MedKoo product information:

EC-20

Description of EC-20: Tc 99m EC20 is a folate receptor-targeting radiopharmaceutical consisting of a folate-containing tetrapeptide chelator to which technetium Tc 99m is linked. The folate component of folate receptor-targeted technetium Tc 99m EC20 binds to folic acid receptors, which are frequently upregulated in many types of tumor cells and activated macrophages. Gamma scintigraphy may then be used to image folate receptor-positive tumors. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:    Endocyte, Inc.

In vivo imaging with 99mTc-EC20 identified approximately two thirds of patients as having FR-positive tumors. Agreement between imaging and in vitro IHC was poor but was potentially confounded by a lack of correlation between the time of tissue sampling and the time of 99mTc-EC20 imaging, the heterogeneous expression of FR in metastatic lesions from the same patient, and the inability to detect the beta-isoform of FR by IHC. The pilot study of 99mTc-EC20 scintigraphy indicates that the agent is safe and well tolerated and that this noninvasive procedure may have utility in selecting patients likely to benefit from FR-targeted therapy. (source: J Nucl Med. 2008 Jun;49(6):899-906. Epub 2008 May 15.).

1: Panwar P, Srivastava V, Tandon V, Mishra P, Chuttani K, Sharma R, Chandra R, Mishra A, Chopra A. 99mTc-Labeled tetraethylenepentamine-folate. 2009 Aug 25 [updated 2009 Oct 01]. Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2010. Available from http://www.ncbi.nlm.nih.gov/bookshelf/br.fcgi?book=micad&part=TEPAfolate99mTc PubMed PMID: 20641314.

2: Chopra A. 99mTc-Labeled peptide derivative of folic acid. 2009 Sep 11 [updated 2009 Nov 12]. Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2010. Available from http://www.ncbi.nlm.nih.gov/bookshelf/br.fcgi?book=micad&part=EC2099mTc PubMed PMID: 20641201.

3: Ayala-López W, Xia W, Varghese B, Low PS. Imaging of atherosclerosis in apoliprotein e knockout mice: targeting of a folate-conjugated radiopharmaceutical to activated macrophages. J Nucl Med. 2010 May;51(5):768-74. Epub 2010 Apr 15. PubMed PMID: 20395331.

4: Müller C, Reddy JA, Leamon CP, Schibli R. Effects of the antifolates pemetrexed and CB3717 on the tissue distribution of (99m)Tc-EC20 in xenografted and syngeneic tumor-bearing mice. Mol Pharm. 2010 Apr 5;7(2):597-604. PubMed PMID: 20199053.

5: Matteson EL, Lowe VJ, Prendergast FG, Crowson CS, Moder KG, Morgenstern DE, Messmann RA, Low PS. Assessment of disease activity in rheumatoid arthritis using a novel folate targeted radiopharmaceutical Folatescan. Clin Exp Rheumatol. 2009 Mar-Apr;27(2):253-9. PubMed PMID: 19473565.

6: Xia W, Hilgenbrink AR, Matteson EL, Lockwood MB, Cheng JX, Low PS. A functional folate receptor is induced during macrophage activation and can be used to target drugs to activated macrophages. Blood. 2009 Jan 8;113(2):438-46. Epub 2008 Oct 24. PubMed PMID: 18952896.

7: Fisher RE, Siegel BA, Edell SL, Oyesiku NM, Morgenstern DE, Messmann RA, Amato RJ. Exploratory study of 99mTc-EC20 imaging for identifying patients with folate receptor-positive solid tumors. J Nucl Med. 2008 Jun;49(6):899-906. Epub 2008 May 15. PubMed PMID: 18483093.

8: Reddy JA, Xu LC, Parker N, Vetzel M, Leamon CP. Preclinical evaluation of (99m)Tc-EC20 for imaging folate receptor-positive tumors. J Nucl Med. 2004 May;45(5):857-66. PubMed PMID: 15136637.

9: Leamon CP, Parker MA, Vlahov IR, Xu LC, Reddy JA, Vetzel M, Douglas N. Synthesis and biological evaluation of EC20: a new folate-derived, (99m)Tc-based radiopharmaceutical. Bioconjug Chem. 2002 Nov-Dec;13(6):1200-10. PubMed PMID: 12440854.

10: Turk MJ, Breur GJ, Widmer WR, Paulos CM, Xu LC, Grote LA, Low PS. Folate-targeted imaging of activated macrophages in rats with adjuvant-induced arthritis. Arthritis Rheum. 2002 Jul;46(7):1947-55. PubMed PMID: 12124880.