Literature DB >> 22462761

EC145: a novel targeted agent for adenocarcinoma of the lung.

Pamela Pribble1, Martin J Edelman.   

Abstract

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.

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Year:  2012        PMID: 22462761     DOI: 10.1517/13543784.2012.671294

Source DB:  PubMed          Journal:  Expert Opin Investig Drugs        ISSN: 1354-3784            Impact factor:   6.206


  10 in total

Review 1.  Vintafolide: a novel targeted therapy for the treatment of folate receptor expressing tumors.

Authors:  Ignace Vergote; Christopher P Leamon
Journal:  Ther Adv Med Oncol       Date:  2015-07       Impact factor: 8.168

2.  Folate receptor α expression and significance in endometrioid endometrium carcinoma and endometrial hyperplasia.

Authors:  Serkan Senol; Ayse Bahar Ceyran; Abdullah Aydin; Ebru Zemheri; Seyma Ozkanli; Duygu Kösemetin; Ibrahim Sehitoglu; Ibrahim Akalin
Journal:  Int J Clin Exp Pathol       Date:  2015-05-01

3.  Significance of folate receptor alpha and thymidylate synthase protein expression in patients with non-small-cell lung cancer treated with pemetrexed.

Authors:  Daniel C Christoph; Bernadette Reyna Asuncion; Biftu Hassan; Cindy Tran; Julia D Maltzman; Daniel J O'Shannessy; Murry W Wynes; Thomas C Gauler; Jeremias Wohlschlaeger; Mathias Hoiczyk; Martin Schuler; Wilfried E Eberhardt; Fred R Hirsch
Journal:  J Thorac Oncol       Date:  2013-01       Impact factor: 15.609

4.  Enhanced receptor-mediated endocytosis and cytotoxicity of a folic acid-desacetylvinblastine monohydrazide conjugate in a pemetrexed-resistant cell line lacking folate-specific facilitative carriers but with increased folate receptor expression.

Authors:  Rongbao Zhao; Ndeye Diop-Bove; I David Goldman
Journal:  Mol Pharmacol       Date:  2013-11-18       Impact factor: 4.436

5.  Identification of a PET Radiotracer for Imaging of the Folate Receptor-α: A Potential Tool to Select Patients for Targeted Tumor Therapy.

Authors:  Patrycja Guzik; Hsin-Yu Fang; Luisa M Deberle; Martina Benešová; Susan Cohrs; Silvan D Boss; Simon M Ametamey; Roger Schibli; Cristina Müller
Journal:  J Nucl Med       Date:  2021-01-15       Impact factor: 10.057

Review 6.  Mechanisms and implications of dual-acting methotrexate in folate-targeted nanotherapeutic delivery.

Authors:  Pamela T Wong; Seok Ki Choi
Journal:  Int J Mol Sci       Date:  2015-01-13       Impact factor: 5.923

7.  Expression of high affinity folate receptor in breast cancer brain metastasis.

Authors:  José Pablo Leone; Rohit Bhargava; Brian K Theisen; Ronald L Hamilton; Adrian V Lee; Adam M Brufsky
Journal:  Oncotarget       Date:  2015-10-06

8.  Folate-Targeted Monodisperse PEG-Based Conjugates Made by Chemo-Enzymatic Methods for Cancer Diagnosis and Treatment.

Authors:  Krisztina S Nagy; Krisztina Toth; Eva Pallinger; Angela Takacs; Laszlo Kohidai; Angela Jedlovszky-Hajdu; Domokos Mathe; Noemi Kovacs; Daniel S Veres; Krisztian Szigeti; Kristof Molnar; Eniko Krisch; Judit E Puskas
Journal:  Int J Mol Sci       Date:  2021-09-26       Impact factor: 6.208

Review 9.  Prospects in folate receptor-targeted radionuclide therapy.

Authors:  Cristina Müller; Roger Schibli
Journal:  Front Oncol       Date:  2013-09-24       Impact factor: 6.244

Review 10.  Targeting folate receptor alpha for cancer treatment.

Authors:  Anthony Cheung; Heather J Bax; Debra H Josephs; Kristina M Ilieva; Giulia Pellizzari; James Opzoomer; Jacinta Bloomfield; Matthew Fittall; Anita Grigoriadis; Mariangela Figini; Silvana Canevari; James F Spicer; Andrew N Tutt; Sophia N Karagiannis
Journal:  Oncotarget       Date:  2016-08-09
  10 in total

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