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Frontiers of Hormone Research 2015Peptide receptor radionuclide therapy (PRRT) has been a well-accepted and effective therapeutic modality for inoperable or metastatic gastroenteropancreatic,... (Review)
Review
Peptide receptor radionuclide therapy (PRRT) has been a well-accepted and effective therapeutic modality for inoperable or metastatic gastroenteropancreatic, bronchopulmonary and other neuroendocrine tumors for almost 2 decades. In general, PRRT is well tolerated with moderate toxicity in the majority of patients if the necessary precautions, appropriate dosage and coadministration of amino acids are undertaken. The two most commonly used radiopeptides, (90)Y-octreotide and (177)Lu-octreotate, produce significant objective response rates, with impact on progression-free survival and overall survival. In addition, biochemical and symptomatic responses are commonly observed. A key issue is the need to establish randomized controlled trials to standardize the treatment and facilitate comparison with other therapeutic strategies available.
Topics: Antineoplastic Agents, Hormonal; Humans; Neuroendocrine Tumors; Octreotide; Radiopharmaceuticals; Receptors, Peptide
PubMed: 26303714
DOI: 10.1159/000402936 -
Current Oncology Reports Feb 2017Peptide receptor radionuclide therapy (PRRT) is a form of systemic radiotherapy that allows targeted delivery of radionuclides to tumor cells expressing high levels of... (Review)
Review
Peptide receptor radionuclide therapy (PRRT) is a form of systemic radiotherapy that allows targeted delivery of radionuclides to tumor cells expressing high levels of somatostatin receptors. The two radiopeptides most commonly used for PRRT, Y-DOTATOC and Lu-DOTATATE, have been successfully employed for more than a decade for the treatment of advanced neuroendocrine tumors (NETs). Recently, the phase III, randomized NETTER-1 trial has compared Lu-DOTATATE versus high-dose octreotide LAR in patients with progressive, metastatic midgut NETs, demonstrating exceptional tolerability and efficacy. This review summarizes recent developments in the field of radionuclide therapy for gastroenteropancreatic and lung NETs and considers possible strategies to further enhance its clinical efficacy.
Topics: Clinical Trials, Phase III as Topic; Humans; Lung; Neuroendocrine Tumors; Octreotide; Organometallic Compounds; Pancreas; Radioisotopes; Radiopharmaceuticals; Receptors, Somatostatin; Stomach
PubMed: 28220446
DOI: 10.1007/s11912-017-0567-8 -
Cancer Treatment Reviews Jun 2023Octreotide and lanreotide are the two somatostatin analogs (SSA) currently available in clinical practice. They have been approved first to control the clinical syndrome... (Review)
Review
Octreotide and lanreotide are the two somatostatin analogs (SSA) currently available in clinical practice. They have been approved first to control the clinical syndrome (mainly carcinoid syndrome) associated with functioning neuroendocrine tumors (NET) and later for tumor growth control in advanced low/intermediate grade NET. Although evidence regarding their role, especially as antiproliferative therapy, has been increasing over the years some clinical indications remain controversial. Solicited by AIOM (Italian Association of Medical Oncology) a group of clinicians from various specialties, including medical oncology, endocrinology, and gastroenterology, deeply involved in NET for their clinical and research activity, addressed eight open questions, critically reviewing evidence and guidelines and sharing clinical take-home messages. The questions regarded the use of long-acting octreotide and lanreotide in the following settings: functioning and non-functioning NET refractory to label dose, first-line metastatic pulmonary NET, combination with other therapy with an antiproliferative intent, maintenance in NET responding to other therapies, adjuvant treatment, Ki-67-related cut-off, somatostatin receptor imaging, safety, and feasibility. The level of evidence is not absolute for the majority of these clinical contexts, so it is recommended to distinguish routine versus sporadic utilization in very selected cases. Mention of such specific issues by the main European guidelines (ENETS, European Neuroendocrine Tumor Society, and ESMO, European Society for Medical Oncology) was explored and their position reported. However, different clinical decisions on single patients could be made if the case is carefully discussed within a NET-dedicated multidisciplinary team.
Topics: Humans; Octreotide; Neuroendocrine Tumors; Somatostatin; Peptides, Cyclic
PubMed: 37088017
DOI: 10.1016/j.ctrv.2023.102560 -
British Journal of Clinical Pharmacology Mar 2016The most common toxicity associated with sulfonylureas and insulin is hypoglycaemia. The article reviews existing evidence to better guide hypoglycaemia management.... (Review)
Review
The most common toxicity associated with sulfonylureas and insulin is hypoglycaemia. The article reviews existing evidence to better guide hypoglycaemia management. Sulfonylureas and insulin have narrow therapeutic indices. Small doses can cause hypoglycaemia, which may be delayed and persistent. All children and adults with intentional overdoses need to be referred for medical assessment and treatment. Unintentional supratherapeutic ingestions can be initially managed at home but if symptomatic or if there is persistent hypoglycaemia require medical referral. Patients often require intensive care and prolonged observation periods. Blood glucose concentrations should be assessed frequently. Asymptomatic children with unintentional sulfonylurea ingestions should be observed for 12 h, except if this would lead to discharge at night when they should be kept until the morning. Prophylactic intravenous dextrose is not recommended. The goal of therapy is to restore and maintain euglycaemia for the duration of the drug's toxic effect. Enteral feeding is recommended in patients who are alert and able to tolerate oral intake. Once insulin or sulfonylurea-induced hypoglycaemia has developed, it should be initially treated with an intravenous dextrose bolus. Following this the mainstay of therapy for insulin-induced hypoglycaemia is intravenous dextrose infusion to maintain the blood glucose concentration between 5.5 and 11 mmol l(-1) . After sulfonylurea-induced hypoglycaemia is initially corrected with intravenous dextrose, the main treatment is octreotide which is administered to prevent insulin secretion and maintain euglycaemia. The observation period varies depending on drug, product formulation and dose. A general guideline is to observe for 12 h after discontinuation of intravenous dextrose and, if applicable, octreotide.
Topics: Drug Overdose; Glucose; Humans; Hypoglycemia; Infusions, Intravenous; Insulin; Octreotide; Sulfonylurea Compounds
PubMed: 26551662
DOI: 10.1111/bcp.12822 -
Anesthesiology Clinics Jun 2017Many patients presenting with a history of foregut, midgut neuroendocrine tumors (NETs) or carcinoid syndrome can experience life-threatening carcinoid crises during... (Review)
Review
Many patients presenting with a history of foregut, midgut neuroendocrine tumors (NETs) or carcinoid syndrome can experience life-threatening carcinoid crises during anesthesia or surgery. Clinicians should understand the pharmacology of octreotide and appreciate the use of continuous infusions of high-dose octreotide, which can minimize intraoperative carcinoid crises. We administer a prophylactic 500-μg bolus of octreotide intravenously (IV) and begin a continuous infusion of 500 μg/h for all NET patients. Advantages include low cost and excellent safety profile. High-dose octreotide for midgut and foregut NETs requires an appreciation of the pathophysiology involved in the disease, pharmacology, drug-drug interactions, and side effects.
Topics: Anesthesia; Anesthesiologists; Carcinoid Tumor; Gastrointestinal Agents; Humans; Intraoperative Complications; Malignant Carcinoid Syndrome; Neuroendocrine Tumors; Octreotide; Risk
PubMed: 28526153
DOI: 10.1016/j.anclin.2017.01.021 -
Journal of Neonatal-perinatal Medicine 2021Being a rare condition, the incidence of chylothorax among neonates is low, but the mortality rate is high. In a dire effort to reduce the risk of death, octreotide... (Review)
Review
BACKGROUND
Being a rare condition, the incidence of chylothorax among neonates is low, but the mortality rate is high. In a dire effort to reduce the risk of death, octreotide treatment is used to effectively treat acquired and congenital chylothorax. Octreotide is proven to effectively treat chylothorax in pre-term and full-term neonates. However, previous studies have not consistently demonstrated the optimal dose of octreotide or the best mode of administration. The objectives of this work were to review previous literature to determine the outcomes of administering high doses of octreotide compared to lower dose regimens in neonates with chylothorax and to determine best practices.
METHODS
A literature search was performed using electronic databases using the key words neonates, chylothorax, and octreotide.
RESULTS
Octreotide has been administrated in doses ranging from 0.5μg/kg/h to > 20μg/kg/h. Both low- and high-doses of octreotide are effective in resolving chylothorax with little to no side effects. When side effects were reported, neonates experienced side effects that are less significant in nature and scope.
CONCLUSIONS
We recommend that the dose of octreotide in neonatal chylothorax can be titrated safely to a maximum of 20μg/kg/h without significant side effects.
Topics: Chylothorax; Humans; Infant, Newborn; Octreotide
PubMed: 33843702
DOI: 10.3233/NPM-200644 -
Journal of Pediatric Gastroenterology... Jan 2022Octreotide, a somatostatin analogue, has been used for more than 20 years in children with gastrointestinal bleeding, chylothorax or chylous ascites, intestinal... (Review)
Review
Octreotide, a somatostatin analogue, has been used for more than 20 years in children with gastrointestinal bleeding, chylothorax or chylous ascites, intestinal lymphangiectasia, pancreatitis, intestinal dysmotility, and severe diarrhoea; however, until now, there is a lack of randomised clinical trials evaluating the efficacy of this compound in childhood. Hence, we aimed to review the literature in order to determine the evidence of its use and safety in children, using PubMed from 2000 to 2021 with the search terms "octreotide" and "children" and "bleeding or chylous ascites or chylothorax or acute pancreatitis or lymphangiectasia or diarrhoea or intestinal dysmotility".
Topics: Acute Disease; Child; Gastrointestinal Agents; Gastrointestinal Diseases; Humans; Octreotide; Pancreatitis; Pharmaceutical Preparations
PubMed: 34508049
DOI: 10.1097/MPG.0000000000003294 -
The Lancet. Oncology Jul 2017Targeted radionuclide therapy (TRT) is a branch of cancer medicine concerned with the use of radioisotopes, radiolabelled molecules, nanoparticles, or microparticles... (Review)
Review
Targeted radionuclide therapy (TRT) is a branch of cancer medicine concerned with the use of radioisotopes, radiolabelled molecules, nanoparticles, or microparticles that either naturally accumulate in or are designed to target tumours. TRT combines the specificity of molecular and sometimes physical targeting with the potent cytotoxicity of ionising radiation. Targeting vectors for TRT include antibodies, antibody fragments, proteins, peptides, and small molecules. The diversity of available carrier molecules, together with the large panel of suitable radioisotopes with unique physicochemical properties, allows vector-radionuclide pairings to be matched to the molecular, pathological, and physical characteristics of a tumour. Some pairings are designed for dual therapeutic and diagnostic applications. Use of TRT is increasing with the adoption into practice of radium-223 dichloride for the treatment of bone metastases and with the ongoing clinical development of, among others, Lu-dodecanetetraacetic acid tyrosine-3-octreotate (DOTATATE) for the treatment of neuroendocrine tumours and Y-microspheres for the treatment of hepatic tumours. The increasing use of TRT raises the question of how best to integrate TRT into multimodality protocols. Achievements in this area and the future prospects of TRT are evaluated in this Review.
Topics: 3-Iodobenzylguanidine; Antibodies, Monoclonal; Antineoplastic Agents; Chemoradiotherapy; DNA Repair; Humans; Immunotoxins; Microspheres; Molecular Targeted Therapy; Neoplasms; Octreotide; Organometallic Compounds; Radioisotopes; Radiotherapy; Radium
PubMed: 28677577
DOI: 10.1016/S1470-2045(17)30379-0 -
ChemPlusChem Apr 2020Many methods have been developed for attaching an alcohol functionality to a solid support. However, not all of these methods are used to obtain peptide alcohols. In... (Review)
Review
Many methods have been developed for attaching an alcohol functionality to a solid support. However, not all of these methods are used to obtain peptide alcohols. In this Minireview, we will discuss several of the most important methods and approaches for the synthesis of peptide alcohols and the attachment of hydroxy groups to a solid support for the synthesis of cyclic peptides. Some of the methods include the use of functionalized Wang resin and the attachment of an alcohol to an enol ether resin. We also discuss the use of the chlorotrityl resin, one of the most common linkers used to obtain peptide alcohols. In addition, we outline the recently developed resins with the Rink, Ramage and Sieber handles. The majority of these methods have been used to synthesize many important drugs, such as octreotide and the antibiotic peptaibols.
Topics: Alcohols; Anti-Bacterial Agents; Octreotide; Peptaibols; Polystyrenes; Solid-Phase Synthesis Techniques
PubMed: 32237227
DOI: 10.1002/cplu.201900749 -
European Journal of Endocrinology Nov 2019Octreotide remains 40 years after its development a drug, which is commonly used in the treatment of acromegaly and GEP-NETs. Very little innovation that competes with... (Review)
Review
Octreotide remains 40 years after its development a drug, which is commonly used in the treatment of acromegaly and GEP-NETs. Very little innovation that competes with this drug occurred over this period. This review discusses several aspects of 40 years of clinical use of octreotide, including the application of radiolabeled forms of the peptide.
Topics: Acromegaly; Endocrine Gland Neoplasms; History, 20th Century; Humans; Octreotide
PubMed: 31398712
DOI: 10.1530/EJE-19-0074