A phase I study of the folate-targeted conjugate EC0489 in patients with refractory or advanced metastatic cancer
| Autor: | Patricia LoRusso, Edward A. Sausville, Barbara A. Conley, Elisabeth I. Heath, M. Hamm, J. Carter, W. J. Perez, Wael A. Harb, S. R. Chandana, Richard A. Messmann |
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| Rok vydání: | 2010 |
| Předmět: | |
| Zdroj: | Journal of Clinical Oncology. 28:3088-3088 |
| ISSN: | 1527-7755 0732-183X |
| Popis: | 3088 Background: The folate receptor (FR) is expressed on many human tumors (e.g., ovarian, NSCLC, etc.) where it functions as a high-affinity receptor for folic acid. The FR is minimally expressed in normal tissue, making it a logical target for anti-cancer therapy. Indeed, the relevance of FR as a molecular target for anti-tumor agents was discussed in detail at the 2008 ASCO Annual Meeting. Folic acid can be used as a carrier molecule to deliver covalently-linked therapeutic and diagnostic moieties to the FR. EC0489, a conjugate of folic acid and desacetyl vinblastine hydrazide (DAVLBH), is a high-affinity ligand for the FR. This phase I study assessed the safety and pharmacokinetics (PK) of escalating intravenous bolus doses of EC0489. Methods: Eligible patients with adequate performance status and organ function that had previously failed standard therapy were treated with EC0489 on days 1, 3, 5 and 15, 17, 19 of a 28-day cycle. Endpoints included determination of a safe and tolerable EC0489 dose and... |
| Databáze: | OpenAIRE |
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