Pentixafor

Demmer O, Gourni E, Schumacher U, Kessler H, Wester HJ.

ChemMedChem. 2011 Oct 4;6(10):1789-91.

doi: 10.1002/cmdc.201100320.

PET imaging of CXCR4 receptors in cancer by a new optimized ligand.

No abstract available

Gourni E, Demmer O, Schottelius M, D’Alessandria C, Schulz S, Dijkgraaf I, Schumacher U, Schwaiger M, Kessler H, Wester HJ.

J Nucl Med. 2011 Nov;52(11):1803-10. doi: 10.2967/jnumed.111.098798.

PET of CXCR4 expression by a (68)Ga-labeled highly specific targeted contrast agent.

CONCLUSION:

The small and optimized cyclic peptide CPCR4-2 labeled with (68)Ga is a suitable tracer for targeting and imaging of human CXCR4 receptor expression in vivo. The high affinity for CXCR4, its in vivo stability, and the excellent pharmacokinetics recommend the further evaluation of (68)Ga-CPCR4-2 in a proof-of-concept study in humans.

Herrmann K, Lapa C, Wester HJ, Schottelius M, Schiepers C, Eberlein U, Bluemel C, Keller U, Knop S, Kropf S, Schirbel A, Buck AK, Lassmann M.

J Nucl Med. 2015 Mar;56(3):410-6.

doi: 10.2967/jnumed.114.151647.

Biodistribution and radiation dosimetry for the chemokine receptor CXCR4-targeting probe 68Ga-pentixafor.

CONCLUSION:

(68)Ga-pentixafor exhibits a favorable dosimetry, delivering absorbed doses to organs that are lower than those delivered by (18)F-FDG- or (68)Ga-labeled somatostatin receptor ligands.

Philipp-Abbrederis K, Herrmann K, Knop S, Schottelius M, Eiber M, Lückerath K, Pietschmann E, Habringer S, Gerngroß C, Franke K, Rudelius M, Schirbel A, Lapa C, Schwamborn K, Steidle S, Hartmann E, Rosenwald A, Kropf S, Beer AJ, Peschel C, Einsele H, Buck AK, Schwaiger M, Götze K, Wester HJ, Keller U.

EMBO Mol Med. 2015 Mar 3;7(4):477-87.

doi: 10.15252/emmm.201404698.

In vivo molecular imaging of chemokine receptor CXCR4 expression in patients with advanced multiple myeloma.

CONCLUSION:

Based on these highly encouraging data on clinical PET imaging of CXCR4 expression in a cohort of MM patients, we conclude that [(68)Ga]Pentixafor PET opens a broad field for clinical investigations on CXCR4 expression and for CXCR4-directed therapeutic approaches in MM and other diseases

Wester HJ, Keller U, Schottelius M, Beer A, Philipp-Abbrederis K, Hoffmann F, Šimeček J, Gerngross C, Lassmann M, Herrmann K, Pellegata N, Rudelius M, Kessler H, Schwaiger M.

Theranostics. 2015 Mar 1;5(6):618-30.

doi: 10.7150/thno.11251.

Disclosing the CXCR4 expression in lymphoproliferative diseases by targeted molecular imaging.

SUMMARY:

This non-invasive Pentixafor based imaging technology for quantitative assessment of CXCR4 expression allows to further elucidate the role of CXCR4/CXCL12 ligand interaction in the pathogenesis and treatment of cancer, cardiovascular diseases and autoimmune and inflammatory disorders.

Thackeray JT, Derlin T, Haghikia A, Napp LC, Wang Y, Ross TL, Schäfer A, Tillmanns J, Wester HJ, Wollert KC, Bauersachs J, Bengel FM.

JACC Cardiovasc Imaging. 2015 Dec;8(12):1417-26.

doi: 10.1016/j.jcmg.2015.09.008.

Molecular Imaging of the Chemokine Receptor CXCR4 After Acute Myocardial Infarction.

CONCLUSION:

Targeted PET imaging with 68Ga-pentixafor identifies the global and regional CXCR4 expression pattern in myocardium and systemic organs. CXCR4 upregulation after AMI coincides with in flammatory cell in filtration, but shows interindividual variability in patients. This may have implications for the response to CXCR4- or other in

flammation-targeted therapy, and for subsequent ventricular remodeling.

Rischpler C, Nekolla SG, Kossmann H, Dirschinger RJ, Schottelius M, Hyafil F, Wester HJ, Laugwitz KL, Schwaiger M.

J Nucl Cardiol. 2016 Feb;23(1):131-3.

doi: 10.1007/s12350-015-0347-5.

Upregulated myocardial CXCR4-expression after myocardial infarction assessed by simultaneous GA-68 pentixafor PET/MRI.

No abstract available

Lapa C, Reiter T, Werner RA, Ertl G, Wester HJ, Buck AK, Bauer WR, Herrmann K.

JACC Cardiovasc Imaging. 2015 Dec;8(12):1466-8.

doi: 10.1016/j.jcmg.2015.09.007.

[68Ga]Pentixafor-PET/CT for Imaging of CXCR4 Expression After Myocardial Infarction.

No abstract available

Machado JS, Beykan S, Herrmann K, Lassmann M.

Eur J Nucl Med Mol Imaging. 2016 Oct;43(11):2036-9.

doi: 10.1007/s00259-015-3289-x.

Recommended administered activities for (68)Ga-labelled peptides in paediatric nuclear medicine.

CONCLUSION:

For paediatric nuclear medicine applications involving (68)Ga-labelled peptides, we suggest determining administered activities based on the formalism proposed in this work. The corresponding effective doses from these procedures will remain age-independent.

Derlin T, Jonigk D, Bauersachs J, Bengel FM.

Clin Nucl Med. 2016 Apr;41(4):e204-5.

doi: 10.1097/RLU.0000000000001092

Molecular Imaging of Chemokine Receptor CXCR4 in Non-Small Cell Lung Cancer Using 68Ga-Pentixafor PET/CT: Comparison With 18F-FDG.

CONCLUSION:

68Ga-Pentixafor is a novel CXCR4-targeted probe for PET imaging of CXCR4-positive tumors and holds promise for tumor staging and prognostic stratification. CXCR4-targeted radionuclide therapy represents a therapy option in metastasized diseases.

Vag T, Gerngross C, Herhaus P, Eiber M, Philipp-Abbrederis K, Graner FP, Ettl J, Keller U, Wester HJ, Schwaiger M.

J Nucl Med. 2016 May;57(5):741-6.

doi: 10.2967/jnumed.115.161034.

First Experience with Chemokine Receptor CXCR4-Targeted PET Imaging of Patients with Solid Cancers.

CONCLUSION:

On the basis of these first observations in a small and heterogeneous patient cohort, the in vitro CXCR4 expression profile of solid cancers and metastases described in the previous literature does not seem to sufficiently depict the in vivo distribution revealed by CXCR4-targeted PET. Moreover, the detectability of solid cancers seems to be generally lower for (68)Ga-pentixafor than for (18)F-FDG PET.

Lapa C, Lückerath K, Rudelius M, Schmid JS, Schoene A, Schirbel A, Samnick S, Pelzer T, Buck AK, Kropf S, Wester HJ, Herrmann K.

Oncotarget. 2016 Feb 23;7(8):9288-95.

doi: 10.18632/oncotarget.7063.

[68Ga]Pentixafor-PET/CT for imaging of chemokine receptor 4 expression in small cell lung cancer--initial experience.

CONCLUSION:

Non-invasive imaging of CXCR4 expression in SCLC is feasible. [68Ga]Pentixafor as a novel PET tracer might serve as readout for confirmation of CXCR4 expression as prerequisite for potential CXCR4-directed treatment including receptor-radio(drug)peptide therapy.

Lapa C, Lückerath K, Kleinlein I, Monoranu CM, Linsenmann T, Kessler AF, Rudelius M, Kropf S, Buck AK, Ernestus RI, Wester HJ, Löhr M, Herrmann K.

Theranostics. 2016 Jan 25;6(3):428-34.

doi: 10.7150/thno.13986.

(68)Ga-Pentixafor-PET/CT for Imaging of Chemokine Receptor 4 Expression in Glioblastoma.

CONCLUSION:

In this pilot study, 68Ga-Pentixafor retention has been observed in the vast majority of glioblastoma lesions and served as readout for non-invasive determination of CXCR4 expression. Given the paramount importance of the CXCR4/SDF-1 axis in tumor biology, 68Ga-Pentixafor-PET/CT might prove a useful tool for sensitive, non-invasive in-vivo quantification of CXCR4 as well as selection of patients who might benefit from CXCR4-directed therapy.

Herhaus P, Habringer S, Philipp-Abbrederis K, Vag T, Gerngross C, Schottelius M, Slotta-Huspenina J, Steiger K, Altmann T, Weißer T, Steidle S, Schick M, Jacobs L, Slawska J, Müller-Thomas C, Verbeek M, Subklewe M, Peschel C, Wester HJ, Schwaiger M, Götze K, Keller U.

Haematologica. 2016 Aug;101(8):932-40.

doi: 10.3324/haematol.2016.142976.

Targeted positron emission tomography imaging of CXCR4 expression in patients with acute myeloid leukemia.

In summary, in vivo molecular CXCR4 imaging by means of positron emission tomography is feasible in acute myeloid leukemia. These data provide a framework for future diagnostic and theranostic approaches targeting the CXCR4/CXCL12-defined leukemia-initiating cell niche.

Schmid JS, Schirbel A, Buck AK, Kropf S, Wester HJ, Lapa C.

Circ Cardiovasc Imaging. 2016 Sep;9(9):e005217.

doi: 10.1161/CIRCIMAGING.116.005217.

[68Ga]Pentixafor-Positron Emission Tomography/Computed Tomography Detects Chemokine Receptor CXCR4 Expression After Ischemic Stroke.

No abstract available.

Poschenrieder A, Schottelius M, Schwaiger M, Wester HJ.

EJNMMI Res. 2016 Dec;6(1):70.

doi: 10.1186/s13550-016-0227-2.

Preclinical evaluation of [(68)Ga]NOTA-pentixafor for PET imaging of CXCR4 expression in vivo - a comparison to [(68)Ga]pentixafor.

Conclusions:

Despite enhanced CXCR4-affinity in vitro, the [68Ga]NOTA-analog of pentixafor showed reduced CXCR4 targeting efficiency in vivo. In combination with enhanced background accumulation, this resulted in significantly inferior PET imaging contrast, and thus, [68Ga]NOTA-pentixafor offers no advantages over [68Ga]pentixafor.

Hyafil F, Pelisek J, Laitinen I, Schottelius M, Mohring M, Döring Y, van der Vorst EP, Kallmayer M, Steiger K, Poschenrieder A, Notni J, Fischer J, Baumgartner C, Rischpler C, Nekolla SG, Weber C, Eckstein HH, Wester HJ, Schwaiger M.

J Nucl Med. 2017 Mar;58(3):499-506.

doi: 10.2967/jnumed.116.179663

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Imaging the Cytokine Receptor CXCR4 in Atherosclerotic Plaques with the Radiotracer 68Ga-Pentixafor for PET.

Conclusion:

68Ga-pentixafor allows for the noninvasive detection of CXCR4 expression in the vessel wall with PET and emerges as a potential alternative to 18F-FDG for the assessment of macrophage infiltration in atherosclerotic plaques.

Bluemel C, Hahner S, Heinze B, Fassnacht M, Kroiss M, Bley TA, Wester HJ, Kropf S, Lapa C, Schirbel A, Buck AK, Herrmann K.

Clin Nucl Med. 2017 Jan;42(1):e29-e34.

Investigating the Chemokine Receptor 4 as Potential Theranostic Target in Adrenocortical Cancer Patients.

CONCLUSIONS:
Ga-pentixafor allows in vivo imaging of CXCR4 expression in patients with advanced ACC and may serve as companion diagnostic tool in selecting patients for potential CXCR4-directed endoradiotherapy. Seventy percent of the patients with advanced, metastasized ACC may be suitable for a CXCR4-directed treatment after failure of standard treatment options

Werner RA, Weich A, Schirbel A, Samnick S, Buck AK, Higuchi T, Wester HJ, Lapa C.

Eur J Nucl Med Mol Imaging. 2017 Mar;44(3):553-554.

doi: 10.1007/s00259-016-3566-3.

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Intraindividual tumor heterogeneity in NET - Further insight by C-X-C motif chemokine receptor 4-directed imaging.

No abstract available

Lapa C, Schreder M, Schirbel A, Samnick S, Kortüm KM, Herrmann K, Kropf S, Einsele H, Buck AK, Wester HJ, Knop S, Lückerath K.

Theranostics. 2017 Jan 1;7(1):205-212.

doi: 10.7150/thno.16576.

[68Ga]Pentixafor-PET/CT for imaging of chemokine receptor CXCR4 expression in multiple myeloma - Comparison to [18F]FDG and laboratory values.

Conclusions:

[68Ga]Pentixafor-PET provides further evidence that CXCR4 expression frequently occurs in advanced multiple myeloma, representing a negative prognostic factor and a potential target for myeloma specific treatment. However, selecting patients for CXCR4 directed therapies and prognostic stratification seem to be more relevant clinical applications for this novel imaging modality, rather than diagnostic imaging of myeloma.

Watts A, Singh B, Basher R, Singh H, Bal A, Kapoor R, Arora SK, Wester HJ, Mittal BR, Behera D.

Eur J Nucl Med Mol Imaging. 2017 Jan 21.

doi: 10.1007/s00259-017-3622-7.

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68Ga-Pentixafor PET/CT demonstrating higher CXCR4 density in small cell lung carcinoma than in non-small cell variant.

No abstract available

Derlin T, Wester HJ, Bengel FM, Hueper K.

Clin Nucl Med. 2017 Feb 13.

doi: 10.1097/RLU.0000000000001590

Visualization of Posttraumatic Splenosis on Chemokine Receptor CXCR4-Targeted PET/CT.

Conclusions:

It is important to be aware that CXCR4-directed imaging may identify splenic tissue based on the presence of inflammatory cells and that both benign and malignant cells may show CXCR4 expression to avoid misinterpretation.