Automated synthesis of 18F analogue of paclitaxel (PAC): [18F]Paclitaxel (FPAC).
A positron-emitting paclitaxel (PAC) derivative could allow in vivo measurement of multidrug resistance in tumors and, therefore, predict a potential chemotherapeutic benefit to patients. [18F]Paclitaxel was produced using a 2-reaction vessel automated synthesizer followed by HPLC purification. Optimized reaction conditions resulted in radiochemical yields of 21.2+/-9.6% at end of bombardment, radiochemical purity >99%, and specific activity of 159+/-43 G Bq/micromol. [18F]Paclitaxel activities of 1.33+/-0.729 G Bq (n=7) were obtained in sterile, pyrogen-free solution for IV administration.
Kalen
Joseph D
JD
Molecular Imaging Center, Department of Radiology, Virginia Commonwealth University, Richmond, VA, USA. jdkalen@vcu.edu
Hirsch
Jerry I
JI
Kurdziel
Karen A
KA
Eckelman
William C
WC
Kiesewetter
Dale O
DO
D001331:Automation; D019008:Drug Resistance, Neoplasm; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D006801:Humans; D009369:Neoplasms / Q000000981:diagnostic imaging / Q000188:drug therapy; D017239:Paclitaxel / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D011786:Quality Control; D011854:Radiochemistry / Q000295:instrumentation* / Q000592:standards; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*
D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D017239:Paclitaxel