Clinical Application of CAIX-Targeted PET Imaging in Tumors
试验速览
- 阶段
- 1 期
- 状态
- 招募中
- 发起方
- 入组人数
- 3
- 试验地点
- 1
- 主要终点
- Standardized Uptake Value (SUV) of target or suspected tumor lesions in malignant tumor subjects for 68Ga/18F-CAIX-LT-BCH across imaging time points
研究概览
简要总结
According to the 2020 global cancer statistics, renal carcinoma ranks as the fourteenth most common malignant tumor worldwide. In 2020, there were 431,288 new cases and 179,368 deaths from renal cancer, and both the incidence and mortality rates are projected to continue rising by 2025. Early non-invasive diagnosis of clear cell renal cell carcinoma (ccRCC) is crucial for improving prognosis. Nuclear medicine molecular imaging offers the advantages of real-time, dynamic, and non-invasive detection of lesions throughout the body. However, there is currently a lack of highly efficient and targeted molecular probes for early and accurate diagnosis of this tumor in clinical practice.
The high expression of CAIX plays a central role in the pathogenesis of renal cancer by altering cellular metabolism, inducing angiogenesis, promoting epithelial-mesenchymal transition (EMT), invasion, and metastatic spread. CAIX is highly expressed in 95% of ccRCC cases. In fact, CAIX expression levels have been reported as an independent predictor of survival in advanced ccRCC. Moreover, CAIX expression in normal tissues is limited, primarily restricted to the stomach, the basolateral aspects of proliferating small intestinal crypt epithelial cells, and the gallbladder. Therefore, the differential expression of CAIX between ccRCC tumors and normal tissues highlights its potential as a robust target for nuclear medicine molecular probe research and development in ccRCC.
This study utilized high-throughput screening to identify small molecules with high affinity for CAIX. These molecules were subsequently cyclized and modified to enhance their in vivo stability. A bifunctional chelator, H3RESCA, was introduced at the C-terminus to construct the small-molecule compound RESCA-CAIX-LT. PET probes were prepared by radiolabeling with 68Ga or 18F, and their diagnostic efficacy for renal cancer was investigated. Small-animal PET imaging initially demonstrated that the probe exhibits high affinity and excellent imaging performance. The modifications also altered the in vivo metabolic profile of the original design, reducing non-specific uptake in organs such as the stomach, small intestine, and gallbladder. Furthermore, toxicological experiments confirmed the probe's high safety profile and in vivo stability.
研究设计
- 研究类型
- Interventional
- 分配方式
- Na
- 干预模型
- Single Group
- 主要目的
- Diagnostic
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 75 Years（Adult, Older Adult）
- 性别
- All
- 接受健康志愿者
- 否
入选标准
- •Hematological, hepatic, and renal functions meeting the following criteria: Complete Blood Count: WBC ≥4.0×10⁹/L or Neutrophils ≥1.5×10⁹/L, PLT ≥100×10⁹/L, Hb ≥90 g/L; Coagulation: PT or APTT ≤1.5 × ULN (Upper Limit of Normal); Hepatic Function: T-Bil ≤1.5 × ULN; ALT/AST ≤2.5 × ULN (or ≤5 × ULN for subjects with liver metastases); ALP ≤2.5 × ULN (or ≤4.5 × ULN for subjects with bone or liver metastases); Renal Function: BUN ≤1.5 × ULN, SCr ≤1.5 × ULN.
- •Normal cardiac function;
- •Expected survival ≥12 weeks;
- •Good compliance with follow-up;
- •At least one measurable target lesion according to RECIST 1.1 criteria;
- •Women of childbearing potential (aged 18-49) must have a negative pregnancy test within 7 days prior to the examination. Male and female patients of childbearing potential must agree to use effective contraception to prevent pregnancy during the study and for 3 months after the examination;
- •Patients for whom the clinician recommends a PET/CT examination for tumor diagnosis and staging;
- •Patients are fully capable of understanding the study, voluntarily agree to participate, and provide written informed consent.
排除标准
- •Severe abnormalities in hepatic, renal, or hematological function;
- •Patients planning for pregnancy;
- •Pregnant or lactating women;
- •Inability to lie flat for 30 minutes;
- •Refusal to participate in this clinical study;
- •Presence of claustrophobia or other psychiatric disorders;
- •Any other condition deemed unsuitable for participation by the investigator.
研究组 & 干预措施
Renal cancer patients
This is an exploratory study. Initially, we plan to enroll renal cancer patients or suspected patients scheduled for pathological biopsy or surgical tumor resection within the next 2 months. Following the collection of preliminary sample data, a further analysis will be conducted to calculate the required sample size.
干预措施: Each patient will undergo 68Ga/18F-CAIX-LT-BCH PET/CT imaging, with an administered radioactive dose of approximately 0.05-0.1 mCi/kg. (Drug)
结局指标
主要结局
Standardized Uptake Value (SUV) of target or suspected tumor lesions in malignant tumor subjects for 68Ga/18F-CAIX-LT-BCH across imaging time points
时间窗: Immediately after completion of imaging
次要结局
未报告次要终点