Automated synthesis of [18F]gefitinib on a modular system

Applied Radiation and Isotopes

Volumn 70, Issue 1, 2012, Pages 205-209

  Läppchen, Tilman ^a   Vlaming, Maria L H ^b   Custers, Erica ^a   Lub, Johan ^a   Sio, Charles F ^a   DeGroot, Jeroen ^b   Steinbach, Oliver C ^a  

^a PHILIPS RESEARCH LABORATORIES   (Netherlands)

^b TNO   (Netherlands)

Author keywords

18F gefitinib; Automated synthesis; Imaging of drug transporters; Modular system; PET tracer

Indexed keywords

AUTOMATED PROCEDURES; AUTOMATED SYNTHESIS; GEFITINIB; IN-VIVO; MODULAR SYSTEM; PET TRACER; RADIOCHEMICAL PURITY; RADIOCHEMICAL YIELD; RADIOSYNTHESIS; TOTAL SYNTHESIS; TRANSPORTER PROTEINS;

AUTOMATION;

BIOSYNTHESIS;

GEFITINIB F 18; RADIOPHARMACEUTICAL AGENT; UNCLASSIFIED DRUG; FLUORINE; GEFITINIB; QUINAZOLINE DERIVATIVE;

ANALYTIC METHOD; ARTICLE; AUTOMATION; DRUG PURIFICATION; DRUG STRUCTURE; DRUG SYNTHESIS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; PRIORITY JOURNAL; QUALITY CONTROL; RADIOCHEMISTRY; RADIOISOTOPE DECAY; CHEMISTRY; EQUIPMENT DESIGN; INSTRUMENTATION; ISOTOPE LABELING; ROBOTICS; SYNTHESIS;

CHROMATOGRAPHY, HIGH PRESSURE LIQUID; EQUIPMENT DESIGN; FLUORINE RADIOISOTOPES; ISOTOPE LABELING; QUINAZOLINES; RADIOPHARMACEUTICALS; ROBOTICS;

EID: 80955130856     PISSN: 09698043     EISSN: 18729800     Source Type: Journal    
DOI: 10.1016/j.apradiso.2011.09.005     Document Type: Article

References (12)

1. Agarwal S., Sane R., Gallardo J.L., Ohlfest J.R., Elmquist W.F. Distribution of gefitinib to the brain is limited by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2)-mediated active efflux. J. Pharmacol. Exp. Ther. 2010, 334(1):147-155.
2. Avraham R., Yarden Y. Feedback regulation of EGFR signalling: decision making by early and delayed loops. Nat. Rev. Mol. Cell Biol. 2011, 12(2):104-117.
3. DeJesus O., Murali D., Flores L., Converse A., Dick D.W., Oakes T.R., Roberts A., Nickles R. Synthesis of [F-18]-ZD1839 as a PET imaging agent for epidermal growth factor receptors. J. Labelled Compd. Radiopharm. 2003, 46:S1.
4. Gutteridge E., Robertson J.F. Are current drug development programmes realising the full potential of new agents? Tyrosine kinase inhibitors. Breast Cancer Res. 2009, 11(Suppl 3):S24.
5. Kawamura K., Yamasaki T., Yui J., Hatori A., Konno F., Kumata K., Irie T., Fukumura T., Suzuki K., Kanno I., Zhang M.R. In vivo evaluation of P-glycoprotein and breast cancer resistance protein modulation in the brain using [(11)C]gefitinib. Nucl. Med. Biol. 2009, 36(3):239-246.
6. Minniti G., Muni R., Lanzetta G., Marchetti P., Enrici R.M. Chemotherapy for glioblastoma: current treatment and future perspectives for cytotoxic and targeted agents. Anticancer Res. 2009, 29(12):5171-5184.
7. Moon C., Chae Y.K., Lee J. Targeting epidermal growth factor receptor in head and neck cancer: lessons learned from cetuximab. Exp. Biol. Med. 2010, 235(8):907-920.
8. Murali D., Flores L., Converse A., Bartlett R., Barnhart T., Armstrong E., Nickles R., Harari P., DeJesus O. Evaluation of [F-18]Iressa as a PET imaging agent for tumors overexpressing epidermal growth factor (EGF) receptors. J. Labelled Compd. Radiopharm. 2005, 48:S294.
9. 18F]-FMAU using a novel dual reactor radiosynthesis module. J. Labelled Compd. Radiopharm. 2009, 52:553-558.
10. 18F-Iressa and related molecular probes. J. Labelled Compd. Radiopharm. 2005, 48:829-843.
11. 18F]gefitinib as a molecular imaging probe for the assessment of the epidermal growth factor receptor status in malignant tumors. Eur. J. Nucl. Med. Mol. Imaging 2008, 35(6):1089-1099.
12. 11C]Iressa): radiosynthesis, in vitro uptake, and in vivo imaging of intact murine fibrosarcoma. Mol. Imaging Biol. 2010, 12(2):181-191.