General
Preferred name
STRONTIUM RANELATE
Synonyms
RANELIC ACID DISTRONTIUM SALT ()
Distrontium renelate ()
S12911 ()
Osseor ()
Strontium ranelate nonahydrate ()
Strontium ranelate anhydrous ()
Protelos ()
Ranelic acid strontium salt ()
P&D ID
PD008981
CAS
135459-87-9
Tags
available
drug
Drug Status
approved
withdrawn
Max Phase
Phase 4
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
ABSORPTION The absolute bioavailability of strontium is about 25% (within a range of 19-27%) after an oral dose of 2 g strontium ranelate. Maximum plasma concentrations are reached approximately 3-5 hours after a single dose of 2 g. Steady state is reached after 2 weeks of treatement. The intake of strontium ranelate with calcium or food reduces the bioavailablity of strontium ranelate by about 60-70%, compared with administration 3 hours after a meal [L1127].; ; Due to the relatively slow absorption of strontium, food and calcium intake should be avoided both before and after administration of strontium ranelate. Conversely, oral supplementation with vitamin D has no effect on strontium exposure whatsoever. [L1127]
PHARMACODYNAMICS In general, it is believed that strontium ranelate is capable of affecting a rebalance in bone turnover in favour of bone formation by: (1) increasing osteoblast differentiation from progenitors, osteoblast activity and survival, as well as regulating osteoblast-induced osteoclastogenesis, and (2) decreasing osteoclast differentiation and activity, as well as increasing osteoclast apoptosis [A31541]. ; ; It has also been shown that strontium ranelate is capable of improving and strengthening various components of overall bone tissue quality like bone mineral density and bone microarchitecture [A31541, A31542, A31553].
INDICATION Strontium ranelate is therapeutically indicated for the treatment of severe osteoperosis in: a) postmenopasual women, and b) adult men, who are at high risk of fractures, for whom treatment with other medical products approved for the treatment of osteoperosis is not possible due to, for example, contraindications or intolerance. [L1127]; ; In postmenopausal women, strontium ranelate can also reduce the risk of vertebral and hip fractures [L1127].
DESCRIPTION Strontium ranelate is a dual action bone agent (DABA). It inhibits bone resorption and stimulates bone formation, inhibiting osteoclast differentiation while activating gene expression in osteoblasts. While its exact mechanism of action is unknown, one hypothesis is that both anabolic and anti-catabolic activities may involve antagonizing nuclear factor-KB (NF-KB) activation in bone cells. Strontium ranelate has been shown to inhibit the receptor activator of NF-KB ligand (RANKL)-induced nuclear translocation of NF-KB and activator protein-1. Strontium ranelate has been used clinically for the treatment of osteoporosis and a recent multinational study indicates the drug can also be used to treat osteoarthritis. (BOC Sciences Bioactive Compounds)
Compound Sets
9
BOC Sciences Bioactive Compounds
strontium-ranelate-cas-135459-87-9-item-84-57806
Cayman Chemical Bioactives
30272
ChEMBL Approved Drugs
CHEMBL3707306
ChEMBL Drugs
CHEMBL3707306
DrugBank
DB09267
DrugBank Approved Drugs
DB09267
MedChem Express Bioactive Compound Library
HY-17397
ReFrame library
Selleckchem Bioactive Compound Library
strontium-ranelate-protelos
External IDs
18
Properties
(calculated by RDKit )
Molecular Weight
513.8
Hydrogen Bond Acceptors
11
Hydrogen Bond Donors
0
Rotatable Bonds
1
Ring Count
3
Aromatic Ring Count
1
cLogP
-1.15
TPSA
132.23
Fraction CSP3
0.25
Chiral centers
0.0
Largest ring
8.0
QED
0.42
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
MOA
Calcium Channel inhibitor
Pathway
Membrane Transporter/Ion Channel
GPCR/G protein
Target
CaSR
Calcium Channel
Source data