Automated synthesis of 18F analogue of paclitaxel (PAC): [18F]Paclitaxel (FPAC)

Appl Radiat Isot. 2007 Jun;65(6):696-700. doi: 10.1016/j.apradiso.2006.10.015. Epub 2006 Dec 11.

Abstract

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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Automation
  • Drug Resistance, Neoplasm
  • Fluorine Radioisotopes / chemistry*
  • Humans
  • Neoplasms / diagnostic imaging
  • Neoplasms / drug therapy
  • Paclitaxel / analogs & derivatives*
  • Paclitaxel / chemical synthesis
  • Quality Control
  • Radiochemistry / instrumentation*
  • Radiochemistry / standards
  • Radionuclide Imaging
  • Radiopharmaceuticals / chemical synthesis*

Substances

  • Fluorine Radioisotopes
  • Radiopharmaceuticals
  • Paclitaxel