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Yttrium (90Y) Tacatuzumab Tetraxetan
Yttrium (90Y) tacatuzumab tetraxetan (trade name AFP-Cide) is a humanized monoclonal antibody intended for the treatment of cancer. The antibody itself, tacatuzumab, is conjugated with tetraxetan, a chelator for yttrium-90, a radioisotope A radionuclide (radioactive nuclide, radioisotope or radioactive isotope) is a nuclide that has excess nuclear energy, making it unstable. This excess energy can be used in one of three ways: emitted from the nucleus as gamma radiation; transferr ... which destroys the tumour cells. References Monoclonal antibodies for tumors Antibody-drug conjugates Radiopharmaceuticals Yttrium compounds Experimental cancer drugs DOTA (chelator) derivatives {{antineoplastic-drug-stub ...
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α-fetoprotein
Alpha-fetoprotein (AFP, α-fetoprotein; also sometimes called alpha-1-fetoprotein, alpha-fetoglobulin, or alpha fetal protein) is a protein that in humans is encoded by the ''AFP'' gene. The ''AFP'' gene is located on the ''q'' arm of chromosome 4 (4q25). Maternal AFP serum level is used to screen for Down syndrome, neural tube defects, and other chromosomal abnormalities. AFP is a major plasma protein produced by the yolk sac and the fetal liver during fetal development. It is thought to be the fetal analog of serum albumin. AFP binds to copper, nickel, fatty acids and bilirubin and is found in monomeric, dimeric and trimeric forms. Structure AFP is a glycoprotein of 591 amino acids and a carbohydrate moiety. Function The function of AFP in adult humans is unknown. AFP is the most abundant plasma protein found in the human fetus. Maternal plasma levels peak near the end of the first trimester, and begin decreasing prenatally at that time, then decrease rapidly after b ...
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Humanized Monoclonal Antibody
Humanized antibodies are antibodies from non-human species whose protein sequences have been modified to increase their similarity to antibody variants produced naturally in humans. The process of "humanization" is usually applied to monoclonal antibodies developed for administration to humans (for example, antibodies developed as anti-cancer drugs). Humanization can be necessary when the process of developing a specific antibody involves generation in a non-human immune system (such as that in mice). The protein sequences of antibodies produced in this way are partially distinct from homologous antibodies occurring naturally in humans, and are therefore potentially immunogenic when administered to human patients (see also Human anti-mouse antibody). The International Nonproprietary Names of humanized antibodies end in ''-zumab'', as in ''omalizumab'' (see Nomenclature of monoclonal antibodies). Humanized antibodies are distinct from chimeric antibodies. The latter also have thei ...
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Tetraxetan
DOTA (also known as tetraxetan) is an organic compound with the formula (CH2CH2NCH2CO2H)4. The molecule consists of a central 12-membered tetraaza (i.e., containing four nitrogen atoms) ring. DOTA is used as a complexing agent, especially for lanthanide ions. Its complexes have medical applications as contrast agents and cancer treatments. Terminology The acronym DOTA (for dodecane tetraacetic acid) is shorthand for both the tetracarboxylic acid and its various conjugate bases. In the area of coordination chemistry, the tetraacid is called H4DOTA and its fully deprotonated derivative is DOTA4−. Many related ligands are referred to using the DOTA acronym, although these derivatives are generally not ''tetra''carboxylic acids or the conjugate bases. Structure DOTA is derived from the macrocycle known as cyclen. The four secondary amine groups are modified by replacement of the N-H centers with N-CH2CO2H groups. The resulting aminopolycarboxylic acid, upon ionization of the car ...
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Chelator
Chelation is a type of bonding of ions and molecules to metal ions. It involves the formation or presence of two or more separate coordinate bonds between a polydentate (multiple bonded) ligand and a single central metal atom. These ligands are called chelants, chelators, chelating agents, or sequestering agents. They are usually organic compounds, but this is not a necessity, as in the case of zinc and its use as a maintenance therapy to prevent the absorption of copper in people with Wilson's disease. Chelation is useful in applications such as providing nutritional supplements, in chelation therapy to remove toxic metals from the body, as contrast agents in MRI scanning, in manufacturing using homogeneous catalysts, in chemical water treatment to assist in the removal of metals, and in fertilizers. Chelate effect The chelate effect is the greater affinity of chelating ligands for a metal ion than that of similar nonchelating (monodentate) ligands for the same metal. ...
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Yttrium-90
Yttrium-90 () is an isotope of yttrium. Yttrium-90 has found a wide range of uses in radiation therapy to treat some forms of cancer. Decay undergoes β− decay to zirconium-90 with a half-life of 64.1 hours and a decay energy of 2.28 MeV with an average beta energy of 0.9336 MeV. It also produces 0.01% 1.7 MeV photons during its decay process to the 0+ state of 90Zr, followed by pair production. The interaction between emitted electrons and matter can lead to the emission of Bremsstrahlung radiation. Production Yttrium-90 is produced by the nuclear decay of strontium-90 which has a half-life of nearly 29 years and is a fission product of uranium used in nuclear reactors. As the strontium-90 decays, chemical high-purity separation is used to isolate the yttrium-90 before precipitation. Medical application 90Y plays a significant role in the treatment of hepatocellular carcinoma (HCC), leukemia, and lymphoma, although it has the potential to treat a range of tumo ...
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Radioisotope
A radionuclide (radioactive nuclide, radioisotope or radioactive isotope) is a nuclide that has excess nuclear energy, making it unstable. This excess energy can be used in one of three ways: emitted from the nucleus as gamma radiation; transferred to one of its electrons to release it as a conversion electron; or used to create and emit a new particle (alpha particle or beta particle) from the nucleus. During those processes, the radionuclide is said to undergo radioactive decay. These emissions are considered ionizing radiation because they are energetic enough to liberate an electron from another atom. The radioactive decay can produce a stable nuclide or will sometimes produce a new unstable radionuclide which may undergo further decay. Radioactive decay is a random process at the level of single atoms: it is impossible to predict when one particular atom will decay. However, for a collection of atoms of a single nuclide the decay rate, and thus the half-life (''t''1/2) for t ...
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Monoclonal Antibodies For Tumors
Monoclonality refers to the state of a line of cells that have been derived from a single clonal origin. Thus "monoclonal cells" can be said to form a single clone. The term ''monoclonal'' comes from the Ancient Greek ''monos'', meaning "alone" or "single", and ''klon'', meaning "twig". The process of replication can occur ''in vivo'', or may be stimulated ''in vitro'' for laboratory manipulations. The use of the term typically implies that there is some method to distinguish between the cells of the original population from which the single ancestral cell is derived, such as a random genetic alteration, which is inherited by the progeny. Common usages of this term include: * Monoclonal antibody: A single hybridoma cell, which by chance includes the appropriate V(D)J recombination to produce the desired antibody, is cloned to produce a large population of identical cells. In informal laboratory jargon, the monoclonal antibodies isolated from cell culture supernatants of these ...
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Antibody-drug Conjugates
Antibody-drug conjugates or ADCs are a class of biopharmaceutical drugs designed as a targeted therapy for treating cancer. Unlike chemotherapy, ADCs are intended to target and kill tumor cells while sparing healthy cells. As of 2019, some 56 pharmaceutical companies were developing ADCs. ADCs are complex molecules composed of an antibody linked to a biologically active cytotoxic (anticancer) payload or drug. Antibody-drug conjugates are an example of bioconjugates and immunoconjugates. ADCs combine the targeting properties of monoclonal antibodies with the cancer-killing capabilities of cytotoxic drugs, designed to discriminate between healthy and diseased tissue. Mechanism of action An anticancer drug is coupled to an antibody that targets a specific tumor antigen (or protein) that, ideally, is only found in or on tumor cells. Antibodies attach themselves to the antigens on the surface of cancerous cells. The biochemical reaction that occurs upon attaching triggers a signal ...
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Radiopharmaceuticals
Radiopharmaceuticals, or medicinal radiocompounds, are a group of pharmaceutical drugs containing radioactive isotopes. Radiopharmaceuticals can be used as diagnostic and therapeutic agents. Radiopharmaceuticals emit radiation themselves, which is different from contrast media which absorb or alter external electromagnetism or ultrasound. Radiopharmacology is the branch of pharmacology that specializes in these agents. The main group of these compounds are the radiotracers used to diagnose dysfunction in body tissues. While not all medical isotopes are radioactive, radiopharmaceuticals are the oldest and still most common such drugs. Drug nomenclature As with other pharmaceutical drugs, there is standardization of the drug nomenclature for radiopharmaceuticals, although various standards coexist. The International Nonproprietary Names (INNs), United States Pharmacopeia (USP) names, and IUPAC names for these agents are usually similar other than trivial style differences. The de ...
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Yttrium Compounds
An yttrium compound is a chemical compound containing yttrium (element symbol: Y). Among these compounds, yttrium generally has a +3 valence. The solubility properties of yttrium compounds are similar to those of the lanthanides. For example oxalates and carbonates are hardly soluble in water, but soluble in excess oxalate or carbonate solutions as complexes are formed. Sulfates and double sulfates are generally soluble. They resemble the "yttrium group" of heavy lanthanide elements. Chalcogenides The oxides and hydroxides of yttrium are yttrium oxide (Y2O3) and yttrium hydroxide (Y(OH)3), respectively, and they are both white solids which are hardly soluble in water. Among them, yttrium oxide can be prepared by heating yttrium carbonate or yttrium oxalate. Alternatively the oxychloride, Y3O4Cl can be heated in air to yield the oxide. Yttrium hydroxide can be precipitated by the reaction of soluble yttrium compounds with sodium hydroxide or ammonia, and can also be obtained ...
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Experimental Cancer Drugs
An experiment is a procedure carried out to support or refute a hypothesis, or determine the efficacy or likelihood of something previously untried. Experiments provide insight into cause-and-effect by demonstrating what outcome occurs when a particular factor is manipulated. Experiments vary greatly in goal and scale but always rely on repeatable procedure and logical analysis of the results. There also exist natural experimental studies. A child may carry out basic experiments to understand how things fall to the ground, while teams of scientists may take years of systematic investigation to advance their understanding of a phenomenon. Experiments and other types of hands-on activities are very important to student learning in the science classroom. Experiments can raise test scores and help a student become more engaged and interested in the material they are learning, especially when used over time. Experiments can vary from personal and informal natural comparisons (e. ...
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