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Discodermolide is a polyketide from the sponge Discodermia dissoluta with a mechanism of action similar to both paclitaxel and the epothilones. Discodermolide has several promising features such as its broad-spectrum antitumor activity, its potent inhibition of taxane and epothilone-resistant tumors in cell cultures and in animal models, and its synergic effect when combined with paclitaxel.64 Early clinical evaluations with discodermolide have begun in patients with various advanced solid malig-nancies,65 but because only small amounts are available from natural sources, all discodermolide used for preclinical activities as well as for the ongoing clinical trials has been supplied by total synthesis.66,67 This has required developing an impressive 39-step process that has been described by a leading synthetic chemist as ''probably the best piece of synthetic work to come out from an industrial company.''68

The Okinawan ocean sponge Fasciospongia rimosa and other Pacific sponges produce a potent microtubule stabilizing agent named laulimalide or figianolide B. Although laulimalide is less potent than paclitaxel in drug-sensitive laboratory cell lines, it is up to 100 times more potent in MDR-resistant cell lines, again because it is a very poor substrate of Pgp-170. Another similarity of laulimalide with discodermolide is its synergistic action with paclitaxel.69

Discodermolide

Discodermolide

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