Samarium (153Sm) lexidronam
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
- 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.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Bone pain •••••••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- 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
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- 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
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Samarium (153Sm) lexidronam pentasodium 7389YR3OOV 176669-18-4 SZZACTGRBZTAKY-NKNBZPHVSA-F - Active Moieties
Name Kind UNII CAS InChI Key Samarium Sm-153 unknown 6Q1KA41UWM 15766-00-4 KZUNJOHGWZRPMI-AKLPVKDBSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Quadramet Injection, solution 50 mCi/1mL Intravenous Jazz Pharmaceuticals, Inc. 1997-05-19 2013-12-12 US Quadramet Injection, suspension 50 mCi/1mL Intravenous Cytogen Corporation 2006-06-01 2006-06-01 US Quadramet Injection, solution 50 mCi/1mL Intravenous Lantheus Medical Imaging 1997-05-19 Not applicable US Quadramet Injection, solution 1.3 Gbq/ml Intravenous Cis Bio International 2016-09-08 Not applicable EU
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
- 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]
- 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]
- 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]
- External Links
- PubChem Compound
- 76962714
- PubChem Substance
- 347827722
- ChemSpider
- 143933
- 177906
- Wikipedia
- Samarium_(153Sm)_lexidronam
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 2 Completed Treatment Prostate Cancer 1 2 Terminated Treatment Metastatic Bone Sarcomas 1 1 Completed Treatment Prostate Cancer 1 1, 2 Unknown Status Treatment Neoplasms of the Prostate 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Intravenous 1.3 Gbq/ml Injection, solution Intravenous 50 mCi/1mL Injection, suspension Intravenous 50 mCi/1mL Injection; injection, solution 50 mCi/mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 20.0 mg/mL ALOGPS logP 0.03 ALOGPS logP -4.2 Chemaxon logS -1.5 ALOGPS pKa (Strongest Acidic) 0.96 Chemaxon Physiological Charge -5 Chemaxon Hydrogen Acceptor Count 14 Chemaxon Hydrogen Donor Count 5 Chemaxon Polar Surface Area 245.09 Å2 Chemaxon Rotatable Bond Count 11 Chemaxon Refractivity 76.95 m3·mol-1 Chemaxon Polarizability 31.44 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-0uyr-3292010000-ccd6cd8505474a9272d0 - Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Drug created at November 18, 2007 18:23 / Updated at February 21, 2021 18:51