Gallium 8-quinolinolate (tris(8-quinolinolato)gallium(III); GQ; Figure 14.1) was developed to provide high oral gallium bioavailability for use in cancer treatment.123 GQ inhibited the in vitro proliferation of A549 human lung adenocarcinoma cells: the IC50 was 2.5 mM, similar to that for GN and about a tenth the value for GC.124 In rats transplanted with Walker carcinosarcoma 256, tumor reduction of >50% was observed following oral gavage at 24mg/ kg/day on days 3-9 after transplantation; an equimolar oral dose of GN had no anti-tumor effect.125 An anti-hypercalcemic effect was also observed. A dose of 62.5 mg/kg/day for two weeks was well tolerated in healthy Swiss mice, whereas doses of 125 mg/kg/day proved toxic (including leucopenia, but not anemia) and sometimes fatal.123 In the animals that received 62.5 mg/kg/day, gallium was concentrated in the bone (7(3) mg/g), liver (4(2) mg/g), spleen (2(1) mg/g) and
kidneys (1.8(2) mg/g), with <0.03 ng/g gallium found in the brain, lungs, testes, and ovaries (serum concentration not given).123 This compound entered human clinical trials in 2004 (B. Keppler, personal communication, 2004).
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