TY - JOUR
T1 - EC145
T2 - A novel targeted agent for adenocarcinoma of the lung
AU - Pribble, Pamela
AU - Edelman, Martin J.
PY - 2012/5
Y1 - 2012/5
N2 - Introduction: EC145 is a folate receptor (FR)-targeted vinca alkaloid conjugate currently under development as an anticancer agent. The FR is overexpressed on a number of major malignancies including adenocarcinoma of the lung and ovarian cancer. A companion diagnostic radiopharmaceutical, EC20, allows for non-invasive determination of the presence of functionally active FR. Areas covered: This review will discuss the rationale for the FR as a target for anticancer agents, the pharmacology of EC145 and the preclinical and clinical results for EC145 and related compounds. In addition, it will discuss the utility of a companion imaging diagnostic, EC20, for the selection of patients who might benefit from EC145. Expert opinion: EC145 is a first in class, novel agent with a unique target. The companion diagnostic, EC20 may allow for enrichment of the patient population, and therefore accelerate development of the drug. The drug has demonstrated benefit in preliminary reports of trials in ovarian cancer. If similar benefit is demonstrated in lung cancer, the drug is likely to have significant use in lung cancer and other malignancies with overexpression of FRs.
AB - Introduction: EC145 is a folate receptor (FR)-targeted vinca alkaloid conjugate currently under development as an anticancer agent. The FR is overexpressed on a number of major malignancies including adenocarcinoma of the lung and ovarian cancer. A companion diagnostic radiopharmaceutical, EC20, allows for non-invasive determination of the presence of functionally active FR. Areas covered: This review will discuss the rationale for the FR as a target for anticancer agents, the pharmacology of EC145 and the preclinical and clinical results for EC145 and related compounds. In addition, it will discuss the utility of a companion imaging diagnostic, EC20, for the selection of patients who might benefit from EC145. Expert opinion: EC145 is a first in class, novel agent with a unique target. The companion diagnostic, EC20 may allow for enrichment of the patient population, and therefore accelerate development of the drug. The drug has demonstrated benefit in preliminary reports of trials in ovarian cancer. If similar benefit is demonstrated in lung cancer, the drug is likely to have significant use in lung cancer and other malignancies with overexpression of FRs.
KW - Desacetylvinblastine monohydrazide
KW - EC120
KW - EC145
KW - Folic acid receptor
KW - Vinca alkaloid conjugate
UR - http://www.scopus.com/inward/record.url?scp=84859727702&partnerID=8YFLogxK
UR - https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=purepublist2023&SrcAuth=WosAPI&KeyUT=WOS:000302753200016&DestLinkType=FullRecord&DestApp=WOS
U2 - 10.1517/13543784.2012.671294
DO - 10.1517/13543784.2012.671294
M3 - Review article
C2 - 22462761
SN - 1354-3784
VL - 21
SP - 755
EP - 761
JO - Expert Opinion on Investigational Drugs
JF - Expert Opinion on Investigational Drugs
IS - 5
ER -