Carbon-11 Labelled Compounds in the Development of Pharmaceuticals


Carbon-11 Labelled Compounds in the Development of Pharmaceuticals

Wüst, F.

Positron emission tomography (PET) is a powerful non-invasive clinical and research imaging technique which allows in vivo measurements and quantification of biochemical processes at the molecular level. Besides the success story of PET as valuable diagnostic tool in oncology, neutrology and cardiology, PET technology has also emerged the process of drug research and development. Its strength stems from the ability to obtain directly quantitative knowledge of the distribution and bioavailability of drugs and their therapeutic and toxic effects on living systems. The direct assessment of pharmacokinetic and pharmacodynamic events in humans and animals combined with the new generation of high-resolution PET cameras place PET in a unique position to contribute significantly to the process of drug development and evaluation. PET helps to understand the molecular mechanism underlying drug action while addressing some very practical questions such as determining effective drug doses, determining the duration of drug action and examining potential drug interactions. To fully exploit PET technology in drug development, appropriately labeled compounds are needed. The drug usually must be labeled with carbon-11 (t1/2 = 20 min) to aviod changing the characteristics of the parent compound. Alternatively, fluorine-18 (t1/2 = 110 min) can be used if the drug contains a fluorine atom. The short half lives of 11C and 18F require rapid and selective labelling techniques, since time dominates all aspects of PET. In this connection the extensive performance of organic radiochemistry using 11C and 18F is fundamental but also a special challenge. This presentation will address the recent developments of organic PET radiochemistry in the synthesis of PET radiotracers with sprecial focus on the potential role of 11C-labelled compounds in the design, development and evaluation of pharmaceuticals.

  • Lecture (Conference)
    11th Conference of the International Isotope Society, Bad Soden, 25.-26.09.2003
  • Abstract in refereed journal
    Journal of Labelled Compounds and Radiopharmceuticals 47(2004), 261-262

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Publ.-Id: 5680