Delving into the Latest Updates on Yttrium-90 (90Y) DOTATATE with Synapse

Overview

Basic Info

Drug Type

Peptide Conjugate Radionuclide, Therapeutic radiopharmaceuticals

Synonyms

DOTA-0-Tyr3-Octreotate

Target

SSTR

Mechanism

SSTR modulators(Somatostatin receptor modulators), Ionising radiation emitters

Therapeutic Areas

NeoplasmsDigestive System DisordersEndocrinology and Metabolic Disease+ [2]

Active Indication-

Inactive Indication

Actinic CheilitisCarcinoid TumorGastro-Enteropancreatic Neuroendocrine Tumor+ [1]

Originator Organization-

Active Organization-

Inactive Organization

Uniwersytet Warminsko Mazurski

Drug Highest PhasePendingPhase 2

First Approval Date-

Regulation-

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Structure

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Gene Sequence

Sequence Code 19721

The sequence is quoted from: *****

173/5000 Forse cercavi: Terapia radiometabolica recettoriale-mediata con [90Y-DOTA0-Tyr3]-octreotide (90Y-DOTATOC) nei tumori endocrini del tratto gastroenteropancreatico e bronchiale. (Yttrium-90-02) Receptor-mediated radiometabolic therapy with [90Y-DOTA0-Tyr3] -octreotide (90Y-DOTATOC) in endocrine gastroenteropancreatic and bronchial tumors. (Yttrium-90-02) - Radiometabolic therapy in endocrin cancer

Start Date15 Nov 2017

Sponsor / Collaborator-

EUCTR2012-003155-11-IT / Unknown statusNot Applicable

Radiometabolic treatment with 90Y-DOTA0-Tyr3]-octreotide (90Y-DOTATOC) or[90Y-DOTA0-Tyr3-Thr8]-octreotate (90Y-DOTATATE)in tumours expressing somatostatin receptors - Yttrium-90-01

Start Date17 Jul 2012

Sponsor / Collaborator-

EUCTR2009-014737-24-AT / Not yet recruitingNot Applicable

Vergleichende Studie zur Darstellung der Somatostatinrezeptoren bei Kopf-Hals-Tumoren mit Immunhistochemie und PET (68Ga-DOTA-Tyr3-Octreotid) - SSTR in HNSCC: Vergleich von IHC und PET

Start Date19 Nov 2010

Sponsor / Collaborator

Medizinische Universität Graz

100 Clinical Results associated with Yttrium-90 (90Y) DOTATATE

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100 Translational Medicine associated with Yttrium-90 (90Y) DOTATATE

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100 Patents (Medical) associated with Yttrium-90 (90Y) DOTATATE

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46

Literatures (Medical) associated with Yttrium-90 (90Y) DOTATATE

01 Dec 2023·Journal of Surgical Oncology

Accuracy of DOTATATE PET imaging in the preoperative planning of small bowel neuroendocrine tumor resection

Article

Author: Warner, Susanne ; Zhang, Chi ; Thiels, Cornelius ; Truty, Mark ; Cleary, Sean ; Glasgow, Amy ; Grotz, Travis ; Wasif, Nabil ; Halfdanarson, Thorvardur R ; Nagorney, David ; Kendrick, Michael ; Smoot, Rory ; Day, Courtney ; Gudmundsdottir, Hallbera ; Navin, Patrick ; Starlinger, Patrick ; Takahashi, Hiroaki

AbstractBackground and ObjectivesWe assessed the accuracy of preoperative gallium‐68 DOTA‐Tyr3‐octreotate (DOTATATE) positron emission tomography (PET) imaging in estimating multifocality and nodal metastases of small bowel neuroendocrine tumors (sbNETs).MethodsA multicenter analysis was performed on patients with sbNETs who underwent preoperative DOTATATE PET imaging and surgical resection, with manual palpation of the entire length of the small bowel, between January 2016 and August 2022. Preoperative imaging reports and blinded secondary imaging reviews were compared to the final postoperative pathology reports. Descriptive statistics were applied.ResultsOne‐hundred and four patients met inclusion criteria. Pathology showed 53 (51%) patients had multifocal sbNETs and 96 (92%) had nodal metastases. The original preoperative DOTATATE PET imaging identified multifocal sbNET in 28 (27%) patients and lymph node (LN) metastases in 80 (77%) patients. Based on original radiology reports, sensitivity for multifocal sbNET identification was 45%, specificity was 92%, positive predictive value (PPV) was 86%, and negative predictive value (NPV) was 62%. For the identification of LN metastases, sensitivity was 82%, specificity was 88%, PPV was 99%, and NPV was 29%.ConclusionsAlthough DOTATATE PET imaging is specific and relatively accurate, sensitivity and NPV are insufficient to guide surgical planning. Preoperative use should not replace open palpation to identify additional synchronous lesions or to omit regional lymphadenectomy.

24 Oct 2022·Angewandte Chemie International Edition

Boosting Bismuth(III) Complexation for Targeted α‐Therapy (TAT) Applications with the Mesocyclic Chelating Agent AAZTA**

Article

Author: Guidolin, Nicol ; Ghiani, Simona ; Maiocchi, Alessandro ; Baranyai, Zsolt ; Horváth, Dávid ; Demitri, Nicola ; Szikra, Dezsö ; Giovenzana, Giovanni B. ; Travagin, Fabio ; Vágner, Adrienn ; Trencsényi, György

AbstractTargeted α therapy (TAT) is a promising tool in the therapy of cancer. The radionuclide 213BiIII shows favourable physical properties for this application, but the fast and stable chelation of this metal ion remains challenging. Herein, we demonstrate that the mesocyclic chelator AAZTA quickly coordinates BiIII at room temperature, leading to a robust complex. A comprehensive study of the structural, thermodynamic and kinetic properties of [Bi(AAZTA)]− is reported, along with bifunctional [Bi(AAZTA‐C4‐COO−)]2− and the targeted agent [Bi(AAZTA‐C4‐TATE)]−, which incorporates the SSR agonist Tyr3‐octreotate. An unexpected increase in the stability and kinetic inertness of the metal chelate was observed for the bifunctional derivative and was maintained for the peptide conjugate. A cyclotron‐produced 205/206Bi mixture was used as a model of 213Bi in labelling, stability, and biodistribution experiments, allowing the efficiency of [213Bi(AAZTA‐C4‐TATE)]− to be estimated. High accumulation in AR42J tumours and reduced kidney uptake were observed with respect to the macrocyclic chelate [213Bi(DOTA‐TATE)]−.

01 Apr 2022·Nuclear Medicine CommunicationsQ4 · MEDICINE

Development of neutron-activated samarium-153-loaded polystyrene microspheres as a potential theranostic agent for hepatic radioembolization

Q4 · MEDICINE

Article

Author: Wong, Yin How ; Kasbollah, Azahari ; Abdullah, Basri Johan Jeet ; Tan, Hun Yee ; Yeong, Chai Hong ; Md Shah, Mohammad Nazri ; Perkins, Alan Christopher

PurposeHepatic radioembolization is an effective minimally invasive treatment for primary and metastatic liver cancers. Yttrium-90 [90Y]-labelled resin or glass beads are typically used as the radioembolic agent for this treatment; however, these are not readily available in many countries. In this study, novel samarium-153 oxide-loaded polystyrene ([153Sm]Sm2O3-PS) microspheres were developed as a potential alternative to 90Y microspheres for hepatic radioembolization.MethodsThe [152Sm]Sm2O3-PS microspheres were synthesized using solid-in-oil-in-water solvent evaporation. The microspheres underwent neutron activation using a 1 MW open-pool research reactor to produce radioactive [153Sm]Sm2O3-PS microspheres via 152Sm(n,γ)153Sm reaction. Physicochemical characterization, gamma spectroscopy and in-vitro radionuclide retention efficiency were carried out to evaluate the properties and stability of the microspheres before and after neutron activation.ResultsThe [153Sm]Sm2O3-PS microspheres achieved specific activity of 5.04 ± 0.52 GBq·g−1 after a 6 h neutron activation. Scanning electron microscopy and particle size analysis showed that the microspheres remained spherical with an average diameter of ~33 μm before and after neutron activation. No long half-life radionuclide and elemental impurities were found in the samples. The radionuclide retention efficiencies of the [153Sm]Sm2O3-PS microspheres at 550 h were 99.64 ± 0.07 and 98.76 ± 1.10% when tested in saline solution and human blood plasma, respectively.ConclusionsA neutron-activated [153Sm]Sm2O3-PS microsphere formulation was successfully developed for potential application as a theranostic agent for liver radioembolization. The microspheres achieved suitable physical properties for radioembolization and demonstrated high radionuclide retention efficiency in saline solution and human blood plasma.

100 Deals associated with Yttrium-90 (90Y) DOTATATE

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Actinic Cheilitis	Phase 2	PL	Uniwersytet Warminsko Mazurski	02 Nov 2004
Carcinoid Tumor	Phase 2	PL	Uniwersytet Warminsko Mazurski	02 Nov 2004
Gastro-Enteropancreatic Neuroendocrine Tumor	Phase 2	PL	Uniwersytet Warminsko Mazurski	02 Nov 2004
Pheochromocytoma	Phase 2	PL	Uniwersytet Warminsko Mazurski	02 Nov 2004

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASCO2009	Not Applicable	Advanced Neuroendocrine Neoplasm	89	90-Yttrium-tyr3-DOTA-octreotate	(plnqpdnmuz) = akqvtoqjgp plisfyzdkl (tpzoxmhdte )	Positive	20 May 2009