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A Practical Guide for the Production and PET/CT Imaging of 68Ga-DOTATATE for Neuroendocrine Tumors in Daily Clinical Practice
Published on: April 17, 2019
Naphthalene-containing octreotide radioligand elevates selectivity and radionuclide therapy for somatostatin receptor
Juan Sun1, Jiangtao Yang2, Jiakun Guo2
1Biomedical Polymers Laboratory, College of Chemistry, Chemical Engineering and Materials Science, and State Key Laboratory of Radiation Medicine and Protection, Soochow University, Suzhou 215123, China; College of Pharmaceutical Sciences, and State Key Laboratory of Radiation Medicine and Protection, Soochow University, Suzhou 215123, China.
Abstract:
Peptide receptor radionuclide therapy (PRRT) with proven targeting ability has emerged as a new paradigm for clinical tumor therapy. The selective binding of octreotide to somatostatin receptor 2 (SSTR2) renders the successful development of 177Lu-DOTATATE for SSTR2-positive neuroendocrine tumor patients. Here, we find that naphthalene-containing octreotide radioligand (OCT(naph)) induces elevated tumor uptake and radionuclide therapy for SSTR2-positive tumor over DOTATATE. 177Lu-OCT(naph) demonstrated high radiochemical purity and radiostability, and increased binding affinity to human serum albumin, which led to prolonged blood circulation time and a peak accumulation of 20.8 ± 3.2 %ID/g, 1.6-fold of that for 177Lu-DOTATATE, in SSTR2+ HCT-116 tumor. A single injection of 177Lu-OCT(naph) at 7.4 MBq while induced no apparent toxicity effectively suppressed tumor growth, significantly outperforming 177Lu-DOTATATE. Overall, 177Lu-OCT(naph) with optimized albumin binding appears as a potentially better radionuclide therapy for SSTR2-positive tumors.
Insights
A novel naphthalene-containing octreotide radioligand (OCT(naph)) shows superior tumor uptake and therapeutic efficacy compared to DOTATATE in somatostatin receptor 2-positive tumors. This enhanced peptide receptor radionuclide therapy (PRRT) offers improved treatment potential.
Area of Science:
- Nuclear Medicine
- Radiopharmaceutical Chemistry
- Oncology
Background:
- Peptide receptor radionuclide therapy (PRRT) utilizes targeted radioligands for tumor treatment.
- Octreotide targets somatostatin receptor 2 (SSTR2), leading to 177Lu-DOTATATE development for neuroendocrine tumors.
Purpose of the Study:
- To evaluate a novel naphthalene-containing octreotide radioligand (OCT(naph)) for enhanced SSTR2-positive tumor targeting and therapy.
- To compare the efficacy of 177Lu-OCT(naph) with 177Lu-DOTATATE.
Main Methods:
- Synthesis and characterization of 177Lu-OCT(naph).
- Assessment of radiochemical purity, radiostability, and albumin binding affinity.
- In vivo evaluation of tumor uptake, biodistribution, and therapeutic efficacy in SSTR2+ tumor models.
Main Results:
- 177Lu-OCT(naph) exhibited high radiochemical purity and stability.
- Enhanced binding to human serum albumin resulted in prolonged circulation and increased tumor accumulation (1.6-fold higher than 177Lu-DOTATATE).
- A single dose of 177Lu-OCT(naph) effectively suppressed tumor growth with no apparent toxicity, outperforming 177Lu-DOTATATE.
Conclusions:
- 177Lu-OCT(naph) demonstrates superior tumor uptake and therapeutic efficacy for SSTR2-positive tumors compared to 177Lu-DOTATATE.
- Optimized albumin binding of 177Lu-OCT(naph) contributes to its enhanced performance.
- 177Lu-OCT(naph) represents a promising advancement in PRRT for SSTR2-positive malignancies.
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