PET Imaging of Multidrug Resistance in Tumors Using 18F-Fluoropaclitaxel
Authors: A. Kurdziel, Karen; O. Kiesewetter, Dale
Source: Current Topics in Medicinal Chemistry, Volume 10, Number 17, December 2010 , pp. 1792-1798(7)
Publisher: Bentham Science Publishers
Abstract:The failure of solid tumors to respond to chemotherapy is a complicated and clinically frustrating issue. The ability to predict which tumors will respond to treatment could reduce the human and monetary costs of cancer therapy by allowing pro-active selection of a chemotherapeutic to which the tumor does not express resistance. PET/CT imaging with a radiolabeled form of paclitaxel, F-18 fluoropaclitaxel (FPAC), may be able to predict the uptake of paclitaxel in solid tumors, and as a substrate of P-glycoprotein, it may also predict which tumors exhibit multidrug resistance (MDR), a phenotype in which tumors fail to respond to a wide variety of chemically unrelated chemotherapeutic agents. This article reviews the synthetic, preclinical and early human data obtained during the development phase of this promising new radiopharmaceutical.
Keywords: Drug development; Molecular Imaging; F-18 fluoropaclitaxel; Multidrug resistance; Paclitaxel; PET; Pgp; PET Imaging; Multidrug Resistance; 18F-Fluoropaclitaxel; P-glycoprotein; Drug development; Molecular Imaging; PET; Tumor cells; chemotherapeutic agent; ABC (ATP Binding Cassette); Pgp expression; Cytochrome p450; Taxus brevifolia; Taxus baccata; Docetaxel; b-tubulin; Phenylisoserine moiety; [99mTc] sestamibi; [99mTc] tetrofosmin; tariquidar; XR9576; microPET; Pgp inhibitor; [18F]FPAC DMSO; Human breast tumor cell line; Standardized uptake value; MCF tumors; MIRDOSE; MDR modulator; Pgp modulation
Document Type: Research article
Publication date: 2010-12-01