Lutetium-177 (¹⁷⁷Lu) Targeted Radionuclide Therapy

Indications: Selected patients with advanced PSMA-positive prostate cancer; patients with advanced SSTR-positive gastroenteropancreatic neuroendocrine tumors; and patients with other neuroendocrine tumors following specialist evaluation.

Key Advantages:Molecular target-guided delivery, precision systemic therapy, short-range radiation (on the millimeter scale), post-treatment imaging to track radiopharmaceutical distribution, and support from multiple international clinical studies.

¹⁷⁷Lu radioligand therapy is one of the key approaches in precision nuclear medicine. By recognizing specific molecular targets on the surface of tumor cells, it delivers ¹⁷⁷Lu-containing radiopharmaceuticals to targeted tumor lesions, offering new opportunities for disease control in selected patients with multiple metastases and limited treatment options.

1. Clinical Applications

① ¹⁷⁷Lu-PSMA: A New Treatment Option for Selected Patients with Advanced Prostate Cancer
Prostate-specific membrane antigen (PSMA) is highly expressed on the cell membranes of the vast majority of prostate cancers, making it an important target for radionuclide therapy.

Eligible Patients:For patients with PSMA-positive metastatic castration-resistant prostate cancer (mCRPC), particularly those whose disease has progressed despite previous treatment, ¹⁷⁷Lu-PSMA is a therapeutic option that warrants further evaluation.

Treatment Goals:Control metastatic lesions throughout the body, delay disease progression, and potentially extend survival. Some patients may also experience relief from tumor-related symptoms, including pain caused by bone metastases.

② ¹⁷⁷Lu-DOTATATE: A New Treatment Approach for Selected Patients with Neuroendocrine Tumors
Some neuroendocrine tumors express somatostatin receptors (SSTRs) on their cell surfaces. ¹⁷⁷Lu-DOTATATE takes advantage of this characteristic to deliver targeted radiation to tumor lesions expressing these receptors.

Eligible Patients:Primarily patients with well-differentiated, SSTR-positive neuroendocrine tumors that are unresectable or metastatic, particularly gastroenteropancreatic neuroendocrine tumors. Selected patients with G3 neuroendocrine tumors, as well as those with neuroendocrine tumors originating in the lungs or thymus, may also undergo further specialist evaluation based on histologic differentiation, target expression, and available clinical evidence.

Treatment Goals: Control tumor burden, alleviate clinical syndromes associated with hormone secretion (such as flushing, diarrhea, and hypoglycemia), and slow disease progression.

2. Key Advantages

① Theranostics: Integrating Imaging and Precision Treatment Through the Same Molecular Target
Before treatment, physicians use PET imaging to determine whether tumor lesions express the relevant molecular targets. During treatment, ¹⁷⁷Lu-labeled radiopharmaceuticals deliver therapeutic radiation to the targeted lesions. After treatment, SPECT/CT can be used to visualize the actual distribution of the radiopharmaceutical in the body, providing information for dosimetric assessment and subsequent treatment decisions.
This integrated diagnostic and therapeutic approach enables treatment selection based on more precise molecular imaging assessments.

② Short-Range β Radiation with Reduced Exposure to Surrounding Healthy Tissues
The β particles emitted by ¹⁷⁷Lu have an average range of approximately 0.67 mm in tissue. This provides a favorable dose distribution when treating certain smaller lesions, helping to destroy tumor cells while reducing radiation exposure to healthy tissues farther from the target

③ Combination with Different Targeting Molecules for Various Tumor Types
¹⁷⁷Lu itself does not possess tumor-targeting properties. It must be linked to a ligand capable of recognizing a specific molecular target to form a therapeutic radiopharmaceutical.
Representative applications include ¹⁷⁷Lu-PSMA for PSMA-positive prostate cancer and ¹⁷⁷Lu-DOTATATE for SSTR-positive neuroendocrine tumors. These radiopharmaceuticals can accumulate in multiple lesions expressing the appropriate molecular targets, providing a systemic treatment option for patients with multiple metastases.

④ Therapeutic Benefits Supported by Clinical Research
¹⁷⁷Lu-based therapies are supported by several large international clinical studies. The VISION trial demonstrated that ¹⁷⁷Lu-PSMA-617 can improve survival outcomes in selected patients with advanced prostate cancer. The NETTER-1 and NETTER-2 trials also demonstrated that ¹⁷⁷Lu-DOTATATE can delay disease progression in certain patients with neuroendocrine tumors.

3. Why Choose Jinshazhou Hospital of Guangzhou University of Chinese Medicine?

① Official Authorization for ¹⁷⁷Lu-Based Nuclear Medicine Procedures, Expanding Precision Treatment Options
Our hospital's Nuclear Medicine Department has officially obtained authorization to perform diagnostic and therapeutic nuclear medicine procedures using ¹⁷⁷Lu. The department meets the relevant regulatory and facility requirements for these procedures and has established supporting radiation protection and quality management systems. This marks a further expansion of the hospital's nuclear medicine capabilities, providing additional precision treatment options for eligible patients with advanced cancer.

② Comprehensive Nuclear Medicine Infrastructure Integrating Diagnosis and Treatment
The hospital is equipped with PET-CT, PET-MRI, and SPECT/CT imaging systems and operates a PET radiopharmaceutical preparation center. Supported by its molecular imaging and nuclear medicine infrastructure, the hospital provides the technical capabilities needed for tumor target assessment, treatment decision-making, and subsequent monitoring.

③ Coordinated Treatment Modalities for Comprehensive, Individualized Care
In addition to radionuclide therapy, the hospital offers precision radiation therapy, minimally invasive interventional procedures, targeted therapy, immunotherapy, and chemotherapy. For patients with complex conditions or disease progression following previous treatment, multidisciplinary team (MDT) consultations bring together specialists to evaluate both local and systemic treatment options and develop individualized diagnostic and treatment plans.

④ One-Stop International Medical Services Throughout the Treatment Journey
For international patients, the hospital provides remote medical record evaluations, multilingual interpretation and translation, and coordination of examinations and hospitalization. For patients requiring multiple treatment cycles, the hospital can also assist in arranging follow-up examinations and remote follow-up care between cycles, making cross-border medical care more convenient and well organized.

4. Mechanism of Action

After intravenous administration, the ligand recognizes specific molecular targets on the surface of tumor cells, directing the accumulation of the ¹⁷⁷Lu-labeled radiopharmaceutical in the corresponding lesions. ¹⁷⁷Lu emits β particles that irradiate tumor cells and surrounding cells. This mechanism allows ¹⁷⁷Lu therapy to target multiple lesions throughout the body that express the relevant molecular targets.

Figure 1. Mechanism of Action of ¹⁷⁷Lu-PSMA

Figure 2. Four Steps of ¹⁷⁷Lu-DOTATATE Peptide Receptor Radionuclide Therapy

5. Treatment Process

① Initial Remote Medical Record Review. Patients can submit pathology reports, imaging results, and previous treatment records in advance for an initial assessment by specialists.

② Molecular Target Imaging. Upon arrival at the hospital, patients undergo PSMA- or SSTR-targeted PET imaging to assess target expression in tumor lesions.

③ MDT Treatment Planning. The Nuclear Medicine Department coordinates a multidisciplinary team (MDT) consultation. Specialists review the patient's condition, treatment history, and overall health to determine whether ¹⁷⁷Lu therapy is appropriate.

④ Pre-Treatment Evaluation. Patients undergo a complete blood count, liver and kidney function tests, and other necessary examinations to assess treatment safety.

⑤ Intravenous Administration. No surgery is required. Administration of the radiopharmaceutical and associated supportive care typically takes from approximately 30 minutes to several hours, depending on the medication and treatment protocol. Most patients tolerate the procedure well, with continuous monitoring by medical staff throughout.

⑥ Post-Administration Monitoring and Imaging Assessment. Patients remain hospitalized for a short observation period in accordance with radiation protection requirements. SPECT/CT imaging is performed to assess the distribution of the radiopharmaceutical in the body. Once discharge criteria are met, patients may return home to recover and undergo scheduled follow-up examinations. Physicians assess the patient's treatment response and overall condition to evaluate the timing and arrangements for the next treatment cycle.

6. Frequently Asked Questions

① How Many Cycles of ¹⁷⁷Lu Therapy Are Needed?
Answer: ¹⁷⁷Lu therapy is typically administered in multiple cycles. Typical treatment protocols involve 4–6 cycles, spaced 6–8 weeks apart, with the entire course extending over approximately 6–9 months. However, not all patients need to complete every planned cycle. Before each treatment, physicians assess the patient's response and tolerance, adjusting the treatment plan as needed to balance efficacy and safety.
The total time spent at the hospital is usually only 2–4 weeks. International patients who meet discharge criteria and are medically fit to travel may return to their country of residence between treatment cycles, without having to remain in China throughout the entire course.

② How Does ¹⁷⁷Lu Radioligand Therapy Differ from Conventional External Beam Radiation Therapy and Chemotherapy?
Answer: Answer: Conventional external beam radiation therapy delivers radiation from outside the body to treat localized lesions, making it difficult to cover multiple small metastatic lesions throughout the body. Chemotherapy uses systemic cytotoxic drugs that can also damage normal proliferating cells and have relatively low specificity. ¹⁷⁷Lu therapy is a form of systemic targeted radionuclide therapy. The radiopharmaceutical travels through the bloodstream and acts on multiple lesions expressing the relevant molecular targets. Compared with conventional radiation therapy and chemotherapy, ¹⁷⁷Lu therapy offers an additional treatment option for selected patients with multiple metastases.

③ How Can I Find Out Whether ¹⁷⁷Lu Therapy Is Right for Me?
Answer: Physicians typically review pathology findings, previous treatment records, and PSMA- or SSTR-targeted imaging results to assess whether a patient is likely to benefit from the corresponding therapy. Kidney function, bone marrow reserve, and overall health must also be evaluated to help ensure treatment safety. Patients with severe organ dysfunction require further assessment of potential treatment risks. Special circumstances, including pregnancy and breastfeeding, must be managed in accordance with the contraindications and safety requirements of the specific radiopharmaceutical.
Patients can first submit their existing examination results and treatment records to determine whether further molecular target assessment is warranted. If the available records already indicate that ¹⁷⁷Lu therapy is unsuitable, the hospital will inform the patient in advance. This helps minimize the risk of patients traveling to China only to discover that they cannot receive the treatment, reducing unnecessary international travel.

④ Does Radioactivity Remain After Treatment? Can Family Members Stay with the Patient?
Answer: After ¹⁷⁷Lu administration, some radioactivity remains in the patient's body. Patients must therefore undergo a short observation period in a dedicated nuclear medicine ward in accordance with hospital regulations. During the radiation protection period, family members are generally not permitted to enter the ward to provide close bedside care. Specific visitation and caregiving arrangements are subject to the Nuclear Medicine Department's regulations.
The patient's excreta may contain radioactive substances and must be handled according to established safety procedures. Before discharge, medical staff assess the residual radioactivity in the patient's body and explain the necessary precautions. These include temporarily avoiding close contact with pregnant women, infants, and young children, as well as following appropriate personal hygiene and excreta handling precautions. Adhering to the radiation protection instructions provided by medical staff can effectively reduce radiation exposure to family members.