Identification

Summary

Samarium (153Sm) lexidronam is a chelated complex of samarium isotope and EDTMP that concentrates in areas with high bone turnover such as sites of metastases to relieve pain associated with osteoblastic metastatic bone lesions.

Brand Names
Quadramet
Generic Name
Samarium (153Sm) lexidronam
DrugBank Accession Number
DB05273
Background

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.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 586.021
Monoisotopic: 585.895290894
Chemical Formula
C6H17N2O12P4Sm
Synonyms
  • 153SM-EDTMP
  • Samarium (153 Sm) lexidronam
  • Samarium (153Sm) lexidronam
  • Samarium Sm-153 lexidronam
  • Samarium-153 lexidronam
  • Samarium-153-EDTMP

Pharmacology

Indication

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

Pharmacology
Reduce drug development failure rates
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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.

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

Adverse Effects
Adverseeffects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
No interactions found.

Products

Products2
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Product Ingredients
IngredientUNIICASInChI Key
Samarium (153Sm) lexidronam pentasodium7389YR3OOV176669-18-4SZZACTGRBZTAKY-NKNBZPHVSA-F
Active Moieties
NameKindUNIICASInChI Key
Samarium Sm-153unknown6Q1KA41UWM15766-00-4KZUNJOHGWZRPMI-AKLPVKDBSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
QuadrametInjection, solution1.3 Gbq/mlIntravenousCis Bio International2016-09-08Not applicableEU flag
QuadrametInjection, solution50 mCi/1mLIntravenousLantheus Medical Imaging1997-05-19Not applicableUS flag
QuadrametInjection, solution50 mCi/1mLIntravenousJazz Pharmaceuticals, Inc.1997-05-192013-12-12US flag
QuadrametInjection, suspension50 mCi/1mLIntravenousCytogen Corporation2006-06-012006-06-01US flag

Categories

ATC Codes
V10BX02 — Samarium (153sm) lexidronam
Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
745X144DZY
CAS number
122575-21-7
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

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. [Article]
  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. [Article]
  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. [Article]
PubChem Compound
76962714
PubChem Substance
347827722
ChemSpider
143933
RxNav
177906
Wikipedia
Samarium_(153Sm)_lexidronam

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentProstate Cancer1
2TerminatedTreatmentMetastatic Bone Sarcomas1
1CompletedTreatmentProstate Cancer1
1, 2Unknown StatusTreatmentProstatic Neoplasms1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, solutionIntravenous1.3 Gbq/ml
Injection, solutionIntravenous50 mCi/1mL
Injection, suspensionIntravenous50 mCi/1mL
Injection; injection, solution50 mCi/mL
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

Drug created at November 18, 2007 18:23 / Updated at February 21, 2021 18:51