Cited by 290Pituitary Gland Disorders and TreatmentsNeuroendocrine Tumor Research AdvancesGrowth Hormone and Insulin-like Growth Factors

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Pasireotide (SOM230): Development, mechanism of action and potential applications

Schmid, Herbert A.·2008·Molecular and Cellular Endocrinology

DOI 10.1016/j.mce.2007.09.006

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Abstract

Pasireotide (SOM230) is a multi-receptor ligand somatostatin analogue with high binding affinity for somatostatin receptor subtypes sst(1,2,3) and sst(5). Pasireotide potently suppresses GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. The prolonged inhibition of hormone secretion by pasireotide in animal models and expression of multiple sst receptors in carcinoid tumors suggests that pasireotide may have clinical advantages over octreotide in patients with carcinoid tumors. Direct and indirect antitumor activity has been observed in vitro with pasireotide, including sst receptor-mediated apoptosis and antiangiogenesis, suggesting a possible role for pasireotide in antineoplastic therapy. In summary, preclinical evidence, as well as preliminary results from clinical studies suggests that pasireotide is a promising new treatment for patients with symptoms of metastatic carcinoid tumors refractory or resistant to octreotide, de novo or persistent acromegaly, and that pasireotide has the potential to be the first directed medical therapy for Cushing's disease.

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Authors: Schmid, H. A.
Affiliations: Novartis (Switzerland) (CH)
Corresponding author: Schmid, Herbert A.
Venue: Molecular and Cellular Endocrinology
Publisher: Elsevier BV
Published: 2008-05
Volume: 286
Issue: 1-2
Pages: 69-74
ISSN: 0303-7207 (ISSN-L)
DOI: 10.1016/j.mce.2007.09.006
OpenAlex: W2012451298
Cited by: 290
References: 0
Citations by year: 2026: 3 · 2025: 5 · 2024: 13 · 2023: 10 · 2022: 9 · 2021: 11 · 2020: 11 · 2019: 12 · 2018: 18 · 2017: 15 · 2016: 19 · 2015: 17 · 2014: 23 · 2013: 21 · 2012: 30
FWCI: 2.34
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Molecular and Cellular Endocrinology (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Pituitary Gland Disorders and Treatments
Health Sciences › Medicine › Oncology › Neuroendocrine Tumor Research Advances
Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Growth Hormone and Insulin-like Growth Factors
Keywords: pasireotide, somatostatin analogues, somatostatin receptor subtypes, acromegaly, Cushing's disease, carcinoid tumor, octreotide, anticancer activity, apoptosis, angiogenesis inhibition, growth hormone suppression, ACTH suppression
MeSH terms: Acromegaly, Adrenocorticotropic Hormone, Animals, Carcinoid Tumor, Humans, Insulin-Like Growth Factor I, Somatostatin, Growth Hormone, Structure-Activity Relationship, Octreotide, Receptors, Somatostatin, Antineoplastic Agents, Hormonal, Drug Resistance, Neoplasm, Pituitary ACTH Hypersecretion

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Pasireotide (SOM230): Development, mechanism of action and potential applications

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