Samarium (153Sm) lexidronam

Identification

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Name
Samarium (153Sm) lexidronam
Accession Number
DB05273
Type
Small Molecule
Groups
Approved, Investigational
Description

Samarium Sm 153 lexidronam is a radioactive medication used to treat pain caused by cancer that has spread to the bone. It is a radiopharmaceutical. Radiopharmaceuticals are radioactive agents that may be used to diagnose some diseases by studying the function of the body's organs or to treat certain diseases.Samarium Sm 153 lexidronam is used to help relieve the bone pain that may occur with certain kinds of cancer. The radioactive samarium is taken up in the bone cancer area and gives off radiation that helps provide relief of pain.

Structure
Thumb
Synonyms
  • 153SM-EDTMP
  • Samarium (153 Sm) lexidronam
  • Samarium (153Sm) lexidronam
  • Samarium Sm-153 lexidronam
  • Samarium-153 lexidronam
  • Samarium-153-EDTMP
Product Ingredients
IngredientUNIICASInChI Key
Samarium (153Sm) lexidronam pentasodium7389YR3OOV176669-18-4SZZACTGRBZTAKY-NKNBZPHVSA-F
Active Moieties
NameKindUNIICASInChI Key
Samarium Sm-153unknown6Q1KA41UWM15766-00-4KZUNJOHGWZRPMI-AKLPVKDBSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
QuadrametInjection, suspension50 mCi/1mLIntravenousCytogen Corporation2006-06-012006-06-01Us
QuadrametInjection, solution50 mCi/1mLIntravenousLantheus Medical Imaging1997-05-19Not applicableUs
QuadrametInjection, solution50 mCi/1mLIntravenousJazz Pharmaceuticals2003-09-012013-07-11Us
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories
UNII
745X144DZY
CAS number
122575-21-7
Weight
Average: 586.021
Monoisotopic: 585.895290894
Chemical Formula
C6H17N2O12P4Sm
InChI Key
JSTADIGKFYFAIY-GJNDDOAHSA-K
InChI
InChI=1S/C6H20N2O12P4.Sm/c9-21(10,11)3-7(4-22(12,13)14)1-2-8(5-23(15,16)17)6-24(18,19)20;/h1-6H2,(H2,9,10,11)(H2,12,13,14)(H2,15,16,17)(H2,18,19,20);/q;+3/p-3/i;1+3
IUPAC Name
(153Sm)samarium(3+) ion hydrogen {[(hydrogen phosphonomethyl)({2-[(hydrogen phosphonomethyl)(phosphonomethyl)amino]ethyl})amino]methyl}phosphonate
SMILES
[153Sm+3].OP(O)(=O)CN(CCN(CP(O)([O-])=O)CP(O)([O-])=O)CP(O)([O-])=O

Pharmacology

Indication

Investigated for use/treatment in bone metastases, multiple myeloma, prostate cancer, and rheumatoid arthritis.

Associated Conditions
Pharmacodynamics
Not Available
Mechanism of action

Samarium Sm 153 lexidronam targets the sites of new bone formation, concentrating in regions of the bone that have been invaded with metastatic tumor. The drug goes to the source of cancer bone pain and irradiates the osteoblastic tumor sites resulting in relief of pain. The onset of pain relief was experienced as early as one week in the majority of patients.

Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
Not Available

References

General References
  1. Sartor O, Reid RH, Bushnell DL, Quick DP, Ell PJ: Safety and efficacy of repeat administration of samarium Sm-153 lexidronam to patients with metastatic bone pain. Cancer. 2007 Feb 1;109(3):637-43. [PubMed:17167764]
  2. Menda Y, Bushnell DL, Williams RD, Miller S, Thomas MO: Efficacy and safety of repeated samarium-153 lexidronam treatment in a patient with prostate cancer and metastatic bone pain. Clin Nucl Med. 2000 Sep;25(9):698-700. [PubMed:10983757]
  3. Vigna L, Matheoud R, Ridone S, Arginelli D, Della Monica P, Rudoni M, Inglese E, Brambilla M: Characterization of the [(153)Sm]Sm-EDTMP pharmacokinetics and estimation of radiation absorbed dose on an individual basis. Phys Med. 2011 Jul;27(3):144-52. doi: 10.1016/j.ejmp.2010.08.001. Epub 2010 Sep 23. [PubMed:20864370]
External Links
PubChem Compound
76962714
PubChem Substance
347827722
ChemSpider
143933
Wikipedia
Samarium_(153Sm)_lexidronam
ATC Codes
V10BX02 — Samarium (153sm) lexidronam

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentProstate Cancer1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, solutionIntravenous50 mCi/1mL
Injection, suspensionIntravenous50 mCi/1mL
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility20.0 mg/mLALOGPS
logP0.03ALOGPS
logP-4.2ChemAxon
logS-1.5ALOGPS
pKa (Strongest Acidic)0.96ChemAxon
Physiological Charge-5ChemAxon
Hydrogen Acceptor Count14ChemAxon
Hydrogen Donor Count5ChemAxon
Polar Surface Area245.09 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity76.95 m3·mol-1ChemAxon
Polarizability31.44 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available

Taxonomy

Classification
Not classified

Drug created on November 18, 2007 11:23 / Updated on May 01, 2019 13:31