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SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profile

European Journal of Endocrinology · 2002 · Vol. 146(5) · pp. 707–716

Christian Bruns✉(Novartis (Switzerland))Ian Lewis(Novartis (Switzerland))U. Briner(Novartis (Switzerland))Guy Meno‐Tetang(Novartis (Switzerland))Gisbert Weckbecker✉(Novartis (Switzerland))

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Abstract

We have identified a novel short synthetic SRIF peptidomimetic, which exhibits high affinity binding to four of the five human SRIF receptor subtypes and has potent, long lasting inhibitory effects on GH and IGF-I release. Therefore SOM230 is a promising development candidate for effective GH and IGF-I inhibition and is currently under evaluation in phase 1 clinical trials.

Neuroendocrine Tumor Research Advances Growth Hormone and Insulin-like Growth Factors Pituitary Gland Disorders and TreatmentsSomatostatinInternal medicineIn vivoSomatostatin receptorEndocrinologyReceptorChemistryPharmacologyBiologyMedicine

MeSH terms

AnimalsBinding, CompetitiveDose-Response Relationship, DrugGlucagonHumansInsulin AntagonistsInsulin-Like Growth Factor IMaleRats, Inbred LewSomatostatinReceptors, SomatostatinHuman Growth HormoneProtein IsoformsRats

Citations

683

FWCI

16.90

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99%

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