A freeze-dried kit formulation for the preparation of Lys²⁷(^99mTc-EDDA/HYNIC)-Exendin(9-39)/^99mTc-EDDA/HYNIC-Tyr³-Octreotide to detect benign and malignant insulinomas

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• 作者：Veronica Medina-Garcí ; a^a ; ^b ; Blanca E. Ocampo-Garcí ; a^a ; ^{ocampo_be@yahoo.com.mx" class="auth_mail" title="E-mail the corresponding author} ; ^{blanca.ocampo@inin.gob.mx" class="auth_mail" title="E-mail the corresponding author} ; Guillermina Ferro-Flores^a ; Clara L. Santos-Cuevas^a ; Liliana Aranda-Lara^a ; ^b ; Rocio Garcí ; a-Becerra^c ; David Ordaz-Rosado^c ; Laura Melendez-Alafort^d
• 关键词：Insulinomas ; Lys27(99mTc-EDDA/HYNIC)-Exendin(9-39) ; Glucagon-like peptide 1 receptor ; Somatostatin receptor
• 刊名：Nuclear Medicine and Biology
• 出版年：2015
• 出版时间：December 2015
• 年：2015
• 卷：42
• 期：12
• 页码：911-916
• 全文大小：512 K

文摘

About 90% of insulinomas are benign and 5%–15% are malignant. Benign insulinomas express the glucagon-like peptide-1 receptor (GLP-1R) and low levels of somatostatin receptors (SSTR), while malignant insulinomas over-express SSTR or GLP-1R in low levels. A kit for the preparation of Lys²⁷(^99mTc-EDDA/HYNIC)-Exendin(9-39)/^99mTc-EDDA/HYNIC-Tyr³Octreotide was formulated to detect 100% of insulinomas. The formulation showed radiochemical purity of 97 ± 1%, high stability in human serum, and GLP-1R and SSTR affinity. The biodistribution and imaging studies demonstrated properties suitable for its use as a target-specific agent for the simultaneous molecular imaging of GRP-1R- and/or SSTR-positive tumors.