Technetium (99mTc) nofetumomab merpentan

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Technetium (99mTc) nofetumomab merpentan
Technetium-99m nofetumomab merpentan skeletal.svg
Monoclonal antibody
Type Fab fragment
Source Mouse
Clinical data
Trade names Verluma
ATC code
  • none
Pharmacokinetic data
Elimination half-life 10.5 hours
Excretion renal (64%)
Identifiers
CAS Number
ChemSpider
  • none
UNII
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Technetium (99mTc) nofetumomab merpentan (trade name Verluma) is a mouse monoclonal antibody derivative used in the diagnosis of lung cancer, [1] gastrointestinal, breast, ovary, pancreas, kidney, cervix, and bladder carcinoma. [2] The antibody part, nofetumomab, is attached to the chelator merpentan, which links it to the radioisotope technetium-99m (99mTc). [3]

Contents

Nofetumomab

Nofetumomab is an antibody fragment that recognises the pancarcinoma glycoprotein antigen EpCAM. [4] and/or CD20/MS4A1 [5]

It is the Fab part of murine MAb NR-LU-10. [6]

Merpentan

The chelator part : merpentan is a phenthioate ligand, 2,3,5,6-tetrafluorophenyl-4,5-bis-5-[1-ethoxyethyl]-thioacetoamidopentanoate. [6]

Phenthioate

Phenthioate is an insecticide (Cidial) = O,o-dimethyl-S-(carbethoxy-phenylmethyl)dithiophosphate [7]

Related Research Articles

Technetium Chemical element, symbol Tc and atomic number 43

Technetium is a chemical element with the symbol Tc and atomic number 43. It is the lightest element whose isotopes are all radioactive. Nearly all available technetium is produced as a synthetic element. Naturally occurring technetium is a spontaneous fission product in uranium ore and thorium ore, the most common source, or the product of neutron capture in molybdenum ores. This silvery gray, crystalline transition metal lies between manganese and rhenium in group 7 of the periodic table, and its chemical properties are intermediate between those of both adjacent elements. The most common naturally occurring isotope is 99Tc, in traces only.

Scintigraphy Diagnostic imaging test in nuclear medicine

Scintigraphy, also known as a gamma scan, is a diagnostic test in nuclear medicine, where radioisotopes attached to drugs that travel to a specific organ or tissue (radiopharmaceuticals) are taken internally and the emitted gamma radiation is captured by external detectors to form two-dimensional images in a similar process to the capture of x-ray images. In contrast, SPECT and positron emission tomography (PET) form 3-dimensional images and are therefore classified as separate techniques from scintigraphy, although they also use gamma cameras to detect internal radiation. Scintigraphy is unlike a diagnostic X-ray where external radiation is passed through the body to form an image.

Carcinoembryonic antigen Glycoprotein secreted into the luminal surface of the epithelia in the gastrointestinal tract

Carcinoembryonic antigen (CEA) describes a set of highly related glycoproteins involved in cell adhesion. CEA is normally produced in gastrointestinal tissue during fetal development, but the production stops before birth. Consequently, CEA is usually present at very low levels in the blood of healthy adults. However, the serum levels are raised in some types of cancer, which means that it can be used as a tumor marker in clinical tests. Serum levels can also be elevated in heavy smokers.

Sodium pertechnetate Chemical compound

Sodium pertechnetate is the inorganic compound with the formula NaTcO4. This colourless salt contains the pertechnetate anion, [TcO4]. The radioactive 99mTcO4 anion is an important radiopharmaceutical for diagnostic use. The advantages to 99mTc include its short half-life of 6 hours and the low radiation exposure to the patient, which allow a patient to be injected with activities of more than 30 millicuries. Na[99mTcO4] is a precursor to a variety of derivatives that are used to image different parts of the body.

Radioisotope renography

Radioisotope renography is a form of medical imaging of the kidneys that uses radiolabelling. A renogram, which may also be known as a MAG3 scan, allows a nuclear medicine physician or a radiologist to visualize the kidneys and learn more about how they are functioning. MAG3 is an acronym for mercapto acetyl tri glycine, a compound that is chelated with a radioactive element – technetium-99m.

The nomenclature of monoclonal antibodies is a naming scheme for assigning generic, or nonproprietary, names to monoclonal antibodies. An antibody is a protein that is produced in B cells and used by the immune system of humans and other vertebrate animals to identify a specific foreign object like a bacterium or a virus. Monoclonal antibodies are those that were produced in identical cells, often artificially, and so share the same target object. They have a wide range of applications including medical uses.

Ventilation/perfusion scan

A ventilation/perfusion lung scan, also called a V/Q lung scan, or ventilation/perfusion scintigraphy, is a type of medical imaging using scintigraphy and medical isotopes to evaluate the circulation of air and blood within a patient's lungs, in order to determine the ventilation/perfusion ratio. The ventilation part of the test looks at the ability of air to reach all parts of the lungs, while the perfusion part evaluates how well blood circulates within the lungs. As Q in physiology is the letter used to describe bloodflow the term V/Q scan emerged.

Technetium (99mTc) fanolesomab is a mouse monoclonal antibody formerly used to aid in the diagnosis of appendicitis. It is labeled with a radioisotope, technetium-99m (99mTc).

Technetium (99mTc) sulesomab is a radio-pharmaceutical composed of anti-human mouse monoclonal antibody that targets the granulocyte associated NCA-90 cell antigen and a conjugated technetium-99m radionuclide. After intravenous administration, Leukoscan enables sensitive and specific whole body measurement of granulocyte infiltration and activation by gamma camera imaging of 99mTc-antibody bound cells. Total clearance of LeukoScan from blood samples after administration and imaging has been reported at 48 hour time points indicating limited retention of the agent in circulation

Technetium-99m Metastable nuclear isomer of technetium-99

Technetium-99m (99mTc) is a metastable nuclear isomer of technetium-99, symbolized as 99mTc, that is used in tens of millions of medical diagnostic procedures annually, making it the most commonly used medical radioisotope in the world.

Technetium (99mTc) arcitumomab is a drug used for the diagnostic imaging of colorectal cancers, marketed by Immunomedics. It consists of the Fab' fragment of a monoclonal antibody and a radionuclide, technetium-99m.

Matuzumab is a humanized monoclonal antibody for the treatment of cancer. It binds to the epidermal growth factor receptor (EGFR) with high affinity. The mouse monoclonal antibody (mAb425) from which matuzumab was developed at the Wistar Institute in Philadelphia, Pennsylvania

Technetium (<sup>99m</sup>Tc) medronic acid

Technetium (99mTc) medronic acid is a pharmaceutical product used in nuclear medicine to localize bone metastases as well as other diseases that can alter the natural turn-over in the bone by bone scintigraphy.

Technetium 99mTc albumin aggregated (99mTc-MAA) is an injectable radiopharmaceutical used in nuclear medicine. It consists of a sterile aqueous suspension of Technetium-99m (99mTc) labeled to human albumin aggregate particles. It is commonly used for lung perfusion scanning. It is also less commonly used to visualise a peritoneovenous shunt and for isotope venography.

Octreotide scan

An octreotide scan is a type of SPECT scintigraphy used to find carcinoid, pancreatic neuroendocrine tumors, and to localize sarcoidosis. It is also called somatostatin receptor scintigraphy (SRS). Octreotide, a drug similar to somatostatin, is radiolabeled with indium-111, and is injected into a vein and travels through the bloodstream. The radioactive octreotide attaches to tumor cells that have receptors for somatostatin. A gamma camera detects the radioactive octreotide, and makes pictures showing where the tumor cells are in the body, typically by a SPECT technique. A technetium-99m based radiopharmaceutical kit is also available.

Perfusion is the passage of fluid through the lymphatic system or blood vessels to an organ or a tissue. The practice of perfusion scanning is the process by which this perfusion can be observed, recorded and quantified. The term perfusion scanning encompasses a wide range of medical imaging modalities.

Technetium (99mTc) votumumab is a human monoclonal antibody labelled with the radionuclide technetium-99m. It was developed for the detection of colorectal tumors, but has never been marketed.

Affibody molecules are small, robust proteins engineered to bind to a large number of target proteins or peptides with high affinity, imitating monoclonal antibodies, and are therefore a member of the family of antibody mimetics. Affibody molecules are used in biochemical research and are being developed as potential new biopharmaceutical drugs. These molecules can be used for molecular recognition in diagnostic and therapeutic applications.


DMTHF-Tc is a radiopharmaceutical which combines DMTHF, a modified folate, with technetium-99m (99mTc), a gamma emitting radionuclide, in a chelate conjugate. It shows selectivity for certain cancer cells which overexpress FR-α, and can therefore be used for diagnostic imaging in nuclear medicine. DMTHF-Tc was developed by the Philip Low lab at Purdue University.

Pretargeting (imaging)

Pretargeting (imaging) is a tool for nuclear medicine and radiotherapy. Imaging studies require a high contrast of target to background. This can be provided by using a biomarker which has a high affinity and specificity for its target.

References

  1. Straka MR, Joyce JM, Myers DT (January 2000). "Tc-99m nofetumomab merpentan complements an equivocal bone scan for detecting skeletal metastatic disease from lung cancer". Clinical Nuclear Medicine. 25 (1): 54–5. doi:10.1097/00003072-200001000-00013. PMID   10634533.
  2. Breitz HB, Tyler A, Bjorn MJ, Lesley T, Weiden PL (September 1997). "Clinical experience with Tc-99m nofetumomab merpentan (Verluma) radioimmunoscintigraphy". Clinical Nuclear Medicine. 22 (9): 615–20. doi:10.1097/00003072-199709000-00007. PMID   9298295.
  3. "International Nonproprietary Names (INN) for pharmaceutical substances" (PDF). Geneva: World Health Organization. 2002. Archived from the original (PDF) on July 3, 2011.
  4. Tsurushita N, Vasquez M (January 2004). "Humanization of monoclonal antibodies". In Reth M, Radbruch A, Alt F, Honjo T, Neuberger M (eds.). Molecular Biology of B Cells. Academic Press. pp. 533–545. ISBN   978-0-08-047950-7.
  5. "Anti-MS4A1 Therapeutic Antibody (Technetium (99MTC) Nofetumomab Merpentan)". Creative BioLabs.
  6. 1 2 Mudd E (27 February 2015). "Monoclonal Antibody Radionuclide Test Kits". Pharmacological Sciences.
  7. US 3934010,Drabek J, Varsanyi D,"Insecticidal composition and method utilizing phosphoric acid phenylsulphonamide esters",issued 20 January 1976, assigned to Ciba Geigy Corporation