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35 Results Found

  • Article
  • Open Access
15 Citations
3,460 Views
15 Pages

P720R USP8 Mutation Is Associated with a Better Responsiveness to Pasireotide in ACTH-Secreting PitNETs

  • Donatella Treppiedi,
  • Giusy Marra,
  • Genesio Di Muro,
  • Emanuela Esposito,
  • Anna Maria Barbieri,
  • Rosa Catalano,
  • Federica Mangili,
  • Francesca Bravi,
  • Marco Locatelli and
  • Erika Peverelli
  • + 8 authors

16 May 2022

Somatic mutations in the ubiquitin specific peptidase 8 (USP8) gene have been associated with higher levels of somatostatin (SS) receptor subtype 5 (SSTR5) in adrenocorticotroph hormone (ACTH)-secreting pituitary neuroendocrine tumors (PitNETs). Howe...

  • Article
  • Open Access
2 Citations
2,178 Views
14 Pages

18 April 2025

Background/Objectives: Pasireotide-LAR represents a novel therapeutic option for patients with Cushing’s disease (CD). Its efficacy and safety were assessed in clinical trials; however, the real-world evidence is still scarce. Methods: The stud...

  • Article
  • Open Access
6 Citations
5,262 Views
13 Pages

A Practical and Total Synthesis of Pasireotide: Synthesis of Cyclic Hexapeptide via a Three-Component Condensation

  • Chunying Ma,
  • Miao Chen,
  • Weiming Chu,
  • Jiayi Tao,
  • Delong Kong,
  • Mengmeng Zhang and
  • Wenhua Feng

11 June 2019

Pasireotide is a multi-receptor ligand somatostatin analogue approved for medical treatment of Cushing’s disease and acromegaly. The liquid-phase total synthesis of pasireotide-a 18-membered cyclic hexapeptide-was achieved by the 3 + 2 + 1 stra...

  • Article
  • Open Access
14 Citations
4,292 Views
19 Pages

Gender-Specific Efficacy Revealed by Head-to-Head Comparison of Pasireotide and Octreotide in a Representative In Vivo Model of Nonfunctioning Pituitary Tumors

  • Sebastian Gulde,
  • Tobias Wiedemann,
  • Mathias Schillmaier,
  • Isabel Valença,
  • Amelie Lupp,
  • Katja Steiger,
  • Hsi-Yu Yen,
  • Stephen Bäuerle,
  • Johannes Notni and
  • Natalia S. Pellegata
  • + 5 authors

21 June 2021

Invasive nonfunctioning pituitary tumors (NFPTs) are non-resectable neoplasms associated with frequent relapse and significant comorbidities. Current treatments, including somatostatin receptor 2 (SSTR2)-directed somatostatin analogs (SSAs), often fa...

  • Article
  • Open Access
1 Citations
2,672 Views
9 Pages

Clinical Evaluation of Response to Octreotide and Chemotherapy in High-Grade Malignant Neuroendocrine Tumors and Promising In Vitro Preclinical Results with Pasireotide

  • Kevin Doello,
  • Maria Angeles Chico,
  • Francisco Quiñonero,
  • Raúl Ortiz,
  • Jose Prados,
  • Cristina Mesas and
  • Consolación Melguizo

25 June 2024

Background and Objectives: High-grade malignant neuroendocrine tumors (G3 NETs) and neuroendocrine carcinomas (NECs) are characterized by rapid proliferation, high metastatic capacity, and strong expression of somatostatin receptors (SSTRs). We aimed...

  • Article
  • Open Access
9 Citations
4,644 Views
12 Pages

A Multicenter Randomized Phase II Study of Single Agent Efficacy and Optimal Combination Sequence of Everolimus and Pasireotide LAR in Advanced Thyroid Cancer

  • Julie E. Bauman,
  • Zhengjia Chen,
  • Chao Zhang,
  • James P. Ohr,
  • Robert L. Ferris,
  • Gerald M. McGorisk,
  • Stephen Brandt,
  • Sumathi Srivatsa,
  • Amy Y. Chen and
  • Taofeek K. Owonikoko
  • + 4 authors

26 May 2022

Purpose: Aberrant mTOR pathway and somatostatin receptor signaling are implicated in thyroid cancer and offer potential therapeutic targets. We assessed the clinical efficacy of everolimus and Pasireotide long-acting release (LAR) in radioiodine-refr...

  • Article
  • Open Access
4 Citations
3,274 Views
22 Pages

Real-Life Data on the Safety of Pasireotide in Acromegaly: Insights from EudraVigilance

  • Ioana Rada Popa Ilie,
  • Carmen Maximiliana Dobrea,
  • Anca Butuca,
  • Calin Homorodean,
  • Claudiu Morgovan,
  • Andreea Loredana Vonica-Tincu,
  • Felicia Gabriela Gligor,
  • Steliana Ghibu and
  • Adina Frum

4 December 2024

Background/Objectives: Pasireotide (PAS) is a somatostatin receptor ligand (SRL) used to treat acromegaly, a chronic condition caused by excess growth hormone. While it offers significant benefits as a second-line treatment for uncontrolled acromegal...

  • Article
  • Open Access
5 Citations
2,954 Views
13 Pages

Incretin Response to Mixed Meal Challenge in Active Cushing’s Disease and after Pasireotide Therapy

  • Mattia Barbot,
  • Alessandro Mondin,
  • Daniela Regazzo,
  • Valentina Guarnotta,
  • Daniela Basso,
  • Carla Giordano,
  • Carla Scaroni and
  • Filippo Ceccato

Cushing’s disease (CD) causes diabetes mellitus (DM) through different mechanisms in a significant proportion of patients. Glucose metabolism has rarely been assessed with appropriate testing in CD; we aimed to evaluate hormonal response to a m...

  • Article
  • Open Access
12 Citations
3,266 Views
18 Pages

Octreotide and Pasireotide Combination Treatment in Somatotroph Tumor Cells: Predominant Role of SST2 in Mediating Ligand Effects

  • Jessica Amarù,
  • Federica Barbieri,
  • Marica Arvigo,
  • Agnese Solari,
  • Adriana Bajetto,
  • Federica Nista,
  • Claudia Campana,
  • Gabriele Gaggero,
  • Alessandro Prior and
  • Federico Gatto
  • + 4 authors

10 April 2021

First-generation somatostatin receptor ligands (fg-SRLs), such as octreotide (OCT), represent the first-line medical therapy in acromegaly. Fg-SRLs show a preferential binding affinity for somatostatin receptor subtype-2 (SST2), while the second-gene...

  • Communication
  • Open Access
3 Citations
1,548 Views
9 Pages

Protective Effects of Pasireotide in LPS-Induced Acute Lung Injury

  • Saikat Fakir,
  • Md Matiur Rahman Sarker,
  • Madan Sigdel and
  • Nektarios Barabutis

Background/Objectives: Acute lung injury (ALI) is an inflammatory condition characterized by tissue barrier damage, which leads to vascular leakage, pulmonary edema, and compromised gas exchange. Lipopolysaccharides (LPS) are a component of Gram-nega...

  • Article
  • Open Access
7 Citations
3,844 Views
11 Pages

Evaluation of PepT1 (SLC15A1) Substrate Characteristics of Therapeutic Cyclic Peptides

  • Gzona Bajraktari-Sylejmani,
  • Teresa von Linde,
  • Jürgen Burhenne,
  • Walter Emil Haefeli,
  • Max Sauter and
  • Johanna Weiss

The human peptide transporter hPepT1 (SLC15A1), physiologically transporting dipeptides and tripeptides generated during food digestion, also plays a role in the uptake of small bioactive peptides and peptide-like drugs. Moreover, it might be address...

  • Review
  • Open Access
8 Citations
4,597 Views
14 Pages

Meningiomas and Somatostatin Analogs: A Systematic Scoping Review on Current Insights and Future Perspectives

  • Sofie Eline Tollefsen,
  • Ole Solheim,
  • Patricia Mjønes and
  • Sverre Helge Torp

Meningioma is the most frequent brain tumor, and the incidence is ever-increasing. Though often benign and slow growth, recurrence rates are substantial and today’s surgical and radiation-based treatment are not without complications. No drugs...

  • Review
  • Open Access
50 Citations
23,303 Views
56 Pages

Cushing’s Disease

  • Hiroshi Nishioka and
  • Shozo Yamada

12 November 2019

In patients with Cushing’s disease (CD), prompt diagnosis and treatment are essential for favorable long-term outcomes, although this remains a challenging task. The differential diagnosis of CD is still difficult in some patients, even with an...

  • Review
  • Open Access
188 Citations
31,469 Views
27 Pages

Somatostatin Analogs in Clinical Practice: A Review

  • Mariana Gomes-Porras,
  • Jersy Cárdenas-Salas and
  • Cristina Álvarez-Escolá

29 February 2020

Somatostatin analogs are an invaluable therapeutic option in the diagnosis and treatment of somatotropinomas, thyrotropinomas, and functioning and non-functioning gastroenteropancreatic neuroendocrine tumors. They should also be considered an effecti...

  • Review
  • Open Access
1 Citations
3,707 Views
17 Pages

Differential Impact of Medical Therapies for Acromegaly on Glucose Metabolism

  • Federico Gatto,
  • Anna Arecco,
  • Jessica Amarù,
  • Marica Arvigo,
  • Claudia Campana,
  • Angelo Milioto,
  • Daniela Esposito,
  • Gudmundur Johannsson,
  • Francesco Cocchiara and
  • Alessandra Puddu
  • + 2 authors

Acromegaly is a rare endocrine disorder caused by excessive growth hormone (GH) production, due, in the vast majority of cases, to the presence of a GH-secreting pituitary tumour. The chronic elevation of GH and the resulting high circulating levels...

  • Review
  • Open Access
8 Citations
5,460 Views
39 Pages

Agonists, Antagonists and Receptors of Somatostatin: Pathophysiological and Therapeutical Implications in Neoplasias

  • Argyrios Periferakis,
  • Georgios Tsigas,
  • Aristodemos-Theodoros Periferakis,
  • Carla Mihaela Tone,
  • Daria Alexandra Hemes,
  • Konstantinos Periferakis,
  • Lamprini Troumpata,
  • Ioana Anca Badarau,
  • Cristian Scheau and
  • Andreea-Elena Scheau
  • + 3 authors

2 September 2024

Somatostatin is a peptide that plays a variety of roles such as neurotransmitter and endocrine regulator; its actions as a cell regulator in various tissues of the human body are represented mainly by inhibitory effects, and it shows potent activity...

  • Case Report
  • Open Access
5 Citations
2,861 Views
10 Pages

Somatostatin Receptor Subtype Expression in Patients with Acromegaly and Complicated Clinical Course

  • Robert Pichler,
  • Ognian Kalev,
  • Berndt Tomancok,
  • Michael Sonnberger,
  • Daniela Ehrlich and
  • Marina Hodolic

Somatostatin analogues are considered to be the first line of treatment in acromegaly. Somatostatin analogues of the first generation mainly target the somatostatin receptor (SSTR) subtype 2 and have been proven efficient in the majority of patients...

  • Review
  • Open Access
3 Citations
6,039 Views
12 Pages

Clinical Management of Acromegaly: Therapeutic Frontiers and New Perspectives for Somatostatin Receptor Ligands (SRLs)

  • Alessandro Brunetti,
  • Simone Antonini,
  • Andrea Saladino,
  • Elisabetta Lavezzi,
  • Benedetta Zampetti and
  • Renato Cozzi

13 June 2022

Somatostatin receptor ligands (SRLs) represent a true milestone in the medical therapy for acromegaly. The first-generation SRLs (FG-SRLs), octreotide and lanreotide, have demonstrated good efficacy in disease control and tumor shrinkage, and are sti...

  • Article
  • Open Access
4 Citations
3,506 Views
19 Pages

Identification of a Novel SSTR3 Full Agonist for the Treatment of Nonfunctioning Pituitary Adenomas

  • Daniela Modena,
  • Maria Luisa Moras,
  • Giovanni Sandrone,
  • Andrea Stevenazzi,
  • Barbara Vergani,
  • Pooja Dasgupta,
  • Andrea Kliever,
  • Sebastian Gulde,
  • Alessandro Marangelo and
  • Christian Steinkühler
  • + 5 authors

30 June 2023

Somatostatin receptor (SSTR) agonists have been extensively used for treating neuroendocrine tumors. Synthetic therapeutic agonists showing selectivity for SSTR2 (Octreotide) or for SSTR2 and SSTR5 (Pasireotide) have been approved for the treatment o...

  • Article
  • Open Access
6 Citations
1,888 Views
17 Pages

Resistance to first-generation somatostatin receptor ligand (fgSRL) treatment in acromegaly is common, making the identification of biomarkers that predict fgSRL response a desired goal. We conducted a retrospective analysis on 21 patients with acrom...

  • Review
  • Open Access
39 Citations
8,725 Views
31 Pages

Biological and Biochemical Basis of the Differential Efficacy of First and Second Generation Somatostatin Receptor Ligands in Neuroendocrine Neoplasms

  • Federico Gatto,
  • Federica Barbieri,
  • Marica Arvigo,
  • Stefano Thellung,
  • Jessica Amarù,
  • Manuela Albertelli,
  • Diego Ferone and
  • Tullio Florio

13 August 2019

Endogenous somatostatin shows anti-secretory effects in both physiological and pathological settings, as well as inhibitory activity on cell growth. Since somatostatin is not suitable for clinical practice, researchers developed synthetic somatostati...

  • Review
  • Open Access
10 Citations
6,378 Views
17 Pages

13 January 2023

Cushing’s disease is caused by autonomous secretion of adrenocorticotropic hormone (ACTH) from corticotroph pituitary neuroendocrine tumors. As a result, excess cortisol production leads to the overt manifestation of the clinical features of Cu...

  • Review
  • Open Access
14 Citations
9,929 Views
8 Pages

Pancreatic Fistulas: Current Evidence and Strategy—A Narrative Review

  • Clara Meierhofer,
  • Reinhold Fuegger,
  • Matthias Biebl and
  • Rainer Schoefl

31 July 2023

Pancreatic fistulas are highly feared complications following surgery on or near the pancreas, abdominal trauma, or severe inflammation. These fistulas arise from leaks in the pancreatic ductal system, leading to various complications such as abscess...

  • Article
  • Open Access
9 Citations
3,027 Views
12 Pages

12 October 2021

Veldoreotide, a somatostatin analogue, binds to the somatostatin receptors (SSTR) 2, 4, and 5. The current aim was to assess its pharmacological activity as an SSTR4 agonist. G-protein signaling was assessed using a fluorescence-based membrane potent...

  • Case Report
  • Open Access
6 Citations
5,414 Views
10 Pages

Role of Receptor Profiling for Personalized Therapy in a Patient with a Growth Hormone-Secreting Macroadenoma Resistant to First-Generation Somatostatin Analogues

  • Krystallenia I. Alexandraki,
  • Eirini Papadimitriou,
  • Vasiliki Mavroeidi,
  • Georgios Kyriakopoulos,
  • Antonios Xydakis,
  • Theodoros G. Papaioannou,
  • Denise Kolomodi,
  • Gregory A. Kaltsas and
  • Ashley B. Grossman

15 November 2019

Background: Acromegaly is almost always caused by a pituitary adenoma and is associated with high morbidity and mortality when uncontrolled. Trans-sphenoidal removal of the adenoma is the mainstay of therapy, but fails to control the disease in a sig...

  • Article
  • Open Access
7 Citations
2,900 Views
14 Pages

Molecular and Clinical Implications of Somatostatin Receptor Profile and Somatostatin Analogues Treatment in Oral Cavity Squamous Cell Carcinoma

  • Alba Sanjuan-Sanjuan,
  • Emilia Alors-Perez,
  • Marina Sanchez-Frías,
  • Alicia Dean-Ferrer,
  • Manuel D. Gahete,
  • Susana Heredero-Jung and
  • Raúl M. Luque

27 September 2021

Oral squamous cell carcinoma (OSCC) incidence has increased by 50% over the last decade. Unfortunately, surgery and adjuvant radiotherapy and chemotherapy are still the mainstream modality of treatment, underscoring the need for alternative therapies...

  • Article
  • Open Access
3 Citations
2,145 Views
10 Pages

The Novel SSTR3 Agonist ITF2984 Exerts Antimitotic and Proapoptotic Effects in Human Non-Functioning Pituitary Neuroendocrine Tumor (NF-PitNET) Cells

  • Genesio Di Muro,
  • Rosa Catalano,
  • Donatella Treppiedi,
  • Anna Maria Barbieri,
  • Federica Mangili,
  • Giusy Marra,
  • Sonia Di Bari,
  • Emanuela Esposito,
  • Emma Nozza and
  • Giovanna Mantovani
  • + 6 authors

Somatostatin receptor ligands (SRLs) with high affinity for somatostatin receptors 2 and 5 (SSTR2 and SSTR5) are poorly efficacious in NF-PitNETs, expressing high levels of SSTR3. ITF2984 is a pan-SSTR ligand with high affinity for SSTR3, able to ind...

  • Article
  • Open Access
2 Citations
1,160 Views
17 Pages

The human genome is widely transcribed, with part of these transcribed regions producing stably expressed protein-coding or non-coding RNAs. Long intergenic non-coding RNAs (lincRNAs) are significantly differentially expressed in various cell lines a...

  • Review
  • Open Access
4,334 Views
23 Pages

Dumping Syndrome After Bariatric Surgery: Advanced Nutritional Perspectives and Integrated Pharmacological Management

  • Raquel Cano,
  • Daniel Rodríguez,
  • Pablo Duran,
  • Clímaco Cano,
  • Diana Rojas-Gómez,
  • Diego Rivera-Porras,
  • Paola Barboza-González,
  • Héctor Fuentes-Barría,
  • Lissé Angarita and
  • Valmore Bermúdez
  • + 1 author

30 September 2025

Dumping Syndrome (DS) is a significant complication following bariatric surgery, particularly Roux-en-Y gastric bypass (RYGB). This condition is characterised by gastrointestinal and vasomotor symptoms resulting from altered anatomy and hormonal dysr...

  • Review
  • Open Access
1 Citations
1,529 Views
20 Pages

Clinical Implications of Molecular and Genetic Biomarkers in Cushing’s Disease: A Literature Review

  • Laura Chinezu,
  • Maximilian Cosma Gliga,
  • Mihnea Bogdan Borz,
  • Camelia Gliga and
  • Ionela Maria Pascanu

26 April 2025

Cushing’s disease (CD) is a rare disorder caused by adrenocorticotropic hormone (ACTH)-secreting pituitary neuroendocrine tumors, which lead to chronic hypercortisolism and significant complications with increased mortality. These tumors are ch...

  • Review
  • Open Access
2,164 Views
10 Pages

Navigating the Spectrum of Pancreatic Surgery Complications: A Review

  • Sibi Krishna Thiyagarajan,
  • Alfredo Verastegui,
  • John A. Stauffer and
  • Katherine Poruk

Background: Despite advances in surgical techniques and perioperative care, pancreatic resections such as pancreaticoduodenectomy (PD) and distal pancreatectomy (DP) remain high-risk procedures. Postoperative complications significantly impact morbid...

  • Article
  • Open Access
9 Citations
4,209 Views
17 Pages

Somatostatin Receptor Splicing Variant sst5TMD4 Overexpression in Glioblastoma Is Associated with Poor Survival, Increased Aggressiveness Features, and Somatostatin Analogs Resistance

  • Antonio C. Fuentes-Fayos,
  • Miguel E. G-García,
  • Jesús M. Pérez-Gómez,
  • Annabel Peel,
  • Cristóbal Blanco-Acevedo,
  • Juan Solivera,
  • Alejandro Ibáñez-Costa,
  • Manuel D. Gahete,
  • Justo P. Castaño and
  • Raúl M. Luque

20 January 2022

Glioblastoma (GBM) is the most malignant and lethal brain tumor. Current standard treatment consists of surgery followed by radiotherapy/chemotherapy; however, this is only a palliative approach with a mean post-operative survival of scarcely ~12&nda...

  • Article
  • Open Access
7 Citations
3,473 Views
17 Pages

Somatostatin, Cortistatin and Their Receptors Exert Antitumor Actions in Androgen-Independent Prostate Cancer Cells: Critical Role of Endogenous Cortistatin

  • Prudencio Sáez-Martínez,
  • Francisco Porcel-Pastrana,
  • Jesús M. Pérez-Gómez,
  • Sergio Pedraza-Arévalo,
  • Enrique Gómez-Gómez,
  • Juan M. Jiménez-Vacas,
  • Manuel D. Gahete and
  • Raúl M. Luque

27 October 2022

Somatostatin (SST), cortistatin (CORT), and their receptors (SSTR1-5/sst5TMD4-TMD5) comprise a multifactorial hormonal system involved in the regulation of numerous pathophysiological processes. Certain components of this system are dysregulated and...

  • Review
  • Open Access
28 Citations
8,372 Views
22 Pages

Management and Medical Therapy of Mild Hypercortisolism

  • Vittoria Favero,
  • Arianna Cremaschi,
  • Alberto Falchetti,
  • Agostino Gaudio,
  • Luigi Gennari,
  • Alfredo Scillitani,
  • Fabio Vescini,
  • Valentina Morelli,
  • Carmen Aresta and
  • Iacopo Chiodini

26 October 2021

Mild hypercortisolism (mHC) is defined as an excessive cortisol secretion, without the classical manifestations of clinically overt Cushing’s syndrome. This condition increases the risk of bone fragility, neuropsychological alterations, hypertension,...

  • Review
  • Open Access
35 Citations
5,538 Views
24 Pages

Approach of Acromegaly during Pregnancy

  • Alexandru Dan Popescu,
  • Mara Carsote,
  • Ana Valea,
  • Andreea Gabriela Nicola,
  • Ionela Teodora Dascălu,
  • Tiberiu Tircă,
  • Jaqueline Abdul-Razzak and
  • Mihaela Jana Țuculină

2 November 2022

Acromegaly-related sub/infertility, tidily related to suboptimal disease control (1/2 of cases), correlates with hyperprolactinemia (1/3 of patients), hypogonadotropic hypogonadism—mostly affecting the pituitary axis in hypopituitarism (10&ndas...