Synthesis and preliminary evaluation of novel 99mTc-labeled folate derivative via click reaction for SPECT imaging

• An efficient synthetic strategy (click chemistry) was used to improve the overall efficiency.
• 99mTc-HYNIC-T-FA showed a high tumor uptake but low no-target tissues uptakes.
• Excellent tumor-to-kidney ratio was achieved by injecting PMX.
• A kit formulation was developed to obtain the desired product without any purification.

The folate receptor is over expressed in a wide variety of human tumors. In this study, a novel 99mTc-labeled folate derivative (99mTc-HYNIC-T-FA) was synthesized as a potential FR-targeting imaging probe and its efficiency was evaluated. This 99mTc-complex could be obtained through practical manner and showed improved in vivo characteristics compared with other radiofolates. Thus, this novel 99mTc-HYNIC-T-FA compound could serve as a potential imaging agent for folate receptor positive tumors.

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