Technetium (99mTc) etarfolatide

Technetium (^99mTc) etarfolatide
Clinical data
ATC code	V09IA08 ( WHO );
Legal status
Legal status	Investigational;
Identifiers
	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);
CAS Number	479410-20-3 ;
PubChem CID	71300440 ;
UNII	WVU7R99FQ6 ;
KEGG	D10491 ;
CompTox Dashboard (EPA)	DTXSID20197365 ;
Chemical and physical data
Formula	C29H32N11O12S99mTc
Molar mass	855.595g/mol
3D model (JSmol)	Interactive image ;
	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];

Last updated August 10, 2025

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

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[autogenerated1-1] 1 2 http://www.fiercemedicaldevices.com/story/endocytes-dx-spots-ovarian-and-lung-cancer-patients-ripe-merck-drug/2013-03-03

[autogenerated2-2] 1 2 http://www.radiologytoday.net/archive/rt0213p12.shtml

[3] http://health.universityofcalifornia.edu/2012/08/02/new-drug-shows-promise-for-kidney-diseas%5B%5De/

[4] http://www.insideindianabusiness.com/life-sciences.asp?ID=3298&Detail=Tr%5B%5Due

[5] ↑

[1]

[2]

[3]

[4]

[5]

Clinical data

ATC code	V09IA08 ( WHO )
Legal status
Legal status	Investigational
Identifiers
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)
CAS Number	479410-20-3 ^Y
PubChem CID	71300440
UNII	WVU7R99FQ6
KEGG	D10491
CompTox Dashboard (EPA)	DTXSID20197365
Chemical and physical data
Formula	C₂₉H₃₂N₁₁O₁₂S^99mTc
Molar mass	855.595g/mol
3D model (JSmol)	Interactive image
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]