Tracer library / [177Lu]Lu-FAPI-46
[177Lu]Lu-FAPI-46
Also written as 177Lu-FAPI-46; [177Lu]Lu-FAPI-46; [Lu-177]Lu-FAPI-46
- Radionuclide
- Lu-177 t½ 9585 min
- Modality
- Therapy
- Production route
- —
- Stage
- Preclinical
- Syntheses indexed
- 8
What it is
- Compound class
- FAP inhibitor (FAPI) small-molecule radioligand, DOTA-conjugated
- Target / mechanism
- Targets fibroblast activation protein (FAP), expressed on cancer-associated fibroblasts and tumor cells PMID 40177850
- Clinical application
- Targeted radionuclide therapy of FAP-expressing tumors (e.g., glioblastoma) and fibrosing mediastinitis PMID 40815689
- Theranostic pair
- [68Ga]Ga-FAPI-46
Published syntheses
| Module | Cassette | Purification | Yield % | RCP % | Precursor / supplier | Source |
|---|---|---|---|---|---|---|
| Modular-Lab EAZY Eckert & Ziegler | vendor cassette | none | 95 ± 1.0 synthesis no. 3-5 | 99.8 radio-HPLC, synthesis no.3 | FAPI-46 ABX | 37233924 2023 EJNMMI Radiopharm Chem ModularLab EAZY (Eckert & Ziegler Eurotope GmbH, Berlin, Germany) - we increased the balanced radiochemical yield from 86.0% ± 1.4% (synthesis no 1 and 2) to 95% ± 1.0% (synthesis no. 3–5) |
| Modular-Lab EAZY Eckert & Ziegler | vendor cassette | SPE | 86% ± 3 | ≥99 | FAPI-46 ABX | 33864154 2021 EJNMMI Radiopharm Chem A fully automated synthesis of [177Lu]Lu-FAPI derivatives was achieved on the Modular Lab Eazy (ML Eazy) - [177Lu]Lu-FAPI-04; 88% ± 3, [177Lu]Lu-FAPI-46; 86% ± 3 |
| Modular-Lab EAZY | — | — | — | — | FAPI-46 | 34009498 2021 EJNMMI Radiopharm Chem Fully-automated synthesis of 177Lu labelled FAPI derivatives on the module modular lab-Eazy |
| Manual synthesis | — | SPE | — | — | DOTA-FAPI-46 | 41688618 2026 EJNMMI Res FAPI-46 and FAP-2286 were radiolabeled with 111In and 177Lu at a selected pH for 10 min at 100 °C, then purified with a SepPak cartridge |
| Manual synthesis | — | SPE | — | >95% | FAPI-46 Nanchang Tanzhen Biological Technology Co., Ltd., China | 40177850 2025 Mol Cancer Ther [177Lu]LuCl3 (185–740 MBq) was mixed with 0.2 mL of 0.5 mol/L NaOAc (pH = 5.5) and incubated with FAPI-46, DOTA-LP, DOTA-ALB-01, DOTA-ALB-02, and DOTA-ALB-03 (20 μg) at 95°C for 15 minutes. |
| Manual synthesis | — | SPE | >90% | >95% | FAPI-46 | 37321827 2023 J Nucl Med For 177Lu labeling, each of the aforementioned precursors was dissolved in 1 mL of NaAc (0.25 M in water) and added to 4 mL of 177LuCl3 solution (740 MBq in 0.05 M HCl). - 68Ga, 64Cu, and 177Lu were labeled in more than 90% yield with radiochemical purity of more than 95%. |
| Manual synthesis | — | — | — | ≥ 93% | FAPI-46 | 37261473 2023 Eur J Nucl Med Mol Imaging 177Lu-labeling was performed at different conditions, depending on the ligand (Supplementary Table 1). |
| Modular-Lab EAZY Eckert & Ziegler | vendor cassette | none | 95 ± 1.0 | 99.8 | FAPI-46 ABX | 37233924 2023 EJNMMI Radiopharm Chem All three radiopharmaceuticals were successfully synthesized in high radiochemical purities and yields on the ML Eazy. - we increased the balanced radiochemical yield from 86.0% ± 1.4% (synthesis no 1 and 2) to 95% ± 1.0% (synthesis no. 3–5) |
Clinical literature
Clinical studies in the indexed corpus, ordered by design (multicentre, prospective, retrospective, others, case reports last) and then by year. Titles and links only, as published; this is not a summary of the evidence.
- Significant 99mTc-FAPI-46 Uptake in 2 Cases of TENIS Syndrome With Negative Tc-OCTREOTIDE Scan, a New Hope in Theranostic Applications.2025 · Clin Nucl Med · Clinical study
Precursor
- Common precursor
- —
- Suppliers seen in the literature
- —
- Cited suppliers in indexed syntheses
- ABX, Nanchang Tanzhen Biological Technology Co., Ltd.
- Typical final purification
- —
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Get in touchQuality control Derived from the published synthesis
- Ph. Eur. monograph
- not verified No Ph. Eur. check is recorded for this entry.
- USP monograph
- not verified No USP check is recorded for this entry.
How this set was arrived at. base set per Ph. Eur. general monograph 0125 (rule); radiometal tracer -> metal impurities (rule); Lu-177 preparation -> Lu-177m content (rule); therapeutic radiopharmaceutical -> osmolality (rule); receptor ligand with a saturable target -> molar activity (rule)
Tests listed by reference only. Monograph texts are copyrighted and are not reproduced here. How these are derived
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Get in touchNotes
Stage 8: 1 corpus article with Lu-177 FAPI-46 (PMID 37233924) was collapsed onto the Ga-68 anchor [68Ga]Ga-FAPI-46. Added as the therapy partner of the FAPI-46 anchor. Compound class inferred from precursor name (not stated outright) -- PMID 41688618: '[177Lu]Lu-DOTA-FAPI-46'. Stage set/updated at stage 39 from PMID 40815689: 'A radioisotope-based therapeutic approach using 177Lu-FAPI-46 has demonstrated promising results in preclinical models'.