Clinical pharmacokinetics of the phosphate binder lanthanum carbonate

Clinical Pharmacokinetics

Volumn 47, Issue 9, 2008, Pages 553-563

  Damment, Stephen J P ^a   Pennick, Michael ^a  

^a Shire Pharmaceuticals   (United Kingdom)

Author keywords

Hyperphosphataemia; Lanthanum carbonate, pharmacokinetics; Phosphate binders, pharmacokinetics; Renal failure

Indexed keywords

ALUMINUM SALT; CALCIUM; CALCIUM ACETATE; CALCIUM CARBONATE; CIPROFLOXACIN; DIGOXIN; GADOLINIUM; LANTHANUM; LANTHANUM CARBONATE; MAGNESIUM; METOPROLOL; PHOSPHATE; PHOSPHATE BINDING AGENT; PLASMA PROTEIN; QUINOLINE DERIVED ANTIINFECTIVE AGENT; SEVELAMER; WARFARIN;

AREA UNDER THE CURVE; CLINICAL TRIAL; COMPLEX FORMATION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG EFFECT; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG MEGADOSE; DRUG PROTEIN BINDING; DRUG SAFETY; DRUG SOLUBILITY; DRUG TISSUE LEVEL; FIBROSIS; GASTROINTESTINAL ABSORPTION; HUMAN; HYPERPHOSPHATEMIA; MAXIMUM PLASMA CONCENTRATION; NEPHROGENIC SYSTEMIC FIBROSIS; NONHUMAN; PRECIPITATION; PRIORITY JOURNAL; REVIEW; SINGLE DRUG DOSE; STEADY STATE; TIME TO MAXIMUM PLASMA CONCENTRATION; TOXICITY TESTING; URINARY EXCRETION;

ANIMALS; BIOLOGICAL AVAILABILITY; CLINICAL TRIALS AS TOPIC; HUMANS; HYPERPHOSPHATEMIA; KIDNEY FAILURE, CHRONIC; LANTHANUM; PHOSPHATES; TISSUE DISTRIBUTION;

EID: 49549101560     PISSN: 03125963     EISSN: 03125963     Source Type: Journal    
DOI: 10.2165/00003088-200847090-00001     Document Type: Review

References (80)

1. Hruska KA, Lederer ED. Hyperphosphatemia and hypophosphatemia. In: Favus MJ, editor. Primer on the metabolic bone diseases and disorders on mineral metabolism. 5th ed. Washington, DC: American Society of Bone and Mineral Research, 2003: 296-306
2. Block GA, Klassen PS, Lazarus JM, et al. Mineral metabolism, mortality, and morbidity in maintenance hemodialysis. J Am Soc Nephrol 2004; 15: 2208-18
3. Goodman WG. The consequences of uncontrolled secondary hyperparathyroidism and its treatment in chronic kidney disease. Semin Dial 2004; 17: 209-16
4. US Renal Data System. 2004 annual data report: atlas of end-stage renal disease in the United States [online]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2004. Available from URL: http://www.usrds.org/adr_2004.htm [Accessed 2008 Jun 5]
5. Block GA, Hulbert-Shearon TE, Levin NW, et al. Association of serum phosphorus and calcium x phosphate product with mortality risk in chronic hemodialysis patients: a national study. Am J Kidney Dis 1998; 31: 607-17
6. Giachelli CM. Vascular calcification mechanisms. J Am Soc Nephrol 2004; 15: 2959-64
7. Moe SM. Vascular calcification and renal osteodystrophy relationship in chronic kidney disease. Eur J Clin Invest 2006; 36 Suppl. 2: 51-62
8. Blacher J, Guerin AP, Pannier B, et al. Arterial calcifications, arterial stiffness, and cardiovascular risk in end-stage renal disease. Hypertension 2001; 38: 938-42
9. Autissier V, Damment SJP, Henderson RA. Relative in vitro efficacy of the phosphate binders lanthanum carbonate and sevelamer hydrochloride. J Pharm Sci 2007; 96: 2818-27
10. Damment SJP, Webster I. The pharmacology of lanthanum carbonate (Fosrenol): a novel non-aluminium, non-calcium-based phosphate binder [poster]. 36th Annual Meeting of the American Society of Nephrology (ASN); 2003 Nov 12-17; San Diego (CA)
11. Finn WF. Lanthanum carbonate versus standard therapy for the treatment of hyperphosphatemia: safety and efficacy in chronic maintenance hemodialysis patients. Clin Nephrol 2006; 65: 191-202
12. Schäfer U, Jahreis G. Exposure, bioavailability, distribution and excretion of aluminum and its toxicological relevance to humans. Trace Elem Electrolytes 2006; 23: 162-72
13. Rostand SG, Sanders C, Kirk KA, et al. Myocardial calcification and cardiac dysfunction in chronic renal failure. Am J Med 1988; 85: 651-7
14. 3): an efficient and safe phosphate binder in haemodialysis patients? A 3-year study. Nephrol Dial Transplant 1993; 8: 530-4
15. Goodman WG, Goldin J, Kuizon BD, et al. Coronary-artery calcification in young adults with end-stage renal disease who are undergoing dialysis. N Engl J Med 2000; 342: 1478-83
16. Evans CH. Biochemistry of the lanthanides. New York: Plenum Press, 1990
17. 26Al-labelled aluminium citrate and aluminium hydroxide in volunteers. BioMetals 1996; 9: 221-8
18. Damment SJP, Pennick M. Systemic lanthanum is excreted in the bile of rats. Toxicol Lett 2007; 171: 69-77
19. Pennick M, Dennis K, Damment SJ. Absolute bioavailability and disposition of lanthanum in healthy human subjects administered lanthanum carbonate. J Clin Pharmacol 2006; 46: 738-46
20. Bioavailability and absorption half-life of lanthanum carbonate in dialysis patients. Data on file, Shire Pharmaceuticals, 2004
21. D'Haese PC, Behets GJ, De Broe ME, et al. Lanthanum pharmacokinetics: are rat data misleading? Kidney Int 2005; 67: 2907-8
22. Pennick M, Damment SJP, Gill M. The pharmacokinetics and tissue distribution of lanthanum carbonate (Fosrenol), a novel non-aluminium, non-calcium phosphate binder [poster]. 36th Annual Meeting of the American Society of Nephrology (ASN); 2003 Nov 12-17; San Diego (CA)
23. Pennick M, Damment SJP, Fiddler G, et al. Overview of the pharmacokinetics of lanthanum carbonate (Fosrenol): a novel non-aluminium, non-calcium phosphate binder [poster]. 36th Annual Meeting of the American Society of Nephrology (ASN); 2003 Nov 12-17; San Diego (CA)
24. Bronner F, Slepchenko BM, Pennick M, et al. A model of the kinetics of lanthanum in human bone, using data collected during the clinical development of the phosphate binder lanthanum carbonate. Clin Pharmacokinet 2008; 47: 543-52
25. Pennick M, Qiu P, Zhang P. A lanthanum carbonate pharmacodynamic dose response study in healthy volunteers [abstract]. In: ISN Nexus: The Bone and the Kidney; 2006 Oct 12-15; Copenhagen. Copenhagen: International Society of Nephrology, 2006: 25
26. Joy MS, Finn WF. Randomized, double-blind, placebo-controlled, dose-titration, phase III study assessing the efficacy and tolerability of lanthanum carbonate: a new phosphate binder for the treatment of hyperphosphatemia. Am J Kidney Dis 2003; 42: 96-107
27. Hutchison AJ, Maes B, Vanwalleghem J, et al. Efficacy, tolerability, and safety of lanthanum carbonate in hyperphosphatemia: a 6-month, randomized, comparative trial versus calcium carbonate. Nephron Clin Pract 2005; 100: c8-19
28. Plasma lanthanum concentrations in dialysis patients by average dose over 12 months: data from phase II and III studies. Data on file, Shire Pharmaceuticals, 2004
29. Data on file, Shire Pharmaceuticals, 1996
30. Magnusson G. The behavior of certain lanthanons in rats. Acta Pharmacol Toxicol (Copenh) 1963; 20 Suppl. 2: 1-95
31. Floren C, Tekaya L, Escaig F, et al. Analytical microscopy observations of rat enterocytes after oral administration of soluble salts of lanthanides, actinides and elements of group III-A of the periodic chart. Cell Mol Biol (Noisy-le-grand) 2001; 47: 419-25
32. Fehri E, Ayadi A, Boubaker S, et al. Lanthanides and microanalysis: effects of oral administration of two lanthanides: ultrastructural and microanalytical study [in French]. Arch Inst Pasteur Tunis 2005; 82: 59-67
33. Slatopolsky E, Liapis H, Finch J. Progressive accumulation of lanthanum in the liver of normal and uremic rats. Kidney Int 2005; 68: 2809-13
34. Lacour B, Lucas A, Auchere D, et al. Chronic renal failure is associated with increased tissue deposition of lanthanum after 28-day oral administration. Kidney Int 2005; 67: 1062-9
35. Bush VJ, Moyer TP, Batts KP, et al. Essential and toxic element concentrations in fresh and formalin-fixed human autopsy tissues. Clin Chem 1995; 41: 284-94
36. Bervoets AR, Behets GJ, De Broe ME, et al. Steady state liver lanthanum (LA) kinetics in chronic renal failure (CRF) rats are consistent with a transcellular lysosomal biliary excretion pathway [abstract]. J Am Soc Nephrol 2007; 18 (Abstracts Issue): 304A-5A
37. Hutchison AJ, Pratt RD. Lanthanum carbonate: no evidence of adverse effects on liver with up to 6 years of treatment in patients with stage 5 CKD [abstract]. J Am Soc Nephrol 2006; 17: 356A
38. Yang Z, Schryvers D, Roels F, et al. Demonstration of lanthanum in liver cells by energy-dispersive x-ray spectroscopy, electron energy loss spectroscopy and high-resolution transmission electron microscopy. J Microsc 2006; 223: 133-9
39. LeSage GD, Kost LJ, Barham SS, et al. Biliary excretion of iron from hepatocyte lysosomes in the rat: a major excretory pathway in experimental iron overload. J Clin Invest 1986; 77: 90-7
40. Gross Jr JB, Myers BM, Kost LJ, et al. Biliary copper excretion by hepatocyte lysosomes in the rat: major excretory pathway in experimental copper overload. J Clin Invest 1989; 83: 30-9
41. Kato M, Sugihara J, Nakamura T, et al. Electron microscopic study of the blood-brain barrier in rats with brain edema and encephalopathy due to acute hepatic failure. Gastroenterol Jpn 1989; 24: 135-42
42. Xu J, Ling EA. Studies of the ultrastructure and permeability of the blood-brain barrier in the developing corpus callosum in postnatal rat brain using electron dense tracers. J Anat 1994; 184 (Pt 2): 227-37
43. Greenwood J, Howes R, Lightman S. The blood-retinal barrier in experimental autoimmune uveoretinitis: leukocyte interactions and functional damage. Lab Invest 1994; 70: 39-52
44. McLeod C, Cox A, Bramall N. The need for contamination control in studies on lanthanum biodisposition. Kidney Int 2005; 68: 2906
45. Damment SJ. Incredulous effects of lanthanum? Toxicol Lett 2006; 168: 186-9
46. Damment SJP, Secker R, Cox AG. Lanthanum does not cross the blood-brain barrier: the need for stringent contamination controls in deposition studies [abstract]. Nephrol Dial Transplant 2006; 21 Suppl. 4: IV8
47. Altmann P, Barnett ME, Finn WF. Cognitive function in stage 5 chronic kidney disease patients on hemodialysis: no adverse effects of lanthanum carbonate compared with standard phosphate-binder therapy. Kidney Int 2007; 71: 252-9
48. Behets GJ, Verberckmoes SC, D'Haese PC, et al. Lanthanum carbonate: a new phosphate binder. Curr Opin Nephrol Hypertens 2004; 13: 403-9
49. Damment SJ, Shen V. Assessment of effects of lanthanum carbonate with and without phosphate supplementation on bone mineralization in uremic rats. Clin Nephrol 2005; 63: 127-37
50. D'Haese PC, Spasovski GB, Sikole A, et al. A multicenter study on the effects of lanthanum carbonate (Fosrenol) and calcium carbonate on renal bone disease in dialysis patients. Kidney Int Suppl 2003; 85: S73-8
51. Lanthanum concentrations in bone samples from patients treated with lanthanum carbonate over 4-5 years. Data on file, Shire Pharmaceuticals, 2004
52. Behets GJ, Verberckmoes SC, Oste L, et al. Localization of lanthanum in bone of chronic renal failure rats after oral dosing with lanthanum carbonate. Kidney Int 2005; 67: 1830-6
53. Grobner T, Prischl FC. Gadolinium and nephrogenic systemic fibrosis. Kidney Int 2007; 72: 260-4
54. Thakral C, Abraham JL. Automated scanning electron microscopy and x-ray microanalysis for in situ quantification of gadolinium deposits in skin. J Electron Microsc (Tokyo) 2007; 56: 181-7
55. Aime S, Canavese C, Stratta P. Advisory about gadolinium calls for caution in the treatment of uremic patients with lanthanum carbonate. Kidney Int 2007; 72: 1162-3
56. De Broe ME. Can the risk of gadolinium be extrapolated to lanthanum? Semin Dial 2008; 21: 142-4
57. Damment SJP, Secker R, Cox AG. Lanthanum does not cross the blood-brain barrier: the need for stringent contamination controls in deposition studies [abstract]. XLIII ERA-EDTA Congress; 2006 Jul 15-18; Glasgow
58. Cerny S, Kunzendorf U. Images in clinical medicine: radiographic appearance of lanthanum. N Engl J Med 2006; 355: 1160
59. Fosrenol®: summary of product characteristics. Basingstoke: Shire Pharmaceutical Contracts Ltd, 2007
60. Fiddler G, Taubel J, Webster I, et al. Lanthanum carbonate does not have a clinically significant effect on the pharmacokinetics of digoxin, warfarin, or metoprolol [poster]. World Congress of Nephrology; 2003 Jun 8-12; Berlin
61. Nix DE, Watson WA, Lener ME, et al. Effects of aluminum and magnesium antacids and ranitidine on the absorption of ciprofloxacin. Clin Pharmacol Ther 1989; 46: 700-5
62. Frost RW, Lasseter KC, Noe AJ, et al. Effects of aluminum hydroxide and calcium carbonate antacids on the bioavailability of ciprofloxacin. Antimicrob Agents Chemother 1992; 36: 830-2
63. Sahai J, Healy DP, Stotka J, et al. The influence of chronic administration of calcium carbonate on the bioavailability of oral ciprofloxacin. Br J Clin Pharmacol 1993; 35: 302-4
64. Kays MB, Overholser BR, Mueller BA, et al. Effects of sevelamer hydrochloride and calcium acetate on the oral bioavailability of ciprofloxacin. Am J Kidney Dis 2003; 42: 1253-9
65. How PP, Fischer JH, Arruda JA, et al. Effects of lanthanum carbonate on the absorption and oral bioavailability of ciprofloxacin. Clin J Am Soc Nephrol 2007; 2: 1235-40
66. Tapia R, Arias C, Morales E. Binding of lanthanum ions and ruthenium red to synaptosomes and its effects on neurotransmitter release. J Neurochem 1985; 45: 1464-70
67. Ishizawa M, Nitta H, Miyazaki E. Inhibitory action of lanthanum (La) on PGF2 alpha-induced contraction of guinea-pig stomach muscle. Prostaglandins 1980; 19: 407-13
68. Fawzi AB, McNeill JH. Effect of lanthanum on the inotropic response of isoproterenol: role of the superficially bound calcium. Can J Physiol Pharmacol 1985; 63: 1106-12
69. 2+ fluxes. Endocrinology 1980; 107: 1007-13
70. Foreman JC, Mongar JL. The action of lanthanum and manganese on anaphylactic histamine secretion. Br J Pharmacol 1973; 48: 527-37
71. Drueke T. Lanthanum carbonate as a first-line phospahte binder: the "cons". Semin Dial 2007; 20: 329-32
72. Damment SJ, Greaves P, Downes N. The toxicology of lanthanum carbonate (Fosrenol®): a novel non-aluminium, non-calcium phosphate binder [abstract]. J Am Soc Nephrol 2003; 14 (Abstracts Issue): 204A
73. Damment SJ, Beevers C, Gatehouse DG. Evaluation of the potential genotoxicity of the phosphate binder lanthanum carbonate. Mutagenesis 2005; 20: 29-37
74. Hutchison AJ, Barnett ME, Krause R, et al. Long-term efficacy and safety profile of lanthanum carbonate: results for up to 6 years of treatment. Nephron Clin Pract. In press
75. 2+ channel in 1,25-dihydroxyvitamin D3-responsive epithelia. J Biol Chem 1999; 274: 8375-8
76. Sprague SM. A comparative review of the efficacy and safety of established phosphate binders: calcium, sevelamer, and lanthanum carbonate. Curr Med Res Opin 2007; 23: 3167-75
77. Levine MA. Normal mineral homeostasis: interplay of parathyroid hormone and vitamin D. Endocr Dev 2003; 6: 14-33
78. Lotz M, Zisman E, Bartter FC. Evidence for a phosphorus-depletion syndrome in man. N Engl J Med 1968; 278: 409-15
79. Burke SK, Slatopolsky EA, Goldberg DI. RenaGel, a novel calcium- and aluminium-free phosphate binder, inhibits phosphate absorption in normal volunteers. Nephrol Dial Transplant 1997; 12: 1640-4
80. Damment SJP, Pennick M, Dennis K, et al. A new 1000 mg formulation of lanthanum carbonate effectively reduces urinary phosphorus excretion in healthy volunteers [abstract]. J Am Soc Nephrol 2005; 16 (Abstracts Issue): 550A