Delving into the Latest Updates on Pentetreotide with Synapse

Overview

Basic Info

Drug Type

Peptide Conjugate Radionuclide, Diagnostic radiopharmaceuticals

Synonyms

111In-octreotid, 111In-octreotide, 111In-oktreotid

+ [16]

Target

SSTR

Mechanism

SSTR antagonists(Somatostatin receptor antagonists), SPECT(Single-photon emission-computed tomography enhancers)

Therapeutic Areas

NeoplasmsOther DiseasesEye Diseases

Active Indication

Diagnostic agentsNeuroendocrine TumorsRetinal Diseases

Inactive Indication-

Originator Organization

Louisiana State University

Active Organization

Curium US Holdings LLC

Louisiana State University Health ShreveportPDRadiopharma, Inc.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

US (02 Jun 1994),

Neuroendocrine Tumors

RegulationOrphan Drug (US)

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Structure

Molecular FormulaC63H87N13O19S2

InChIKeyCNLWNYCFDMAZCB-HUVROIHYSA-N

CAS Registry138661-02-6

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Gene Sequence

Sequence Code 526024272

TERAVECT is a phase III randomized study of patients with digestive neuroendocrine tumors after complete surgical resection of liver metastases treated with In111-Pentetreotide-based adjuvant radiotherapy.
In this study, targeted radionuclide therapy is used at an earlier stage of the disease.The objective is to target residual tumor cells and/or micrometastases which escaped surgical resection. Given the poor prognosis associated with recurrence, this treatment should prevent relapse.

Start Date01 Sep 2015

Sponsor / Collaborator-

JPRN-UMIN000010183 / CompletedIIT

Diagnosis for the patients with neuroendocrine tumor by 111In-DTPA-octreotide - Diagnosis of NET by OctreoScan

Start Date06 Mar 2013

Sponsor / Collaborator-

100 Clinical Results associated with Pentetreotide

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100 Translational Medicine associated with Pentetreotide

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100 Patents (Medical) associated with Pentetreotide

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874

Literatures (Medical) associated with Pentetreotide

01 Nov 2024·Seminars in Nuclear Medicine

Radiolabeled Somatostatin Analogs for Cancer Imaging

Review

Author: K Nazar, Aamir ; Basu, Sandip

Somatostatin receptors (SSTR) are expressed by many tumours especially those related to neuro-endocrine origin and molecular functional imaging of SSTR expression using radiolabelled somatostatin analogs have revolutionized imaging of patients with these group of malignancies. Coming a long way from the first radiolabelled somatostatin analog ¹²³I-Tyr-3-octreotide, there has been significant developments in terms of radionuclides used, the ligands and somatostatin derivatives. ¹¹¹In-Pentetreotide extensively employed for imaging NETs at the beginning has now been replaced by ⁶⁸Ga-SSA based PET-CT. SSA-PET/CT performs superior to conventional imaging modalities and has evolved in the mainframe for NET imaging. The advantages were multiple: (i) superior spatial resolution of PET versus SPECT, (ii) quantitative capabilities of PET aiding in disease activity and treatment response monitoring with better precision, (iii) shorter scan time and (iv) less patient exposure to radiation. The modality is indicated for staging, detecting the primary in CUP-NETs, restaging, treatment planning (along with FDG: the concept of dual-tracer PET-CT) as well as treatment response evaluation and follow-up of NETs. SSA PET/CT has also been incorporated in the guidelines for imaging of Pheochromocytoma-Paraganglioma, Medullary carcinoma thyroid, Meningioma and Tumor induced osteomalacia. At present, there is rising interest on (a) ¹⁸F-labelled SSA, (b) ⁶⁴Cu-labelled SSA, and (c) somatostatin antagonists. ¹⁸F offers excellent imaging properties, ⁶⁴Cu makes delayed imaging feasible which has implications in dosimetry and SSTR antagonists bind with the SST receptors with high affinity and specificity, providing high contrast images with less background, which can be translated to theranostics effectively. SSTR have been demonstrated in non-neuroendocrine tumours as well in the peer-reviewed literature, with studies demonstrating the potential of SSA PET/CT in Neuroblastoma, Nasopharyngeal carcinoma, carcinoma prostate (neuroendocrine differentiation) and lymphoma. This review will focus on the currently available SSAs and their history, different SPECT/PET agents, SSTR antagonists, comparison between the various imaging tracers, and their utility in both neuroendocrine and non-neuroendocrine tumors.

01 Sep 2024·Journal of Nuclear Medicine

Peptide Receptor Radionuclide Therapy in Advanced Refractory Meningiomas: Efficacy and Toxicity in a Long Follow-up

Article

Author: Sarnelli, Anna ; Manuela, Monti ; Arpa, Donatella ; Severi, Stefano ; Grassi, Ilaria ; Fabbri, Lucia ; Nicolini, Silvia ; Azzali, Irene ; Calabro, Luana ; Amadori, Elena ; Bongiovanni, Alberto ; Marini, Irene ; Riva, Nada ; Di Iorio, Valentina ; Tosatto, Luigino ; Di Meco, Francesco ; Matteucci, Federica ; Sansovini, Maddalena ; Bartolini, Daniela ; Paganelli, Giovanni ; Gurrieri, Lorena ; Ranallo, Nicoletta

Recurrence of meningiomas after surgery and radiotherapy deserves specific attention because of the lack of active third-line therapies. Somatostatin receptors are usually overexpressed on the cell membrane of meningiomas, and this has led the way to a radionuclide theranostic approach. Diagnoses with ⁶⁸Ga-DOTA-octreotide and peptide receptor radionuclide therapy (PRRT) with ⁹⁰Y/¹⁷⁷Lu-DOTA-octreotide are currently possible options within experimental protocols or as compassionate use in small patient groups. Methods: From October 2009 to October 2021, 42 meningioma patients with radiologic recurrence after standard therapies were treated with ⁹⁰Y-DOTATOC (dosage of 1.1 or 5.5 GBq) or with ¹⁷⁷Lu-DOTATATE (dosage of 3.7 or 5.5 GBq) in a mean of 4 cycles. All patients showed intense uptake at diagnostic ⁶⁸Ga-DOTATOC PET/CT or in an ¹¹¹In-octreotide scan. Results: Of 42 patients treated, 5 patients received ⁹⁰Y-DOTATOC with a cumulative activity of 11.1 GBq and 37 patients received ¹⁷⁷Lu-DOTATATE with a cumulative activity of 22 GBq. The disease control rate was 57%. With a median follow-up of 63 mo, median progression-free survival was 16 mo, and median overall survival was 36 mo. Retreatment ¹⁷⁷Lu-PRRT was performed in 6 patients with an administered median activity of 13 GBq in a mean of 5 cycles. With a 75.8-mo follow-up, median progression-free survival and overall survival were 6.5 and 17 mo, respectively. Only 1 patient discontinued the treatment because of grade 3 platelet toxicity. A rapidly transient grade 2 neutropenia was recorded in 1 retreated patient. Conclusion: PRRT in patients with advanced meningiomas overexpressing somatostatin receptor 2 was active and well tolerated, showing a 57% disease control rate. Furthermore, PRRT could represent a potential retreatment option. Further studies, also in combination with other treatments, are warranted.

01 Jul 2024·Clinical Nuclear Medicine

111In-Pentetreotide–Guided Radiosurgery for Intraoperative Localization of Retroperitoneal Nodal Metastasis in a Patient With Ileal Neuroendocrine Tumor

Article

Author: Forester, Jared ; Giuliano, Peter ; Ulaner, Gary A. ; Zakry, Nazila ; Ulaner, Gary A ; Demeure, Michael J.

Abstract64Cu-DOTATATE PET/CT of a 44-year-old man with an ileal neuroendocrine tumor demonstrated the primary tumor, local nodal metastases, and a pericaval nodal metastasis. Localization of the pericaval node during surgery may be difficult, thus 4.4 mCi of 111In-pentetreotide was administered before surgery to assist with localization and resection. At surgery, the pericaval nodal metastasis was readily detected by gamma probe, which could then be resected and pathologically proven to be a metastasis. This demonstrates the use of somatostatin receptor–targeted imaging for intraoperative localization of an otherwise difficult to surgically localize metastasis. Without intraoperative somatostatin receptor–targeted radiosurgery, disease may have been incompletely resected.

100 Deals associated with Pentetreotide

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	V09IB01	DB11835

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Diagnostic agents	JP	PDRadiopharma, Inc.	28 Sep 2015
Neuroendocrine Tumors	US	Curium US Holdings LLC	02 Jun 1994

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Retinal Diseases	Preclinical	US	Louisiana State University Health Shreveport	01 May 2004

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02546388 (CTgov)	Not Applicable	Cardiac sarcoidosis	17	Gallium-68 DOTATATE (Gallium-68 DOTATATE)	kjuvcbmnle(psmewqsfvh) = bdblnodnob tdebaiydjq (vsvrswvuch, ysluaaifst - cuhdkzwalz) View more	-	25 Mar 2020
NCT02546388 (CTgov)	Not Applicable	Cardiac sarcoidosis	17	Indium-111 Pentreotide (Indium-111 Pentreotide (OctreoScan))	kjuvcbmnle(psmewqsfvh) = sxczgzzwnc tdebaiydjq (vsvrswvuch, arbtlchddx - xouvybltel) View more	-	25 Mar 2020
ASCO2010	Not Applicable	Neuroendocrine Tumors	83	500 mCi doses of <sup>111</sup>In-pentetreotide	(dshbgixxrh) = wwuikofdwo sxbouubqmo (ylugqvfltu )	Positive	20 May 2010
ASCO2007	Not Applicable	Neuroendocrine Tumors	18	Multiple 500 mCi doses of 111In-pentetreotide	htkgrnuncp(tciuuquyov) = yxntauzfvu abfxlmxdym (kwxpmmiglw )	-	20 Jun 2007
ASCO2004	Not Applicable	Neoplasms	85	In-111 pentetreotide	(xvtcmpkqnz) = lkkdcfxhdg wfvervpuuz (gcoqhsrhno )	-	15 Jul 2004