Samarium (153Sm) lexidronam

Last updated
Samarium (153Sm) lexidronam
153Sm-lexidronam structure.svg
Clinical data
License data
Pregnancy
category
  • US:D (Evidence of risk)
    Routes of
    administration
    Intravenous
    ATC code
    Legal status
    Legal status
    • In general: ℞ (Prescription only)
    Pharmacokinetic data
    Bioavailability N/A
    Identifiers
    CAS Number
    PubChem CID
    UNII
    ChEMBL
    CompTox Dashboard (EPA)
    Chemical and physical data
    Formula C6H12N2Na5O12P4153Sm
    Molar mass 695.93 g/mol
    3D model (JSmol)

    Samarium (153Sm) lexidronam (chemical name Samarium-153-ethylene diamine tetramethylene phosphonate, abbreviated Samarium-153 EDTMP, trade name Quadramet) is a chelated complex of a radioisotope of the element samarium with EDTMP. It is used to treat pain when cancer has spread to the bone. [1] [2]

    Contents

    It is injected into a vein and distributed throughout the body, where it is preferentially absorbed in areas where cancer has invaded the bone. The radioisotope 153Sm, with a half-life of 46.3 hours, decays by emitting beta particles (electrons), which kill the nearby cells. Pain begins to improve in the first week for most people and the effects can last several months. It is commonly used in lung cancer, prostate cancer, breast cancer, and osteosarcoma.

    Side effects

    Side effects [3] include the following:

    Supply and administration

    Samarium lexidronam is supplied as a frozen solution for intravenous use with an activity of 50±5  mCi/mL [4] and a maximum beta energy of 0.808 MeV. [5] Due to the short half-life of the radioisotope, the drug expires 56 hours after the noted calibration time. [4]

    Related Research Articles

    Radiation therapy Therapy using ionizing radiation, usually to treat cancer

    Radiation therapy or radiotherapy, often abbreviated RT, RTx, or XRT, is a therapy using ionizing radiation, generally as part of cancer treatment to control or kill malignant cells and normally delivered by a linear accelerator. Radiation therapy may be curative in a number of types of cancer if they are localized to one area of the body. It may also be used as part of adjuvant therapy, to prevent tumor recurrence after surgery to remove a primary malignant tumor. Radiation therapy is synergistic with chemotherapy, and has been used before, during, and after chemotherapy in susceptible cancers. The subspecialty of oncology concerned with radiotherapy is called radiation oncology.

    Samarium Chemical element with atomic number 62

    Samarium is a chemical element with the symbol Sm and atomic number 62. It is a moderately hard silvery metal that slowly oxidizes in air. Being a typical member of the lanthanide series, samarium usually assumes the oxidation state +3. Compounds of samarium(II) are also known, most notably the monoxide SmO, monochalcogenides SmS, SmSe and SmTe, as well as samarium(II) iodide. The last compound is a common reducing agent in chemical synthesis. Samarium has no significant biological role but is only slightly toxic.

    Unsealed source radiotherapy uses radioactive substances called radiopharmaceuticals to treat medical conditions, particularly cancer. These are introduced into the body by various means and localise to specific locations, organs or tissues depending on their properties and administration routes. This includes anything from a simple compound such as sodium iodide that locates to the thyroid via trapping the iodide ion, to complex biopharmaceuticals such as recombinant antibodies which are attached to radionuclides and seek out specific antigens on cell surfaces.

    Osteosarcoma

    An osteosarcoma (OS) or osteogenic sarcoma (OGS) is a cancerous tumor in a bone. Specifically, it is an aggressive malignant neoplasm that arises from primitive transformed cells of mesenchymal origin and that exhibits osteoblastic differentiation and produces malignant osteoid.

    Hydromorphone

    Hydromorphone, also known as dihydromorphinone, and sold under the brand name Dilaudid among others, is an opioid used to treat moderate to severe pain. Typically, long-term use is only recommended for pain due to cancer. It may be used by mouth or by injection into a vein, muscle, or under the skin. Effects generally begin within half an hour and last for up to five hours.

    Bisphosphonate

    Bisphosphonates are a class of drugs that prevent the loss of bone density, used to treat osteoporosis and similar diseases. They are the most commonly prescribed drugs used to treat osteoporosis. They are called bisphosphonates because they have two phosphonate groups. They are thus also called diphosphonates.

    Phenylbutazone

    Phenylbutazone, often referred to as "bute", is a nonsteroidal anti-inflammatory drug (NSAID) for the short-term treatment of pain and fever in animals.

    Zoledronic acid

    Zoledronic acid, also known as zoledronate, is a medication used to treat a number of bone diseases. These include osteoporosis, high blood calcium due to cancer, bone breakdown due to cancer, and Paget’s disease of bone. It is given by injection into a vein.

    Bone pain is pain coming from a bone. It occurs as a result of a wide range of diseases and/or physical conditions and may severely impair the quality of life.

    Naturally occurring gadolinium (64Gd) is composed of 6 stable isotopes, 154Gd, 155Gd, 156Gd, 157Gd, 158Gd and 160Gd, and 1 radioisotope, 152Gd, with 158Gd being the most abundant (24.84% natural abundance). The predicted double beta decay of 160Gd has never been observed; only a lower limit on its half-life of more than 1.3×1021 years has been set experimentally.

    Naturally occurring europium (63Eu) is composed of 2 isotopes, 151Eu and 153Eu, with 153Eu being the most abundant (52.2% natural abundance). While 153Eu is observationally stable, 151Eu was found in 2007 to be unstable and undergo alpha decay. The half-life is measured to be (4.62 ± 0.95(stat.) ± 0.68(syst.)) × 1018 y which corresponds to 1 alpha decay per two minutes in every kilogram of natural europium. Besides the natural radioisotope 151Eu, 36 artificial radioisotopes have been characterized, with the most stable being 150Eu with a half-life of 36.9 years, 152Eu with a half-life of 13.516 years, 154Eu with a half-life of 8.593 years, and 155Eu with a half-life of 4.7612 years. The majority of the remaining radioactive isotopes have half-lives that are less than 12.2 seconds. This element also has 17 meta states, with the most stable being 150mEu (t1/2 12.8 hours), 152m1Eu (t1/2 9.3116 hours) and 152m2Eu (t1/2 96 minutes).

    Naturally occurring samarium (62Sm) is composed of five stable isotopes, 144Sm, 149Sm, 150Sm, 152Sm and 154Sm, and two extremely long-lived radioisotopes, 147Sm (half life: 1.06×1011 y) and 148Sm (7×1015 y), with 152Sm being the most abundant (26.75% natural abundance). 146Sm is also fairly long-lived (6.8×107 y), but is not long-lived enough to have survived in significant quantities from the formation of the Solar System on Earth, although it remains useful in radiometric dating in the Solar System as an extinct radionuclide.

    Isotopes of iodine

    There are 37 known isotopes of iodine (53I) from 108I to 144I; all undergo radioactive decay except 127I, which is stable. Iodine is thus a monoisotopic element.

    Acemetacin

    Acemetacin is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of osteoarthritis, rheumatoid arthritis, lower back pain, and relieving post-operative pain. It is manufactured by Merck KGaA under the tradename Emflex, and is available in the UK and other countries as a prescription-only drug.

    Radium-223 was discovered in 1905 by T. Godlewski, a Polish chemist from Kraków, and is historically known as actinium X, or AcX. It is an isotope of radium with an 11.4-day half-life, in contrast to the more common isotope radium-226, discovered by the Curies, which has a 1600-year half-life. Radium-223 dichloride is an alpha particle-emitting radiotherapy drug that mimics calcium and forms complexes with hydroxyapatite at areas of increased bone turnover. The principal use of radium-223, as a radiopharmaceutical to treat metastatic cancers in bone, takes advantage of its chemical similarity to calcium, and the short range of the alpha radiation it emits.

    Mifamurtide

    Mifamurtide is a drug against osteosarcoma, a kind of bone cancer mainly affecting children and young adults, which is lethal in over half of cases. The drug was approved in Europe in March 2009.

    Pain in cancer may arise from a tumor compressing or infiltrating nearby body parts; from treatments and diagnostic procedures; or from skin, nerve and other changes caused by a hormone imbalance or immune response. Most chronic (long-lasting) pain is caused by the illness and most acute (short-term) pain is caused by treatment or diagnostic procedures. However, radiotherapy, surgery and chemotherapy may produce painful conditions that persist long after treatment has ended.

    PROSTVAC is a cancer immunotherapy candidate in clinical development by Bavarian Nordic for the treatment of all prostate cancer although clinical trials are focusing on more advanced cases of metastatic castration-resistant prostate cancer (mCRPC). PROSTVAC is a vaccine designed to enable the immune system to recognize and attack prostate cancer cells by triggering a specific and targeted T cell immune response to cancer cells that express the tumor-associated antigen prostate-specific antigen (PSA).

    Radiopharmaceutical

    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.

    Dinutuximab and Dinutuximab beta are monoclonal antibodies used as a second-line treatment for children with high-risk neuroblastoma. Each antibody is made of both mouse and human components and targets glycolipid GD2, expressed on neuroblastoma cells and on normal cells of neuroectodermal origin, including the central nervous system and peripheral nerves. They differ in that dinutuximab is manufactured using mouse cells, and dinutuximab beta is manufactured using hamster cells. The dosing regime differs, and dinutuximab is given in combination with granulocyte-macrophage colony stimulating factor (GM-CSF), interleukin-2 (IL-2) and 13-cis-retinoic acid (RA), while dinutuximab beta can be given alone.

    References

    1. Anderson P (August 2006). "Samarium for osteoblastic bone metastases and osteosarcoma". Expert Opinion on Pharmacotherapy. 7 (11): 1475–86. doi:10.1517/14656566.7.11.1475. PMID   16859431. S2CID   36773109.
    2. Finlay IG, Mason MD, Shelley M (June 2005). "Radioisotopes for the palliation of metastatic bone cancer: a systematic review". The Lancet. Oncology. 6 (6): 392–400. doi:10.1016/S1470-2045(05)70206-0. PMID   15925817.
    3. "Quadramet Side Effects in Detail". Drugs.com.
    4. 1 2 FDA Professional Drug Information on Quadramet. 2009.
    5. Bé M, Coursol N, Duchemin B, Lagoutine F, Legrand J. "Table of Radionuclides" (PDF). Henry Becquerel National Laboratory. Retrieved 22 April 2020.