Selected Auger Electron-Emitting Radionuclides for Therapeutic Nuclear Medicine
Auger electron-emitting radionuclides offer innovative therapeutic potential through highly localised DNA damage with minimal collateral effects.
The landscape of medical radiotherapeutics is rapidly evolving, showcasing a multitude of innovative treatments that target specific cancers and related symptoms with unprecedented precision. Utilising various radionuclides, these therapies represent a new frontier in the fight against cancer, offering hope for more effective and personalised treatment options.
Central to this advancement is the use of Actinium-225 (Ac-225), an alpha-emitting radionuclide, in a range of promising therapies. Alpha particles, with their high energy and short range, are effective in destroying cancer cells while minimising collateral damage to surrounding healthy tissues.
For instance, Ac-225-DOTA-SP targets Substance P receptors in glioblastoma, a notably aggressive brain tumour, delivering alpha radiation directly to the tumour site. This targeted approach is echoed in Ac-225-DOTA-YS5 and Ac-225-FPI-2265, both aimed at treating prostate cancer through different mechanisms. Ac-225-DOTA-YS5 targets CD46 using monoclonal antibody IgG1, whereas Ac-225-FPI-2265 focuses on the Prostate-Specific Membrane Antigen (PSMA) with PSMA-I&T.
The targeting of neuroendocrine tumours (NETs) has also seen significant developments with agents like Ac-225-DOTATOC and Ac-225-RYZ101, which focus on somatostatin receptors, delivering alpha radiation precisely to tumour cells. Further, Ac-225-DOTAZOL for bone pain palliation in patients with bone metastases exemplifies the versatility of radiotherapeutics, directly targeting bone tissues to provide pain relief.
Beyond alpha emitters, beta-emitting radionuclides like Yttrium-90 (Y-90) and Lutetium-177 (Lu-177) are also making strides in radiotherapeutics. Y-90 is employed in treating hepatocellular carcinoma and non-Hodgkin’s lymphoma, while Lu-177 is used in therapies for prostate cancer and neuroendocrine tumours.
Expanding the repertoire, treatments like At-211-81C6 mAb (Neuradiab) target brain cancer by using Astatine-211, another alpha emitter, conjugated with the monoclonal antibody 81C6. Similarly, At-211-MABG, targeting adrenergic tissues, is being developed for conditions like paragangliomas and pheochromocytoma.
Furthermore, Radium-223 (Ra-223) in Radium Dichloride therapy stands out for its application in bone pain palliation, particularly for metastatic prostate cancer. This therapy mimics calcium and selectively targets bone metastases, delivering alpha radiation.
The field also sees the development of therapies like Iodine-131 (I-131) in various forms, such as I-131-Apamistamab (Iomab-Bâ„¢) for acute lymphoblastic leukaemia and Hodgkin’s lymphoma and I-131-Metuximab for hepatocarcinoma. Each of these I-131-based therapies leverages the beta radiation emitted by I-131 to target specific cancer cells.
In conclusion, the diversity of radiotherapeutics, from alpha and beta emitters to different targeting mechanisms, underscores the remarkable progress in this field. These therapies are advancing and redefining cancer treatment, offering more precise, effective, and patient-tailored options. As research and clinical trials continue, these groundbreaking developments in radiotherapeutics are poised to significantly impact the future of cancer therapy.
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Auger electron-emitting radionuclides offer innovative therapeutic potential through highly localised DNA damage with minimal collateral effects.
Beta particle emitting radionuclides are utilised in therapeutic nuclear medicine for precise tumour targeting and improved treatment outcomes.
Alpha particle emitting radionuclides are highly effective in delivering targeted radiation therapy for various cancers.
Yttrium-90 Citrate delivers targeted beta radiation, effectively treating synovial hypertrophy while minimising extra-articular radioactive escape risks.
Yttrium-90 microspheres therapy utilises brachytherapy to treat liver cancer, offering precise tumour targeting and extended survival.
Yttrium-90 IsoPet provides localised cancer treatment by polymerising into a lattice, trapping radioactive microspheres within tumour tissues.
Yttrium-90 DOTALAN delivers targeted beta radiation to somatostatin receptor-expressing tumours, treating neuroendocrine neoplasms effectively.
Yttrium-90 labelled humanised anti-Tac is a monoclonal antibody designed for targeted radioimmunotherapy.
Yttrium-90 Carbon Microspheres offer advanced therapy for liver tumours, enhancing survival rates while ensuring precise radiation delivery.
Yttrium-90 BetaGlue utilises polymerising microspheres to deliver precise brachytherapy, enhancing tumour control and improving patient outcomes.
Yttrium-90 Basiliximab combines targeted immunotherapy and radiotherapy, selectively attacking CD25-positive tumours with high therapeutic precision.
Thorium-227 Pelgifatamab utilises PSMA targeting and alpha emissions to destroy cancer cells while sparing healthy tissue effectively.
Thorium-227 Epratuzumab combines alpha-emitting thorium with CD-22 targeting epratuzumab, offering precision treatment for lymphoma patients.
Strontium-89 Chloride Therapy delivers targeted beta emissions to osteoblastic lesions, often reducing malignant bone pain substantially.
Tin-117m HTC is a novel therapeutic radiopharmaceutical designed for targeted arthritis treatment using conversion electron brachytherapy technology.
Samarium-153 Oxabiphor targets osteoblastic lesions, delivering therapeutic beta radiation to relieve pain and improve quality.
Samarium-153 Lexidronam remains a reliable radiopharmaceutical delivering targeted beta radiation, alleviating painful metastases in suitable patients.
Rhenium-SCT®: Innovative, precise, non-surgical therapy for non-melanoma skin cancer, ensuring safe and effective outcomes.
Rhenium-186 Nano Liposomes deliver targeted beta radiation directly to tumours, minimising surrounding tissue damage.
Rhenium-186 Colloidal Sulfide is a reliable treatment for medium-sized joint inflammation through targeted beta radiation.
Rhenium-186 Etidronate, a radiopharmaceutical, delivers beta radiation to metastatic bone lesions, effectively reducing cancer-related pain.
Radium-224 RadSpherin utilises biodegradable calcium carbonate microparticles for precise alpha radiation delivery targeting metastatic cancer cells.
Ankylosing Spondylitis is a progressive inflammatory condition targeting the spine, leading to chronic pain and joint fusion.
Radium-223 Dichloride is a groundbreaking alpha-emitting radiopharmaceutical offering significant survival benefits for metastatic prostate cancer patients.
Lead-212 DOTAM-GRPR1 combines targeted GRPR binding with alpha radiation, offering innovative treatment for resistant cancers.
Lead-212 ADVC001 offers innovative alpha-emitting therapy, targeting PSMA-positive mCRPC with precise and potent tumour eradication.
32P-Sodium Phosphate effectively reduces metastatic bone pain while managing Polycythaemia Vera, enhancing patient quality of life.
Pancreatic cancer treatment has advanced significantly with the introduction of OncoSil brachytherapy for pancreatic cancer therapy.
Intraoperative Avidination Radionuclide Treatment utilises avidin-biotin technology to deliver targeted tumour radiation therapy.
Iodine-131 Weimeisheng revolutionises advanced lung cancer treatment by combining targeted monoclonal antibody precision with beta radiation for improved outcomes.
Peptide Receptor Radionuclide Therapy utilises radiopharmaceuticals to target somatostatin receptor-expressing tumours, improving treatment outcomes significantly.