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In addition to classical antibody\u2010 and peptide\u2010targeting for the development of positron emission tomography (PET) radiopharmaceuticals, this receptor possesses a range of small organic inhibitors that can be exploited. These are based mainly on nitrogen\u2010rich scaffolds, such as AMD070, and cyclic polyamines, such as cyclam, in the AMD3100 skeleton. The latter has been explored as a direct <jats:sup>64<\/jats:sup>Cu chelator, but examples of CXCR4 PET imaging with small organic targeting units are still scarce in the literature. Herein, the synthesis of two novel CXCR4\u2010directed radiopharmaceuticals is described, combining the AMD070 scaffold as a targeting unit and bifunctional te1pa macrocycle as a strong <jats:sup>64<\/jats:sup>Cu chelator. The synthesis of the conjugates and optimization of <jats:sup>64<\/jats:sup>Cu\u2010radiolabeling are presented, opening the way for future <jats:italic>in\u2009vitro<\/jats:italic> and <jats:italic>in\u2009vivo<\/jats:italic> studies.<\/jats:p>","DOI":"10.1002\/cmdc.202500243","type":"journal-article","created":{"date-parts":[[2025,5,21]],"date-time":"2025-05-21T03:29:22Z","timestamp":1747798162000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":1,"title":["Synthesis and <sup>64<\/sup>Cu\u2010Radiolabeling Strategies of Small Organic Radioconjugates Based on the AMD070 Scaffold"],"prefix":"10.1002","volume":"20","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-1063-4050","authenticated-orcid":false,"given":"Marie M.","family":"Le Roy","sequence":"first","affiliation":[{"name":"Univ. 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