhibit resorption. J. Bone Miner. Res. (1991) 6:1003–1011.
  • EBETINO FH, DANSEREAU SM: Bisphosphonates: Struc-ture activity relationships and therapeutic implica-tions. In: Bisphosphonate Therapy in Acute and Chronic Bone LOSS. Bijvoet OLM, Canfield R, Fleisch H, Russell RGG (Eds.). Elsevier, Amsterdam (In press).
  • POWELL JH, DEMARK BR: Clinical pharmacokinetics of diphosphonates. In: Bone Resorption, Metastasis, and Diphosphonates. Monographs of the Mario Negri Institute for Pharmacological Research. Garattini S (Ed). New York, NY: Raven Press, 1984:41–49.
  • This paper was the first to recognise the complexity of bisphosphon-ate compartmental modelling. The authors have taken data from published papers and re-analysed them using a non-compartmental approach more suited for bisphosphonte pharmacokinetics.
  • YAKATAN GJ, POYNOR WJ, TALBERT RL, ET AL.: CID- dronate kinetics and bioavailabRity. Clin PharmacoL Ther. (1982) 31:402–410.
  • Very comprehensive treatise of clodronate pharmacokinetics.
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  • UN JH, DUGGAN DE, CHEN IW, ELLSWORTH RL: Physi-ological disposition of alendronate, a potent an-tiosteolytk bisphosphonate, in laboratory animals. Drug Metab. Dispos. (1991) 19:926–932.
  • GERTZ, BJ, KLINE WF, MATUSZEWSKI BK, SACCO JF, LASSETER KC, PORRAS AG: Oral bioavailability and dose proportionality of alendronate (aminohydroxy-butylidene bisphosphonate) in postmenopausal women.]. Bone Miner. Res. (1991) 6\(suppl. 1):S281.
  • FOGELMAN I, SMITH L, MAZESS R, WILSON MA, BEVAN JA: Absorption of oral diphosphonate in normal subjects. Clin. Endocrinot (1986) 24:57–62.
  • NECCIARI J, TOUSSAIN P, FELS JP, DERBY G, LUYCKX A, SCHEEN A: Effect of food intake on kinetics and bioavail-ability of (4-chlorophenyl) thiomethylene bisphos-phonic acid. Calcif. Tissue Int. (1989) 44(suppl):S104.
  • EBRAHIMPOUR A, FRANCIS MD: Physical chemical con-siderations in bisphosphonate related therapeutics. In: Bisphosphonate Therapy in Acute and Chronic Bone Loss. Bijvoet OLM, Canfield R, Fleisch H, Russell RGG (Eds.). Elsevier, Amsterdam (In press).
  • HOGGARTH CR, BENNETT' R, DALEY-YATES PT: The phar- macokinetics and distribution of pamidronate for a range of doses in the mouse. Cakif. Tissue Int. (1991) 49:416–420.
  • A well-executed series of experiments looking at pharmacokinetics of bisphosphonates.
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  • MICHAEL WR, KING WR, WAKIM JM: Metabolism of diso- dium ethane-1-hydroxy-1,1-diphosphonate (disodium etidronate) in the rat, rabbit, dog, and monkey. Toxicol. Appl. Pharmacol (1972) 21:503515.
  • Very thorough review of etidronate metabolism in several species.
  • OSTERMAN T, LAUREN L: level of clodronate in bone after single and repeated subcutaneous injections in rats. Pharmacol. Toxicol. (1991) 69:369–371.
  • KASTING GB, FRANCIS MD: Retention of etidronate in human, dog, and rat.]. Bone Miner. Res. (1992) 7:513-522.An important paper on the theory behind accumulation of bisphos-phonate in bone tissue.
  • HUGHES DE, MIAN M, GUILLAND-CUMMING DF, RUSSELL RGG: The cellular mechanism of action of bisphos-phonates. Drugs Exp. Clin. Res. (1991) 17:109–114.
  • SATO M, GRASSER W: Effects of bisphosphonates on Isolated rat osteoclasts as examined by reflected light microscopy. Bone Miner. Res. (1990) 5:31–40.
  • GEDDES AD, D'SOUZA SM, EBETINO FH, IBBOTSON KJ: Bisphosphonates: structure-activity relationships and therapeutic implications. Reprint in: Bone and Mineral Research 1994. A regular survey of developments in the field of bone and mineral metabolism. Heersche JNM, Kanis JA (Eds.). Amsterdam, 1994. Volume 8. Elsievier Science BV; 1994: 265–306.
  • EBETINO FH, KAAS SM, CRAWFORD RJ: Bisphosphon- ates: Molecular modelling, structure-activity relation-ships and the rational design of new analogs. Phosphorus, Sulfur and Silicon (1993) 76:151–154.
  • An introduction of the structure activity data supporting a specific recognition event within the cellular mechanism of bisphosphonate antiresorptive activity.
  • BOONEKAMP PM, VAN DER WEE-PALS LJA, VAN WIJK-VANLENNEP MML, THESINGH CW, BIJVOET OLM: Two modes of action of bisphosphonates on osteoclastic resorption of mineralized matrix. Bone Miner (1986) 1:27–39.
  • FLANAGAN AM, CHAMBERS TJ: Dkhloromethylene-bisphosphonate (C12MBP) inhibits bone resorption through injury to osteoclasts that resorb C12MBP-coated bone. Bone Miner. (1989) 6:33–43.
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  • Very novel experiments suggesting new mechanism of action.
  • SAHNI M, GUENTHER, HL, FLEISCH H, COLLIN P, MARTINTJ: Bisphos phonates act on rat bone resorption through the mediation of osteoblasts. J. Clin. Invest. (1993) 91:2004–2011.
  • VITTE C, FLEISCH H, GUENTHER HL: Osteoblasts mediatethe bisphosphonate inhibition on bone resorption through synthesis of an osteoclast-inhibiting activity. Bone and Miner. (suppl.) S142.
  • ROGERS MJ, WATTS DJ, RUSSELL RGG, JI X, XTONG 3g,BLACKBURN M, BA'YLESS AV, EBETINO FH: Inhibitory effects of bisphosphonates on growth of amoebae of the cellular slime mold dictyostelium discoideum. Bone Miner. Res. (1993) 9(7):1029–1039.
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  • Dr. Parfitt is one of the world's two most renowned histomor- phometrists. This paper contains important discussion and perspec- tive on mechanisms of bone gain/loss during remodelling.
  • ERIKSEN EF: Normal and pathological remodeling of human trabecular bone: Three dimensional reconstruc- tion of the remodeling sequence in nortnals and in metabolic bone disease. Endocr. Rev. (1986) 7:379-408. Dr. Eriksen is the second of the world's two most renowned histomorphometrists. This paper outlines methods for histomor-phometric analysis of bone. Very technical.
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  • This landmark paper demonstrates that oestrogen prevents the loss of bone during the postmenopausal period but that when oestrogen therapy is discontinued, bone loss will resume at the same rate as if oestrogen were never given.
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  • SHIOTA E: Effects of diphosphonate on osteoporosis Induced in rats: Roentogenological, histological, and biomechanical studies. Fukuoka Igaku Zasshi (1985) 76:317–342.
  • ARAI M, TOGARI A, MATSUMOTO S: Femoral mechanical properties in rat: Effects of EHDP. Jpn. J. Pharmacol. (1990) 52\(suppl 1):303P.
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  • FERRETTI JL, COINTRY G, CAPOZZA R, MONTUORI E, ROLDAN E, PEREZ LLORET A: Biomechanical effects of the full range of useful doses of (3-amino-1-hy-droxypropylidene)-1,1-bisphosphonate (API)) on fe-mur diaphyses and cortical bone tissue in rats. Bone Miner. (1990) 11:111–122.
  • KAWAMUKI K, ABE T, KUDO M, ETAL.: Prophylactic and therapeutic effect of YM-175 on bone loss induced by ovariectomy and immobilization in rats. J. Bone Miner. Res. (1991) 6\(suppl. 1):S214.
  • FERRETI JL: Effects of bisphosphonates on bone biomechanics. In: Bisphosphonate Therapy in Acute andChronic Bone Loss. Bijvoet OLM, Canfield R, Fleisch H, Russell RGG (Eds.). Elsevier, Amsterdam (In press).
  • Excellent review of biomechanics and bisphosphonates.
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  • Good source of information on pamidronate.
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  • HOSKING DJ: Advances in the management of Paget's disease of bone. Drugs (1990) 40:829–840.
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  • This paper and the two following references were the first to report the fracture-reducing effects of etidronate.
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