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Strontium chloride Sr-89

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Identification

Summary

Strontium chloride Sr-89 is a radiopharmaceutical agent used for the relief of bone pain in patients with painful skeletal metastases.

Generic Name
Strontium chloride Sr-89
DrugBank Accession Number
DB09498
Background

Strontium chloride (Sr-89), initially FDA-approved in 1993, is used as a paliative therapeutic option to help relieve the pain from bone metastases. Strontium chloride is mainly used in cases of metastatic castrate-resistant prostate cancer.9 Bone metastases is a common and severe complication presented in advanced stages of the disease. It is usually presented mainly in patients with prostatic and breast cancer, as well as in cancer of lung, bladder and thyroid. There has been some cases of apparent tumor regression which has given it a potential tumoricidal effect.8

Type
Small Molecule
Groups
Approved, Investigational
Structure
Similar Structures
Weight
Average: 159.81
Monoisotopic: 158.8451583
Chemical Formula
Cl2Sr
Synonyms
  • Strontium (89Sr) chloride
  • Strontium chloride Sr 89
  • strontium chloride, 89Sr-labeled
  • Strontium chloride, Sr-89
  • Strontium-89 chloride
External IDs
  • SMS-2PA
  • SMS2PA
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Pharmacology

Indication

Strontium-89 Chloride Injection is indicated as a paliative for the relief of bone pain in patients with skeletal metastases. It is impotant to confirm the presence of bone metastases prior the beginning of therapy.9

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofBone pain••••••••••••
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Pharmacodynamics

Metastatic bone lesions are zones of high bone mineral turnover. Thus, there is a constant need of calcium supply for the development of the malignancy. Strontium chloride 89 is a divalent ion, similar to calcium, therefore it is taken up by sites of active osteogenesis. This relieves bone metastatic-driven pain withouth generating important side effects and it also presents a very little radioprotection concern.10 Once combined with external beam radiotherapy, strontium chloride 89 can emit β particules with a maximum range in tissue of 6-8mm. This radiation is capable to reduce new bone metastases and produces an analgesic role.11

Mechanism of action

Strontium chloride 89, a similar to calcium divalent ion, concentrates in areas of increased osteogenesis, by being taken up into the inorganic matter of the bone. Strontium chloride 89 presents a 10-fold higher affinity for metastatic bone.9 Some reports indicate that after Strontium chloride 89 is incorporated into the osteoid matrix adjascently to the metastatic cells, it emits β-rays getting even to 1.3-64Gy. Thus, there is a possible tumoricidal effect driven by the radiation selectively emited by strontium chloride 89 into metastatic bones.8

Absorption

Following intravenous injection, strontium chloride 89 behaves like its calcium analog. It clears rapidly from the blood stream and selectively gets localized on the bone mineral, preferentially in zones of osteogenesis, where it can stay retained for about 14 days.Label

Volume of distribution

There have been several studies regarding the pharmacokinetics of different administration routes of strontium chloride 89. The values are different but it ranges between 40-67L.12,13

Protein binding

In some studies performed in polluted water, it was showed that strontium is able to bind to plasma proteins. In human plasma studies, it has been shown a possible recovery of 45-60% of administered strontium by ultrafiltration, while other studies confirm a protein binding of 30-40%.14

Metabolism

Strontium can interact with components than normally bind to calcium, including hydroxyapatite (main component of mineralized bone), calcium-binding or calcium-transport proteins. It can form complexes with different inorganic anions like carbonate, citrate, phosphate, carboxylic acid or lactate.14

Route of elimination

The elimination is done mainly by urinary excretion greatly in the two first days after injection. The rest of the elimination route is found in faeces. The percentage of urinary excretion may vary depending on the presence of bone lesions.Label The presence of strontium chloride 89 in faeces suggests an absorption into the gastrointestinal tract either by the bile or from the plasma.14

Half-life

Strontium chloride 89 presents a half-life of 50.5 days.11

Clearance

Strontium chloride 89 is mainly cleared by urine on a 3:1 ratio compared with fecal excretion. The total drug clearance can be slow, giving it a long half-life.14

Adverse Effects
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Toxicity

A single case of fatal septicemia following leukopenia has been reported during clinical trials. Bone marrow depression leading to thrombocytopenia (unusual bleeding or bruising; black, tarry stools; blood in urine or stools; pinpoint red spots on skin), and leukopenia (cough or hoarseness; fever or chills; lower back or side pain; painful or difficult urination)

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

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Active Moieties
NameKindUNIICASInChI Key
Strontium cation Sr-89ionic06A33308KHNot AvailablePWYYWQHXAPXYMF-OUBTZVSYSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
MetastronInjection, powder, lyophilized, for solution1 mCi/1mLIntravenousMedi-Physics Inc.1993-06-182019-01-10US flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
STRONTIUM CHLORIDE Sr-89Injection1 mCi/1mLIntravenousBio Nucleonics Inc2003-01-062019-10-23US flag
STRONTIUM CHLORIDE Sr-89Injection1 mCi/1mLIntravenousQ BioMed Inc2003-01-06Not applicableUS flag

Categories

ATC Codes
V10BX01 — Strontium (89sr) chloride
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of inorganic compounds known as alkaline earth metal chlorides. These are inorganic compounds in which the largest halogen atom is Chlorine, and the heaviest metal atom is a lanthanide.
Kingdom
Inorganic compounds
Super Class
Mixed metal/non-metal compounds
Class
Alkaline earth metal salts
Sub Class
Alkaline earth metal chlorides
Direct Parent
Alkaline earth metal chlorides
Alternative Parents
Inorganic chloride salts
Substituents
Alkaline earth metal chloride / Inorganic chloride salt / Inorganic salt
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
5R78837D4A
CAS number
38270-90-5
InChI Key
AHBGXTDRMVNFER-FCHARDOESA-L
InChI
InChI=1S/2ClH.Sr/h2*1H;/q;;+2/p-2/i;;1+1
IUPAC Name
(89Sr)strontium(2+) dichloride
SMILES
[Cl-].[Cl-].[89Sr++]

References

General References
  1. Fossa SD, Paus E, Lochoff M, Backe SM, Aas M: 89Strontium in bone metastases from hormone resistant prostate cancer: palliation effect and biochemical changes. Br J Cancer. 1992 Jul;66(1):177-80. [Article]
  2. Laing AH, Ackery DM, Bayly RJ, Buchanan RB, Lewington VJ, McEwan AJ, Macleod PM, Zivanovic MA: Strontium-89 chloride for pain palliation in prostatic skeletal malignancy. Br J Radiol. 1991 Sep;64(765):816-22. [Article]
  3. Montebello JF, Hartson-Eaton M: The palliation of osseous metastasis with 32P or 89Sr compared with external beam and hemibody irradiation: a historical perspective. Cancer Invest. 1989;7(2):139-60. [Article]
  4. Ackery D, Yardley J: Radionuclide-targeted therapy for the management of metastatic bone pain. Semin Oncol. 1993 Jun;20(3 Suppl 2):27-31. [Article]
  5. Breen SL, Powe JE, Porter AT: Dose estimation in strontium-89 radiotherapy of metastatic prostatic carcinoma. J Nucl Med. 1992 Jul;33(7):1316-23. [Article]
  6. Hansen DV, Holmes ER, Catton G, Thorne DA, Chadwick DH, Schmutz DA: Strontium-89 therapy for painful osseous metastatic prostate and breast cancer. Am Fam Physician. 1993 Jun;47(8):1795-800. [Article]
  7. Lewington VJ, McEwan AJ, Ackery DM, Bayly RJ, Keeling DH, Macleod PM, Porter AT, Zivanovic MA: A prospective, randomised double-blind crossover study to examine the efficacy of strontium-89 in pain palliation in patients with advanced prostate cancer metastatic to bone. Eur J Cancer. 1991;27(8):954-8. [Article]
  8. Heianna J, Miyauchi T, Endo W, Miura N, Terui K, Kamata S, Hashimoto M: Tumor regression of multiple bone metastases from breast cancer after administration of strontium-89 chloride (Metastron). Acta Radiol Short Rep. 2014 May 10;3(4):2047981613493412. doi: 10.1177/2047981613493412. eCollection 2014 May. [Article]
  9. El-Amm J, Aragon-Ching JB: Targeting Bone Metastases in Metastatic Castration-Resistant Prostate Cancer. Clin Med Insights Oncol. 2016 Mar 23;10(Suppl 1):11-9. doi: 10.4137/CMO.S30751. eCollection 2016. [Article]
  10. Giammarile F, Mognetti T, Resche I: Bone pain palliation with strontium-89 in cancer patients with bone metastases. Q J Nucl Med. 2001 Mar;45(1):78-83. [Article]
  11. Rose JN, Crook JM: The role of radiation therapy in the treatment of metastatic castrate-resistant prostate cancer. Ther Adv Urol. 2015 Jun;7(3):135-45. doi: 10.1177/1756287215576647. [Article]
  12. Moraes ME, Aronson JK, Grahame-Smith DG: Intravenous strontium gluconate as a kinetic marker for calcium in healthy volunteers. Br J Clin Pharmacol. 1991 Apr;31(4):423-7. [Article]
  13. Sips AJ, van der Vijgh WJ, Barto R, Netelenbos JC: Intestinal absorption of strontium chloride in healthy volunteers: pharmacokinetics and reproducibility. Br J Clin Pharmacol. 1996 Jun;41(6):543-9. [Article]
  14. Peter Watts and Paul Howe (2010). Strontium and Strontium compounds. World Health Organization. [ISBN:978 92 4 153077 4]
PubChem Compound
5362485
PubChem Substance
347827865
ChemSpider
64523
RxNav
281890
ChEBI
36383
ChEMBL
CHEMBL1200625
FDA label
Download (115 KB)
MSDS
Download (80.2 KB)

Clinical Trials

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PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
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4Not Yet RecruitingTreatmentBone Metastases / Thyroid Neoplasm Follicular1somestatusstop reasonjust information to hide
2CompletedTreatmentBone Metastases / Hormone-Refractory Prostate Cancer1somestatusstop reasonjust information to hide

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, powder, lyophilized, for solutionIntravenous1 mCi/1mL
Injection, solutionIntravenous; Parenteral150 MBq/4ml
InjectionIntravenous1 mCi/1mL
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)0ºC'MSDS'
boiling point (°C)100ºC'MSDS'
water solubility10.9-22.6 mg/ml'FDA label'
Radioactivity (mCi/mL)1'FDA label'
Predicted Properties
PropertyValueSource
Water Solubility51.8 mg/mLALOGPS
logP0.84ALOGPS
logP0.61Chemaxon
logS-0.49ALOGPS
pKa (Strongest Acidic)-7Chemaxon
Physiological Charge-1Chemaxon
Hydrogen Acceptor Count0Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area0 Å2Chemaxon
Rotatable Bond Count0Chemaxon
Refractivity5.62 m3·mol-1Chemaxon
Polarizability2.39 Å3Chemaxon
Number of Rings0Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterNoChemaxon
Veber's RuleYesChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Enzymes

Details1. Alkaline phosphatase, germ cell type
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Cofactor
General Function
Alkaline phosphatase that can hydrolyze various phosphate compounds
Specific Function
Alkaline phosphatase activity
Gene Name
ALPG
Uniprot ID
P10696
Uniprot Name
Alkaline phosphatase, germ cell type
Molecular Weight
57376.515 Da
References
  1. Llinas P, Masella M, Stigbrand T, Menez A, Stura EA, Le Du MH: Structural studies of human alkaline phosphatase in complex with strontium: implication for its secondary effect in bones. Protein Sci. 2006 Jul;15(7):1691-700. [Article]
Details2. Alkaline phosphatase, tissue-nonspecific isozyme
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Cofactor
General Function
Alkaline phosphatase that metabolizes various phosphate compounds and plays a key role in skeletal mineralization and adaptive thermogenesis (PubMed:12162492, PubMed:23688511, PubMed:25982064). Has broad substrate specificity and can hydrolyze a considerable variety of compounds: however, only a few substrates, such as diphosphate (inorganic pyrophosphate; PPi), pyridoxal 5'-phosphate (PLP) and N-phosphocreatine are natural substrates (PubMed:12162492, PubMed:2220817). Plays an essential role in skeletal and dental mineralization via its ability to hydrolyze extracellular diphosphate, a potent mineralization inhibitor, to phosphate: it thereby promotes hydroxyapatite crystal formation and increases inorganic phosphate concentration (PubMed:23688511, PubMed:25982064). Acts in a non-redundant manner with PHOSPHO1 in skeletal mineralization: while PHOSPHO1 mediates the initiation of hydroxyapatite crystallization in the matrix vesicles (MVs), ALPL/TNAP catalyzes the spread of hydroxyapatite crystallization in the extracellular matrix (By similarity). Also promotes dephosphorylation of osteopontin (SSP1), an inhibitor of hydroxyapatite crystallization in its phosphorylated state; it is however unclear whether ALPL/TNAP mediates SSP1 dephosphorylation via a direct or indirect manner (By similarity). Catalyzes dephosphorylation of PLP to pyridoxal (PL), the transportable form of vitamin B6, in order to provide a sufficient amount of PLP in the brain, an essential cofactor for enzymes catalyzing the synthesis of diverse neurotransmitters (PubMed:20049532, PubMed:2220817). Additionally, also able to mediate ATP degradation in a stepwise manner to adenosine, thereby regulating the availability of ligands for purinergic receptors (By similarity). Also capable of dephosphorylating microbial products, such as lipopolysaccharides (LPS) as well as other phosphorylated small-molecules, such as poly-inosine:cytosine (poly I:C) (PubMed:28448526). Acts as a key regulator of adaptive thermogenesis as part of the futile creatine cycle: localizes to the mitochondria of thermogenic fat cells and acts by mediating hydrolysis of N-phosphocreatine to initiate a futile cycle of creatine dephosphorylation and phosphorylation (By similarity). During the futile creatine cycle, creatine and N-phosphocreatine are in a futile cycle, which dissipates the high energy charge of N-phosphocreatine as heat without performing any mechanical or chemical work (By similarity)
Specific Function
Adp phosphatase activity
Gene Name
ALPL
Uniprot ID
P05186
Uniprot Name
Alkaline phosphatase, tissue-nonspecific isozyme
Molecular Weight
57304.435 Da
References
  1. Llinas P, Masella M, Stigbrand T, Menez A, Stura EA, Le Du MH: Structural studies of human alkaline phosphatase in complex with strontium: implication for its secondary effect in bones. Protein Sci. 2006 Jul;15(7):1691-700. [Article]
Details3. Adenosine triphosphate (ATP)
Kind
Small molecule
Organism
Humans
Pharmacological action
Unknown
Actions
Cofactor
References
  1. Peter Watts and Paul Howe (2010). Strontium and Strontium compounds. World Health Organization. [ISBN:978 92 4 153077 4]

Transporters

Details1. Sodium/calcium exchanger 1
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inducer
General Function
Mediates the exchange of one Ca(2+) ion against three to four Na(+) ions across the cell membrane, and thereby contributes to the regulation of cytoplasmic Ca(2+) levels and Ca(2+)-dependent cellular processes (PubMed:11241183, PubMed:1374913, PubMed:1476165). Contributes to Ca(2+) transport during excitation-contraction coupling in muscle (PubMed:11241183, PubMed:1374913, PubMed:1476165). In a first phase, voltage-gated channels mediate the rapid increase of cytoplasmic Ca(2+) levels due to release of Ca(2+) stores from the endoplasmic reticulum (PubMed:11241183, PubMed:1374913, PubMed:1476165). SLC8A1 mediates the export of Ca(2+) from the cell during the next phase, so that cytoplasmic Ca(2+) levels rapidly return to baseline (PubMed:11241183, PubMed:1374913, PubMed:1476165). Required for normal embryonic heart development and the onset of heart contractions (By similarity)
Specific Function
Ankyrin binding
Gene Name
SLC8A1
Uniprot ID
P32418
Uniprot Name
Sodium/calcium exchanger 1
Molecular Weight
108546.06 Da
References
  1. Peter Watts and Paul Howe (2010). Strontium and Strontium compounds. World Health Organization. [ISBN:978 92 4 153077 4]
Details2. Voltage-dependent T-type calcium channel subunit alpha-1I
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inducer
General Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. This channel gives rise to T-type calcium currents. T-type calcium channels belong to the 'low-voltage activated (LVA)' group and are strongly blocked by nickel and mibefradil. A particularity of this type of channels is an opening at quite negative potentials, and a voltage-dependent inactivation. T-type channels serve pacemaking functions in both central neurons and cardiac nodal cells and support calcium signaling in secretory cells and vascular smooth muscle. They may also be involved in the modulation of firing patterns of neurons which is important for information processing as well as in cell growth processes. Gates in voltage ranges similar to, but higher than alpha 1G or alpha 1H (By similarity)
Specific Function
High voltage-gated calcium channel activity
Gene Name
CACNA1I
Uniprot ID
Q9P0X4
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1I
Molecular Weight
245100.8 Da
References
  1. Peter Watts and Paul Howe (2010). Strontium and Strontium compounds. World Health Organization. [ISBN:978 92 4 153077 4]

Drug created at November 30, 2015 19:10 / Updated at June 12, 2020 17:42