Inecalcitol is a synthetic chemical derivative of calcitriol, the naturally active form of vitamin D.It is 10 times more potent than calcitriol on cancer cell lines in culture, and around 100 times less hypercalcemic than calcitriol in rats. This high dissociation ratio between beneficial antiproliferative properties and low risk of toxicity positions inecalcitol as a unique drug candidate for therapeutic use against cancer.
 > Calcitriol chemical structure > Inecalcitol chemical structure Vitamin D, calcitriol and their analogues exert their different activities through activation of the same vitamin D receptor (VDR). However, the protein complexes that build up around the VDR once it has been bound by its ligand, may differ according to the vitamin D molecule involved in the binding, which is how the different resulting spectrum of activities can be explained. Hybrigenics, thanks to its expertise and comprehensive platform to analyze protein interactions , is in a unique position to decipher the subtle differences in mechanisms of action that make inecalcitol best fitted for an anticancer application, in prostate cancer for example.
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The first patient has been treated in France on November 7, 2007 at the European Hospital Georges Pompidou in Paris. |
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