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<p>Cardiology is continually evolving towards increased personalization with targeted diagnostics and therapeutics. Peptide-based radiopharmaceuticals have emerged as a valuable tool for noninvasive, receptor-specific imaging, addressing limitations of traditional perfusion-based radiotracers like [<sup>15</sup>O]H<sub>2</sub>O, [<sup>13</sup>N]NH<sub>3</sub>, [<sup>82</sup>Rb]RbCl and [<sup>99m</sup>Tc]Tc-Sestamibi, which lack molecular specificity. While these conventional tracers provide crucial insights into myocardial perfusion and ventricular function, receptor-targeted imaging can illuminate the molecular mechanisms underlying cardiovascular diseases. This, in turn, offers novel insights into disease progression, enhanced diagnostic accuracy, and a tool for companion diagnostics of molecularly targeted therapeutics. Beyond receptor-mediated targeting, recent advances in cell-penetrating peptides (CPPs), such as the development of the cardiac targeting peptide (CTP), offer new opportunities for the enhanced delivery of a therapeutic payload to the injured heart. Their biodistribution can be effectively monitored using radiolabeled analogs. This review explores the role of peptide-based radiopharmaceuticals in nuclear cardiology, highlighting their applications in receptor-mediated imaging and briefly discussing non-receptor-specific CPPs. Select examples illustrate how these innovations are advancing molecular characterization of cardiovascular diseases such as fibrosis, cardiac amyloidosis, atherosclerosis, and more, reshaping the nuclear cardiology landscape.</p>

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Beyond perfusion: a review of peptide radiopharmaceuticals for cardiovascular imaging

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年11月25日

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  • Viktoria E. Krol,
  • Vani Sharma,
  • Joanna E. Kusmirek,
  • Maliha Zahid,
  • Derek R. Johnson,
  • Mukesh K. Pandey

摘要

Cardiology is continually evolving towards increased personalization with targeted diagnostics and therapeutics. Peptide-based radiopharmaceuticals have emerged as a valuable tool for noninvasive, receptor-specific imaging, addressing limitations of traditional perfusion-based radiotracers like [15O]H2O, [13N]NH3, [82Rb]RbCl and [99mTc]Tc-Sestamibi, which lack molecular specificity. While these conventional tracers provide crucial insights into myocardial perfusion and ventricular function, receptor-targeted imaging can illuminate the molecular mechanisms underlying cardiovascular diseases. This, in turn, offers novel insights into disease progression, enhanced diagnostic accuracy, and a tool for companion diagnostics of molecularly targeted therapeutics. Beyond receptor-mediated targeting, recent advances in cell-penetrating peptides (CPPs), such as the development of the cardiac targeting peptide (CTP), offer new opportunities for the enhanced delivery of a therapeutic payload to the injured heart. Their biodistribution can be effectively monitored using radiolabeled analogs. This review explores the role of peptide-based radiopharmaceuticals in nuclear cardiology, highlighting their applications in receptor-mediated imaging and briefly discussing non-receptor-specific CPPs. Select examples illustrate how these innovations are advancing molecular characterization of cardiovascular diseases such as fibrosis, cardiac amyloidosis, atherosclerosis, and more, reshaping the nuclear cardiology landscape.