Technetium (99mTc) etarfolatide

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Technetium (99m
Tc) etarfolatide
Technetium etarfolatide.svg
Clinical data
ATC code
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 855.595g/mol
3D model (JSmol)
  • n1c2C(=O)NC(N)=Nc2ncc1CNc(cc3)ccc3C(=O)N[C@@H](C(=O)O)CCC(=O)NC[C@H]([N+H2]4)C(=O)N5[C@@H](CC(=O)O)C(=O)N6[C@H](C(=O)O)CS[99Tc-]456=O

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

  1. 1 2 Endocytes-dx-spots-ovarian-and-lung-cancer-patients-ripe-merck-drug
  2. 1 2 "Ultrasound First — AIUM Initiative Points Out the Diagnostic Benefits and Cost Savings of Using Ultrasound as the Primary Imaging Modality in Many Cases". www.radiologytoday.net.
  3. ↑ new-drug-shows-promise-for-kidney-diseas
  4. ↑ http://www.insideindianabusiness.com/life-sciences.asp?ID=3298&Detail=Tr%5B%5Due
  5. ↑ "Bloomberg Businessweek - Bloomberg". Bloomberg.com.


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