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Epothilones have received unusual attention over the past ten
years. They are novel antitumor drugs which very much like their
predecessor paclitaxel (Taxol) act via microtubule stabilization.
In comparison to paclitaxel and a number of alternative drugs with
a similar mode of bioaction (e.g. laulimalide, eleutherobin,
peluroside, discodermolide) the epothilones have significant
advantages, above all very high activity in the nanomolar range and
low susceptibility towards multidrug resistance. Epothilone B and
several derivatives thereof are in phase I-III clinical trials; one
of them (ixabepilone, BMS) is already on the market, others are
supposed to appear on the market in the near future. All naturally
occurring epothilones have been isolated from Sorangium cellulosum;
their antitumor action is traced back to the stabilization of
microtubules. In consequence, the formation of the mitototic
spindle is prohibited and the cell undergoes apoptosis.
Epothilones have received unusual attention over the past ten
years. They are novel antitumor drugs which very much like their
predecessor paclitaxel (Taxol) act via microtubule stabilization.
In comparison to paclitaxel and a number of alternative drugs with
a similar mode of bioaction (e.g. laulimalide, eleutherobin,
peluroside, discodermolide) the epothilones have significant
advantages, above all very high activity in the nanomolar range and
low susceptibility towards multidrug resistance. Epothilone B and
several derivatives thereof are in phase I-III clinical trials; one
of them (ixabepilone, BMS) is already on the market, others are
supposed to appear on the market in the near future. All naturally
occurring epothilones have been isolated from Sorangium cellulosum;
their antitumor action is traced back to the stabilization of
microtubules. In consequence, the formation of the mitototic
spindle is prohibited and the cell undergoes apoptosis.
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