Tracers / [68Ga]Ga-Pentixafor

[68Ga]Ga-Pentixafor

Also written as [68Ga]Ga-PentixaFor; [68Ga]PentixaFor; [Ga-68]Ga-PentixaFor; [Ga-68]PentixaFor; Ga-68 PENTIXAFOR; Ga-68-Pentixafor; PENTIXAFOR
Radionuclide
Ga-68 t½ 67.71 min
Modality
PET
Production route
Stage
Investigational (academic clinical studies)
Syntheses indexed
65

What it is

Compound class
Radiolabelled cyclic pentapeptide, CXCR4 antagonist analogue
Target / mechanism
Chemokine receptor CXCR4, overexpressed in several haematologic and solid malignancies PMID 35674738
Clinical application
CXCR4-receptor imaging in lymphoproliferative disorders (lymphoma, multiple myeloma) and other CXCR4-overexpressing tumours PMID 35674738
Theranostic pair
<a href="/tracers/lu177-pentixather/">lu177-pentixather</a>

Regulatory status

FDA
No FDA (Drugs@FDA/openFDA): no CXCR4/pentixafor product found (searched substance_name 'pentixafor')
EMA (centralised)
No EMA medicines register export (2026-09-09): no 'pentixafor' entry
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
Scintomics GRP / GRP-3V
Scintomics
26909116
2016 Theranostics
fully GMP compliant automated synthesizer (GRP, Scintomics, Germany)
EasyOne
Trasis
vendor cassetteSPE91 ± 5%
yes
>99.4%Pentixafor
MedChemExpress
41701433
2026 EJNMMI Radiopharm Chem
The fully automated synthesis of [68Ga]Ga-Pentixafor was also performed with Trasis EasyOne synthesizer. — The corrected yield of the labelled products was 91 ± 5% (72 ± 5% non-decay corrected).
Modular-Lab Standard
Eckert & Ziegler
fixed tubingSPE84.4±0.9%
no
99.4±0.3%DOTA-Pentixafor
Lympholucin, South Korea
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 (84.4±0.9)% (n=12)
Scintomics GRP / GRP-3V
Scintomics
vendor cassette
ABX
33805264
2021 Diagnostics (Basel)
a fully automated, GMP-compliant method using a GRP module (Scintomics, Fürstenfeldbruck, Germany) that was equipped with disposable single-use cassette kits (ABX, Radeberg, Germany) was used
Scintomics; ABX
vendor cassetteCPCR4.2
ABX
33579381
2021 Cancer Imaging
Pentixafor was prepared in a fully automated procedure using a module equipped with a single-use cassette kit (Scintomics GmbH, Germany; ABX, Germany) [12].
Scintomics GRP / GRP-3V
Scintomics
SPEPentixafor33391493
2021 Theranostics
[68Ga]Pentixafor was synthesized using a fully automated Scintomics GRP+ module.
SPE>95%pentixafor
ABX
33287237
2020 Biomolecules
Scintomics GRP / GRP-3V
Scintomics
vendor cassette30191351
2018 EJNMMI Res
Synthesis of 68Ga-Pentixafor was performed on a fully automated, GMP-compliant procedure using GRP module (Scintomics GmbH, Germany) equipped with disposable single-use cassette kits following the previously described method [19, 21].
Scintomics GRP / GRP-3V
Scintomics
vendor cassette> 98%Pentixafor
Scintomics, Fürstenfeldbruck, Germany
29228566
2017 Oncotarget
using a GRP® module (SCINTOMICS GmbH, Fürstenfeldbruck, Germany)
Scintomics GRP / GRP-3V
Scintomics
28529632
2017 Theranostics
fully GMP compliant automated synthesizer (GRP, Scintomics, Germany)
Scintomics GRP / GRP-3V
Scintomics
vendor cassetteSPEPentixafor
Scintomics, Fürstenfeldbruck, Germany
28042328
2017 Theranostics
a GRP® module (SCINTOMICS GmbH, Germany)
Scintomics GRP / GRP-3V
Scintomics
vendor cassetteSPEPentixafor
Scintomics, Fürstenfeldbruck, Germany
26843617
2016 Oncotarget
using a GRP® module (SCINTOMICS GmbH, Germany) equipped with a disposable single-use cassette kit (ABX, Germany)
Scintomics GRP / GRP-3V
Scintomics
vendor cassettePentixafor25736399
2015 EMBO Mol Med
using a GRP® module (SCINTOMICS GmbH, Germany)
Modular-Lab Standard
Eckert & Ziegler
fixed tubingSPE97.11 ± 0.60
yes
99.4 ± 0.3Pentixafor acetate (DOTA conjugated Pentixafor)
Lympholucin, South Korea
39987209
2025 Sci Rep
Modular-Lab Standard (a fixed tubing or non-cassette based fully automated radiochemistry module) — The decay corrected RCY of all the produced batches of [68Ga]Ga-Pentixafor (n = 16) were in the range of (97.11 ± 0.60)%
Elysia-Raytest
vendor cassetteSPE87.0%
yes
99.1% (ITLC), 99.8% (HPLC)PentixaFor
PentixaPharm
36749409
2023 EJNMMI Radiopharm Chem
commercial labeling synthesis module Gaia/Luna (Elysia-Raytest, GmbH, Straubenhardt, Germany) — the mean radiochemical yield was 87.0% [standard deviation (SD) 6.67%]
Scintomics GallElut
Scintomics
SPE>99%pentixafor25825601
2015 Theranostics
[68Ga]pentixafor was prepared using 3.5 nmol of pentixafor in a Gallelut+ module (SCINTOMICS GmbH, Germany)
Scintomics GRP / GRP-3V
Scintomics
vendor cassetteSPE>99%pentixafor25825601
2015 Theranostics
performed in a fully automated, GMP-compliant procedure using a GRP® module (SCINTOMICS GmbH, Germany)
Scintomics GRP / GRP-3V
Scintomics
vendor cassetteSPEPentixafor
Scintomics, Fürstenfeldbruck, Germany
28529638
2017 Theranostics
using a GRP® module (SCINTOMICS GmbH, Fürstenfeldbruck, Germany)
Scintomics GRP / GRP-3V
Scintomics
SPEPentixafor28932900
2018 Eur J Nucl Med Mol Imaging
[68Ga]Pentixafor production was carried out as already described [22, 23] in a fully automated manner by using a Scintomics GRP module.
31408441
2019 J Clin Invest
34417915
2021 EJNMMI Res
Scintomics GRP / GRP-3V
Scintomics
35966583
2022 Theranostics
fully GMP compliant automated synthesizer (GRP, Scintomics, Fürstenfeldbruck, Germany)
Modular-Lab PharmTracer
Eckert & Ziegler
vendor cassetteSPE94.7
yes
99.8%PentixaFor
PentixaPharm
32107654
2020 EJNMMI Radiopharm Chem
Modular Lab PharmTracer (MLPT) from Eckert & Ziegler — 50 μg PentixaFor resulted in 94.7% radiochemical yield (RCY, n.d.c.) in the product vial
Scintomics GRP / GRP-3V
Scintomics
vendor cassetteSPE73.1% ± 7.7%
yes
>99%CPCR4.2 trifluoroacetate
ABX
34658546
2021 Indian J Nucl Med
fully automatic synthesizer (Scintomics, Munich, Germany) — Mean radiolabelling efficiency of 73.1% ± 7.7% (n = 57) was obtained with synthesis time approximatively of 34 min
40269029
2025 Sci Rep
Scintomics GRP / GRP-3V
Scintomics
vendor cassette
ABX
29721166
2018 Oncotarget
[68Ga]-Pentixafor was synthesized in a fully automated procedure on a Scintomics GRP module (SCINTOMICS GmbH, Germany)
31004184
2019 Eur J Nucl Med Mol Imaging
41706122
2026 Eur J Nucl Med Mol Imaging
Scintomics
29967943
2018 Eur J Nucl Med Mol Imaging
connected to an automated module (Scintomics, Fürstenfeldbruck, Germany)
Scintomics GRP / GRP-3V
Scintomics
vendor cassettePentixafor29290814
2018 Theranostics
using a GRP® module (SCINTOMICS GmbH, Fürstenfeldbruck, Germany)
31410585
2019 EJNMMI Res
Scintomics GRP / GRP-3V
Scintomics
31281504
2019 Theranostics
[68Ga]Ga-Pentixafor production was carried out, as previously described, in a fully automated manner using a Scintomics GRP module
32724470
2020 Theranostics
42244984
2026 Theranostics
41807884
2026 Mol Diagn Ther
Manual synthesisSPE83 ± 5%
yes
98.6 ± 0.4%Pentixafor
Nanchang Tanzhen Biological Technology Co., Ltd., China
41764676
2026 EJNMMI Radiopharm Chem
Radiolabeling of 68Ga with DOTA-TATE, Pentixafor and FAP-2286 was performed manually using a similar operating procedure — 83 ± 5%
EasyOne
Trasis
vendor cassetteSPE91.06
yes
>99.4%Pentixafor precursor
MedChemExpress
41701433
2026 EJNMMI Radiopharm Chem
The fully automated synthesis of [68Ga]Ga-Pentixafor was also performed with Trasis EasyOne synthesizer. — 91,06%
40447542
2025 Semin Nucl Med
40323995
2025 Clin Nucl Med
FASTlab 2
GE HealthCare
custom manifoldnone98.64 ± 0.26DOTA-(Tyr3)-pentixafor
ABX
39598846
2024 Molecules
Automated labeling of the precursor was accomplished using a FASTLab 2 synthesizer.
Modular-Lab Standard
Eckert & Ziegler
fixed tubingSPE84.4±0.9%
no
99.4±0.3%DOTA-Pentixafor
Lympholucin, South Korea
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 (84.4±0.9)% (n=12)
38082196
2024 Eur J Nucl Med Mol Imaging
Manual synthesisSPEpentixafor
PentixaPharm
37989124
2024 Radiat Res
Twenty micrograms of pentixafor (PentixaPharm®, Germany, reconstituted in metal-free H2O) was labeled with ~3–4 μCi (111–148 MBq) of 68Ga in 0.5 ml 0.4 M sodium acetate buffer (pH 5.3–5.5) at 95°C for 15 min.
37286923
2023 Mol Imaging Biol
Scintomics GRP / GRP-3V
Scintomics
vendor cassetteSPEPentixafor
PentixaPharm
35889351
2022 Molecules
the automated synthesis module Scintomics GRPTM (Scintomics GmbH, Fürstenfeldbruck, Germany)
33550492
2022 Eur J Nucl Med Mol Imaging
32724470
2020 Theranostics
Modular-Lab PharmTracer
Eckert & Ziegler
vendor cassetteSPE94.7
no
99.8%PentixaFor
PentixaPharm
32107654
2020 EJNMMI Radiopharm Chem
Modular Lab PharmTracer (Eckert & Ziegler Eurotope GmbH, Germany) — 50 μg PentixaFor resulted in 94.7% radiochemical yield (RCY, n.d.c.) in the product vial
Scintomics
SPEpentixafor30042959
2016 Tomography
[68Ga]pentixafor was prepared on a fully automated system (Scintomics GmbH) similar to that previously described (42)
Scintomics GRP / GRP-3V
Scintomics
vendor cassettePentixafor29290814
2018 Theranostics
using a GRP® module (SCINTOMICS GmbH, Fürstenfeldbruck, Germany) equipped with disposable single-use cassette kits
26877786
2016 Theranostics
Scintomics GRP / GRP-3V
Scintomics
vendor cassetteSPEPentixafor
Scintomics, Fürstenfeldbruck, Germany
26843617
2016 Oncotarget
using a GRP® module (SCINTOMICS GmbH, Germany) equipped with a disposable single-use cassette kit (ABX, Germany)
HPLC5798 ± 0.22%PENTIXAFOR35190517
2022 Nucl Med Commun
35452014
2022 Clin Nucl Med
28729430
2018 J Nucl Med
27819856
2017 Clin Nucl Med
25698782
2015 J Nucl Med
94.8 ± 2.6%37679888
2023 J Labelled Comp Radiopharm
on the Trasis miniAllinOne synthesizer — Validation batches were performed with a radiochemical yield of 94.8 ± 2.6%.
30002148
2018 Stroke
29279316
2018 Hypertension
28775206
2018 J Nucl Med
42544987
2026 Clin Nucl Med
42544986
2026 Clin Nucl Med
42273741
2026 Circ Cardiovasc Imaging
42018345
2026 Clin Exp Rheumatol

Precursor

Common precursor
Pentixafor (peptide precursor) PMID 41701433 (DOI 10.1186/s41181-026-00426-2)
Suppliers seen in the literature
MedChemExpress (Monmouth Junction, NJ, USA)
Cited suppliers in indexed syntheses
ABX, Lympholucin, MedChemExpress, Nanchang Tanzhen Biological Technology Co., Ltd., PentixaPharm, Scintomics, Fürstenfeldbruck
Typical final purification
SPE

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Quality control Derived from the published synthesis

Ph. Eur. monograph
USP monograph
AppearancepHRCP HPLCHPLC UVRadionuclidic (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 41701433) -> Ge-68 breakthrough; 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

Setting up quality control?We can help you scope the equipment needed to release [68Ga]Ga-Pentixafor.

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Notes

Added from reverse module search (stage 6); 49 article(s) with Ga-68.