ArticleMolecular pharmaceutics2015
Evaluation of (68)Ga- and (177)Lu-DOTA-PEG4-LLP2A for VLA-4-Targeted PET Imaging and Treatment of Metastatic Melanoma.
Article in Molecular pharmaceutics, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 51 citations in OpenAlex.
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- Recent Developments in the Diagnosis and Treatment of Disseminated and Rare Melanoma with Radiotheranostics.ACS pharmacology & translational science · 2026Review
- Designing Programmable Peptide Nucleic Acid-based Nanovaccines for Anticancer Immune Activation.Small (Weinheim an der Bergstrasse, Germany) · 2025Article
- Evaluation of VLA-4 (Integrin α4β1) as a Shared Target for Radiopharmaceutical Therapy across Solid Tumors.Molecular cancer therapeutics · 2025Article
- Single Chelator-Minibody Theranostic Agents forJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2024Article
- Targeted imaging of very late antigen-4 for noninvasive assessment of lung inflammation-fibrosis axis.EJNMMI research · 2023Article
- Combined Targeted Radiopharmaceutical Therapy and Immune Checkpoint Blockade: From Preclinical Advances to the Clinic.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2022Article
- Visualizing γδ T cells by very late antigen-4-targeted positron emission tomography.European journal of nuclear medicine and molecular imaging · 2022Article
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- PET Imaging of VLA-4 in a New BRAFMolecular imaging and biology · 2022Article
- Translating a radiolabeled imaging agent to the clinic.Advanced drug delivery reviews · 2022Review
- It's Time to Shift the Paradigm: Translation and Clinical Application of Non-αvβ3 Integrin Targeting Radiopharmaceuticals.Cancers · 2021Review
- Immunostimulatory effects of targeted thorium-227 conjugates as single agent and in combination with anti-PD-L1 therapy.Journal for immunotherapy of cancer · 2021Article
- Advances in Receptor-Targeted Radiolabeled Peptides for Melanoma Imaging and Therapy.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2021Review
- Molecular Imaging of Very Late Antigen-4 in Acute Lung Injury.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2021Article
- Novel Agents and Future Perspectives on Theranostics.Seminars in radiation oncology · 2021Review
- Integrin VLA-4 as a PET imaging biomarker of hyper-adhesion in transgenic sickle mice.Blood advances · 2020Article
- Comparison of AlJournal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2020Article
- Targeted radiotherapy of pigmented melanoma withJournal of experimental & clinical cancer research : CR · 2018Article
- Combined VLA-4-Targeted Radionuclide Therapy and Immunotherapy in a Mouse Model of Melanoma.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2018Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Malignant melanoma is a highly aggressive cancer, and the incidence of this disease is increasing worldwide at an alarming rate. Despite advances in the treatment of melanoma, patients with metastatic disease still have a poor prognosis and low survival rate. New strategies, including targeted radiotherapy, would provide options for patients who become resistant to therapies such as BRAF inhibitors. Very late antigen-4 (VLA-4) is expressed on melanoma tumor cells in higher levels in more aggressive and metastatic disease and may provide an ideal target for drug delivery and targeted radiotherapy. In this study, we evaluated (177)Lu- and (68)Ga-labeled DOTA-PEG4-LLP2A as a VLA-4-targeted radiotherapeutic with a companion PET agent for diagnosis and monitoring metastatic melanoma treatment. DOTA-PEG4-LLP2A was synthesized by solid-phase synthesis. The affinity of (177)Lu- and (68)Ga-labeled DOTA-PEG4-LLP2A to VLA-4 was determined in B16F10 melanoma cells by saturation binding and competitive binding assays, respectively. Biodistribution of the LLP2A conjugates was determined in C57BL/6 mice bearing B16F10 subcutaneous tumors, while PET/CT imaging was performed in subcutaneous and metastatic models. (177)Lu-DOTA-PEG4-LLP2A showed high affinity to VLA-4 with a Kd of 4.1 ± 1.5 nM and demonstrated significant accumulation in the B16F10 melanoma tumor after 4 h (31.5 ± 7.8%ID/g). The tumor/blood ratio of (177)Lu-DOTA-PEG4-LLP2A was highest at 24 h (185 ± 26). PET imaging of metastatic melanoma with (68)Ga-DOTA-PEG4-LLP2A showed high uptake in sites of metastases and correlated with bioluminescence imaging of the tumors. These data demonstrate that (177)Lu-DOTA-PEG4-LLP2A has potential as a targeted therapeutic for treating melanoma as well as other VLA-4-expressing tumors. In addition, (68)Ga-DOTA-PEG4-LLP2A is a readily translatable companion PET tracer for imaging of metastatic melanoma.
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