MedKoo product information:

EC-145

EC145  is a water-soluble, folate-receptor-targeted conjugate of folate and the vinca alkaloid desacetylvinblastine monohydrazide (DAVLBH) with potential antineoplastic activity. The folate moiety of folate-vinca alkaloid conjugate EC145 binds to folic acid receptors on the tumor cell surface and the agent is internalized via folate receptor-mediated endocytosis, delivering the tubulin-binding DAVLBH moiety directly into the tumor cell; DAVLBH binding to tubulin results in the disruption of microtubule assembly-disassembly dynamics, cell cycle arrest, and tumor cell apoptosis. Folic acid receptors are frequently upregulated on the surfaces of many tumor cell types. DAVLBH is a derivative of the natural product vinblastine. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

EC145 is a conjugate of the vitamin folate and a super-potent vinca alkaloid. Folate is required for cell division and rapidly dividing cancer cells often over-express folate receptors in order to capture enough folate to support cell division. By attaching a chemotherapy drug to folate through proprietary chemistry, EC145 targets cancer cells while avoiding most normal cells. This targeted approach is designed to provide treatment with super-potent drugs while lowering toxicity compared to standard chemotherapy.

Current developer:    Endocyte Inc.

1: Dosio F, Milla P, Cattel L. EC-145, a folate-targeted Vinca alkaloid conjugate for the potential treatment of folate receptor-expressing cancers. Curr Opin Investig Drugs. 2010 Dec;11(12):1424-33. Review. PubMed PMID: 21154124.

2. Leamon CP, Reddy JA, Klein PJ, Vlahov IR, Dorton R, Bloomfield A, Nelson M, Westrick E, Parker N, Bruna K, Vetzel M, Gehrke M, Nicoson JS, Messmann RA, LoRusso PM, Sausville EA. Reducing undesirable hepatic clearance of a tumor-targeted vinca alkaloid via novel saccharopeptidic modifications. J Pharmacol Exp Ther. 2011 Feb;336(2):336-43. Epub 2010 Oct 26. PubMed PMID: 20978169.