Multidrug resistance (MDR) describes the resistance of tumor cells to chemotherapy
and has been ascribed to the overexpression of drug efflux pumps. Molecular imaging
of drug efflux pumps is helpful to identify the patients who may be resistant to the chemotherapy
and thus will avoid the unnecessary treatment and increase the therapeutic effectiveness.
Imaging probes targeting drug efflux pumps can non-invasively evaluate the Pgp
function and play an important role in identification of MDR, prediction of response, and
monitoring MDR modulation. On the other hand, new anticancer agents based on molecular
targets such as epidermal growth factor receptor (EGFR) and angiogenic factor receptor may
potentially be combined with chemotherapeutic drugs to overcome the MDR. Imaging of
molecular targets visualize treatment response of patients at molecular level vividly and help
to select right patients for certain targeted anticancer therapy. Among all the imaging modalities,
nuclear imaging including positron emission tomography (PET) and single photon emission
computed tomography (SPECT) imaging has the greatest promise for rapid translation to
the clinic and can realize quantitative visualization of biochemical processes in vivo. In this
review, we will summarize the nuclear imaging probes utilized for predicting and evaluating
the early anticancer therapy response. 99mTc labeled agents and PET based radiopharmaceuticals
like 18F-Paclitaxel, 11C-Verapamil for drug efflux pumps imaging will be discussed
here. Moreover, molecular imaging probes used for targeted therapy response evaluation
like 18F-Tamoxifen, 89Zr-Trastuzumab will also be introduced in this review.
Keywords: Multidrug resistance, molecular imaging, drug efflux pump, therapy response, SPECT, PET.
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