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Open Access SOM230: A New Therapeutic Modality for Cushing's Disease

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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.

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Keywords: CUSHING'S DISEASE; MEDICINAL CHEMISTRY; SOM230; SOMATOSTATIN

Document Type: Research Article

Affiliations: 1: Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland. [email protected] 2: Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland

Publication date: August 1, 2014

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  • International Journal for Chemistry and Official Membership Journal of the Swiss Chemical Society (SCS) and its Divisions

    CHIMIA, a scientific journal for chemistry in the broadest sense, is published 10 times a year and covers the interests of a wide and diverse readership. Contributions from all fields of chemistry and related areas are considered for publication in the form of Review Articles and Notes. A characteristic feature of CHIMIA are the thematic issues, each devoted to an area of great current significance.

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