Technetium (99mTc) etarfolatide

Technetium (99mTc) etarfolatide
Systematic (IUPAC) name
(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
Legal status
  • Investigational
Identifiers
CAS Number 479410-20-3
ATC code V09IA08 (WHO)
PubChem CID 71300440
Chemical data
Formula C29H32N11O12S99mTc
Molar mass 855.595 g/mol

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 http://www.fiercemedicaldevices.com/story/endocytes-dx-spots-ovarian-and-lung-cancer-patients-ripe-merck-drug/2013-03-03
  2. 1 2 http://www.radiologytoday.net/archive/rt0213p12.shtml
  3. ↑ http://health.universityofcalifornia.edu/2012/08/02/new-drug-shows-promise-for-kidney-disease/
  4. ↑ http://www.insideindianabusiness.com/life-sciences.asp?ID=3298&Detail=True
  5. ↑ http://www.businessweek.com/ap/2012-11-27/eu-reviews-cancer-drug-from-merck-and-endocyte


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