Drug intelligence / Profile preview

technetium [99mTc] pexidartide

Development stage
Unknown
Lead developer
Beijing Giluntai Pharmaceutical
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Gamma Emitters → Radiopharmaceuticals, Peptides
Administration
Intravenous
01

Overview

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.

Brand names
Giluntai吉伦泰
Other names
99mTc-3PRGD2 injection99mTc-HYNIC-3PRGD299mTc-hydrazinonicotinamide-PEG4-E[PEG4-c(RGDfk)]2Technetium[99mTc]hydrazinonicotinamide double-chain Ark peptidetechnetium [99mTc] pexidartide peptide injection锝[99mTc]佩昔瑞特加肽锝[99mTc]佩昔瑞特加肽注射液锝[99mTc]肼基烟酰胺聚乙二醇双环RGD肽锝[99mTc]肼基烟酰胺聚乙二醇双环RGD肽注射液
02

Targets

αVβ3 (Integrin αVβ3)

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