Clinical pharmacology of aromatase inhibitors

  • Jürgen Geisler
  • Per Eystein Lønning
Part of the Milestones in Drug Therapy book series (MDT)


The preclinical pharmacology of aromatase inhibitors has been reviewed in chapter by W.R. Miller. However, preclinical pharmacology may not always be directly extrapolated to the in vivo setting in humans. Thus a drug effect in the human body will depend on factors in addition to its effect on the target enzyme, like general pharmacokinetics, tissue penetration and cellular uptake. In contrast to the selective oestrogen receptor modulators (SERMs), for which a simple biochemical parameter in vivo is lacking, aromatase inhibitors may be assessed by their ability to modulate their target, the aromatase enzyme. Whereas we now have data available comparing the effect of different compounds on total body aromatase inhibition, our understanding of the effects of these compounds at the tissue level, in particular with respect to local effects in the normal breast as well as breast tumour tissue, is still incomplete.


Aromatase Inhibitor Aromatase Enzyme Postmenopausal Breast Cancer Patient Nonsteroidal Aromatase Inhibitor Preclinical Pharmacology 
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Copyright information

© Birkhäuser Verlag/Switzerland 2008

Authors and Affiliations

  • Jürgen Geisler
    • 1
  • Per Eystein Lønning
    • 1
  1. 1.Department of Medicine, Section of OncologyHaukeland University HospitalBergenNorway

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