Dataset Information

DOTA-Derivatives of Octreotide Dicarba-Analogs with High Affinity for Somatostatin sst_2,5 Receptors.

ABSTRACT: In vivo somatostatin receptor scintigraphy is a valuable method for the visualization of human endocrine tumors and their metastases. In fact, peptide ligands of somatostatin receptors (sst's) conjugated with chelating agents are in clinical use. We have recently developed octreotide dicarba-analogs, which show interesting binding profiles at sst's. In this context, it was mandatory to explore the possibility that our analogs could maintain their activity also upon conjugation with DOTA. In this paper, we report and discuss the synthesis, binding affinity and conformational preferences of three DOTA-conjugated dicarba-analogs of octreotide. Interestingly, two conjugated analogs exhibited nanomolar affinities on sst₂ and sst₅ somatostatin receptor subtypes.

SUBMITTER: Pratesi A

PROVIDER: S-EPMC5324734 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature

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DOTA-Derivatives of Octreotide Dicarba-Analogs with High Affinity for Somatostatin sst<sub>2,5</sub> Receptors.

Pratesi Alessandro A Ginanneschi Mauro M Lumini Marco M Papini Anna M AM Novellino Ettore E Brancaccio Diego D Carotenuto Alfonso A

Frontiers in chemistry 20170223

<i>In vivo</i> somatostatin receptor scintigraphy is a valuable method for the visualization of human endocrine tumors and their metastases. In fact, peptide ligands of somatostatin receptors (sst's) conjugated with chelating agents are in clinical use. We have recently developed octreotide dicarba-analogs, which show interesting binding profiles at sst's. In this context, it was mandatory to explore the possibility that our analogs could maintain their activity also upon conjugation with DOTA. ...[more]

PMID: 28286746

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Project description:Background Management of advanced malignant thymoma is very challenging due to the lack of evidence from randomized trials. Despite advanced and non-curable status, most patients achieve long survival and they usually receive several treatment lines along their disease. There is no standard second line, and toxicity of chemotherapy (CT) should be considered for these long survivors. Treatment with somatostatin analogs showed efficacy in patients with refractory recurrent and/or metastatic thymomas. Case Description In January 2010, a 31-year-old woman was diagnosed of a mass in the anterior mediastinum with a biopsy compatible with thymoma B3 and myasthenia gravis. Thymoma was resected after 2 cycles of neoadjuvant CT with acronym: cisplatin, doxorrubicin, vincristine and cyclophosphamide (ADOC) schedule, then she received additional adjuvant ADOC. Disease progressed on November 2012 with pleural implants and lung nodule in upper right lobe. After 6 cycles of systemic CT with carboplatin and etoposide and major partial response, she was operated on twice on November 2013 and March 2014 with resection of residual disease in lung and pleura. After new pleural disease progression 14 months later (May 2015), new surgical resection was dismissed and received several rounds of retreatment with carboplatin and etoposide with rest periods between them. After each course of this CT, the patient presented a tumor response, but in the last cycles she began to present significant bone marrow toxicity. After the last significant progression in November 2021, it was decided to assess a low-toxic treatment alternative to CT, and despite no uptake in the octreotide scan, octreotide 30 mg IM every 28 days was started achieving stable disease according to RECISTv1 criteria (progression-free interval of 9 months to date) and good tolerance. Diagnosis: long survivor patient with advanced thymoma with pleural relapsing disease treated with several rounds of chemotherapy and response to octreotide instead of no uptake in the octreotide scan. Conclusions Somatostatin analogs can be a low-toxic treatment option in pretreated advanced thymoma patients regardless the octreotide scan uptake. This treatment should be studied in prospective clinical trials.

Dataset Information

DOTA-Derivatives of Octreotide Dicarba-Analogs with High Affinity for Somatostatin sst_2,5 Receptors.

Publications

DOTA-Derivatives of Octreotide Dicarba-Analogs with High Affinity for Somatostatin sst<sub>2,5</sub> Receptors.

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Dataset Information

DOTA-Derivatives of Octreotide Dicarba-Analogs with High Affinity for Somatostatin sst2,5 Receptors.

Publications

DOTA-Derivatives of Octreotide Dicarba-Analogs with High Affinity for Somatostatin sst<sub>2,5</sub> Receptors.

Similar Datasets

OmicsDI is part of the ELIXIR infrastructure

Tweets

DOTA-Derivatives of Octreotide Dicarba-Analogs with High Affinity for Somatostatin sst_2,5 Receptors.