Radioligand - Knowledge

514: 425:(SPECT) being the most common types of imaging. PET scans are often utilized after radioligand administration because of the ease of use, image accuracy, and non-invasive nature. While PET and SPECT scans function similarly when imaging radioligands, the main difference lies in the type of radiation used, with PET Scans utilizing positrons and SPECT utilizing gamma rays. When comparing the two modalities, PET offers much better image quality and high diagnostic proficiency, however, the high cost limits the overall availability as well as the short half-lives of the positron-emitting isotopes. Alternatively, SPECT imaging is more dynamic because of the lower cost burden and longer half-lives of single-photon emitters. With advances in technology came hybrid imaging that can combine PET, SPECT, 41: 32:

I-131, I-125, etc. Thus, radioligands must be produced in special nuclear reactors for the radioisotope to remain stable. Radioligands can be used to analyze/characterize receptors, to perform binding assays, to help in diagnostic imaging, and to provide targeted cancer therapy. Radiation is a novel method of treating cancer and is effective in short distances along with being unique/personalizable and causing minimal harm to normal surrounding cells. Furthermore, radioligand binding can provide information about receptor-ligand interactions in vitro and in vivo. Choosing the right radioligand for the desired application is important. The radioligand must be radiochemically pure, stable, and demonstrate a high degree of selectivity, and high affinity for their target.

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radioligand and displaying RIBE can show signs of stress, chromosomal abnormalities, or even experience cell death. However, the type of radiation used, whether 𝜶, β, or both can have a dramatically different effect on both the target binding site and surrounding tissue. Changes in nearby tissue is not the only possible impact of ligand therapy, there may be immunologic responses from the target tissue that cause changes remotely. This has been deemed, "abscopal effect". While this mechanism is not well understood, it explains the impact of other tissue, both benign and malignant, after targeted radiotherapy.

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and Pluvicto is shown in the chemical linkages in the images above. The production, transportation, and storage is the same as Lutathera. The therapy is administered intravenously through gravity, syringe, or a Peristaltic Infusion Pump. The major warnings include renal toxicity, infertility in males, and embryo/fetal harm. General side effects of this radioligand therapy include fatigue, nausea, dry mouth, anemia, decreased appetite, and constipation. Regular blood tests and imaging post-therapy are needed to see if the radioligand therapy is working and its side effects.

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https://www.google.com/url?q=https://www.novartis.com/news/media-releases/novartis-lutathera-significantly-reduced-risk-disease-progression-or-death-72-first-line-treatment-patients-advanced-gastroenteropancreatic-neuroendocrine-tumors%23:~:text%3DNovartis%2520Lutathera%25C2%25AE%2520significantly%2520reduced,advanced%2520gastroenteropancreatic%2520neuroendocrine%2520tumors%2520%257C%2520Novartis&sa=D&source=docs&ust=1711156056791112&usg=AOvVaw3xi8kIkSB6Qy7JxAsCXdIm

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it is better to produce Yb-176 through fission reactors. This is the indirect production method and requires elaborate radiochemical separation, purification, and results in large amounts of radioactive waste. The direct method of producing Lu-177 is by performing neutron irradiation on Lu-176 to Lu-177. This is an inexpensive and effective method to produce Lu-177. In the United States, the main place that Lu-177 is produced is the University of Missouri Research Reactor.

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interest will bind to the receptor with the expected affinity and potency even in the presence of a competitor. This experiment would also help determine if the radioligand will be able to recognize and bind to the correct receptor. Competitive binding experiments also serve to study the binding ability of a low-affinity drug, as it can be used as an unlabeled competitor. Finally, receptor number and affinity can also be determined through this experiment.

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reduce radiation toxicity to the organs - specifically the kidneys. The sites are separate to prevent radioactive contamination after therapy. The patient receives therapy by automated syringe, infusion pump, or gravity using long/short needles, tubing, and sodium chloride solution. Antiemetic (anti-nausea) medications or short/long acting octreotide (cancer growth control) can be used post-therapy for symptom management.

71:, first used nuclear medicine in humans came in 1936 after extensive use of radioactive phosphorus in mouse models. Often called the father of nuclear medicine, Lawrence treated a leukemia patient with radiophosphorus, which was the first time a radioactive isotope has been used to treat human patients. Another pioneer in the field, Sam Seidlin, in partnership with 401:(SPECT) for baseline comparison after radioligand administration. Once the radioligand is administered, the radioligand will travel to the target tissue and selectively bind. The structure of the compound allows clinicians to easily identify the path traveled and the destination via repeated imaging and the signal put out by the radiotracer attached to the ligand. 433:(MRI). Some hybrid imaging modalities include: SPECT/CT, PET/CT and PET/MRI. Although combined imaging presents both cost and availability barriers, the technology is an extremely useful diagnostic tool. Often, the patient does not have to be moved for both imaging types to be completed and the clinicians are provided with rich, multi-dimensional imaging. 380:. Ligands can be divided into two categories, agonists or antagonists. Agonists behave similarly to natural ligands, while antagonists are inhibitors and block the binding of the natural ligand. There are many different subtypes of agonists, including endogenous agonists, super agonist, full agonist, inverse agonist, and irreversible agonist. 1152:

Which is better, 177Lu-PSMA-617 (Pluvicto) or Xofigo (radium-223) — Cancer ABCs. (2022, September 14). Cancer ABCs. https://www.cancerabcs.org/advanced-prostate-cancer-blog/2022/8/29/which-is-better-177lu-psma-617-pluvicto-or-xofigo#:~:text=In%20summary%2C%20Xofigo%20only%20attacks,not%20all%20tumors%20express%20PSMA

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The most common side effects include decreased blood cell counts, increased liver enzymes, vomiting, nausea, increased blood glucose, and decreased blood potassium levels. Lutathera is not given to pregnant or breastfeeding individuals. The therapy shrinks tumors by an average of 30%, reduces disease

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in 1960. The use of radioligands and nuclear tagging started to gain popularity in in the early 1960s when Elwood Jensen and Herbert Jacobsen (1962) and later Jack Gorksi, David Toft, G, Shymala, Donald Smith, and Angelo Notides (1968) attempted to identify the estrogen receptor. The American Medical

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Pruis, I. J., van Doormaal, P. J., Balvers, R. K., van den Bent, M. J., Harteveld, A. A., de Jong, L. C., Konijnenberg, M. W., Segbers, M., Valkema, R., Verburg, F. A., Smits, M., & Veldhuijzen van Zanten, S. E. M. (2024). Potential of PSMA-targeting radioligand therapy for malignant primary and

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based PSMA studies that will be launched in 2024. If these prove successful, there is potential for further studies and clinical trials to be done using α-emitters. Additionally, there is potential for the future use of radioligand therapy in patients with malignant brain tumors. Finally, there have

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Lu-177 is produced by bombarding the stable isotope Yb-176 (which is found in monazite sand as well as the ores euxenite and xenotime) with neutrons. Yb-176 turns into Yb-177 which is unstable and has a half life of 1.9 hours so it quickly decays into the medical isotope Lu-177. For mass production,

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particles are both used in the treatment of cancers, depending on the size and location of the particular tumor. Alpha particles contain overall higher energy and have a shorter path length, and have greater cytotoxic properties for this reason as compared to β particles. However, due to the shorter

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experiments aim to determine the binding of a labeled radioligand at one specific concentration while subjected to various concentrations of a competitor, usually an unlabeled ligand. There are many purposes to competitive binding experiments, including being able to validate that the radioligand of

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Radioligands are administered through four main routes: intravenously, subcutaneous injection, intraperitoneally, and orally. While intravenous application is the most used route of injection, the route is dependent on the mechanism of action and overall aim of the binding. Before application of the

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For example, the PSMA radioligand therapy (Pluvicto) requires the patient to have end-stage prostate cancer that has metastasized in other organs, the PSMA ligand (confirmed through diagnostic imaging), and gone through hormonal therapies and chemotherapies. For patient eligibility to get Lutathera

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24 hours before and 14 days after administration, thyroid protective drugs and KI tablets are administered. I-131 and Tositumomab are administered separately over the course of 14 days intravenously by dosimetric and therapeutic doses. Side-effects include anemia, fever, rigors or chills, sweating,

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Xofigo, a radioligand therapy that was FDA approved in 2013, uses Radium-223 dichloride as the radioisotope, but its ligand varies from Pluvicto. Pluvicto only attacks cancer cells expressing PSMA, but Xofigo attacks all bone metastases. Qualified patients are 30% less likely to die when treated by

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Pluvicto also uses Lu-177 as the radioisotope (which is a beta emitter that decays to Hf-177) but its ligand is a prostate-specific membrane antigen (PSMA) targeted ligand as this radioligand therapy addresses metastatic prostate cancer. It was FDA approved in 2022. The difference between Lutathera

521:β particles emit lower energy as compared to α-emitters, but they have the advantage of having longer path length. However, due to their lower energy, more β particles are required to cause damage to tumor cells as compared to α-emitters. Some examples of β-emitters include Lu-177, Y-90, and I-131. 487:

Kinetic binding experiments differ from saturation and competition experiments in that they are not done at equilibrium. Instead, they measure the course of binding of the radioligand during the experiment as well as the dissociation to determine calculation of the Kd, and rate constants of binding

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Measuring the extent and kinetics of radioligand binding is important in determining information about binding sites of radioligands, and subsequent affinity to potential drugs. Three different binding assays are typically used for radioligand binding; these are saturation, competition, and kinetic

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In the future, radioligand therapy may expand to include more α-emitter based treatments. Currently, β radioligand therapies are more commonly used in oncology. Clinical trials of α-emitters are underway due to their higher potency and ability to induce double-strand DNA breaks. There are multiple

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Each radioligand therapy requires significant patient testing and eligibility requirements before administration. Radioligand therapies for cancer treatment are not the first course of action and generally require the patient to have undergone other previous treatments and many diagnostic imagings

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Bexxar, a radioligand therapy using the radioisotope I-131+Tositumomab (a murine monoclonal antibody) and binding/targeting the ligand CD20 on human B-cells. CD20 is a membrane spanning protein found on B-cell lymphocytes that is a tumor marker as it is in higher concentration in cancer patients -

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Once transported to the hospital or cancer treatment / oncology center, the patient is prepped, all necessary tests are done, and the patient requires two separate IV sites for infusion. One site for radioactive Lu-177 infusion and one site for amino acid infusion. Amino acid infusion is needed to

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Once produced, Lu-177 is stable for 72 hours if stored below room temperature. Freeze dried kits of Lutathera do show reduced effectiveness in radiation therapy but they maintain radiochemical purity. Lu-177 requires radiation shielding for handling. Lu-177 is stored and transported in a vial with

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Radioligands are made up of the radioisotope, linker, and ligand. This structure allows the compound to identify and bind to the target tissue while retaining the ability to be tracked and imaged clinically. When a radioligand binds to its target, it alters the microenvironment of the receptor and

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With radioligand therapy, there is always the risk of damage to non-cancerous surrounding tissues along with radioisotope toxicity which is always a challenge in determining how to administer and create the radioligand. Furthermore, the radioligand vial is only viable for a limited time and under

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is the target binding site, it may be on the surface of the targeted cancer cell for therapeutic purposes. Radioisotopes can occur naturally or be synthesized and produced in a cyclotron/nuclear reactor. The different types of radioisotopes include Y-90, H-3, C-11, Lu-177, Ac-225, Ra-223, In-111,

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is a peptide receptor radioligand/radionuclide therapy (approved by the FDA in 2018) specifically for patients with gastroenteropancreatic neuroendocrine tumors (GEP-NETs) that have somatostatin hormone receptors (SSTR). The radioisotope is Lu-177 and the ligand is a SSTR on the surface of tumor

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Fluorine-18 is used in PET imaging and radioligand diagnostics for the early detection of disease. Furthermore, since F-18 is a small lipophilic molecule, it can readily cross the blood brain barrier and be used in diagnostic imaging of glucose metabolism in the brain. Because it can bind to PET

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can cause tissue damage and hypoxia to tissues other than the target. While this effect is lessened in a target radiotracer therapy utilizing radioligands, there is still an impact on the surrounding tissue described as Radiation Induced Bystander Effect (RIBE). Surrounding cells altered by the

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Carbon-11 can be used to find neuroinflammation through PET imaging of a specific translocator protein that indicates neuroinflammation if found. C-11 can also be used for PET radioligand imaging of serotonin transporters in the primate/pig brain cortical regions. C-11 is also very unstable and

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Lutetium-177 PSMA therapy for prostate cancer (Pluvicto). (n.d.). Hospitals, Clinics & Doctors in IL - UChicago Medicine. https://www.uchicagomedicine.org/cancer/types-treatments/prostate-cancer/treatment/lutetium-177-psma-therapy-for-prostate-cancer#:~:text=Who%20is%20a%20candidate%20for

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Love, C., Desai, N. B., Abraham, T., Banks, K. P., Bodei, L., Boike, T., Brown, R. K., Bushnell, D. L., DeBlanche, L. E., Dominello, M. M., Francis, T., Grady, E. C., Hobbs, R. F., Hope, T. A., Kempf, J. S., Pryma, D. A., Rule, W., Savir-Baruch, B., Sethi, I., ... Schechter, N. R. (2022).

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Saturation binding measures the specific binding of a radioligand at varying concentrations while at equilibrium. Through this method, the number of receptors can be determined as well as affinity of the ligand to these receptors. Saturation binding experiments are often called "Scatchard

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Roohi S, Rizvi SK, Naqvi SAR. 177Lu-DOTATATE Peptide Receptor Radionuclide Therapy: Indigenously Developed Freeze Dried Cold Kit and Biological Response in In-Vitro and In-Vivo Models. Dose Response. 2021 Feb 12;19(1):1559325821990147. doi: 10.1177/1559325821990147. PMID 33628154; PMCID:

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Another limitation is the lack of centers that have trained personnel and equipment for radioligand therapy. Furthermore, individual characteristics affect the exact radiosensitivity to the therapy (thus affecting dosimetry) and are hard to predict without radiobiological models.

1059:(2024, March 18). SHINE Technologies | Illuminating the Path to Fusion Energy. https://www.shinefusion.com/blog/what-is-n-c-a-lutetium-177-lu177#:~:text=To%20produce%20n.c.a.%20Lu%2D177%2C%20we%20bombard%20highly%20pure%20ytterbium,it%20non%2Dcarrier%2Dadded 884:

Klose, J. M., Wosniack, J., Iking, J., Staniszewska, M., Zarrad, F., Trajkovic-Arsic, M., Herrmann, K., Costa, P. F., Lueckerath, K., & Fendler, W. P. (2022). Administration routes for SSTR-/PSMA- and FAP-directed Theranostitic Radioligands in mice.

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Crișan G, Moldovean-Cioroianu NS, Timaru DG, Andrieș G, Căinap C, Chiș V. Radiopharmaceuticals for PET and SPECT Imaging: A Literature Review over the Last Decade. Int J Mol Sci. 2022 Apr 30;23(9):5023. doi: 10.3390/ijms23095023. PMID 35563414; PMCID:

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Since the patient group receiving radioligand therapy is narrow, many health care providers are not equipped or eligible to administer radioligand therapy. PET imaging machines, a lead shielded area, and trained professionals must be available.

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Indium-111 is unstable and decays by electron capture to a stable cadmium-111. It can be used for planar SPECT imaging for diagnostic purposes and diagnostic imaging of the presence of somatostatin receptors on various neuroendocrine tumors.

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Negus SS. Some implications of receptor theory for in vivo assessment of agonists, antagonists and inverse agonists. Biochem Pharmacol. 2006 Jun 14;71(12):1663-70. doi: 10.1016/j.bcp.2005.12.038. Epub 2006 Feb 7. PMID 16460689; PMCID:

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Ytrium-90 can be used for internal radiation therapy to diagnose liver metastases. Y-90 emits the highest amount of beta radiation energy and can be used as radioligand therapy for B-cell non-Hodgkin Lymphoma or pancreatic cancer.

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radioligand therapy the patient must have disease progression despite receiving somatostatin analog therapy (octreotide or lanreotide), have a locally advanced, inoperable, or metastatic well-differentiated disease, and have an

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I-131 is produced by nuclear fission or through neutron irradiation of Te-130 to convert it to Te-131 which decays to I-131 (produced in the University of Missouri Research Reactor). I-131 is stored in lead-shielding vials.

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Friedberg, J. W., & Fisher, R. I. (2004). Iodine-131 tositumomab (Bexxar): Radioimmunoconjugate therapy for indolent and transformed B-cell non-Hodgkin's lymphoma. Expert Review of Anticancer Therapy, 4(1), 18-26.

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was established in 1972. Progress came quickly in 1973 when Edward Hoffman, Michael M. Ter-Pogossian, and Michael E. Phelps invented the first PET camera for human use. The 1980s brought early radioligand studies for

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Haffner, R., Miller, W. H., & Morris, S. (2019). Verification of I-131yields from the neutron irradiation of tellurium. Applied Radiation and Isotopes, 151, 52-61. https://doi.org/10.1016/j.apradiso.2019.05.001

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NOVARTIS. (2024, January 19). Novartis Lutathera significantly reduced risk of disease progression or death by 72% as first-line treatment for patients with advanced gastroenteropancreatic neuroendocrine tumors.

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Herrera FG, Bourhis J, Coukos G. Radiotherapy combination opportunities leveraging immunity for the next oncology practice. CA Cancer J Clin. 2017 Jan;67(1):65-85. doi: 10.3322/caac.21358. Epub 2016 Aug 29. PMID

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hypotension, dyspnea, bronchospasm, and nausea. There is a risk of radiation exposure to other individuals (women/children/fetus), anaphylaxis, neutropenia (low neutrophils), and thrombocytopenia (low platelet).

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Hofman, M. S., Lau, W. F., & Hicks, R. J. (2015). Somatostatin receptor imaging with<sup>68</sup>Ga DOTATATE PET/CT: Clinical utility, normal patterns, pearls, and pitfalls in interpretation.

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Shah, H. J., Ruppell, E., Bokhari, R., Aland, P., Lele, V. R., Ge, C., & McIntosh, L. J. (2023). Current and upcoming radionuclide therapies in the direction of precision oncology: A narrative review.

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Hennrich, U., & Eder, M. (2022). Lu-PSMA-617 (PluvictoTM): The first FDA-approved Radiotherapeutical for treatment of prostate cancer. Pharmaceuticals, 15(10), 1292. https://doi.org/10.3390/ph15101292

1103:. LUTATHERA (lutetium Lu 177 dotatate) | GEP-NET Treatment. https://www.us.lutathera.com/side-effects/understanding-side-effects/#:~:text=The%20most%20common%20and%20most,any%20of%20these%20side%20effects 151:

Iodine-123 is preferred for diagnostic/imaging, especially for the thyroid as it has a short half life (13 hrs) and can clearly show the thyroid’s uptake of iodine with lower radiation energy than I-131.

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National Cancer Institute. FDA Approves New Treatment for Certain Neuroendocrine Tumors. Available from: https://www.cancer.gov/news-events/cancer-currents-blog/2018/lutathera-fda-gastrointestinal-nets

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Iodine-131 is used as a part, along with a urea based ligand MIP-1095 that binds specifically to the prostate membrane, of a radioligand therapy in clinical trials for metastatic prostate cancer.

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Obaldo JM, Hertz BE. The early years of nuclear medicine: A Retelling. Asia Ocean J Nucl Med Biol. 2021 Spring;9(2):207-219. doi: 10.22038/aojnmb.2021.55514.1385. PMID 34250151; PMCID: PMC8255519.

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The most common uses of Iridium-192 are: cervical cancer, head and neck cancer, and prostate cancer. Ir-192 can also be used in the radionuclide therapy called high-dose rate brachytherapy.

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Miller EJ, Lappin SL. Physiology, Cellular Receptor. . In: StatPearls . Treasure Island (FL): StatPearls Publishing; 2024 Jan-. Available from: https://www.ncbi.nlm.nih.gov/books/NBK554403/

459: 1019:(pp. 4–12) . GraphPad Software, Inc. Retrieved March 22, 2024, from https://www.chem.uwec.edu/chem491_w01/Pharmacognosy%20491/%20aaa%20Daily%20Lectures/Lecture%20%202/radiolig.pdf 488:

and dissociation. Kinetic binding experiments are also called dissociation binding experiments and can help evaluate the interaction of the radioligand and the targeted receptor.

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surrounding tissue, partially due to the structure of the radioligand itself. Without both the high affinity ligand and the radioisotope, the efficiency of this process is lost.

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is a molecule utilized for cell-signaling that binds to a target tissue for cellular communication. There are many different types of ligands including: internal receptors,

93:(NETs) which continued into the early 2000s. In 2017 the European Union (EU) approved the use of radioligand therapy for NETs with the U.S. following close behind in 2018. 510:

exist which consist of alpha emitters attached to carrier molecules. Some examples of alpha-emitting radioligands include actinium-225, Ra-223-chloride, and Lead-212.36

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Health system readiness for radioligand therapy in the US. (2021, November). The Health Policy Partnership. https://www.healthpolicypartnership.com/?s=radioligand

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Xe-133 is an inert gas that, along with CO2, can be inhaled to provide diagnostic information on the lung in adults and neonates using SPECT or nuclear imaging.

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Iodine-125 is used in nuclear medicine for biological assays, as iso seeds for localized prostate cancer, and as internal radiation brachytherapy for cancers.

75:, treated a case of thyroid cancer with radioactive iodine (I-131) 1946. In the 1950s, nuclear medicine began to gain traction as a medical specialty with the 582:

The benefits of Pluvicto include delaying tumor growth, extending life by about 20 months, and destroying tumor cells by damaging the DNA inside those cells.

1034:. (2017, April 12). What's New in GU?; What's New in GU? https://weillcornellgucancer.org/2017/04/12/using-alpha-and-beta-radioisotopes-to-kill-cancer-cells/ 554:

lead/plexiglass shielding ready-to-use. Repeated production, timely delivery, and quick administration are important so that the therapy remains effective.

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US Department of Energy – Molecular Nuclear Medicine Legacy. History of PET and MRI. Available from: https://www.doemedicalsciences.org/historypetmri.shtml

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been recent developments in diagnostic tracers using radioligands, as well as with radioligand-based imaging techniques and in the field of theranostics.

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secondary brain tumours using super-selective intra-arterial administration: A Single Centre, open label, non-randomised prospective Imaging Study.

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Gorski, J., Toft, D., Shyamala, G., Smith, D., & Notides, A. (1968). Hormone receptors: studies on the interaction of estrogen with the uterus.

762:. (2023, June 30). PerkinElmer Blog. https://blog.perkinelmer.com/posts/radioligand-binding-assays-from-opiate-receptors-to-drug-discovery-mainstay/ 935:

Herrera, F. G., Bourhis, J., & Coukos, G. (2016). Radiotherapy combination opportunities leveraging immunity for the next oncology practice.

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path length of these particles, the method of delivery needs to be extremely close to the location of the tumor. Currently, treatments using

1047:. ASCO Daily News. https://dailynews.ascopubs.org/do/novel-drug-delivery-systems-patients-advanced-prostate-cancer-focus-radioligand-therapy 1171:

NCI Dictionary of cancer terms. (n.d.). National Cancer Institute. https://www.cancer.gov/publications/dictionaries/cancer-terms/def/cd20

422: 398: 1006:. UNC School of Medicine. http://www.pdg.cnb.uam.es/cursos/Barcelona2002/pages/Farmac/Comput_Lab/Radioligandos/Mailman_Boyer/index.htm 962:

Van der Meulen, N. P., Strobel, K., & Lima, T. V. (2021). New radionuclides and technological advances in SPECT and PET scanners.

649:(i.e. seeing if specific receptors/antigens exist) to determine the benefit vs. adverse effect of undergoing the radioligand therapy. 1220:. GU Oncology Now. https://guoncologynow.com/post/looking-ahead-what-does-the-future-hold-for-radioligand-therapy-in-prostate-cancer 1142:

https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-pluvicto-metastatic-castration-resistant-prostate-cancer

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Hydrogen-3 is used for in vitro radioligand binding analysis of brain tissue and competition/saturation radioligand binding assays.

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FDA. (2022, March 23). FDA approves Pluvicto for metastatic castration-resistant prostate can. U.S. Food and Drug Administration.

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Strontium-89 is used as a radioligand therapy for bone cancers to relieve bone pain as Sr-89 is easily absorbed in osseous tissue.

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SEIDLIN SM, MARINELLI LD, OSHRY E. RADIOACTIVE IODINE THERAPY: Effect on Functioning Metastases of Adenocarcinoma of the Thyroid.

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imaging ligands, it is used for detecting amyloid aggregation which indicates progression of Alzhiemer’s disease in brain tissue.

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Haberkorn, U., Giesel, F., Morgenstern, A., & Kratochwil, C. (2017). The future of Radioligand therapy: α, β, or both?

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Radium-223 is a calcimimetic specifically used for advanced metastatic prostate cancer or B-cell non-hodgkin’s lymphoma.

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Depiction of a Scatchard plot with relation to number of binding sites, Bmax, and equilibrium dissociation constant Kd.

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Novel Drug Delivery Systems for Patients with Advanced Prostate Cancer: A focus on Radioligand Therapy and ADCs

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specific conditions which challenges transport and storage along with feasible application to the patient.

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Schematic illustrating the differences in path length and intensity of alpha, beta, gamma, and x-rays

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Lutetium-177 is utilized for advanced metastatic prostate cancer or B-cell non-hodgkin’s lymphoma

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Iodine-131 tositumomab (Bexxar) and Zevalin (90Y-ibritumomab tiuxetan) for non-Hodgkin's lymphoma

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Holdgate, G. (2017). Kinetics, thermodynamics, and ligand efficiency metrics in drug discovery.

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Xofigo than if treated by a placebo. Ra-223-chloride is an alpha-emitting bone targeting agent.

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Association (AMA) officially recognized Nuclear Medicine as a medical specialty in 1970 and the

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Downer, J. B. (2000). Lawrence, John Hundale (1904-1991), pioneer in nuclear medicine.

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Radioactive biochemical substance used for diagnosis or for study of receptor systems

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Looking ahead: What does the future hold for Radioligand Therapy in prostate cancer?

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ACR-ACNM-ASTRO-SNMMI practice parameter for lutetium-177 (Lu-177) DOTATATE therapy.

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Imaging is a useful tool in visualization of the radioligand after injection, with

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Bylund, D. B., & Enna, S. (2018). Receptor binding assays and drug discovery.

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is credited with the discovery of radioactivity in 1895 with many others such as

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CD20 ligand but using Yttrium-90 as the radioisotope, was FDA approved in 2002.

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https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/125011s0126lbl.pdf

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Radioligand binding assays: From opiate receptors to drug discovery mainstay

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Example of monoclonal antibody (Rituximab) binding to CD20 on B-Cell Surface

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https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/215833s000lbl.pdf

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following closely behind to further advance the field of radioactivity.

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Morris, M., Dorff, T., Yu, E., & McKay, R. (2023, November 16).

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specifically leukemias or lymphomas (like non-hodgkin's lymphoma).

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THEORY AND PRACTICE OF RECEPTOR CHARACTERIZATION AND DRUG ANALYSIS

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1946;132(14):838–847. doi:10.1001/jama.1946.02870490016004

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forming in 1954 and later releasing the first copy of the

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Fundamentals of Receptor, Enzyme, and Transport Kinetics

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The GraphPad Guide to Analyzing Radioligand Binding Data

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Using Alpha and Beta Radioisotopes to Kill Cancer Cells

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ligand, clinicians will perform imaging, generally via

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progression by 72%, and delays the growth of tumors.

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Recent Progress in Hormone Research (ed. EB Astwood)

810:, 21-34. https://doi.org/10.1016/bs.apha.2017.08.007 1043:McKay, R. R., & Hope, T. A. (2022, August 17). 970:(24), 6183. https://doi.org/10.3390/cancers13246183 387: 988:(2), 500-516. https://doi.org/10.1148/rg.352140164 624: 27:and the cell-targeting compound - the ligand. The 1101:Lutathera (lutetium Lu 177 dotatate) side effects 1296: 682: 356:Rendering of a G-Protein coupled receptor (GPCR) 44:Depiction of Wilhelm Roentgen observing an X-ray 1002:Mailman, R., & Boyer, J. (1997, July 31). 943:(1), 65-85. https://doi.org/10.3322/caac.21358 23:is a microscopic particle which consists of a 1238:. https://doi.org/10.1016/j.ebiom.2024.105068 644:Depiction of ECOG Performance scale ratings 617:, another radioligand therapy that targets 524: 491: 423:Single Photon Emission Computed Tomography 399:Single Photon Emission Computed Tomography 451:experiments" as they can be graphed as a 661:Hospital requirements and staff training 639: 597: 573: 540: 512: 457: 351: 39: 1162:https://doi.org/10.1586/14737140.4.1.18 566:Pluvicto and Xofigo for prostate cancer 1297: 635: 470: 1084:American Journal of Clinical Oncology 1067: 1065: 1057:What is n.c.a. lutetium-177 (Lu-177)? 1027: 1025: 998: 996: 994: 907:Comprehensive Medicinal Chemistry III 657:(ECOG) performance status of 0 to 2. 445: 69:The University of California Berkeley 937:CA: A Cancer Journal for Clinicians 530:Lutathera for neuroendocrine tumors 13: 1262: 1250:European Journal of Radiology Open 1062: 1022: 991: 782:American National Biography Online 655:Eastern Cooperative Oncology Group 482: 404:Direct radiotherapy performed via 97:Radioactive isotopes commonly used 86:American Board of Nuclear Medicine 14: 1326: 436: 412: 388:Use in drug delivery and release 1241: 1223: 1210: 1201: 1192: 1183: 1174: 1165: 1155: 1146: 1134: 1125: 1116: 1106: 1093: 1075: 1050: 1037: 1009: 973: 956: 946: 929: 912: 899: 878: 868: 858: 849: 625:Requirements for administration 25:therapeutic radioactive isotope 1305:Biochemistry detection methods 839: 830: 813: 800: 787: 774: 765: 753: 729: 669: 578:Chemical structure of Pluvicto 1: 723: 683:Future potential applications 271:Gamma radiation - low energy 258:decays into stable Boron-11. 419:Positron Emission Tomography 395:Positron Emission Tomography 7: 920:Journal of Nuclear Medicine 696: 374:G-Protein Coupled Receptors 81:Journal of Nuclear Medicine 77:Society of Nuclear Medicine 10: 1331: 628: 545:Skeletal formula of Lu-177 431:Magnetic Resonance Imaging 347: 100: 35: 221:Beta and gamma emissions 808:Advances in Pharmacology 718:Radioactivity in biology 525:Oncological applications 492:Alpha and beta particles 103:Radioactivity in biology 1099:NOVARTIS. (2023, May). 378:enzyme-linked receptors 319:Imagable gamma photons 53:Antoine Henri Becquerel 645: 603: 579: 546: 518: 467: 366:cell-surface receptors 357: 45: 1270:John Charles Matthews 1015:Motulsky, H. (n.d.). 737:"Radioligand Therapy" 643: 629:Further information: 601: 577: 544: 516: 461: 370:Ion-channel receptors 355: 91:neuroendocrine tumors 43: 619:non-Hodgkin lymphoma 185:Beta positive decay 890:of Nuclear Medicine 708:Distribution volume 636:Patient eligibility 631:radioligand therapy 476:Competitive binding 471:Competition binding 427:Computed Tomography 646: 604: 580: 547: 519: 468: 446:Saturation binding 406:ionizing radiation 358: 254:Positron emission 237:pure beta emitter 187:Positron emission 46: 703:Binding potential 345: 344: 280:Hydrogen-3 (H-3) 67:, a physicist at 1322: 1291: 1257: 1245: 1239: 1227: 1221: 1214: 1208: 1205: 1199: 1196: 1190: 1187: 1181: 1178: 1172: 1169: 1163: 1159: 1153: 1150: 1144: 1138: 1132: 1129: 1123: 1120: 1114: 1110: 1104: 1097: 1091: 1079: 1073: 1069: 1060: 1054: 1048: 1041: 1035: 1029: 1020: 1013: 1007: 1000: 989: 977: 971: 960: 954: 950: 944: 933: 927: 916: 910: 903: 897: 882: 876: 872: 866: 862: 856: 853: 847: 843: 837: 834: 828: 817: 811: 804: 798: 791: 785: 778: 772: 769: 763: 757: 751: 750: 748: 747: 733: 321:Beta particles 107: 106: 49:Wilhelm Roentgen 1330: 1329: 1325: 1324: 1323: 1321: 1320: 1319: 1295: 1294: 1288: 1265: 1263:Further reading 1260: 1246: 1242: 1228: 1224: 1215: 1211: 1206: 1202: 1197: 1193: 1188: 1184: 1179: 1175: 1170: 1166: 1160: 1156: 1151: 1147: 1139: 1135: 1130: 1126: 1121: 1117: 1111: 1107: 1098: 1094: 1080: 1076: 1070: 1063: 1055: 1051: 1042: 1038: 1030: 1023: 1014: 1010: 1001: 992: 978: 974: 961: 957: 951: 947: 934: 930: 926:(7), 1017-1018. 917: 913: 904: 900: 883: 879: 873: 869: 863: 859: 854: 850: 844: 840: 835: 831: 818: 814: 805: 801: 792: 788: 779: 775: 770: 766: 758: 754: 745: 743: 735: 734: 730: 726: 713:PET radiotracer 699: 685: 672: 663: 638: 633: 627: 592: 568: 532: 527: 494: 485: 483:Kinetic binding 473: 448: 439: 415: 390: 350: 303:Beta radiation 286:Beta radiation 165:Beta particles 105: 99: 38: 17: 12: 11: 5: 1328: 1318: 1317: 1312: 1307: 1293: 1292: 1286: 1264: 1261: 1259: 1258: 1240: 1222: 1209: 1200: 1191: 1182: 1173: 1164: 1154: 1145: 1133: 1124: 1115: 1105: 1092: 1074: 1061: 1049: 1036: 1021: 1008: 990: 972: 955: 945: 928: 911: 898: 877: 867: 857: 848: 838: 829: 812: 799: 786: 773: 764: 752: 727: 725: 722: 721: 720: 715: 710: 705: 698: 695: 684: 681: 671: 668: 662: 659: 637: 634: 626: 623: 591: 588: 567: 564: 531: 528: 526: 523: 508:alpha-emitters 493: 490: 484: 481: 472: 469: 453:Scatchard plot 447: 444: 438: 437:Binding assays 435: 414: 413:Use in imaging 411: 389: 386: 349: 346: 343: 342: 339: 338:Alpha emitter 336: 333: 327: 326: 323: 317: 314: 308: 307: 304: 301: 298: 291: 290: 287: 284: 281: 277: 276: 272: 269: 266: 260: 259: 255: 252: 249: 243: 242: 238: 235: 232: 226: 225: 222: 219: 216: 210: 209: 206: 203: 200: 194: 193: 189: 183: 182:109.7 minutes 180: 174: 173: 169: 163: 160: 154: 153: 149: 146: 143: 137: 136: 133: 130: 127: 121: 120: 117: 114: 111: 101:Main article: 98: 95: 37: 34: 15: 9: 6: 4: 3: 2: 1327: 1316: 1313: 1311: 1308: 1306: 1303: 1302: 1300: 1289: 1287:0-8493-4426-3 1283: 1279: 1275: 1271: 1267: 1266: 1255: 1251: 1244: 1237: 1233: 1226: 1219: 1213: 1204: 1195: 1186: 1177: 1168: 1158: 1149: 1143: 1137: 1128: 1119: 1109: 1102: 1096: 1089: 1085: 1078: 1068: 1066: 1058: 1053: 1046: 1040: 1033: 1028: 1026: 1018: 1012: 1005: 999: 997: 995: 987: 983: 982:RadioGraphics 976: 969: 965: 959: 949: 942: 938: 932: 925: 921: 915: 908: 902: 895: 891: 888: 881: 871: 861: 852: 842: 833: 826: 822: 816: 809: 803: 796: 790: 783: 777: 768: 761: 756: 742: 738: 732: 728: 719: 716: 714: 711: 709: 706: 704: 701: 700: 694: 691: 680: 676: 667: 658: 656: 650: 642: 632: 622: 620: 616: 612: 608: 600: 596: 587: 583: 576: 572: 563: 559: 555: 551: 543: 539: 536: 522: 515: 511: 509: 504: 500: 499: 489: 480: 477: 466: 465: 460: 456: 454: 443: 434: 432: 428: 424: 420: 410: 407: 402: 400: 396: 385: 381: 379: 376:(GPCRs), and 375: 371: 367: 363: 354: 340: 337: 334: 332: 329: 328: 324: 322: 318: 315: 313: 310: 309: 305: 302: 299: 296: 293: 292: 288: 285: 282: 279: 278: 273: 270: 267: 265: 262: 261: 256: 253: 250: 248: 245: 244: 239: 236: 233: 231: 228: 227: 223: 220: 217: 215: 212: 211: 207: 204: 201: 199: 196: 195: 190: 188: 184: 181: 179: 176: 175: 170: 168: 164: 161: 159: 156: 155: 150: 147: 144: 142: 139: 138: 134: 131: 128: 126: 123: 122: 118: 116:Ray Emission 115: 112: 110:Radioisotope 109: 108: 104: 94: 92: 87: 82: 78: 74: 70: 66: 65:John Lawrence 62: 58: 54: 50: 42: 33: 30: 26: 22: 1310:Biomolecules 1273: 1253: 1249: 1243: 1235: 1232:eBioMedicine 1231: 1225: 1217: 1212: 1203: 1194: 1185: 1176: 1167: 1157: 1148: 1136: 1127: 1118: 1108: 1100: 1095: 1087: 1083: 1077: 1056: 1052: 1044: 1039: 1031: 1016: 1011: 1003: 985: 981: 975: 967: 963: 958: 948: 940: 936: 931: 923: 919: 914: 906: 901: 893: 889: 886: 880: 870: 860: 851: 841: 832: 824: 820: 815: 807: 802: 794: 789: 781: 776: 767: 759: 755: 744:. 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