Tracers / [68Ga]Ga-FAPI-04

[68Ga]Ga-FAPI-04

Also written as [68Ga]Ga-FAPI-04; [68Ga]Ga-FAPI-4; [Ga-68]Ga-FAPI-04; FAPI-04; Ga-68 FAPI-04
Radionuclide
Ga-68 t½ 67.71 min
Modality
PET
Production route
Stage
Syntheses indexed
47

What it is

Compound class
Radiolabelled quinoline-based FAP-inhibitor (small molecule, DOTA-conjugated)
Target / mechanism
Fibroblast activation protein (FAP), a serine protease overexpressed on cancer-associated fibroblasts PMID 30850501
Clinical application
Pan-cancer imaging of tumour-stroma/fibroblast activation (evaluated across 28 cancer types) PMID 30954939
Theranostic pair
<a href="/tracers/lu177-fapi04/">lu177-fapi04</a>

Regulatory status

FDA
EMA (centralised)
Other approvals
Brand names

Clinical use

Typical injected activity
Uptake time

Reported in the literature. Not a dosing recommendation.

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
SPEDOTA-FAPI-04 precursor35991604
2022 Front Chem
Modular-Lab Standard
Eckert & Ziegler
fixed tubingSPE85.5±1.4%
no
DOTA-FAPI-4
MedChemExpress
39050235
2024 Asia Ocean J Nucl Med Biol
Automated radiosynthesis module (Modular-Lab Standard) was from Eckert & Ziegler, Germany. — The non-decay corrected (ndc) RCY for [68Ga]Ga-Pentixafor, [68Ga]Ga-FAPI-4 and [68Ga]Ga-DOTATATE were found to be...(85.5±1.4)% (n=9)
HPLC>98%DOTA-FAPI-04
MedChemExpress
42691023
2026 PLoS One
42591149
2026 Front Immunol
90.2%96.5%FAPI-0442569132
2026 ACS Omega
42318157
2026 Oncol Rev
SPEFAPI-04
Huayi
42180616
2026 Oncol Lett
42115250
2026 Sci Rep
41904503
2026 Breast Cancer Res
41871918
2026 RMD Open
FAPI-0441807884
2026 Mol Diagn Ther
41692852
2026 Eur J Nucl Med Mol Imaging
vendor cassetteFAPI cold kit41689142
2026 Cancer Imaging
41599688
2026 Pharmaceuticals (Basel)
41515390
2025 Molecules
exceeded 95%FAPI-04
MCE, MedChemExpress, USA
41408360
2025 Cancer Imaging
41344856
2026 J Nucl Med
41286125
2026 Eur J Nucl Med Mol Imaging
SPEFAPI precursor
Huayi
41209215
2025 Quant Imaging Med Surg
41129212
2025 JCI Insight
41034790
2025 BMC Cancer
40809416
2025 Front Med (Lausanne)
SPEexceeding 98%FAPI-04
MedChemExpress
40484962
2025 Cancer Imaging
40278857
2025 Eur J Nucl Med Mol Imaging
40263181
2025 Mol Diagn Ther
40263181
2025 Mol Diagn Ther
40213671
2025 Theranostics
40076605
2025 Int J Mol Sci
FASTlab 2
GE HealthCare
custom manifoldnone98.77 ± 0.12DOTA-FAPI-04
MedChemExpress
39598846
2024 Molecules
Automated labeling of the precursor was accomplished using a FASTLab 2 synthesizer.
Modular-Lab Standard
Eckert & Ziegler
fixed tubingSPE85.5±1.4%
no
99.6±0.2%DOTA-FAPI-4
MedChemExpress
39050235
2024 Asia Ocean J Nucl Med Biol
Automated radiosynthesis module (Modular-Lab Standard) was from Eckert & Ziegler, Germany. — [68Ga]Ga-FAPI-4 ... were found to be ... (85.5±1.4)% (n=9)
FAPI-0441946434
2026 J Control Release
97.47 ± 0.26%
yes
99.18 ± 0.34%FAPI-442705038
2026 Appl Radiat Isot
a commercial fixed tubing (non-cassette) based automated module namely Eckert and Ziegler 'Modular-Lab Standard' (EZ-ML) — decay corrected (dc) radiochemical yield (RCY) and radiochemical purity (RCP) of 97.47 ± 0.26% and 99.18 ± 0.34% respectively
42663571
2026 Rheumatology (Oxford)
42660633
2026 J Nucl Med
42410759
2026 Clin Nucl Med
FAPI-0442343548
2026 J Med Chem
42273741
2026 Circ Cardiovasc Imaging
42128000
2026 Br J Radiol
42113378
2026 Ann Surg Oncol
42007813
2026 Clin Nucl Med
41887115
2026 Bioorg Chem
41771036
2026 Clin Nucl Med
41738886
2026 Clin Nucl Med
41649855
2026 Clin Nucl Med
41627842
2026 Clin Nucl Med
41544061
2026 Clin Nucl Med
FAPI-0435658448
2022 J Med Chem

Precursor

Common precursor
DOTA-FAPI-04 precursor PMID 35991604 (DOI 10.3389/fchem.2022.939160)
Suppliers seen in the literature
Cited suppliers in indexed syntheses
Huayi, MCE, MedChemExpress
Typical final purification
SPE

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Quality control Derived from the published synthesis

Ph. Eur. monograph
USP monograph
AppearancepHRCP HPLCHPLC UVResidual solvents (GC)Radionuclidic (HPGe)Half-lifeActivityEndotoxins (LAL)SterilityFilter integrityMolar activityMetal impuritiesGe-68 breakthrough
How this set was arrived at. base set per Ph. Eur. general monograph 0125 (rule); radiometal tracer -> metal impurities (rule); Ga-68, generator-produced per synthesis data (PMID 35991604) -> Ge-68 breakthrough; receptor ligand with a saturable target -> molar activity (rule); organic solvent confirmed in synthesis data (PMID 35991604) -> GC residual solvents

Tests listed by reference only. Monograph texts are copyrighted and are not reproduced here. How these are derived

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Notes

Added from reverse module search (stage 6); 9 article(s) with Ga-68.