Technetium (99mTc) etarfolatide
Technetium (99mTc) etarfolatide
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Systematic (IUPAC) name |
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(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) |
Clinical data |
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Identifiers |
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479410-20-3 |
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V09IA08 |
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PubChem |
CID 71300440 |
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Chemical data |
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Formula |
C29H32N11O12S99mTc |
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855.595 g/mol |
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SMILES
- 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]
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Technetium (99mTc) etarfolatide is an investigational non-invasive, folate receptor-targeting companion imaging agent that is being developed by Endocyte.[1]
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.[2] 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.[1][2]
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.[3][4]
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).[5]
References