Radiotheranostic Agents in Hematological Malignancies

Abstract

Radioimmunotherapy (RIT) is a cancer treatment that combines radiation therapy with tumor-directed monoclonal antibodies (Abs). Although RIT had been introduced for the treatment of CD20 positive non-Hodgkin lymphoma decades ago, it never found a broad clinical application. In recent years, researchers have developed theranostic agents based on Ab fragments or small Ab mimetics such as peptides, affibodies or single-chain Abs with improved tumor-targeting capacities. Theranostics combine diagnostic and therapeutic capabilities into a single pharmaceutical agent; this dual application can be easily achieved after conjugation to radionuclides. The past decade has seen a trend to increased specificity, fastened pharmacokinetics, and personalized medicine. In this review, we discuss the different strategies introduced for the noninvasive detection and treatment of hematological malignancies by radiopharmaceuticals. We also discuss the future applications of these radiotheranostic agents.

The Future of (Radio)‐Labeled Compounds in Research and Development within the Life Science Industry

“…By introduction of this leaving group selectively into pharmaceuticals by late-stage CÀ H functionalization, followed by palladium(II) catalyzed hydrogenation under non-inert atmosphere or dry conditions by tritium gas, the corresponding tritiated products were formed and isolated with high specific activity (26-27 Ci/mmol, > 90 % T). [60] Studer presented a mild metal-free method for the remote selective radical CH-monodeuteration of aliphatic CÀ H bonds in various amides with D 2 O as the deuterium source. The method applied the N-allylsulfonyl group as an N-radical precursor that generated the remote C-radical via site-selective 1,5-or 1,6-deuterium atom transfer (DAT).…”

“…Radiotheranostics differs from other cancer therapies in its capacity for simultaneous imaging and therapy. [57,58,59,60] This approach, also known as targeted radionuclide therapy (TRT), has shown promising results in the treatment of various types of cancer, including neuroendocrine tumors and prostate cancer. [61,62] 177 Lu-DOTA-TATE (Figure 5), a radiolabeled somatostatin analogue for neuroendocrine tumors, and 177 Lu-PSMA-617, targeting the prostate-specific membrane antigen (PSMA), are the most commonly used radiopharmaceuticals in theranostics, specifically in peptide receptor radionuclide therapy (PRRT).…”

“…Researchers have developed a wide range of radiolabeled therapeutic agents, such as radiolabeled peptides, antibodies and small molecules that can be used to selectively target and destroy cancer cells while sparing healthy cells. Radiotheranostics differs from other cancer therapies in its capacity for simultaneous imaging and therapy [57,58,59,60] . This approach, also known as targeted radionuclide therapy (TRT), has shown promising results in the treatment of various types of cancer, including neuroendocrine tumors and prostate cancer [61,62] .…”

Die Zukunft (Radio‐)‐isotopenmarkierter Verbindungen in Forschung und Entwicklung der modernen Lebenswissenschaften

“…Die Radiotheranostik unterscheidet sich von anderen Krebstherapien durch ihre Fähigkeit zur gleichzeitigen Bildgebung. [57,58,59,60] Dieser Ansatz, der auch als gezielte Radionuklidtherapie (targeted radionuclide therapy, TRT) bezeichnet wird, hat vielversprechende Ergebnisse bei der Behandlung verschiedener Krebsarten, einschließlich neuroendokriner Tumore und Prostatakrebs, gezeigt. [61,62] 177 Lu-DOTATATE (Abbildung 5), ein radioaktiv markiertes Somatostatin-Analogon für neuroendokrine Tumore, und 177 Lu-PSMA-617, das auf das prostataspezifische Membranantigen (PSMA) abzielt, sind die am häufigsten verwendeten Radiopharmazeutika in der Theranostik, insbesondere in der Peptidrezeptor-Radionuklidtherapie (PRRT).…”

“…B. radioaktiv markierte Peptide, Antikörper und kleine Moleküle, mit denen Krebszellen selektiv angegriffen und zerstört werden können, während gesunde Zellen geschont werden. Die Radiotheranostik unterscheidet sich von anderen Krebstherapien durch ihre Fähigkeit zur gleichzeitigen Bildgebung [57,58,59,60] . Dieser Ansatz, der auch als gezielte Radionuklidtherapie (targeted radionuclide therapy, TRT) bezeichnet wird, hat vielversprechende Ergebnisse bei der Behandlung verschiedener Krebsarten, einschließlich neuroendokriner Tumore und Prostatakrebs, gezeigt [61,62] .…”