Tracer library / [68Ga]Ga-Pentixafor
Structure of Pentixafor (unlabelled parent compound, from PubChem)
Unlabelled parent compoundPubChem CID 54575322

[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
Clinical research
Syntheses indexed
16
Receptor expression phenotypingLymphoma

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
[177Lu]Lu-pentixather

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
—

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
EasyOne
Trasis
vendor cassetteSPE91 ± 5%
decay-corrected
>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%
not corrected
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)
Modular-Lab Standard
Eckert & Ziegler
fixed tubingSPE97.11 ± 0.60
decay-corrected
99.4 ± 0.3Pentixafor acetate (DOTA conjugated…Pentixafor 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%
decay-corrected
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%]
Modular-Lab PharmTracer
Eckert & Ziegler
vendor cassetteSPE94.7
decay-corrected
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%
decay-corrected
>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
Manual synthesis—SPE83 ± 5%
decay-corrected
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
decay-corrected
>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%
FASTlab 2
GE HealthCare
custom manifoldnone—98.64 ± 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%
not corrected
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)
Manual synthesis—SPE——pentixafor
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.
Scintomics GRP / GRP-3V
Scintomics
vendor cassetteSPE——Pentixafor
PentixaPharm
35889351
2022 Molecules
the automated synthesis module Scintomics GRPTM (Scintomics GmbH, Fürstenfeldbruck, Germany)
Modular-Lab PharmTracer
Eckert & Ziegler
vendor cassetteSPE94.7
not corrected
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
—SPE——pentixafor30042959
2016 Tomography
[68Ga]pentixafor was prepared on a fully automated system (Scintomics GmbH) similar to that previously described (42)
——HPLC5798 ± 0.22%PENTIXAFOR35190517
2022 Nucl Med Commun
miniAllinOne
Trasis
——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%.

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.

  1. CXCR4 PET imaging of mantle cell lymphoma using [68Ga]Pentixafor: comparison with [18F]FDG-PET.
    2021 · Theranostics · Prospective
  2. [68Ga]Ga-Pentixafor for PET Imaging of Vascular Expression of CXCR-4 as a Marker of Arterial Inflammation in HIV-Infected Patients: A Comparison with 18F[FDG] PET Imaging.
    2020 · Biomolecules · Prospective
  3. Prospective non-invasive evaluation of CXCR4 expression for the diagnosis of MALT lymphoma using [68Ga]Ga-Pentixafor-PET/MRI.
    2019 · Theranostics · Prospective
  4. [68Ga]Pentixafor PET/MR imaging of chemokine receptor 4 expression in the human carotid artery.
    2019 · Eur J Nucl Med Mol Imaging · Prospective
  5. Lesion-level dual-tracer PET biomarkers predict prognosis in multiple myeloma treated with CXCR4-directed radiopharmaceutical therapy.
    2026 · Eur J Nucl Med Mol Imaging · Retrospective
  6. Lymphoma-Sink Effect in Marginal Zone Lymphoma Based on CXCR4-Targeted Molecular Imaging.
    2023 · Mol Imaging Biol · Retrospective
  7. Usefulness of 68 Ga-Pentixafor PET/CT on Diagnosis and Management of Cushing Syndrome.
    2022 · Clin Nucl Med · Retrospective
  8. Investigation of spleen CXCR4 expression by [68Ga]Pentixafor PET in a cohort of 145 solid cancer patients.
    2021 · EJNMMI Res · Retrospective
  9. CXCR4-Directed PET/CT in Patients with Newly Diagnosed Neuroendocrine Carcinomas.
    2021 · Diagnostics (Basel) · Retrospective
  10. Pentixafor PET/CT for imaging of chemokine receptor 4 expression in esophageal cancer - a first clinical approach.
    2021 · Cancer Imaging · Retrospective
Show all 35 clinical studies
  1. PET imaging of chemokine receptor CXCR4 in patients with primary and recurrent breast carcinoma.
    2018 · EJNMMI Res · Retrospective
  2. Clinical Molecular Imaging of Chemokine Receptor CXCR4 Expression in Atherosclerotic Plaque Using 68Ga-Pentixafor PET: Correlation with Cardiovascular Risk Factors and Calcified Plaque Burden.
    2018 · J Nucl Med · Retrospective
  3. 68Ga-Pentixafor PET/CT Imaging of Chemokine Receptor CXCR4 in Chronic Infection of the Bone: First Insights.
    2018 · J Nucl Med · Retrospective
  4. Investigating the Chemokine Receptor 4 as Potential Theranostic Target in Adrenocortical Cancer Patients.
    2017 · Clin Nucl Med · Retrospective
  5. 68 Ga-Pentixafor PET/CT as a Noninvasive Alternative in Evaluation of Suspected Aldosterone-producing Adenoma.
    2026 · Clin Nucl Med · Clinical study
  6. Metachronous Ectopic CRH-Secreting Tumors Detected by 68 Ga-Pentixafor PET/CT.
    2026 · Clin Nucl Med · Clinical study
  7. Primary Aldosteronism: CXCR4- and FAP-Targeted PET/MR for Adrenal-Cardiac Axis.
    2026 · Circ Cardiovasc Imaging · Clinical study
  8. Design, Preclinical Evaluation, and Clinical Translation of [68Ga]Ga/[177Lu]Lu-JH120061, a Novel Radiopharmaceutical Targeting CXCR4.
    2026 · Clin Cancer Res · Clinical study
  9. CXCR4-directed PET/CT with [68 Ga]Ga-pentixafor in solid tumors-a comprehensive analysis of imaging findings and comparison with histopathology.
    2024 · Eur J Nucl Med Mol Imaging · Clinical study
  10. Reduced splenic uptake on 68Ga-Pentixafor-PET/CT imaging in multiple myeloma - a potential imaging biomarker for disease prognosis.
    2022 · Theranostics · Clinical study
  11. CXCR4 expression in glioblastoma tissue and the potential for PET imaging and treatment with [68Ga]Ga-Pentixafor /[177Lu]Lu-Pentixather.
    2022 · Eur J Nucl Med Mol Imaging · Clinical study
  12. Targeting Chemokine Receptor CXCR4 and Translocator Protein for Characterization of High-Risk Plaque in Carotid Stenosis Ex Vivo.
    2018 · Stroke · Clinical study
  13. Imaging of chemokine receptor CXCR4 expression in culprit and nonculprit coronary atherosclerotic plaque using motion-corrected [68Ga]pentixafor PET/CT.
    2018 · Eur J Nucl Med Mol Imaging · Clinical study
  14. Dual Targeting of Acute Leukemia and Supporting Niche by CXCR4-Directed Theranostics.
    2018 · Theranostics · Clinical study
  15. Targeting CXCR4 (CXC Chemokine Receptor Type 4) for Molecular Imaging of Aldosterone-Producing Adenoma.
    2018 · Hypertension · Clinical study
  16. [68Ga]Pentixafor-PET/MRI for the detection of Chemokine receptor 4 expression in atherosclerotic plaques.
    2018 · Eur J Nucl Med Mol Imaging · Clinical study
  17. Targeting CXCR4 with [68Ga]Pentixafor: a suitable theranostic approach in pleural mesothelioma?
    2017 · Oncotarget · Clinical study
  18. Imaging of Chemokine Receptor 4 Expression in Neuroendocrine Tumors - a Triple Tracer Comparative Approach.
    2017 · Theranostics · Clinical study
  19. [68Ga]Pentixafor-PET/CT for imaging of chemokine receptor CXCR4 expression in multiple myeloma - Comparison to [18F]FDG and laboratory values.
    2017 · Theranostics · Clinical study
  20. (68)Ga-Pentixafor-PET/CT for Imaging of Chemokine Receptor 4 Expression in Glioblastoma.
    2016 · Theranostics · Clinical study
  21. [68Ga]Pentixafor-PET/CT for imaging of chemokine receptor 4 expression in small cell lung cancer--initial experience.
    2016 · Oncotarget · Clinical study
  22. First-in-Human Experience of CXCR4-Directed Endoradiotherapy with 177Lu- and 90Y-Labeled Pentixather in Advanced-Stage Multiple Myeloma with Extensive Intra- and Extramedullary Disease.
    2016 · J Nucl Med · Clinical study
  23. Disclosing the CXCR4 expression in lymphoproliferative diseases by targeted molecular imaging.
    2015 · Theranostics · Clinical study
  24. In vivo molecular imaging of chemokine receptor CXCR4 expression in patients with advanced multiple myeloma.
    2015 · EMBO Mol Med · Clinical study
  25. Isolated metastasis of an EGFR-L858R-mutated NSCLC of the meninges: the potential impact of CXCL12/CXCR4 axis in EGFRmut NSCLC in diagnosis, follow-up and treatment.
    2018 · Oncotarget · Case report

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
Typical final purification
SPE

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Quality 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.
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

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Notes

Added from reverse module search (stage 6); 49 article(s) with Ga-68. | Stage 30 (2026-09-18): Stage was 'Investigational (academic clinical studies)'; normalised to 'Clinical research', original wording kept here.
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