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Pharmacology stubs
Technetium (99mTc) etarfolatide
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    Technetium (99mTc) etarfolatide

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    Technetium (99mTc) etarfolatide
    Technetium etarfolatide.svg
    Clinical data
    ATC code
    Legal status
    Legal status
    • Investigational
    Identifiers
    • (2R)-2-[(2S)-2-[(2S)-3-[[(4R)-4-[[4-[(2-amino-4-oxo-1H-pteridin-6-yl)methylamino]benzoyl]amino]-4-carboxybutanoyl]amino]-2-azanidylpropanoyl]azanidyl-3-carboxypropanoyl]azanidyl-3-hydroxy-3-oxopropane-1-thiolate oxotechnetium(4+) (99mTc)
    CAS Number
    PubChem CID
    UNII
    KEGG
    CompTox Dashboard (EPA)
    Chemical and physical data
    Formula C29H32N11O12S99mTc
    Molar mass 855.595 g/mol
    3D model (JSmol)
    • C1=CC(=CC=C1C(=O)N[C@H](CCC(=O)NC[C@@H](C(=O)[N-][C@@H](CC(=O)O)C(=O)[N-][C@@H](C[S-])C(=O)O)[NH-])C(=O)O)NCC2=CN=C3C(=N2)C(=O)N=C(N3)N.O=[99Tc+4]

    Technetium (99mTc) etarfolatide is an investigational non-invasive, folate receptor-targeting companion imaging agent that is being developed by Endocyte. Etarfolatide consists of a small molecule targeting the folate receptor and an imaging agent, which is based on technetium-99m. This companion imaging agent identifies cells expressing the folate receptor, including cancer and inflammatory cells.

    Etarfolatide is currently being investigated together with the corresponding small molecule drug conjugate (SMDC) vintafolide in a Phase 3 study in platinum-resistant ovarian cancer and in a Phase 2b study in non-small cell lung cancer. It identifies patients with metastases that are positive for the folate receptor and therefore more likely to respond to treatment with vintafolide. Other folate receptor targeting SMDCs for the treatment of cancer, inflammatory diseases and kidney disease are in preclinical development and will also utilize etarfolatide as companion imaging agent.

    The European Medicines Agency (EMA) is reviewing the Marketing Authorization Application (MAA) filings for both vintafolide and etarfolatide, for the treatment of patients with folate receptor-positive platinum-resistant ovarian cancer in combination with pegylated liposomal doxorubicin (PLD).



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