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Development of Targeted Alpha Particle Therapy for Solid Tumors.

Targeted alpha-particle therapy (TAT) aims to selectively deliver radionuclides emitting α-particles (cytotoxic payload) to tumors by chelation to monoclonal antibodies, peptides or small molecules that recognize tumor-associated antigens or cell-surface receptors. Because of the high linear energy transfer (LET) and short range of alpha (α) particles in tissue, cancer cells can be significantly damaged while causing minimal toxicity to surrounding healthy cells. Recent clinical studies have demonstrated the remarkable efficacy of TAT in the treatment of metastatic, castration-resistant prosta

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… The FDA approved octreotide (OC, Figure 4 ), the cyclic octapeptide, upon which much of the early peptide receptor radionuclide therapy (PRRT) was based. Chelating molecules attached and various radionuclides for β and α-emission therapies have been reported. … Figure 4 The somatostatin mimetic octreotide and its DOTA-containing analogs. Octreotide: R 1 = H, R 2 = H and R 3 = CH 2 OH; DOTATOC (endotreotide): R 1 = DOTA, R 2 = OH and R 3 = CO 2 H; DOTATATE (Octreotate): R 1 = DOTA, R 2 = OH and R 3 = CH 2 OH. …

Mechanisms of resistance to antibody-drug conjugates in cancer therapy: molecular basis and therapeutic strategies.

Antibody-drug conjugates (ADCs) have emerged as a transformative class in oncology, integrating the target specificity of monoclonal antibodies with the potent cytotoxicity of small-molecule payloads. By harnessing tumor-specific antigen recognition, ADCs enable the selective delivery of chemotherapeutic agents, thereby enhancing therapeutic efficacy while reducing systemic toxicity. Their clinical success across both hematologic malignancies and solid tumors underscores their potential to redefine targeted cancer therapy. However, the clinical durability of ADCs is increasingly undermined by

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… For instance, DOTA-(Tyr 3 )-octreotide ( 68 Ga-DOTATOC) rapidly localizes to tumors, achieving approximately 80% uptake within 30 min and a target-to-nontarget ratio of 100:1 in central nervous system lesions compared to normal brain tissue [ 89 ] . …

Multimodal imaging of bone metastases: From preclinical to clinical applications.

Metastases to the skeletal system are commonly observed in cancer patients, highly affecting the patients' quality of life. Imaging plays a major role in detection, follow-up, and molecular characterisation of metastatic disease. Thus, imaging techniques have been optimised and combined in a multimodal and multiparametric manner for assessment of complementary aspects in osseous metastases. This review summarises both application of the most relevant imaging techniques for bone metastasis in preclinical models and the clinical setting.

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… Gabriel M., Oberauer A., Dobrozemsky G., Decristoforo C., Putzer D., Kendler D. 68Ga-DOTA-Tyr3-octreotide PET for assessing response to somatostatin-receptor-mediated radionuclide therapy. J Nucl Med. 2009;50:1427–1434. doi: 10.2967/jnumed.108.053421. 89. …

Current landscape and future directions of targeted-alpha-therapy for glioblastoma treatment.

Glioblastoma (GB) is the most aggressive malignancy of the central nervous system. Despite two decades of intensive research since the establishment of the standard of care, emerging strategies have yet to produce consistent satisfactory outcomes. Because of its specific localisation and intricate characteristics, GB is a uniquely regulated solid tumour with a strong resistance to therapy. Advances in targeted radionuclide therapy (TRT), particularly with the introduction of a-emitting radionuclides, have unveiled potential avenues for the management of GB. Recent preclinical and clinical stud

Clinical Posters From JADPRO Live 2024

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Advancements in Targeted Radiopharmaceuticals: Innovations in Diagnosis and Therapy for Enhanced Cancer Management.

Radiopharmaceuticals (RPhs) represent a breakthrough in nuclear medicine due to their ability to provide precise diagnosis and targeted therapy for cancer by incorporating radioactive isotopes into carrier molecules. This review systematically discusses the recent advances in the development of RPhs, focusing on state-of-the-art probe design strategies and click chemistry applications that accelerate RPh syntheses and improve targeting efficiency. The manuscript synthesizes literature from multiple databases spanning January 2014 to April 2025, encompassing diagnostic modalities including posi

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… The NETTER‐1 trial demonstrated survival advantages compared to octreotide treatment. [ 88 ] Patients achieved 28.4 months of progression‐free survival, showing 18% response rates and 79% disease control. Benefits included life quality improvements and symptom reduction. … BC | D | PET | HER2 | HER2 | [ 261 ] 68 Ga‐DOTATATE | β+ | NET | D/S | PET | SSTR | SSTR | [ 262 ] 18 F‐FLT | β+ | Various cancers | D/S | PET | DNA syn | TK1 | [ 263 ] 64 Cu‐ATSM | β+ | Hypoxic tumors | D | PET | HT | – | [ 264 ] 18 F‐FMISO | β+ | Hypoxic tumors | D | PET | HT | – | [ 265 ] 111 In‐Octreotide …

Bioactivities and Mechanisms of Action of Sinomenine and Its Derivatives: A Comprehensive Review.

Sinomenine, an isoquinoline alkaloid extracted from the roots and stems of Sinomenium acutum, has been extensively studied for its derivatives as bioactive agents. This review concentrates on the research advancements in the biological activities and action mechanisms of sinomenine-related compounds until November 2023. The findings indicate a broad spectrum of pharmacological effects, including antitumor, anti-inflammation, neuroprotection, and immunosuppressive properties. These compounds are notably effective against breast, lung, liver, and prostate cancers, exhibiting IC50 values of appro

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… Li and associates reported that SIN increased the intestinal absorption of octreotide (OCT). SIN (0.5% w / v ) boosted OCT absorption in the gut through the activation of the PKC signaling pathway, thereby improving the pharmacokinetic behavior of OCT in rats. … necrosis factor; APAP: alleviated acetaminophen; IR: ischemia reperfusion; OVA: ovalbumin; TRPV-l: transient receptor potential vanilloid-1; NKA: neurokinin A; GDM: gestational diabetes mellitus; LPO: lipid peroxidation; GST: glutathione S-transferase; TEER: transepithelial electrical resistance; OCT: octreotide …

NETs: organ-related epigenetic derangements and potential clinical applications.

High-throughput next-generation sequencing methods have recently provided a detailed picture of the genetic landscape of neuroendocrine tumors (NETs), revealing recurrent mutations of chromatin-remodeling genes and little-to-no pathogenetic role for oncogenes commonly mutated in cancer. Concurrently, multiple epigenetic modifications have been described across the whole spectrum of NETs, and their putative function as tumorigenic drivers has been envisaged. As result, it is still unclear whether or not NETs are epigenetically-driven, rather than genetically-induced malignancies. Although the N

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… No synergistic effects were noted after combination with somatostatin or octreotide [ 88 ]. The antiproliferative effects of valproic acid (VPA) as a class I and IIa HDAC inhibitor have been extensively investigated in NETs. …

Acute Kidney Injury in the Patient with Cancer.

Over the last three decades, advancements in the diagnosis, treatment, and supportive care of patients with cancer have significantly improved their overall survival. However, these advancements have also led to a higher rate of cancer-related complications. Acute kidney injury (AKI) and chronic kidney disease (CKD) are highly prevalent in patients with cancer, and they are associated with an increased risk of all-cause mortality. This bidirectional interplay between cancer and kidney, termed "the kidney-cancer connection" has become a very active area of research. This review aims to provide

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… Management includes treating HRS precipitants and restoring effective arterial circulation with vasopressors: terlipressin, norepinephrine or midodrine in combination with octreotide [ 38 ]. Tense ascites may increase intraabdominal pressure, causing abdominal compartmental syndrome. …

Политика и перспективы в отношении амбулаторных программ для аутологической трансплантации клеток и лечения иммуноэффективных клеток.

Высокодозированная химиотерапия с автоматической трансплантацией гематопоиетических клеток (AutoHCT) давно является комплексной формой лечения множественной миеломы и неходгкинской лимфомы. В прошлом 25 Многие учреждения сместили эту практику с госпитализации на one , которые могут быть выполнены в амбулаторном порядке, что приведет к экономии средств и повышению качества жизни пациентов. Недавно появившиеся методы лечения иммуноэффективных клеток (ИЭК) и расширение их масштабов приводят к изменению ландшафта лечения гематологовых и негематологических магнатов. Однако нынешние финансовые модел

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… advance including prochlorperazine, 5-HTRA, benzodiazepine, with potential addition of transdermal scopolamine or olanzapine Mucositis prophylaxis with cryotherapy Anti-diarrheal agents for treatment of diarrhea prescribed in advance including loperamide and diphenoxylate/atropine, potential addition of octreotide …

Alignment of a Ritchey-Chrétien telescope with primary mirror figure error guided by the rapid measurement of binodal astigmatism.

AbstractHereditary hemorrhagic telangiectasia (HHT) causes severe recurrent epistaxis, chronic gastrointestinal bleeding, solid organ arteriovenous malformations, and significant anemia. Although it is the second most common inherited bleeding disorder worldwide, no approved therapies exist. The multicenter, US randomized, controlled PATH-HHT trial demonstrated efficacy of short-term pomalidomide treatment of epistaxis in HHT. However, questions regarding long-term safety, effectiveness, and utility for HHT-associated gastrointestinal bleeding remain. The PATH-HHT ATLAS (after trial longitudin

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… . § Includes pazopanib, tamoxifen, estradiol, doxycycline, and octreotide. …

Overdiagnosis of a typical carcinoid tumor as an adenocarcinoma of the lung: a case report and review of the literature.

BackgroundOverdiagnosis of bronchopulmonary carcinoid tumors together with overtreatment can cause serious postoperative consequences for the patient. We report of a patient with a typical bronchopulmonary carcinoid tumor, which was initially misdiagnosed and treated as an adenocarcinoma of the lung. GnrH receptors and the associated Raf-1/MEK/ERK-1/2-pathway are potential targets for analogs in cancer treatment. We suspected a correlation between the lack of tumor growth, application of leuprolide and the Raf-1/MEK/ERK-1/2-pathway. Therefore, we examined GnrH receptor status in the examined s

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… Octreotide and chemotherapy are normally used if a carcinoid syndrome or metastases are present. …

Prevention and management of adverse events of novel agents in multiple myeloma: a consensus of the European Myeloma Network.

During the last few years, several new drugs have been introduced for treatment of patients with multiple myeloma, which have significantly improved the treatment outcome. All of these novel substances differ at least in part in their mode of action from similar drugs of the same drug class, or are representatives of new drug classes, and as such present with very specific side effect profiles. In this review, we summarize these adverse events, provide information on their prevention, and give practical guidance for monitoring of patients and for management of adverse events.

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… Octreotide, a long-acting somatostatin analog, is generally reserved for use in complicated cases or as a second-line treatment for persistent diarrhea after loperamide [ 81 ]. In addition, existent dehydration and/or mineral loss should be compensated. …

The treatment landscape in thyroid cancer: a focus on cabozantinib.

Although patients with thyroid cancer generally fare well, there is a subset for which this is not necessarily true. Progress in understanding the molecular aberrations in thyroid cancer has led to a change in the management of these cases. Since 2011, four multikinase inhibitors (MKIs) have been approved by the US Food and Drug Administration for thyroid cancer - cabozantinib and vandetanib for medullary thyroid cancer and sorafenib and lenvatinib for differentiated thyroid cancer. This change in the treatment landscape has raised challenges for practitioners who may not be familiar with the

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… In more severe cases, other potential options include oral budesonide or parenteral octreotide. However, these two agents have not been evaluated in the context of MKIs. …

Molecular Inhibitors of Growth Signals

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Unlocking the potential of tumor-targeting peptides in precision oncology.

Targeted cancer therapy has emerged as a promising alternative to conventional chemotherapy, which is often plagued by poor selectivity, off-target effects, and drug resistance. Among the various targeting agents in development, peptides stand out for their unique advantages, including minimal immunogenicity, high tissue penetration, and ease of modification. Their small size, specificity, and flexibility allow them to target cancer cells while minimizing damage to healthy tissue selectively. Peptide-based therapies have shown great potential in enhancing the efficacy of drug delivery, improvi

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… Clinical trials showed markedly extended progression-free survival and higher response rates compared to high-dose octreotide long acting release (LAR). While mild myelosuppression was noted, the absence of renal toxicity emphasized its safety and therapeutic potential [ 169 ]. …

mTOR Cross-Talk in Cancer and Potential for Combination Therapy.

The mammalian Target of Rapamycin (mTOR) pathway plays an essential role in sensing and integrating a variety of exogenous cues to regulate cellular growth and metabolism, in both physiological and pathological conditions. mTOR functions through two functionally and structurally distinct multi-component complexes, mTORC1 and mTORC2, which interact with each other and with several elements of other signaling pathways. In the past few years, many new insights into mTOR function and regulation have been gained and extensive genetic and pharmacological studies in mice have enhanced our understandi

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… Tem, Temsirolimus; IFN, Interferon; Beva, bevacizumab; Eve, everolimus; Soraf, sorafenib; Oct, octreotide; Rida, ridaforolimus; Exe, exemestane; Letro, letrozole; Vnr, vinorelbine; Trast, trastuzumab; IC, Investigator Choice; BSC, Best Supportive Care; Lenv, lenvatinib; mRCC, metastatic Renal Cell Carcinoma …

Non-diabetic hypoglycemia: bridging gaps in diagnosis and treatment: a position statement report by the Arabic Association for the Study of Diabetes and Metabolism (AASD).

BACKGROUND: Non-diabetic hypoglycemia presents a substantial diagnostic challenge due to its diverse and often nonspecific symptomatology. The resultant delay in diagnosis can lead to a myriad of misdiagnoses. This misidentification not only prolongs patient suffering but also elevates the risk of severe complications, such as permanent neurologic damage and mortality. Recognizing the clinical nuances of non-diabetic hypoglycemia is paramount for timely and accurate diagnosis, which ultimately enhances patient outcomes and safety. MAIN BODY: A position statement has been formulated by the Ara

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… In severe cases, medications like octreotide, anti-diarrheal, pectin, or guar gum may be used. …

Secondary Neutropenias.

Neutrophils are a critical component of immunity, particularly against bacteria and other pathogens, but also in inflammation and tissue repair. As a consequence, individuals with neutropenia, defined by a reduction in absolute neutrophil counts, exhibit a strong propensity to severe infections that typically present with muted symptoms. Neutropenias encompass a heterogeneous set of disorders, comprising primary neutropenias, in which specific genes are mutated, and the more common secondary neutropenias, which have diverse non-genetic causes. These include hematological and other cancers, inv

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… tetracycline, trimethoprim-sulfamethoxazol antipsychotics | amoxapine, clozapine, diazepam, olanzapine, phenothiazines antirheumatics | gold, levamisole antithyroids | carbimazole, methimazole, propylthiouracil non-cancer biologicals | tocizulimab other | aminopyrine, deferiprone, digoxin, glucocorticoids, octreotide …

Review of cancer therapies for the perioperative physician.

Advances in cancer treatments over the past decades combining chemotherapy with novel technologies in immunotherapies, radiation therapies, and interventional radiology have prolonged life expectancy. Patients have more options for treatments of their primary or metastatic diseases. Increased procedural techniques amid an aging population with multiple comorbidities present risks and challenges in the perioperative period.Chemotherapy remains the mainstay of cancer treatment, can be given intraoperatively, and is combined with other treatment modalities. Immunotherapy is particular to cancer c

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… Preoperative octreotide is given to patients with a history of carcinoid cancer to minimize acute hormone release‐carcinoid crisis. Patients taking bevacizumab, a monoclonal antibody used to treat various cancers, should discontinue its use 4–6 weeks before TACE therapy. …