Gallium 8quinolinolate

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

Figure 14.1 Structure of tris(8-quinolinolato)gallium(III) (gallium 8-quinolinolate; GQ)

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).

Was this article helpful?

0 0
10 Ways To Fight Off Cancer

10 Ways To Fight Off Cancer

Learning About 10 Ways Fight Off Cancer Can Have Amazing Benefits For Your Life The Best Tips On How To Keep This Killer At Bay Discovering that you or a loved one has cancer can be utterly terrifying. All the same, once you comprehend the causes of cancer and learn how to reverse those causes, you or your loved one may have more than a fighting chance of beating out cancer.

Get My Free Ebook


Post a comment