The tissue-specific distribution of 3H-seocalcitol (EB 1089) and 3H-calcitriol in rats.
作者： Anne-Marie Kissmeyer , Jeanet Løgsted Nielsen , Lise Binderup
DOI: 10.1016/J.JSBMB.2004.03.049
关键词: Distribution (pharmacology) 、 Tissue distribution 、 Calcitriol 、 Internal medicine 、 Human liver 、 Seocalcitol 、 Tissue specific 、 Biology 、 Cancer cell proliferation 、 Carcinoma 、 Endocrinology
摘要: Seocalcitol (EB 1089) is under development for the treatment of hepato-cellular carcinoma (HCC). The tissue distribution 3H-seocalcitol was investigated in comparison to 3H-calcitriol rats. Quantitative whole-body autoradiography used quantify distribution. greatest difference between two compounds observed bloodstream. For most tissues ratio seocalcitol/calcitriol varied 0.2 and 3.1. concentration radioactivity liver almost same compounds. seocalcitol 10 times higher than serum. Assuming that liver/serum rats humans, human expected be resulting more 50% inhibition cancer cell proliferation, thus pharmacologically effective HCC. It questionable whether calcitriol would present sufficient concentrations HCC, as antiproliferative activity generally 10-fold lower compared can only administered at a dose ca. three-fold seocalcitol.
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