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IDN 5390 is a seco-derivative cytostatic taxane. Originally selected for its ability to affect endothelial cell motility, the anti-angiogenic properties of IDN 5390 have been documented in experimental models, in vivo and in vitro. Preclinical studies indicate that, in vivo, oral IDN 5390 has a favorable bioavailability, is well tolerated and shows a significant anti-neoplastic activity on a panel of different tumor models, including paclitaxel-resistant tumors. According to its cytostatic rather than cytotoxic nature, frequent administrations of non-toxic doses have proven to be the optimal schedule for IDN 5390 treatment. Preliminary findings suggest the use of this compound in combination with conventional anti-neoplastic therapy. IDN 5390 can be considered the prototype of a new class of well-tolerated, orally available anti-angiogenic taxane derivatives with cytostatic properties.