IDN 5390: a new concept in taxane development.
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.
Taraboletti
Giulia
G
Department of Oncology, Mario Negri Institute for Pharmacological Research, Bergamo, Italy. taraboletti@marionegri.it
Micheletti
Gianluca
G
Giavazzi
Raffaella
R
Riva
Antonella
A
D000284:Administration, Oral; D020533:Angiogenesis Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D001952:Bridged-Ring Compounds / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D009362:Neoplasm Metastasis; D009369:Neoplasms / Q000098:blood supply / Q000188:drug therapy*; D043823:Taxoids / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*
D020533:Angiogenesis Inhibitors; D001952:Bridged-Ring Compounds; C459840:IDN 5390; D043823:Taxoids