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Published on: April 25, 2025
Development and preclinical evaluation of new (124)I-folate conjugates for PET imaging of folate receptor-positive
I AlJammaz1, B Al-Otaibi1, F Al-Rumayan1
1Cyclotron and Radiopharmaceuticals Department, King Faisal Specialist Hospital and Research Centre, P.O. Box 3354, Riyadh 11211, Kingdom of Saudi Arabia.
Abstract:
In an attempt to develop new folate radiotracers with favorable biochemical properties for detecting folate receptor-positive cancers, we have synthesized [(124)I]-SIB- and [(124)I]-SIP-folate conjugates using a straightforward and two-step simple reactions. Radiochemical yields for [(124)I]-SIB- and [(124)I]-SIP-folate conjugates were greater than 90 and 60% respectively, with total synthesis time of 30-40min. Radiochemical purities were always greater than 98% without HPLC purification. These synthetic approaches hold considerable promise as rapid and simple method for (124)I-folate conjugate preparation with high radiochemical yield in short synthesis time. In vitro tests on KB cell line showed that the significant amounts of the radioconjugates were associated with cell fractions. In vivo characterization in normal Balb/c mice revealed rapid blood clearance of these radioconjugates and favorable biodistribution profile for [(124)I]-SIP-folate conjugate over [(124)I]-SIB-folate conjugate. Biodistribution studies of [(124)I]-SIP-folate conjugate in nude mice bearing human KB cell line xenografts, demonstrated significant tumor uptake. The uptake in the tumors was blocked by excess injection of folic acid, suggesting a receptor-mediated process. These results demonstrate that [(124)I]-SIP-folate conjugate may be useful as a molecular probe for detecting and staging of folate receptor-positive cancers, such as ovarian cancer and their metastasis as well as monitoring tumor response to treatment.
Insights
Researchers developed new iodine-124 labeled folate conjugates, [(124)I]-SIB- and [(124)I]-SIP-folate, for imaging folate receptor-positive cancers. The [(124)I]-SIP-folate conjugate showed promising tumor uptake and biodistribution for cancer detection.
Area of Science:
- Nuclear Medicine
- Radiochemistry
- Oncology
Background:
- Folate receptor-positive cancers present a significant challenge for diagnosis and treatment.
- Development of targeted radiotracers is crucial for improving cancer detection and management.
Purpose of the Study:
- To synthesize novel iodine-124 labeled folate conjugates, [(124)I]-SIB-folate and [(124)I]-SIP-folate.
- To evaluate their biochemical properties, in vitro, and in vivo characteristics for potential use as cancer imaging agents.
Main Methods:
- Two-step synthesis of [(124)I]-SIB- and [(124)I]-SIP-folate conjugates.
- Radiochemical yield and purity assessment.
- In vitro cell binding studies using KB cell line.
- In vivo biodistribution studies in normal mice and tumor-bearing xenografts.
Main Results:
- High radiochemical yields (>90% for SIB, >60% for SIP) and purities (>98%) achieved in short synthesis times (30-40 min).
- Significant association of radioconjugates with cell fractions in vitro.
- [(124)I]-SIP-folate demonstrated favorable biodistribution with rapid blood clearance and significant tumor uptake in xenografts, blocked by folic acid.
Conclusions:
- [(124)I]-SIB- and [(124)I]-SIP-folate conjugates are efficiently prepared using a rapid and simple method.
- [(124)I]-SIP-folate conjugate shows potential as a molecular probe for detecting and staging folate receptor-positive cancers.
- This radiotracer may also be valuable for monitoring treatment response in ovarian cancer and other related malignancies.
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