Therapeutic uses of gallium nitrate: Past, present, and future

American Journal of Therapeutics

Volumn 6, Issue 6, 1999, Pages 327-339

  Apseloff, Glen ^a  

^a THE OHIO STATE UNIVERSITY COLLEGE OF MEDICINE   (United States)

Author keywords

Antitumor activity; Autoimmune diseases; Clinical trials; Gallium nitrate; Pharmacokinetics; Toxicity

Indexed keywords

ANTINEOPLASTIC AGENT; ASPARTATE AMINOTRANSFERASE; BILIRUBIN; GALLIUM CITRATE; GALLIUM NITRATE; GAMMA INTERFERON; LIPOPOLYSACCHARIDE; NITRATE; NITRIC OXIDE; NITRIC OXIDE SYNTHASE; NITRITE; PROTEIN TYROSINE PHOSPHATASE; RIBONUCLEOTIDE REDUCTASE; TUMOR NECROSIS FACTOR ALPHA;

ADJUVANT ARTHRITIS; ALLERGIC ENCEPHALOMYELITIS; ANEMIA; ANTINEOPLASTIC ACTIVITY; AUTOIMMUNE DISEASE; CLINICAL TRIAL; DRUG MECHANISM; DRUG METABOLISM; GRAFT REJECTION; HUMAN; INFLAMMATION; INSULIN DEPENDENT DIABETES MELLITUS; INTRAVENOUS DRUG ADMINISTRATION; MALIGNANT NEOPLASTIC DISEASE; NEPHROTOXICITY; NONHUMAN; PAGET BONE DISEASE; PRIORITY JOURNAL; REVIEW; SEPSIS; SUBCUTANEOUS DRUG ADMINISTRATION; SYSTEMIC LUPUS ERYTHEMATOSUS; UVEITIS;

EID: 0032698628     PISSN: 10752765     EISSN: None     Source Type: Journal    
DOI: 10.1097/00045391-199911000-00008     Document Type: Review

References (120)

1. Delbarre F, Rabaud M: Prevention, chez le rat, de la polyarthrite experimentale a adjuvant, par un sel de gallium. Comptes Rendus Hebdomadaires des Seances de l'Academie des Sciences-D: Sciences Naturelles 1976;283:1469-1472.
2. Matkovic V, Balboa A, Clinchot D, et al: Gallium prevents adjuvant arthritis in rats and interferes with macrophage/T-cell function in the immune response. Curr Ther Res 1991;50:255-267.
3. Warrell RP Jr, Bosco B, Weinerman S, et al: Gallium nitrate for advanced Paget disease of bone: effectiveness and dose-response analysis. Ann Intern Med 1990; 113:847-851.
4. Matkovic V, Apseloff G, Shepard DR, Gerber N: Use of gallium to treat Paget's disease of bone: a pilot study. Lancet 1990;335:72-75.
5. Andrews GA, Root SW, Kerman HD: Clinical studies with gallium. Radiology 1953;61:570-588.
6. 72: summary and conclusions. Radiology 1953;61: 534-543.
7. Bedikian AY, Valdivieso M, Bodey GP, et al: Phase I clinical studies with gallium nitrate. Cancer Treat Rep 1978;62:1449-1453.
8. 72. Radiology 1953;61:537-543.
9. Lecoq de Boisbaudran P-E: Caracteres chimiques et spectroscopiques d'un nouveau metal, le Gallium, decouvert dans une blende de la mine de Pierrefitte, vallee d'Argeles (Pyrenees). Comptes rendus hebdomedaires des seances de l'academie de sciences. Paris 1875;81:493-495.
10. Lecoq de Boisbaudran P-E: Caracteres chimiques et spectroscopiques d'un nouveau metal, le gallium, decouvert dans une blende de la mine de Pierrefitte, vallee d'Argeles (Pyrenees). Bull Soc Chim Paris 1875; 24:370-371.
11. Lecoq de Boisbaudran P-E: Sur quelques proprietes du gallium. Comptes rendus hebdomedaires des seances de l'academie de sciences. Paris 1875;81:1100-1105.
12. The New Encyclopaedia Britannica, 15th ed., Encyclopaedia Britannica, Chicago, 1995, vol 7:232.
13. Bowers GN: The gallium melting-point standard: a new fixed point to assure the accuracy of temperature measurements in the clinical laboratory. Clin Chem 1977;23:709-710.
14. Berthelot M: Sur les chaleurs specifiques et la chaleur de fusion du gallium. Bull Soc Chim Paris 1879;31:229-230.
15. Lecoq de Boisbaudran P-E: Sur les alliages de gallium et d'aluminium. Bull Soc Chim Paris 1879;32:393-394.
16. Dupre MA: Recherches sur le gallium. Bull Soc Chim Paris 1878;30:503-504.
17. Levaditi C, Bardet J, Tchakirian A, Vaisman A: La repartition du gallium dans l'organisme. Comptes rendu des seances de l'academie des sciences 1931;193:117-119.
18. Nelson B, Hayes RL, Edwards CL, et al: Distribution of gallium in human tissues after intravenous administration. J Nucl Med 1972;13:92-100.
19. Dudley HC, Levine MD: Studies of the toxic action of gallium. J Pharmacol Exp Ther 1949;95:487-493.
20. Dudley HC: Determination of gallium in biological materials. J Pharmacol Exp Ther 1949;95:482-486.
21. Dudley HC, Garzoli RF: Preparation and properties of gallium lactate. J Am Chem Soc 1948;70:3942-3943.
22. 72) in skeletal tissues. J Pharmacol Exp Ther 1949; 96:224-227.
23. Dudley HC, Maddox GE, La Rue HC: Studies of the metabolism of gallium. J Pharmacol Exp Ther 1949;96: 135-138.
24. Dudley HC, Munn JI, Henry KE: Studies of the metabolism of gallium II. J Pharmacol Exp Ther 1950;98:105-110.
25. Dudley HC, Marrer HH: Studies of the metabolism of gallium III: deposition in and clearance from bone. J Pharmacol Exp Ther 1952;106:129-134.
26. Dudley HC, Henry KE, Lindsley BF: Studies of the toxic action of gallium II. J Pharmacol Exp Ther 1950;98:409-417.
27. Hart MM, Smith CF, Yancey ST, Adamson RH: Toxicity and antitumor activity of gallium nitrate and periodically related metal salts. J Natl Cancer Inst 1971;47: 1121-1127.
28. Warrell RP, Bockman RS, Coonley CJ, et al: Gallium nitrate inhibits calcium resorption from bone and is effective treatment for cancer-related hypercalcaemia. J Clin Invest 1984;72:1487-1490.
29. Warrell RP, Israel R, Frisone M, et al: Gallium nitrate for acute treatment of cancer related hypercalcaemia. Ann Intern Med 1988;108:669-674.
30. Warrell RP Jr, Alcock NW, Bockman RS: Gallium nitrate inhibits accelerated bone turnover in patients with bone metastases. J Clin Oncol 1987;5:292-298.
31. Warrell RP Jr, Skelos A, Alcock NW, Bockman RS: Gallium nitrate for acute treatment of cancer-related hypercalcemia: clinicopharmacological and dose response analysis. Cancer Res 1986;46:4208-4212.
32. Warrell RP Jr: Gallium nitrate for the treatment of bone metastases. Cancer 1997;80:1680-1685.
33. 67Ga citrate. J Nucl Med 1969;10:103-105.
34. Edwards CL, Hayes RL: Scanning malignant neoplasms with gallium 67. JAMA 1970;212:1182-1190.
35. Edwards CL, Nelson B, Hayes RL: Localization of gallium in human tumors. Clin Res 1970;18:39.
36. Adamson RH, Canelios GP, Sieber SM: Studies on the antitumor activity of gallium nitrate (NSC-15200) and other group IIIa metal salts. Cancer Chemother Rep 1975;59(Part 1):599-610.
37. Krakoff IH, Newman RA, Goldberg RS: Clinical toxicologic and pharmacologic studies of gallium nitrate. Cancer 1979;44:1722-1727.
38. Apseloff G, Girten B, Gerber N, et al: Lack of effect of gallium nitrate on bone density in a rat model of simulated microgravity. Aviat Space Environ Med 1992;63: 27-31.
39. Apseloff G, Girten B, Walker M, et al: Aminohydroxybutane bisphosphonate prevents bone loss in a rat model of simulated weightlessness. Curr Ther Res 1991;50:794-803.
40. Apseloff G, Girten B, Walker M, et al: Aminohydroxybutane bisphosphonate and clenbuterol prevent bone changes and retard muscle atrophy respectively in tail-suspended rats. J Pharmacol Exp Ther 1993;264:1071-1078.
41. Apseloff G, Girten B, Weisbrode SE, et al: Effects of aminohydroxybutane bisphosphonate on bone growth when administered after hind-limb bone loss in tail-suspended rats. J Pharmacol Exp Ther 1993;267:515-521.
42. Apseloff G, Shepard DR, Balboa A, et al: The effect of gallium nitrate on osteopenia in rats and postmenopausal women. Eur J Pharmacol 1990;183:1760-1761.
43. Whitacre C, Apseloff G, Cox K, et al: Suppression of experimental autoimmune encephalomyelitis by gallium nitrate. J Neuroimmunol 1992;39:175-182.
44. Orosz CG, Wakely E, Sergese SD, et al: Prevention of murine cardiac allograft rejection with gallium nitrate: comparison with anti-CD4 mAb. Transplantation 1996; 61:783-791.
45. Flynn JC, Serreze DV, Gerber N, Leiter EH: Chronic treatment of prediabetic non obese diabetic (NOD) mice with gallium nitrate protected against the development of diabetes. Diabetes 1992;41:38A.
46. Lobanoff MC, Kozhich AT, Mullet DI, et al: Effect of gallium nitrate on experimental autoimmune uveitis. Exp Eye Res 1997;65:797-801.
47. Apseloff G, Hackshaw K, Whitacre C, et al: Gallium nitrate suppresses lupus in MRL/lpr mice. Naunyn Schmiedeberg's Arch Pharmacol 1997;356:517-525.
48. Krecic ME, Shepard DR, Apseloff G, et al: Gallium nitrate attenuates lipopolysaccharide-induced hepatitis in Balb/c mice. FASEB J 1995;9:A944.
49. Thornton DD: The gallium melting-point standard: a determination of the liquid-solid equilibrium temperature of pure gallium on the International Practical Temperature Scale of 1968. Clin Chem 1977;23:719-724.
50. Bowers GN Jr, Inman SR: The gallium melting-point standard: its application and evaluation for temperature measurements in the clinical laboratory. Clin Chem 1977;23:733-737.
51. Sostman HE: The gallium melting-point standard: its role in manufacture and quality control of electronic thermometers for the clinical laboratory. Clin Chem 1977;23:725-732.
52. Magnum BW: The gallium melting-point standard: its role in our temperature measurement system. Clin Chem 1977;23:711-718.
53. Hillman LJ, Slavik M: Gallium nitrate. Clinical brochure. Investigational Drug Branch, Cancer Therapy Evaluation Program, Division of Cancer Treatment, National Cancer Institute, Bethesda, MD, 1976.
54. Physicians' Desk Reference, 51st ed., Medical Economics Company, Montvale, NJ, 1997, pp 2711-2712.
55. Hall SW, Yeung K, Benjamin RS, et al: Kinetics of gallium nitrate, a new anticancer agent. Clin Pharmacol Ther 1979;25:82-87.
56. Leyland-Jones B: Pharmacokinetics and therapeutic index of gallium nitrate. Semin Oncol 1991;18(Suppl 5): 16-20.
57. Kelsen DP, Alcock N, Yeh S, et al: Pharmacokinetics of gallium nitrate in man. Cancer 1980;46:2009-2013.
58. Kovar J, Seligman P, Gelfand EW: Differential growth-inhibitory effects of gallium on B-lymphocyte lines in high versus low iron concentrations. Cancer Res 1990; 50:5727-5730.
59. Schedle A, Samorapoompichit P, Rausch-Fan XH, et al: Response of L-929 fibroblasts, human gingival fibroblasts, and human tissue mast cells to various metal cations. J Dent Res 1995;74:1513-1520.
60. Chitambar CR, Zivkovic Z: Uptake of gallium-67 by human leukemic cells: demonstration of transferrin receptor-dependent and transferrin-independent mechanisms. Cancer Res 1987,47:3929-3934.
61. Gunasekera SW, King LJ, Lavender PJ: The behaviour of tracer gallium-67 towards serum proteins. Clin Chim Acta 1972;39:401-406.
62. Sephton RG, Harris AW: Brief communication: gallium-67 citrate uptake by cultured tumor cells, stimulated by serum transferrin. J Natl Cancer Inst 1975;54: 1263-1266.
63. Chitambar CR, Craig A, Ash RC: Transferrin receptor-mediated suppression of in vitro hematopoiesis by transferrin-gallium. Exp Hematol 1989;17:418-422.
64. Seligman PA, Kovar J, Gelfand EW: Lymphocyte proliferation is controlled by both iron availability and regulation of iron uptake pathways. Pathobiology 1992; 60:19-26.
65. Chitambar CR, Seligman PA: Effects of different transferrin forms on transferrin receptor expression, iron uptake, and cellular proliferation of human leukemic HL60 cells: mechanisms responsible for the specific cytotoxicity of transferrin-gallium. J Clin Invest 1986;78: 1538-1546.
66. Voet D, Voet JG: Biochemistry, 2nd ed., John Wiley & Sons, New York, 1995, p 807.
67. Chitambar CR, Narasimhan J, Guy J, et al: Inhibition of ribonucleotide reductase by gallium in murine leukemic L1210 cells. Cancer Res 1991;51:6199-6201.
68. Narasimhan J, Antholine WE, Chitambar CR: Effect of gallium on the tyrosyl radical of the iron-dependent M2 subunit of ribonucleotide reductase. Biochem Pharmacol 1992;44:2403-2408.
69. Santarossa S, Vaccher E, Lenardon O, et al: Ribonucleotide reductase inhibition in the treatment of advanced prostate cancer: an experimental approach with hydroxyurea and gallium nitrate in 20 patients. Eur J Cancer 1995;31A:1718.
70. Chitambar CR, Zivkovic-Gilgenbach Z, Narasimhan J, Antholine WE: Development of drug resistance to gallium nitrate through modulation of cellular iron uptake. Cancer Res 1990;50:4468-4472.
71. Berggren MM, Burns LA, Abraham RT, Powis G: Inhibition of protein tyrosine phosphatase by the antitumor agent gallium nitrate. Cancer Res 1993;53:1862-1866.
72. Seligman PA, Moran PL, Schieicher RB, Crawford ED: Treatment with gallium nitrate: evidence for interference with iron metabolism in vivo. Am J Hematol 1992; 41:232-240.
73. Chitambar CR, Zahir SA, Ritch PS, Anderson T: Evaluation of continuous-infusion gallium nitrate and hydroxyurea in combination for the treatment of refractory non-Hodgkin's lymphoma. Am J Clin Oncol 1997; 20:173-178.
74. Larson SM: Mechanisms of localization of gallium-67 in tumors. Semin Nucl Med 1978;8:193-203.
75. Mills BG, Masuoka LS, Graham CC Jr, et al: Gallium-67 citrate localization in osteoclast nuclei of Paget's disease of bone. J Nucl Med 1988;29:1083-1087.
76. Chitambar CR, Wereley JP, Riaz-Ul-Haq: Synergistic inhibition of T-lymphoblastic leukemic CCRF-CEM cell growth by gallium and recombinant human α-interferon through action on cellular iron uptake. Cancer Res 1994;54:3224-3228.
77. Krecic-Shepard ME, Shepard DR, Mullet D, et al: Gallium nitrate suppresses the production of nitric oxide and liver damage in a murine model of LPS-induced septic shock. Life Sci 1999;65:1359-1371.
78. 67Ga-citrate (1st report). Jpn J Nucl Med 1969;6:217-226.
79. Brown J, Santos E, Rosen G, et al: Phase I study of gallium nitrate in patients with advanced cancer. Proc Am Assoc Cancer Res Am Soc Clin Oncol 1978;19:198.
80. Lundberg JH, Chitambar CR: Interaction of gallium nitrate with fludarabine and iron chelators: effects on the proliferation of human leukemic HL60 cells. Cancer Res 1990;50:6466-6470.
81. Keller J, Bartolucci A, Carpenter JT Jr, Feagler J: Phase II evaluation of bolus gallium nitrate in lymphoproliferative disorders: a Southeastern Cancer Study Group trial. Cancer Treat Rep 1986;70:1221-1223.
82. Weick JK, Stephens RL, Baker LH, Jones SE: Gallium nitrate in malignant lymphoma: a Southwest Oncology Group Study. Cancer Treat Rep 1983;67:823-825.
83. Warrell RP, Coonley CJ, Straus DJ, Young CW: Treatment of patients with advanced malignant lymphoma using gallium nitrate administered as a seven-day continuous infusion. Cancer 1983;51:1982-1987.
84. Malfetano JH, Blessing JA, Adelson MD: A phase II trial of gallium nitrate (NSC #15200) in previously treated ovarian carcinoma. Am J Clin Oncol 1991;14: 349-351.
85. Malfetano JH, Blessing JA, Homesley HD: A phase II trial of gallium nitrate (NSC #15200) in nonsquamous cell carcinoma of the cervix: a Gynecologic Oncology Group study. Am J Clin Oncol 1995;18:495-497.
86. Warrell RP Jr, Danieu L, Coonley CJ, Atkins C: Salvage chemotherapy of advanced lymphoma with investigational drugs: mitoguazone, gallium nitrate, and etoposide. Cancer Treat Rep 1987;71:47-51.
87. Roth BJ: Chemotherapy for advanced bladder cancer. Semin Oncol 1996;23:633-644.
88. Seidman AD, Scher HI, Heinemann MH, et al: Continuous infusion gallium nitrate for patients with advanced refractory urothelial tract tumors. Cancer 1991;68:2561-2565.
89. McCaffrey JA, Hilton S, Mazumdar M, et al: Phase II randomized trial of gallium nitrate plus fluorouracil versus methotrexate, vinblastine, doxorubicin, and cisplatin in patients with advanced transitional-cell carcinoma. J Clin Oncol 1997;15:2449-2455.
90. Dreicer R, Propert KJ, Roth BJ, et al: Vinblastine, ifosfamide, and gallium nitrate - an active new regimen in patients with advanced carcinoma of the urothelium: a phase II trial of the Eastern Cooperative Oncology Group (E5892). Cancer 1997;79:110-114.
91. Pelletier RP, Morgan CJ, Sedmak DD, et al: Analysis of inflammatory endothelial changes, including VCAM-1 expression, in murine cardiac grafts. Transplantation 1993;55:315-320.
92. Nussenblatt RB, Rodrigues MM, Wacker WB, et al: Cyclosporin A: inhibition of experimental autoimmune uveitis in Lewis rats. J Clin Invest 1981;67:1228-1231.
93. Wacker WB, Donoso LA, Kalsow CM, et al: Experimental allergic uveitis: isolation, characterization, and localization of a soluble uveitopathogenic antigen from bovine retina. J Immunol 1977;119:1949-1958.
94. Bartlett RR, Popovic S, Raiss RX: Development of autoimmunity in MRL/lpr mice and the effects of drugs on this murine disease. Scand J Rheumatol 1988;75 (Suppl):290-299.
95. Cohen PL, Eisenberg RA: Lpr and gld: single gene models of systemic autoimmunity and lymphoproliferative disease. Annu Rev Immunol 1991;9:243-269.
96. Wayte J, Silva AT, Krausz T, Cohen J: Observations on the role of tumor necrosis factor-alpha in a murine model of shock due to Streptococcus pyogenes. Crit Care Med 1993;21:1207-1212.
97. Makkonen N, Hirvonen MR, Savolainen K, et al: The effect of free gallium and gallium in liposomes on cytokine and nitric oxide secretion from macrophage-like cells in vitro. Inflamm Res 1995;44:523-528.
98. Evans T, Carpenter A, Kinderman H, Cohen J: Evidence of increased nitric oxide production in patients with the sepsis syndrome. Circ Shock 1993;41:77-81.
99. Kung TT, Jones H, Adams III GK, et al: Characterization of a murine model of allergic pulmonary inflammation. Int Arch Allergy Immunol 1994;105:83-90.
100. Apseloff G, LeRoy B, Weisbrode SE, et al: Gallium nitrate ameliorates asthma in B6D2F1/J mice. FASEB J 1996;10:A441.
101. Tassava RA, McCullough WD: Neural control of cell cycle events in regenerating salamander limbs. Am Zool 1978;18:843-854.
102. Aaronson OS, Golding JP, Tonge DA: Oriented growth of regenerating axons in axolotl forelimbs is consistent with guidance by diffusible factors from distal nerve stumps. Neuroscience 1995;66:201-213.
103. Matkovic V, Apseloff G, Shepard DR, et al: Effects of gallium nitrate on bone turnover and serum lipid levels in postmenopausal women. Curr Ther Res 1991;50:247-254.
104. Stern LS, Matkovic V, Weisbrode SE, et al: The effects of gallium nitrate on osteopenia induced by ovariectomy and a low-calcium diet in rats. Bone Miner 1994;25:59-69.
105. Liewehr FR, Craft DW, Primack PD, et al: Effect of bisphosphonates and gallium on dentin resorption in vitro. Endod Dent Traumatol 1995;11:20-26.
106. Bockman RS, Bosco B: Treatment of patients with advanced Paget's disease of bone with two cycles of gallium nitrate. Semin Arthritis Rheum 1994;23:268-269.
107. Newman RA, Brody AR, Krakoff IH: Gallium nitrate (NSC-15200) induced toxicity in the rat: a pharmacologic, histopathologic and microanalytical investigation. Cancer 1979;44:1728-1740.
108. Bruner HD, Cooper BM, Rehbock DJ: Toxicity of gallium citrate in dogs and rats. Radiology 1953;61:550-555.
109. Csaky KG, Caruso RC: Gallium nitrate optic neuropathy. Am J Ophthalmol 1997;124:567-568.
110. Hughes TE, Hansen LA: Gallium nitrate. Ann Pharmacother 1992;26:354-362.
111. Ferm VH, Carpenter SJ: Teratogenic and embryopathic effects of indium, gallium, and germanium. Toxicol Appl Pharmacol 1970;16:166-170.
112. Goihman-Yahr M, Requena MA, Vallecalle-Suegart E, Convit J: Autoimmune diseases and thalidomide: II. adjuvant disease, experimental allergic encephalomyelitis and experimental allergic neuritis of the rat. Int J Lepr Other Mycobact Dis 1974;42:266-275.
113. Tseng S, Pak G, Washenik K, et al: Rediscovering thalidomide: a review of its mechanism of action, side effects, and potential uses. J Am Acad Dermatol 1996;35: 969-979.
114. Carlesimo M, Giustini S, Rossi A, et al: Treatment of cutaneous and pulmonary sarcoidosis with thalidomide. J Am Acad Dermatol 1995;32:866-869.
115. Murphy GP, Mirand EA, Groenewald JH, et al: Erythropoietin release in renal allografted baboons, with and without immunosuppression. Invest Urol 1970;7:271-282.
116. Barnhill RL, Doll NJ, Millikan LE, Hastings RC: Studies on the anti-inflammatory properties of thalidomide: effects on polymorphonuclear leukocytes and monocytes. J Am Acad Dermatol 1984;11:814-819.
117. Hesselton RM, Greiner DL, Mordes JP, et al: High levels of human peripheral blood mononuclear cell engraftment and enhanced susceptibility to human immunodeficiency virus type 1 infection in NOD/LtSz-scid/scid mice. J Infect Dis 1995;172:974-982.
118. Parren PW, Ditzel HJ, Gulizia RJ, et al: Protection against HIV-1 infection in hu-PBL-SCID mice by passive immunization with a neutralizing human monoclonal antibody against the gp120 CD4-binding site. AIDS 1995;9:F1-6.
119. Gibbons C, Killmann TR, Pettoello-Mantovani M, et al: Thy/Liv-SCID-Hu mice implanted with human intestine: an in vivo model for investigation of mucosal transmission of HIV. AIDS Res Hum Retroviruses 1997; 13:1453-1460.
120. Makonkawkeyoon S, Limson-Pobre RNR, Moreira AL, et al: Thalidomide inhibits the replication of human immunodeficiency virus type 1. Proc Natl Acad Sci U S A 1993;90:5974-5978.