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^Y
PubChem (CID)	71300440
UNII	WVU7R99FQ6^Y
Chemical and physical data
Formula	C₂₉H₃₂N₁₁O₁₂S^99mTc
Molar mass	855.595 g/mol
3D model (Jmol)	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]

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

Diagnostic radiopharmaceuticals (V09)

Central nervous system	^99mTc (Exametazime) ¹²³I (Ioflupane Iofetamine Iomazenil) ¹⁸F (Florbetapir, Flutemetamol)

Skeletal system	^99mTc (Medronic acid)

Renal	¹²³I (Sodium iodohippurate) ⁶⁴Cu (Cu-ETS2)

Hepatic/reticuloendothelial	⁷⁵Se (SeHCAT)

Respiratory system	¹³³Xe ^81mKr

Cardiovascular system	^99mTc (Sestamibi Tetrofosmin) ¹¹¹In (Imciromab) ⁸²Rb (Rubidium chloride)

Inflammation/infection	^99mTc (Exametazime Sulesomab Tilmanocept) ¹¹¹In ⁶⁷Ga

Tumor	^99mTc (Arcitumomab Votumumab Hynic-octreotide) ¹¹¹In (Capromab pendetide Satumomab pendetide) ¹²⁵I ( Minretumomab) ¹²³I/¹³¹I (Iobenguane) ¹⁸F (Fluciclovine Fludeoxyglucose Fluoroethyltyrosine Sodium fluoride)

Adrenal cortex	¹²³I/¹²⁵I (Iodocholesterol)

Radionuclides (including tracers)	positron (PET): ¹⁸F ¹¹C ⁶⁴Cu ¹³N ¹⁵O ⁶⁸Ga gamma ray/photon (SPECT/scintigraphy): ^99mTc ¹²³I ¹²⁵I ¹³¹I ¹¹¹In ⁵⁷Co ¹⁵³Sm ¹³³Xe ⁵¹Cr ^81mKr ²⁰¹Tl ⁶⁷Ga ⁷⁵Se

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