SOM230: A New Therapeutic Modality for Cushing's Disease

Authors

  • Ian Lewis Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland. ian.lewis@novartis.com
  • Herbert A. Schmid Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland
  • Rainer Kneuer Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland
  • Daniel Hoyer Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland
  • Antonio P. Silva Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland
  • Gisbert Weckbecker Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland
  • Christian Bruns Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland
  • Janos Pless Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland

DOI:

https://doi.org/10.2533/chimia.2014.483

Keywords:

Cushing's disease, Medicinal chemistry, Som230, Somatostatin

Abstract

A rational drug design approach involving transposition of functional groups from SRIF into a reduced size cyclohexapeptide template has led to the discovery of SOM230, a novel, stable cyclohexapeptide somatostatin mimic which exhibits unique high affinity binding to human somatostatin receptors (sst1-5). This unique receptor subtype binding profile, in particular the exceptional high affinity binding to sst5, led to SOM230 being approved by EMEA and FDA in 2012 as the first effective pituitary directed therapeutic modality for Cushing's disease.
CHIMIA Vol. 68 No. 7-8 (2014): Laureates of the SCS Awards and Fall Meeting 2014

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Published

2014-08-27

Issue

Vol. 68 No. 7-8 (2014): Laureates of the SCS Awards and Fall Meeting 2014

Section

Scientific Articles

License

Copyright (c) 2014 Swiss Chemical Society

Creative Commons License

This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.

How to Cite

[1]
I. Lewis, H. A. Schmid, R. Kneuer, D. Hoyer, A. P. Silva, G. Weckbecker, C. Bruns, J. Pless, Chimia 2014, 68, 483, DOI: 10.2533/chimia.2014.483.