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Radiolabeled Anti-Adenosine Triphosphate Synthase Monoclonal Antibody as a Theragnostic Agent Targeting Angiogenesis
Bok-Nam Park1, Su Jin Lee1, Jung Hyun Roh1
11 Department of Nuclear Medicine and Molecular Imaging, Ajou University School of Medicine, Suwon, South Korea.
Introduction:
The potential of a radioiodine-labeled, anti-adenosine triphosphate synthase monoclonal antibody (ATPS mAb) as a theragnostic agent for simultaneous cancer imaging and treatment was evaluated.
Methods:
Adenosine triphosphate synthase monoclonal antibody was labeled with radioiodine, then radiotracer uptake was measured in 6 different cancer cell lines. In vivo biodistribution was evaluated 24 and 48 hours after intravenous injection of 125I-ATPS mAb into MKN-45 tumor-bearing mice (n = 3). For radioimmunotherapy, 18.5 MBq 131I-ATPS mAb (n = 7), isotype immunoglobulin G (IgG) (n = 6), and vehicle (n = 6) were injected into MKN-45 tumor-bearing mice for 4 weeks, and tumor volume and percentage of tumor growth inhibition (TGI) were compared each week.
Results:
MKN-45 cells showed the highest in vitro cellular binding after 4 hours (0.00324 ± 0.00013%/μg), which was significantly inhibited by unlabeled ATPS mAb at concentrations of greater than 0.4 μM. The in vitro retention rate of 125I-ATPS mAb in MKN-45 cells was 64.1% ± 1.0% at 60 minutes. The highest tumor uptake of 125I-ATPS mAb in MKN-45 tumor-bearing mice was achieved 24 hours after injection (6.26% ± 0.47% injected dose [ID]/g), whereas tumor to muscle and tumor to blood ratios peaked at 48 hours. The 24-hour tumor uptake decreased to 3.43% ± 0.85% ID/g by blocking with unlabeled ATPS mAb. After 4 weeks of treatment, mice receiving 131I-ATPS mAb had significantly smaller tumors (679.4 ± 232.3 mm3) compared with control (1687.6 ± 420.4 mm3, P = .0431) and IgG-treated mice (2870.2 ± 484.1 mm3, P = .0010). The percentage of TGI of 131I-ATPS mAb was greater than 50% during the entire study period (range: 53.7%-75.9%).
Conclusion:
The specific binding and antitumor effects of radioiodinated ATPS mAb were confirmed in in vitro and in vivo models of stomach cancer.
Insights
Radioiodine-labeled anti-adenosine triphosphate synthase monoclonal antibody (ATPS mAb) shows theragnostic potential for stomach cancer. This targeted therapy effectively reduced tumor growth in preclinical models, demonstrating its dual imaging and treatment capabilities.
Area of Science:
- Oncology
- Radiopharmaceuticals
- Immunotherapy
Background:
- Adenosine triphosphate synthase (ATPS) is a potential cancer biomarker.
- Monoclonal antibodies (mAbs) offer targeted delivery for cancer theranostics.
Purpose of the Study:
- To evaluate a radioiodine-labeled anti-ATPS mAb for simultaneous cancer imaging and treatment.
- To assess the theragnostic potential of ATPS mAb in stomach cancer models.
Main Methods:
- ATPS mAb was labeled with radioiodine (125I and 131I).
- In vitro binding and retention assays were performed using MKN-45 cancer cells.
- In vivo biodistribution and tumor growth inhibition studies were conducted in tumor-bearing mice.
Main Results:
- 125I-ATPS mAb demonstrated specific binding and retention in MKN-45 cells.
- Highest tumor uptake of 125I-ATPS mAb was observed 24 hours post-injection in mice.
- 131I-ATPS mAb treatment significantly reduced tumor volume and achieved >50% tumor growth inhibition over 4 weeks.
Conclusions:
- Radioiodinated ATPS mAb exhibits specific binding and potent antitumor effects in preclinical stomach cancer models.
- The study confirms the theragnostic potential of radioiodinated ATPS mAb for stomach cancer.
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