title: SOM230: a new therapeutic modality for Cushing's disease.
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.
authors.affiliation: Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland. ian.lewis@novartis.com.
authors.forename: Ian
authors.initials: I
authors.lastname: Lewis
authors.affiliation: Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland.
authors.forename: Herbert A
authors.initials: HA
authors.lastname: Schmid
authors.affiliation: Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland.
authors.forename: Rainer
authors.initials: R
authors.lastname: Kneuer
authors.affiliation: Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland.
authors.forename: Daniel
authors.initials: D
authors.lastname: Hoyer
authors.affiliation: Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland.
authors.forename: Antonio P
authors.initials: AP
authors.lastname: Silva
authors.affiliation: Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland.
authors.forename: Gisbert
authors.initials: G
authors.lastname: Weckbecker
authors.affiliation: Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland.
authors.forename: Christian
authors.initials: C
authors.lastname: Bruns
authors.affiliation: Global Discovery Chemistry Novartis Institutes of Biomedical Research CH-4002 Basel, Switzerland.
authors.forename: Janos
authors.initials: J
authors.lastname: Pless
mesh_terms: D003480:Cushing Syndrome / Q000188:drug therapy*; D006801:Humans; D008958:Models, Molecular; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use
chemical_list: D013004:Somatostatin; C517782:pasireotide