TY - JOUR
T1 - Eribulin-A review of preclinical and clinical studies
AU - Swami, Umang
AU - Chaudhary, Imran
AU - Ghalib, Mohammad H.
AU - Goel, Sanjay
PY - 2012/2
Y1 - 2012/2
N2 - Eribulin mesylate is a non-taxane, structurally simplified, completely synthetic, halichondrin B derivative with an end poisoning, microtubule inhibitory action. Preclinical studies have demonstrated activity in various cancer cell lines and synergistic action with gemcitabine, epirubicin, trastuzumab, cisplatin, docetaxel and vinorelbine. Eribulin has recently been approved by United States Food and Drug Administration as a third line therapy for metastatic breast cancer patients, who have previously been treated with an anthracycline and a taxane. It has also advanced to phase II trials in non-small cell lung cancer, pancreatic, prostate, bladder, head and neck cancers, sarcomas and ovarian and other gynecological tumors. Combination trials with carboplatin, gemcitabine, pemetrexed, cisplatin, and erlotinib are currently ongoing. Eribulin potentially has a low incidence of peripheral neuropathy. The predominant side effects are neutropenia and fatigue, which are manageable. This article reviews the available information on eribulin with respect to its clinical pharmacology, mechanism of action, pharmacokinetics, pharmacodynamics, metabolism, preclinical studies and clinical trials.
AB - Eribulin mesylate is a non-taxane, structurally simplified, completely synthetic, halichondrin B derivative with an end poisoning, microtubule inhibitory action. Preclinical studies have demonstrated activity in various cancer cell lines and synergistic action with gemcitabine, epirubicin, trastuzumab, cisplatin, docetaxel and vinorelbine. Eribulin has recently been approved by United States Food and Drug Administration as a third line therapy for metastatic breast cancer patients, who have previously been treated with an anthracycline and a taxane. It has also advanced to phase II trials in non-small cell lung cancer, pancreatic, prostate, bladder, head and neck cancers, sarcomas and ovarian and other gynecological tumors. Combination trials with carboplatin, gemcitabine, pemetrexed, cisplatin, and erlotinib are currently ongoing. Eribulin potentially has a low incidence of peripheral neuropathy. The predominant side effects are neutropenia and fatigue, which are manageable. This article reviews the available information on eribulin with respect to its clinical pharmacology, mechanism of action, pharmacokinetics, pharmacodynamics, metabolism, preclinical studies and clinical trials.
KW - Breast cancer
KW - E7389
KW - EMBRACE
KW - Eribulin
KW - Halaven™
KW - Halichondrin B
KW - Microtubule inhibitor
KW - NSC 707389
UR - http://www.scopus.com/inward/record.url?scp=84856235418&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84856235418&partnerID=8YFLogxK
U2 - 10.1016/j.critrevonc.2011.03.002
DO - 10.1016/j.critrevonc.2011.03.002
M3 - Review article
C2 - 21493087
AN - SCOPUS:84856235418
SN - 1040-8428
VL - 81
SP - 163
EP - 184
JO - Critical Reviews in Oncology/Hematology
JF - Critical Reviews in Oncology/Hematology
IS - 2
ER -