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In this paper, the use of (123)I-Annexin V for the detection of farnesyltransferase inhibitor (FTI)-induced apoptosis in tumour-bearing athymic mice is described. In vitro binding assays on LoVo cells show time- and dosage-dependent (125)I-Annexin V binding upon treatment with Tipifarnib (Zarnestra, R115777), a selective and potent FTI. In vivo experiments using planar gamma scintigraphy on LoVo inoculated mice show a 40% increased (123)I-Annexin V uptake 8 h after a single oral administration of 100 mg/kg Tipifarnib in 20% beta-cyclodextrin in 0.1 M HCl, as well as after 3 days of twice daily treatments with the same dose. Ex vivo TUNEL assays, detecting end-stage apoptotic cells, correlate significantly with both in vitro and in vivo results. The percentage of necrosis is also increased by Tipifarnib treatment, but is too low to interfere with the (123)I-Annexin V uptake. It can be concluded that (123)I-Annexin V can be used to monitor Tipifarnib-induced apoptosis in LoVo xenograft tumours in athymic mice. Future applications might include the early prediction of FTI response and the selection of FTI-sensitive patients very shortly after treatment initiation. Subsequently, such patients would greatly benefit from a noninvasive and fast therapy evaluation.

Original publication




Journal article


Nucl Med Biol

Publication Date





233 - 239


Adenocarcinoma, Alkyl and Aryl Transferases, Animals, Annexin A5, Antineoplastic Agents, Apoptosis, Cell Line, Tumor, Dose-Response Relationship, Drug, Farnesyltranstransferase, Humans, Iodine Radioisotopes, Male, Mice, Mice, Nude, Prognosis, Quinolones, Radionuclide Imaging, Radiopharmaceuticals, Reproducibility of Results, Sensitivity and Specificity, Treatment Outcome