Antibody-Based Therapies
David E. Thurston, Ilona Pysz in Chemistry and Pharmacology of Anticancer Drugs, 2021
Developed by GSK and approved in 2003, 131I-tositumomab (BexxarTM) is a murine IgG2a anti-CD20 antibody linked to an Iodine-131 atom covalently attached to an aromatic ring (Figure 7.39). Iodine-131 emits both beta and gamma radiation and has a relatively short half-life of 8 days. Structure of the CD20-targeted radioimmunoconjugate 131I-tositumomab (BexxarTM) (Figure from Hess C., Venetz D., and Neri D., Emerging classes of armed antibody therapeutics against cancer. Med. Chem. Commun., 2014, 5, 408. DOI: 10.1039/c3md00360d. Copyright © The Royal Society of Chemistry 2014).
Radiochemistry of Therapeutic Radionuclides
David M. Goldenberg in Cancer Therapy with Radiolabeled Antibodies, 1995
Table 1 lists some of the isotopes most commonly suggested for RAIT purposes, and includes α- and β-particle emitters, and isotopes which give rise to intense secondary radiation, the Auger electron emitters. Iodine-131 (131I) has been the isotope most utilized in clinical and preclinical RAIT studies, and the chemical aspects of its use will be discussed in this chapter. Such is this isotope’s pre-eminence in RAIT studies that references to it will be found throughout this volume. 131Iodine is a β-emitter, as are the useful isotopes of yttrium and rhenium. The latter two, along with the 212Pb/212Bi pair, merit discussion in greater detail in succeeding chapters, due to the amount of work which has been performed with these isotopes. The rhenium and yttrium isotopes have been developed as second-generation RAIT agents to replace 131I, because one of the perceived weaknesses of 131I as a RAIT agent is the isotope’s suboptimal radiophysical decay properties. 131I has a low- to medium-energy β-emission, which is somewhat compromised by a high abundance, high energy γ-emission (364 keV, 81% abundant), and this results in high nontarget organ irradiation during the MoAb localization phase. All the other isotopes in Table 1, including the well-studied yttrium and rhenium isotopes, are really candidates to replace and improve upon 131I.
Radiochemical Processing of Activated Targets
Frank Helus, Lelio G. Colombetti in Radionuclides Production, 2019
A review of the processing of targets used in the production of radioiodine isotopes will be instructive because it illustrates the application of many of the principles which have been touched upon. Iodine-131 can be produced in a reactor as a result of fission of 235U or by neutron activation of 130Te. In the latter case, the directly produced 131Te rapidly decays to 131I.47,48 Similarly, in the production of 123I using an accelerator either the 124Te(p,2n)123I or the 122Te(d,n)123I nuclear reaction can be used.2-5 In the last three nuclear production schemes a tellurium target is used to produce the desired radioiodine product. In all cases, the radiochemical processing methods are remarkably similar.
New frontier radioiodinated probe based on in silico resveratrol repositioning for microtubules dynamic targeting
Published in International Journal of Radiation Biology, 2023
Ashgan F. Mahmoud, Mohamed H. Aboumanei, Walaa Hamada Abd-Allah, Mohamed M. Swidan, Tamer M. Sakr
The most prominent criteria in radio-theranostics design are the prober selection of a drug with high affinity to the target organ and indeed the convenient radionuclides to be laden on it (Essa et al. 2015; Ibrahim et al. 2015; Al-Wabli et al. 2016; Swidan et al. 2019). Firstly, the molecular modeling study of the radioiodinated resveratrol had showed a good affinity toward β-tubulin binding site in the microtubules domain system with an appropriate binding energy (−34.46 kca/mol). This criterion was further enlightened through the in vivo distribution study in tumor models which showed high accumulation and retention in the tumor lesion. On the other hand, the radioactive iodine [131I] was selected for the radiolabeling process due to its convenient physical and decay characteristics. The radioactive iodine [131I], half-life ≈ 8 days, is considered as one of the most suitable radionuclides for radio-theranostics procedures due to its dual decay mode (10% gamma decay which utilized in the diagnosis while 90% beta decay which utilized in therapeutic application) (Sheikh et al. 2017; Sakr et al. 2018). So, the 131I-radioiodinated resveratrol preparation as a theranostic probe had successfully achieved the criteria mentioned above. From the molecular biology point of view, tracking of the microtubules dynamics is significantly help the physicians with soulful amelioration in the early detection of any abnormal modifications arisen during the cellular division such as tumor cell progression.
Modeling principles of protective thyroid blocking
Published in International Journal of Radiation Biology, 2022
Alexis Rump, Stefan Eder, Cornelius Hermann, Andreas Lamkowski, Manabu Kinoshita, Tetsuo Yamamoto, Junya Take, Michael Abend, Nariyoshi Shinomiya, Matthias Port
Nuclear fission processes release a large number of different fission products, including radioactive iodine nuclides. Uranium-235 usually splits asymmetrically and radioioiodine(s) fall(s) in one of the favored mass number regions of the fission products (peaks between 90–100 and 130–140). The main radioactive iodine isotopes formed by fission are iodine-131 (physical half-life, T1/2 = 8.02 d), iodine-129 (T1/2 = 1.57 107 y) and iodine-132 (T1/2 = 2.3 h; from Te-132) (ICRP 2017). Among the different iodine isotopes, iodine-131 is of particular importance (Blum and Eisenbud 1967). Iodine is characterized by its high volatility compared to most other fission products. In the case of nuclear incidents, e.g. nuclear power plant accidents or the detonation of a nuclear weapon, it must be expected that radioiodine will be released and also carried over greater distances (Verger et al. 2001; Chabot 2016). Radioiodine is quickly absorbed into the organism both by inhalation and via ingestion (Geoffroy et al. 2000; Verger et al. 2001). From a practical point of view, intake through contaminated drinking water and food probably plays the decisive role (Blum and Eisenbud 1967).
Incidence and risk factors for radioactive iodine-induced sialadenitis
Published in Acta Oto-Laryngologica, 2020
Alvaro Sánchez Barrueco, Fernando González Galán, Ignacio Alcalá Rueda, Jessica Mireya Santillán Coello, María Pilar Barrio Dorado, José Miguel Villacampa Aubá, Manuel Escanciano Escanciano, Lucía Llanos Jiménez, Ignacio Mahillo Fernández, Carlos Cenjor Español
Radioactive iodine (131I) can be used both as a diagnostic tool and a treatment approach. Its utility stems from the beta radiation emitted by iodine isotopes. This radiation can be detected in specific locations for diagnostic purposes but can also be used to target thyroid cells in the course of treatment for various thyroid diseases, most commonly hyperthyroidism and differentiated thyroid carcinoma (DTC). Following American Thyroid Association (ATA) [1], radioiodine treatment of DTC has three goals: 1) facilitating the detection of recurrent disease by ablation of remnants, 2) minimising the risk of recurrence, as adjuvant therapy, to destroy remaining thyroid cancer cells, and 3) as a means of addressing persistent disease as reflected by high thyroglobulin (Tg) levels.
Related Knowledge Centers
- Radionuclide
- Iodine
- Nuclear Fission
- Nuclear Fission Product
- Plutonium
- Thorium
- Beta Decay
- Mutation
- Thyroid
- Graves' Disease