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Details

Stereochemistry ACHIRAL
Molecular Formula C12H6N2O8S.2Sr
Molecular Weight 513.4845
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of STRONTIUM RANELATE

SMILES

C(c1c(C#N)c(N(CC(=O)[O-])CC(=O)[O-])sc1C(=O)[O-])C(=O)[O-].[Sr+2].[Sr+2]

InChI

InChIKey=XXUZFRDUEGQHOV-UHFFFAOYSA-J
InChI=1S/C12H10N2O8S.2Sr/c13-2-6-5(1-7(15)16)10(12(21)22)23-11(6)14(3-8(17)18)4-9(19)20;;/h1,3-4H2,(H,15,16)(H,17,18)(H,19,20)(H,21,22);;/q;2*+2/p-4

HIDE SMILES / InChI
Strontium ranelate is composed of an organic moiety (ranelic acid) and of two atoms of stable nonradioactive strontium. In vitro, strontium ranelate increases collagen and noncollagenic proteins synthesis by mature osteoblast enriched cells. The effects of strontium ranelate on bone formation were confirmed as strontium ranelate enhanced pre-osteoblastic cell replication. The stimulation by strontium ranelate of the replication of osteoprogenitor cell and collagen, as well as noncollagenic protein synthesis in osteoblasts, provides substantial evidence to categorize strontium ranelate as a bone-forming agent. In the isolated rat osteoclast assay, a pre-incubation of bone slices with strontium ranelate induced a dose- dependent inhibition of the bone resorbing activity of treated rat osteoclast. Strontium ranelate also dose-dependently inhibited, in a chicken bone marrow culture, the expression of both carbonic anhydrase II and the alpha-subunit of the vitronectin receptor. These effects showing that strontium ranelate significantly affects bone resorption due to a direct and/or matrix-mediated inhibition of osteoclast activity and also inhibits osteoclasts differentiation, are compatible with the profile of an anti-resorptive drug. Pharmacological and clinical studies suggest that strontium ranelate optimizes bone resorption and bone formation, resulting in increased bone mass, which may be of great value in the treatment of osteoporosis. Strontium ranelate is approved by EMA for the treatment of severe osteoporosis in postmenopausal women and in adult men.

CNS Activity

Curator's Comment:: Strontium ranelate had no behavioural effects, no CNS toxicity nor CNS accumulation demonstrated with Strontium ranelate in the non-clinical studies.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
PROTELOS

Approved Use

Treatment of severe osteoporosis: - in postmenopausal women, - in adult men, at high risk of fracture, for whom treatment with other medicinal products approved for the treatment of osteoporosis is not possible due to, for example, contraindications or intolerance. In postmenopausal women, strontium ranelate reduces the risk of vertebral and hip fractures.

Launch Date

1095638400000
PubMed

PubMed

TitleDatePubMed
Adequacy of dialysis: trace elements in dialysis fluids.
1996
Effects of trace metal compounds on HIV-1 reverse transcriptase: an in vitro study.
1999 May
Inhibition of HIV-1 infection by zinc group metal compounds.
1999 Sep
Delay of natural bone loss by higher intakes of specific minerals and vitamins.
2001 May
Strontium ranelate: a novel mode of action optimizing bone formation and resorption.
2005 Jan
Osteoporosis: non-hormonal treatment.
2007 Oct
Could strontium ranelate have a synergistic role in the treatment of osteoporosis?
2009 Aug
Strontium ranelate: a review of its use in the treatment of postmenopausal osteoporosis.
2010 Apr 16
Mechanism of action of strontium ranelate: what are the facts?
2010 Jan
Strontium ranelate: in search for the mechanism of action.
2013 Nov
The position of strontium ranelate in today's management of osteoporosis.
2015 Jun
Strontium ranelate, a promising disease modifying osteoarthritis drug.
2017 Mar
Strontium and strontium ranelate: Historical review of some of their functions.
2017 Sep 1
Patents

Sample Use Guides

The recommended dose is one sachet containing 2 g of strontium ranelate once daily by oral administration.
Route of Administration: Oral
Osteoblastic MC3TE-E1 cell cultures exposed to Strontium ranelate (SR) at 0.5 mM exhibited a decrease in both cell proliferation and cell viability in all time points assayed. High levels of protein and mRNA for Type I Collagen and Osteopontin were detected in cultures exposed to SR, particularly at 0.5 mM. SR allowed the expression of fibronectin in osteoblastic cell cultures as observed by epifluorescence analysis. The mineralized bone-like nodule formation was affected in a concentration-dependent manner by SR, with large bone-like nodules being detected in osteoblastic cell cultures exposed to SR at 0.5 mM.
Name Type Language
STRONTIUM RANELATE
EMA EPAR   WHO-DD  
Common Name English
RANELIC ACID STRONTIUM SALT
MI  
Common Name English
OSSEOR
Brand Name English
PROTELOS
Brand Name English
STRONTIUM RANELATE [WHO-DD]
Common Name English
STRONTIUM RANELATE NONAHYDRATE
Common Name English
RANELIC ACID STRONTIUM SALT [MI]
Common Name English
STRONTIUM RANELATE [EMA EPAR]
Common Name English
STRONTIUM RANELATE ANHYDROUS
Common Name English
DISTRONTIUM RENELATE
Common Name English
5-(BIS(CARBOXYMETHYL)AMINO)-2-CARBOXY-4-CYANO-3-THIOPHENEACETIC ACID STRONTIUM SALT (1:2)
Common Name English
3-THIOPHENEACETIC ACID, 5-(BIS(CARBOXYMETHYL)AMINO)-2-CARBOXY-4-CYANO-, STRONTIUM SALT
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C67439
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
WHO-VATC QM05BX03
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
WHO-VATC QM05BX53
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
EMA ASSESSMENT REPORTS OSSEOR (AUTHORIZED: OSTEOPOROSIS, POSTMENOPAUSAL)
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
WHO-ATC M05BX03
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
EMA ASSESSMENT REPORTS PROTELOS (AUTHORIZED: OSTEOPOROSIS, POSTMENOPAUSAL)
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
WHO-ATC M05BX53
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
Code System Code Type Description
EVMPD
SUB20045
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
PRIMARY
EVMPD
SUB25232
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
PRIMARY
FDA UNII
04NQ160FRU
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
PRIMARY
EPA CompTox
135459-87-9
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
PRIMARY
MESH
C081587
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
PRIMARY
WIKIPEDIA
STRONTIUM RANELATE
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
PRIMARY
MERCK INDEX
M9494
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
PRIMARY Merck Index
NCI_THESAURUS
C93265
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
PRIMARY
PUBCHEM
6918182
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
PRIMARY
DRUG BANK
DB09267
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
PRIMARY
CAS
135459-87-9
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
PRIMARY
DRUG CENTRAL
4714
Created by admin on Fri Jun 25 23:48:54 UTC 2021 , Edited by admin on Fri Jun 25 23:48:54 UTC 2021
PRIMARY