Clinical Application of CAIX-Targeted PET Imaging in Tumors

NCT07590310 | Recruiting Early Phase 1

• 1 other identifier: 2025YJZ37
• Study Type: interventional
• Target: 3
• Locations: 1 country
• Sites: 1

Brief Summary

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.

Conditions

Kidney Cancers

Outcome Measures

Primary Outcomes (1)

• Standardized Uptake Value (SUV) of target or suspected tumor lesions in malignant tumor subjects for 68Ga/18F-CAIX-LT-BCH across imaging time points

  Immediately after completion of imaging

Study Arms (1)

Renal cancer patients

EXPERIMENTAL

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.

Drug: 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.

Interventions

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

68Ga/18F-CAIX-LT-BCH (0.05-0.1 mCi/kg) is intravenously administered, followed immediately by whole-body dynamic imaging using the United Imaging uEXPLORER total-body PET/CT system. If indeterminate lesions are observed on routine imaging, delayed imaging may be performed for further evaluation. The patient is positioned supine and instructed to breathe quietly. The acquired data are reconstructed using the Ordered Subset Expectation Maximization (OSEM) algorithm to generate dynamic PET image frames. Static PET/CT or PET/MRI Protocol: Following intravenous administration of the quality-controlled 68Ga/18F-CAIX-LT-BCH (0.05-0.1 mCi/kg), the patient rests for 50-60 minutes before undergoing whole-body or regional static scanning. The patient is positioned supine and maintains quiet breathing. Image data are reconstructed using the OSEM algorithm to produce dynamic PET image frames.

Renal cancer patients

Eligibility Criteria

• Age: 18 Years - 75 Years
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• 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.

You may not qualify if:

• 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.

Sponsors & Collaborators

• Peking University Cancer Hospital & Institute: lead

Study Sites (1)

Peking University Cancer Hospital

Beijing, Haidian, 10000, China

RECRUITING

MeSH Terms

Conditions

Kidney Neoplasms

Condition Hierarchy (Ancestors)

Urologic Neoplasms; Urogenital Neoplasms; Neoplasms by Site; Neoplasms; Female Urogenital Diseases; Female Urogenital Diseases and Pregnancy Complications; Urogenital Diseases; Kidney Diseases; Urologic Diseases; Male Urogenital Diseases

Central Study Contacts

Lei Xia

CONTACT

+86 18811177191; xialei9012288@126.com

Study Design

• Study Type: interventional
• Phase: early phase 1
• Allocation: NA
• Masking: NONE
• Purpose: DIAGNOSTIC
• Intervention Model: SINGLE GROUP
• Sponsor Type: OTHER
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: December 11, 2025
• First Posted: May 15, 2026
• Study Start: March 1, 2025
• Primary Completion (Estimated): December 31, 2026
• Study Completion (Estimated): December 31, 2026
• Last Updated: May 15, 2026

Record last verified: 2026-05

Data Sharing

• IPD Sharing: Will not share

Locations

CN (1)