TY - JOUR
T1 - Epothilones in development for non-small-cell lung cancer
T2 - Novel anti-tubulin agents with the potential to overcome taxane resistance
AU - Edelman, Martin J.
AU - Shvartsbeyn, Marianna
N1 - Copyright © 2012 Elsevier Inc. All rights reserved.
PY - 2012/5
Y1 - 2012/5
N2 - Progress in the treatment of non-small-cell lung cancer (NSCLC) will require the introduction of new agents as well as better use of existing therapies. Targeted therapies are likely to have a profound effect on the treatment of NSCLC after identification of patients who are most likely to benefit. The epothilones are novel anti-tubulin agents derived from Sorangium cellulosum. β III tubulin overexpression has been implicated as a mechanism of anti-tubulin resistance that can be overcome by epothilones. Several epothilones have advanced to clinical trials; ixabepilone (BMS247550, aza-epothilone B, Bristol-Myers Squibb, New York, NY), patupilone (EPO906, Novartis, Basel, Switzerland) and sagopilone (ZK-EPO, ZK-219477, Schering AG, Berlin-Wedding, Germany) are currently in active development. Several of the epothilones, most notably ixabepilone, have demonstrated activity in lung cancer in phase I and II trials, including taxane-resistant patients. Although a phase II study failed to show superior outcome in patients with β III tubulin overexpression, other aspects of the epothilones argue for their continued development.
AB - Progress in the treatment of non-small-cell lung cancer (NSCLC) will require the introduction of new agents as well as better use of existing therapies. Targeted therapies are likely to have a profound effect on the treatment of NSCLC after identification of patients who are most likely to benefit. The epothilones are novel anti-tubulin agents derived from Sorangium cellulosum. β III tubulin overexpression has been implicated as a mechanism of anti-tubulin resistance that can be overcome by epothilones. Several epothilones have advanced to clinical trials; ixabepilone (BMS247550, aza-epothilone B, Bristol-Myers Squibb, New York, NY), patupilone (EPO906, Novartis, Basel, Switzerland) and sagopilone (ZK-EPO, ZK-219477, Schering AG, Berlin-Wedding, Germany) are currently in active development. Several of the epothilones, most notably ixabepilone, have demonstrated activity in lung cancer in phase I and II trials, including taxane-resistant patients. Although a phase II study failed to show superior outcome in patients with β III tubulin overexpression, other aspects of the epothilones argue for their continued development.
KW - Anti-tubulin agents
KW - Epothilones
KW - Lung cancer
KW - Resistance
KW - β-tubulin III
UR - http://www.scopus.com/inward/record.url?scp=84859874192&partnerID=8YFLogxK
UR - https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=purepublist2023&SrcAuth=WosAPI&KeyUT=WOS:000302895300002&DestLinkType=FullRecord&DestApp=WOS
U2 - 10.1016/j.cllc.2011.02.005
DO - 10.1016/j.cllc.2011.02.005
M3 - Review article
C2 - 22133291
SN - 1525-7304
VL - 13
SP - 171
EP - 180
JO - Clinical Lung Cancer
JF - Clinical Lung Cancer
IS - 3
ER -