TY - JOUR
T1 - Novel drugs targeting microtubules
T2 - The role of epothilones
AU - Ferrandina, Gabriella
AU - Mariani, Marisa
AU - Andreoli, Mirko
AU - Shahabi, Shohreh
AU - Scambia, Giovanni
AU - Ferlini, Cristiano
PY - 2012/6
Y1 - 2012/6
N2 - Among the drugs targeting microtubule functions by interfering with tubulin subunits, epothilones represent a class of anticancer agents which recently entered clinical development. Although epothilones share mechanisms of action similar to taxanes, they have non-overlapping mechanisms of resistance; in particular, while overexpression of class III β-tubulin plays a major role in taxane resistance, epothilones display their highest efficacy in class III β-tubulin overexpressing malignancies. Three compounds belonging to this family (patupilone, ixabepilone and sagopilone), have been actively investigated in clinical trials, and some of them are at an advanced stage of development. This review provides a comprehensive analysis of the available literature on epothilones, focusing on their clinical development and potential as an additional weapon in the arsenal against tumors.
AB - Among the drugs targeting microtubule functions by interfering with tubulin subunits, epothilones represent a class of anticancer agents which recently entered clinical development. Although epothilones share mechanisms of action similar to taxanes, they have non-overlapping mechanisms of resistance; in particular, while overexpression of class III β-tubulin plays a major role in taxane resistance, epothilones display their highest efficacy in class III β-tubulin overexpressing malignancies. Three compounds belonging to this family (patupilone, ixabepilone and sagopilone), have been actively investigated in clinical trials, and some of them are at an advanced stage of development. This review provides a comprehensive analysis of the available literature on epothilones, focusing on their clinical development and potential as an additional weapon in the arsenal against tumors.
KW - Cell survival
KW - Class III β-tubulin
KW - Cytoskeleton
KW - Epothilones
KW - Ovarian cancer
UR - http://www.scopus.com/inward/record.url?scp=84862510018&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84862510018&partnerID=8YFLogxK
U2 - 10.2174/138161212800626238
DO - 10.2174/138161212800626238
M3 - Review article
C2 - 22390763
AN - SCOPUS:84862510018
SN - 1381-6128
VL - 18
SP - 2793
EP - 2803
JO - Current Pharmaceutical Design
JF - Current Pharmaceutical Design
IS - 19
ER -
