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Technetium [99mTc] pexidartide (also known as 99mTc-3PRGD2 or Giluntai) is a first-in-class diagnostic radiopharmaceutical approved in China for the auxiliary diagnosis of regional lymph node metastasis in patients with suspected lung cancer. It is a single-photon emission computed tomography (SPECT) imaging agent that specifically targets integrin αvβ3, which is highly expressed on tumor cells and neovascular endothelial cells during angiogenesis. The drug consists of a double-chain RGD peptide (3PRGD2) conjugated to the radioactive isotope technetium-99m (99mTc) via a hydrazinonicotinamide (HYNIC) linker. By binding specifically to integrin αvβ3, it allows for the non-invasive visualization and staging of lung cancer and other solid tumors, offering higher specificity and accuracy compared to conventional 18F-FDG PET/CT imaging. It was developed by Peking University, Beijing Giluntai Pharmaceutical, and Foshan Ruidiao Pharmaceutical, and is commercialized by Baheal Medical.
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