Delving into the Latest Updates on Al18F-NOTA-octreotide with Synapse

Overview

Basic Info

Drug Type

Peptide Conjugate Radionuclide, Diagnostic radiopharmaceuticals

Synonyms

Target

SSTR

Mechanism

SSTR antagonists(Somatostatin receptor antagonists), PET imaging(Positron-emission tomography enhancers)

Therapeutic Areas

Neoplasms

Active Indication-

Inactive Indication

Neuroendocrine Tumors

Originator Organization

Universitaire Ziekenhuizen Leuven

Active Organization-

Inactive Organization

Universitaire Ziekenhuizen Leuven

Drug Highest PhasePendingPhase 2/3

First Approval Date-

Regulation-

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Structure/Sequence

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We presented a case involving a 56-year-old man who had been experiencing shoulder and back pain for over a year, with extensive bone metastases revealed by a bone scan. To identify the primary source of these issues, the patients underwent a fluorine-18-fluorodeoxyglucose (¹⁸F-FDG) positron emission tomography/computed tomography (PET/CT) scan, which indicated moderate uptake in the right renal soft mass and low uptake in multiple osteolytic lesions. Pathological examination and immunohistochemical staining of the renal mass supported the diagnosis of neuroendocrine tumors. Subsequently, a novel somatostatin receptor imaging agent, Al¹⁸F-NOTA-octreotide (¹⁸F-OC), was performed to further investigate the source of metastatic lesions and to stage the tumor. The ¹⁸F-OC scan revealed a high-uptake lesion in the pancreatic head, as well as additional lymph node and bone metastases lesions.Compared to ¹⁸F-FDG, the ¹⁸F-OC demonstrated superior imaging capabilities and a significantly higher tumor-to-background ratio in neuroendocrine neoplasms, which contributed to improvingthe staging and treatment management.

01 Mar 2024·Clinical Nuclear Medicine

Al18F-NOTA-Octreotide PET/CT and 18F-FDG PET/CT for Detecting Cerebellar Hemangioblastoma in a Patient With Von Hippel-Lindau Disease

Article

Author: Hou, Guozhu ; Wang, Xuejuan ; Cheng, Xin ; Chi, Yihebali ; Zheng, Rong

AbstractVon Hippel-Lindau disease is a hereditary syndrome associated with various benign and malignant tumors, including hemangioblastomas. A 42-year-old man with a history of Von Hippel-Lindau disease underwent surgery for pancreatic neuroendocrine tumor and renal clear cell carcinoma and was recommended to undergo Al18F-NOTA-octreotide and 18F-FDG PETCT examination to assess potential metastases. 18F-FDG PET/CT showed low uptake in the right cerebellum, which demonstrated increased Al18F-NOTA-octreotide activity. Cerebellar mass resection surgery was performed. Pathological result was consistent with hemangioblastoma. This case report indicates the significant role of Al18F-NOTA-octreotide in the diagnosis of hemangioblastoma.

01 Feb 2023·Nuclear Medicine Communications

A novel urokinase plasminogen activator receptor-targeted peptide-based probe for in-vivo molecular imaging of glioblastoma

Article

Author: Sun, Ziyan ; Han, Yunfeng ; Xu, Liying ; Tu, Le ; Zhang, Yongxue

AimThe urokinase plasminogen activator receptor (uPAR) is a promising biomarker for cancer diagnosis and therapy. We herein fabricated a new type of uPAR-targeted imaging probe Al18F-NOTA-VC and preliminarily evaluated its potential application in PET imaging of the glioma model in vivo.MethodsPeptide VC was synthesized and identified by MALDI-TOF-MS. The IC50 between VC/precursor NOTA-VC and uPAR was then determined before the synthesis and purification of Al18F-NOTA-VC, followed by further studies of in-vitro properties of Al18F-NOTA-VC. Meanwhile, the AE105-based probe followed a similar procedure in-vitro test. Finally, the PET imaging properties, including uPAR-targeting ability and the metabolism of Al18F-NOTA-VC, were investigated.ResultsThe VC and NOTA-VC were obtained successfully and demonstrated a good affinity with uPAR. Followed by Al18F labeling successfully, excellent properties, including the serum stability, water solubility, and specificity of Al18F-NOTA-VC, were obtained in-vitro test compared with AE105 based probe. An excellent tumor uptake and renal excretion data of Al18F-NOTA-VC were acquired from in-vivo U87MG tumor model PET imaging, consistent with the subsequent biodistribution study.ConclusionIn addition to the excellent specificity and high tumor/normal tissue contrast for uPAR-targeted PET imaging of U87MG tumor, Al18F-NOTA-VC possessed promising clearance ability by renal system route. These excellent properties facilitated Al18F-NOTA-VC to be a promising imaging agent for uPAR high-expressing tumors and, thus, provided a paradigm for developing peptide-based probes for uPAR-associated disease diagnosis.

100 Deals associated with Al18F-NOTA-octreotide

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Neuroendocrine Tumors	Phase 1	BE	Universitaire Ziekenhuizen Leuven	07 Oct 2020

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


SNMMI2024	Not Applicable	Neuroendocrine Tumors	-	18F-AlF-NOTA-octreotide PET/CT	eardiugjaf(yvpqhudqnf) = rzmpbgksih mewbykwtzv (ywyryymwry ) View more	-	09 Jun 2024
SNMMI2024	Not Applicable	Neuroendocrine Tumors	-	18F-AlF-NOTA-octreotide (Contrast-enhanced CT/MRI)	eardiugjaf(yvpqhudqnf) = deslifydpv mewbykwtzv (ywyryymwry ) View more	-	09 Jun 2024
NCT04552847 (Pubmed)	Phase 2/3	Neuroendocrine Tumors	75	<sup>18</sup>F-AlF-NOTA-octreotide	oizkhwfcvm(lsddzrpokc) = bztxuvexlu rryffmftzc (bqkqjdtnqz, 9.6% - 22.0%) View more	Positive	20 Oct 2022