Page last updated: 2024-12-05

methylene diphosphonate

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Methylene diphosphonate (MDP) is a bisphosphonate that inhibits bone resorption by binding to hydroxyapatite crystals in bone and blocking the activity of osteoclasts. It is used in the treatment of Paget's disease, hypercalcemia, and osteoporosis. MDP is typically administered intravenously or orally. It is synthesized by reacting formaldehyde with phosphorus oxychloride in the presence of a base. The compound is of great interest due to its high affinity for bone mineral and its ability to interfere with bone resorption, making it useful for treating various bone diseases. MDP is also investigated for potential applications in bone regeneration and tissue engineering.'

medronic acid : A 1,1-bis(phosphonic acid) consisting of methane substituted by two phosphonic acid groups. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID16124
CHEMBL ID180570
CHEBI ID43945
SCHEMBL ID66716
MeSH IDM0089278

Synonyms (85)

Synonym
STL302043
smr000060476
MLS000048571 ,
acidum medronicum [inn-latin]
acido medronico [inn-spanish]
einecs 217-851-0
phosphonic acid, methylenebis-
acide medronique [inn-french]
medronic acid (usan)
D04887
methylene bis-phosphonic acid
mdp, methanediphosphonic acid
medronic acid
phosphonomethylphosphonic acid
1984-15-2
methylene diphosphonic acid
methylenediphosphonic acid
MDN ,
methanebisphosphonic acid
methanediphosphonic acid
methylenediphosphonic acid, for molecular studies & mass spectrometry
methylenediphosphonic acid, >=99%
methylene diphsphonate
phosphonomethyl-phosphonic acid
bdbm50162816
chebi:43945 ,
medronate
CHEMBL180570 ,
phosphonic acid, methylenedi-
mbkdynnuvrnnrf-uhfffaoysa-
inchi=1/ch6o6p2/c2-8(3,4)1-9(5,6)7/h1h2,(h2,2,3,4)(h2,5,6,7)
M0843
AKOS001031749
NCGC00037856-02
acido medronico
73os0qin3o ,
unii-73os0qin3o
acide medronique
methylene-1,1-bisphosphonic acid
medronic acid [usan:inn:ban]
acidum medronicum
mdp-bracco
methylenebis(phosphonic acid)
cas-1984-15-2
dtxcid6025696
dtxsid8045696 ,
NCGC00037856-01
tox21_110974
methanediylbis(phosphonic acid)
FT-0628882
medronic acid [mi]
medronic acid [mart.]
medronic acid [ii]
methylene diphosphonic acid [vandf]
medronic acid [usan]
medronic acid [who-dd]
medronic acid [inn]
ch6o6p2
SCHEMBL66716
MBKDYNNUVRNNRF-UHFFFAOYSA-N
methandiphosphonic acid
OPERA_ID_703
mfcd00002139
medronic acid, european pharmacopoeia (ep) reference standard
bis(dihydroxyphosphoryl)methane
BCP20495
Q2823283
Z56782384
DB14078
(phosphonomethyl)phosphonic acid
CS-0028208
HY-108309
phosphonic acid, p,p'-methylenebis-
medronic-acid
AMY31948
A928713
T72027
methylenediphosphonic acidmethylenediphosphonic acid
EN300-1179892
medronic acid (mart.)
medronic acid (ii)
acidum medronicum (inn-latin)
acido medronico (inn-spanish)
acide medronique (inn-french)
SY008079

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
bone density conservation agentAn agent that inhibits bone resorption and/or favor bone mineralization and bone regeneration. Used to heal bone fractures and to treat bone diseases such as osteopenia and osteoporosis.
chelatorA ligand with two or more separate binding sites that can bind to a single metallic central atom, forming a chelate.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
1,1-bis(phosphonic acid)Any member of the class of phosphonic acids in which a carbon atom is directly attached to two phosphonic acid groups. They are analogues of pyrophosphates (with the central oxygen atom replaced by a carbon atom) and like pyrophosphates they tend to have a strong affinity for bone, so are frequently used for their antiresorptive and hypocalcaemic properties.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (19)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency6.29460.140911.194039.8107AID2451
Chain A, HADH2 proteinHomo sapiens (human)Potency6.30960.025120.237639.8107AID886
Chain B, HADH2 proteinHomo sapiens (human)Potency6.30960.025120.237639.8107AID886
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency0.35480.177814.390939.8107AID2147
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency50.11870.707936.904389.1251AID504333
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency7.07950.035520.977089.1251AID504332
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency70.79460.010039.53711,122.0200AID1469
mitogen-activated protein kinase 1Homo sapiens (human)Potency3.54810.039816.784239.8107AID1454
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency1.51010.060110.745337.9330AID485367
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Type IV secretion-like conjugative transfer relaxase protein TraI Escherichia coli SMS-3-5Ki0.00300.00200.00270.0030AID328050
Ornithine transcarbamylase, mitochondrialHomo sapiens (human)Ki16,333.33330.10000.14330.2000AID151017; AID151018; AID151019
Carbonic anhydrase 2Homo sapiens (human)IC50 (µMol)1,250.00000.00021.10608.3000AID1152900
Carbonic anhydrase 2Homo sapiens (human)Ki1,250.00000.00000.72369.9200AID238755
72 kDa type IV collagenaseHomo sapiens (human)IC50 (µMol)49.00000.00001.284810.0000AID1152905
Carbonic anhydrase 4Homo sapiens (human)Ki5,340.00000.00021.97209.9200AID238915
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki730.00000.00001.27259.9000AID239032
Nociceptin receptorMus musculus (house mouse)Ki20,000.00000.00030.06510.1300AID151019
Carbonic anhydrase 9Homo sapiens (human)IC50 (µMol)860.00000.00030.63029.3900AID1152901
Carbonic anhydrase 9Homo sapiens (human)Ki860.00000.00010.78749.9000AID239054
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Carbonic anhydrase 1Homo sapiens (human)KA200.00000.02001.72197.4000AID238032
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (70)

Processvia Protein(s)Taxonomy
urea cycleOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
liver developmentOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
ornithine catabolic processOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
midgut developmentOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
response to xenobiotic stimulusOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
response to zinc ionOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
citrulline biosynthetic processOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
response to insulinOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
monoatomic anion homeostasisOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
response to biotinOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
ammonium homeostasisOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
arginine biosynthetic process via ornithineOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 1Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 2Homo sapiens (human)
positive regulation of synaptic transmission, GABAergicCarbonic anhydrase 2Homo sapiens (human)
positive regulation of cellular pH reductionCarbonic anhydrase 2Homo sapiens (human)
angiotensin-activated signaling pathwayCarbonic anhydrase 2Homo sapiens (human)
regulation of monoatomic anion transportCarbonic anhydrase 2Homo sapiens (human)
secretionCarbonic anhydrase 2Homo sapiens (human)
regulation of intracellular pHCarbonic anhydrase 2Homo sapiens (human)
neuron cellular homeostasisCarbonic anhydrase 2Homo sapiens (human)
positive regulation of dipeptide transmembrane transportCarbonic anhydrase 2Homo sapiens (human)
regulation of chloride transportCarbonic anhydrase 2Homo sapiens (human)
carbon dioxide transportCarbonic anhydrase 2Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 2Homo sapiens (human)
angiogenesis72 kDa type IV collagenaseHomo sapiens (human)
ovarian follicle development72 kDa type IV collagenaseHomo sapiens (human)
ovulation from ovarian follicle72 kDa type IV collagenaseHomo sapiens (human)
luteinization72 kDa type IV collagenaseHomo sapiens (human)
blood vessel maturation72 kDa type IV collagenaseHomo sapiens (human)
intramembranous ossification72 kDa type IV collagenaseHomo sapiens (human)
proteolysis72 kDa type IV collagenaseHomo sapiens (human)
negative regulation of cell adhesion72 kDa type IV collagenaseHomo sapiens (human)
heart development72 kDa type IV collagenaseHomo sapiens (human)
embryo implantation72 kDa type IV collagenaseHomo sapiens (human)
parturition72 kDa type IV collagenaseHomo sapiens (human)
response to xenobiotic stimulus72 kDa type IV collagenaseHomo sapiens (human)
response to mechanical stimulus72 kDa type IV collagenaseHomo sapiens (human)
peripheral nervous system axon regeneration72 kDa type IV collagenaseHomo sapiens (human)
response to activity72 kDa type IV collagenaseHomo sapiens (human)
protein metabolic process72 kDa type IV collagenaseHomo sapiens (human)
extracellular matrix disassembly72 kDa type IV collagenaseHomo sapiens (human)
protein catabolic process72 kDa type IV collagenaseHomo sapiens (human)
positive regulation of cell migration72 kDa type IV collagenaseHomo sapiens (human)
collagen catabolic process72 kDa type IV collagenaseHomo sapiens (human)
response to retinoic acid72 kDa type IV collagenaseHomo sapiens (human)
cellular response to reactive oxygen species72 kDa type IV collagenaseHomo sapiens (human)
response to nicotine72 kDa type IV collagenaseHomo sapiens (human)
endodermal cell differentiation72 kDa type IV collagenaseHomo sapiens (human)
response to hydrogen peroxide72 kDa type IV collagenaseHomo sapiens (human)
response to estrogen72 kDa type IV collagenaseHomo sapiens (human)
negative regulation of vasoconstriction72 kDa type IV collagenaseHomo sapiens (human)
ephrin receptor signaling pathway72 kDa type IV collagenaseHomo sapiens (human)
macrophage chemotaxis72 kDa type IV collagenaseHomo sapiens (human)
response to electrical stimulus72 kDa type IV collagenaseHomo sapiens (human)
response to hyperoxia72 kDa type IV collagenaseHomo sapiens (human)
face morphogenesis72 kDa type IV collagenaseHomo sapiens (human)
bone trabecula formation72 kDa type IV collagenaseHomo sapiens (human)
prostate gland epithelium morphogenesis72 kDa type IV collagenaseHomo sapiens (human)
cellular response to amino acid stimulus72 kDa type IV collagenaseHomo sapiens (human)
cellular response to interleukin-172 kDa type IV collagenaseHomo sapiens (human)
cellular response to estradiol stimulus72 kDa type IV collagenaseHomo sapiens (human)
cellular response to UV-A72 kDa type IV collagenaseHomo sapiens (human)
cellular response to fluid shear stress72 kDa type IV collagenaseHomo sapiens (human)
positive regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathway72 kDa type IV collagenaseHomo sapiens (human)
response to amyloid-beta72 kDa type IV collagenaseHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation72 kDa type IV collagenaseHomo sapiens (human)
extracellular matrix organization72 kDa type IV collagenaseHomo sapiens (human)
response to hypoxia72 kDa type IV collagenaseHomo sapiens (human)
tissue remodeling72 kDa type IV collagenaseHomo sapiens (human)
bicarbonate transportCarbonic anhydrase 4Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 4Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
response to hypoxiaCarbonic anhydrase 9Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 9Homo sapiens (human)
response to xenobiotic stimulusCarbonic anhydrase 9Homo sapiens (human)
response to testosteroneCarbonic anhydrase 9Homo sapiens (human)
secretionCarbonic anhydrase 9Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 9Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (17)

Processvia Protein(s)Taxonomy
ornithine carbamoyltransferase activityOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
phospholipid bindingOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
amino acid bindingOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
phosphate ion bindingOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
identical protein bindingOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
arylesterase activityCarbonic anhydrase 1Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 1Homo sapiens (human)
protein bindingCarbonic anhydrase 1Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 1Homo sapiens (human)
hydro-lyase activityCarbonic anhydrase 1Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 1Homo sapiens (human)
arylesterase activityCarbonic anhydrase 2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 2Homo sapiens (human)
protein bindingCarbonic anhydrase 2Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 2Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 2Homo sapiens (human)
fibronectin binding72 kDa type IV collagenaseHomo sapiens (human)
endopeptidase activity72 kDa type IV collagenaseHomo sapiens (human)
metalloendopeptidase activity72 kDa type IV collagenaseHomo sapiens (human)
serine-type endopeptidase activity72 kDa type IV collagenaseHomo sapiens (human)
protein binding72 kDa type IV collagenaseHomo sapiens (human)
metallopeptidase activity72 kDa type IV collagenaseHomo sapiens (human)
zinc ion binding72 kDa type IV collagenaseHomo sapiens (human)
protein bindingCarbonic anhydrase 4Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 4Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 4Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 9Homo sapiens (human)
protein bindingCarbonic anhydrase 9Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 9Homo sapiens (human)
molecular function activator activityCarbonic anhydrase 9Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (29)

Processvia Protein(s)Taxonomy
mitochondrionOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
mitochondrial inner membraneOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
mitochondrial matrixOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
mitochondrionOrnithine transcarbamylase, mitochondrialHomo sapiens (human)
cytosolCarbonic anhydrase 1Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 1Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
cytosolCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
myelin sheathCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 2Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
collagen-containing extracellular matrix72 kDa type IV collagenaseHomo sapiens (human)
extracellular region72 kDa type IV collagenaseHomo sapiens (human)
extracellular space72 kDa type IV collagenaseHomo sapiens (human)
nucleus72 kDa type IV collagenaseHomo sapiens (human)
mitochondrion72 kDa type IV collagenaseHomo sapiens (human)
plasma membrane72 kDa type IV collagenaseHomo sapiens (human)
sarcomere72 kDa type IV collagenaseHomo sapiens (human)
collagen-containing extracellular matrix72 kDa type IV collagenaseHomo sapiens (human)
extracellular space72 kDa type IV collagenaseHomo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 4Homo sapiens (human)
rough endoplasmic reticulumCarbonic anhydrase 4Homo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartmentCarbonic anhydrase 4Homo sapiens (human)
Golgi apparatusCarbonic anhydrase 4Homo sapiens (human)
trans-Golgi networkCarbonic anhydrase 4Homo sapiens (human)
plasma membraneCarbonic anhydrase 4Homo sapiens (human)
external side of plasma membraneCarbonic anhydrase 4Homo sapiens (human)
cell surfaceCarbonic anhydrase 4Homo sapiens (human)
membraneCarbonic anhydrase 4Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 4Homo sapiens (human)
transport vesicle membraneCarbonic anhydrase 4Homo sapiens (human)
secretory granule membraneCarbonic anhydrase 4Homo sapiens (human)
brush border membraneCarbonic anhydrase 4Homo sapiens (human)
perinuclear region of cytoplasmCarbonic anhydrase 4Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 4Homo sapiens (human)
plasma membraneCarbonic anhydrase 4Homo sapiens (human)
mitochondrial matrixCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
cytoplasmCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
nucleolusCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 9Homo sapiens (human)
membraneCarbonic anhydrase 9Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 9Homo sapiens (human)
microvillus membraneCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 9Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (43)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1459738Inhibition of DLODP in human HepG2 microsomal membrane assessed as reduction in [3H]OSP production at 3 mM using Glc3-0[3H]Man9-5GlcNAc2-PP-dolichol as substrate at pH 5.5 measured after 20 to 60 mins by scintillation counting2017European journal of medicinal chemistry, Jan-05, Volume: 125Synthesis and biological evaluation of chemical tools for the study of Dolichol Linked Oligosaccharide Diphosphatase (DLODP).
AID1128904Inhibition of red kidney beans purple acid phosphatase2014European journal of medicinal chemistry, Apr-09, Volume: 76The applications of binuclear metallohydrolases in medicine: recent advances in the design and development of novel drug leads for purple acid phosphatases, metallo-β-lactamases and arginases.
AID328055Inhibition of conjugate DNA transfer between tetracycline-resistant F plasmid positive Escherichia coli JS10 to streptomycin-resistant F plasmid deficient Escherichia coli JS42007Proceedings of the National Academy of Sciences of the United States of America, Jul-24, Volume: 104, Issue:30
Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase.
AID1152905Inhibition of human recombinant MMP-2 pretreated for 30 mins measured 2 to 4 hrs after Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 substrate addition by fluorescence analysis2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Dual carbonic anhydrase/matrix metalloproteinase inhibitors incorporating bisphosphonic acid moieties targeting bone tumors.
AID238032Activation constant towards human cytosolic carbonic anhydrase I; Activator2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with organic phosphates and phosphonates.
AID328050Inhibition of Escherichia coli F plasmid TraI relaxase Y16F mutant assessed as oriT ssDNA cleavage by competitive inhibition assay2007Proceedings of the National Academy of Sciences of the United States of America, Jul-24, Volume: 104, Issue:30
Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase.
AID239054Binding affinity owards recombinant human transmembrane carbonic anhydrase IX2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with organic phosphates and phosphonates.
AID328057Cytotoxicity against streptomycin-resistant F plasmid deficient Escherichia coli JS42007Proceedings of the National Academy of Sciences of the United States of America, Jul-24, Volume: 104, Issue:30
Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase.
AID328058Selectivity ratio, ratio of EC50 for Escherichia coli JS4 to EC50 for Escherichia coli JS102007Proceedings of the National Academy of Sciences of the United States of America, Jul-24, Volume: 104, Issue:30
Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase.
AID238755Binding affinity towards human cytosolic carbonic anhydrase II2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with organic phosphates and phosphonates.
AID151017Binding affinity against ornithine transcarbamoylase (OTC) produced by Streptococcus faecalis The buffer taken for this study is 50 mM Tris.HCl, 0.5 mM EDTA at pH 8.0.1999Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14
alpha-Functionalized phosphonylphosphinates: synthesis and evaluation as transcarbamoylase inhibitors.
AID619889Drug uptake in human A549 cells at 30 uM after 8 hrs using MTBSTFA by LC/MS/MS analysis2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Bisphosphonamidate clodronate prodrug exhibits potent anticancer activity in non-small-cell lung cancer cells.
AID328060Selectivity ratio, ratio of EC50 for Escherichia coli JS10 to ratio of EC50 for inhibition of conjugate DNA transfer between Escherichia coli JS10 and Escherichia coli JS42007Proceedings of the National Academy of Sciences of the United States of America, Jul-24, Volume: 104, Issue:30
Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase.
AID328056Cytotoxicity against tetracycline-resistant F plasmid positive Escherichia coli JS102007Proceedings of the National Academy of Sciences of the United States of America, Jul-24, Volume: 104, Issue:30
Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase.
AID151019Binding affinity against ornithine transcarbamoylase (OTC) produced by Streptococcus faecalis The buffer taken for this study is 50 mM maleate, 0.5 mM EDTA at pH 6.0.1999Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14
alpha-Functionalized phosphonylphosphinates: synthesis and evaluation as transcarbamoylase inhibitors.
AID1152901Inhibition of human recombinant carbonic anhydrase 9 pretreated for 15 mins by stopped flow CO2 hydrase assay2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Dual carbonic anhydrase/matrix metalloproteinase inhibitors incorporating bisphosphonic acid moieties targeting bone tumors.
AID328059Selectivity ratio, ratio of EC50 for inhibition of conjugate DNA transfer between Escherichia coli JS10 and Escherichia coli JS4 to EC50 for Escherichia coli JS102007Proceedings of the National Academy of Sciences of the United States of America, Jul-24, Volume: 104, Issue:30
Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase.
AID1370016Drug level treated with UTP 5'-O-Palpha,alpha-dithiophosphate-beta,gamma-methylene at 2 mM at pH 11.7 at room temperature after 25 days by 31P NMR method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Highly Selective and Potent Ectonucleotide Pyrophosphatase-1 (NPP1) Inhibitors Based on Uridine 5'-P
AID1370014Drug level treated with UTP 5'-O-Palpha,alpha-dithiophosphate-beta,gamma-methylene at 2 mM at pH 1.7 at room temperature after 25 days by 31P NMR method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Highly Selective and Potent Ectonucleotide Pyrophosphatase-1 (NPP1) Inhibitors Based on Uridine 5'-P
AID328053Inhibition of Escherichia coli F plasmid TraI relaxase Y16F mutant assessed as oriT ssDNA cleavage at 200 nM2007Proceedings of the National Academy of Sciences of the United States of America, Jul-24, Volume: 104, Issue:30
Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase.
AID328061Selectivity ratio, ratio of EC50 for Escherichia coli JS4 to ratio of EC50 for inhibition of conjugate DNA transfer between Escherichia coli JS10 and Escherichia coli JS42007Proceedings of the National Academy of Sciences of the United States of America, Jul-24, Volume: 104, Issue:30
Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase.
AID1226174Binding affinity to hydroxyapatite at 3.2 to 3.7 mM after 1 hr by NMR analysis relative to control2015ACS medicinal chemistry letters, Apr-09, Volume: 6, Issue:4
Structural requirements for bisphosphonate binding on hydroxyapatite: NMR study of bisphosphonate partial esters.
AID1152900Inhibition of human recombinant carbonic anhydrase 2 pretreated for 15 mins by stopped flow CO2 hydrase assay2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Dual carbonic anhydrase/matrix metalloproteinase inhibitors incorporating bisphosphonic acid moieties targeting bone tumors.
AID1152904Activation of human recombinant carbonic anhydrase 1 pretreated for 15 mins by stopped flow CO2 hydrase assay2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Dual carbonic anhydrase/matrix metalloproteinase inhibitors incorporating bisphosphonic acid moieties targeting bone tumors.
AID151018Binding affinity against ornithine transcarbamoylase (OTC) produced by Streptococcus faecalis The buffer taken for this study is 50 mM Tris.HCl, 0.5 mM EDTA at pH 7.0.1999Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14
alpha-Functionalized phosphonylphosphinates: synthesis and evaluation as transcarbamoylase inhibitors.
AID238915Binding affinity towards human membrane associated carbonic anhydrase IV2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with organic phosphates and phosphonates.
AID239032Binding affinity towards recombinant human mitochondrial carbonic anhydrase V2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with organic phosphates and phosphonates.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (17)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (5.88)18.2507
2000's3 (17.65)29.6817
2010's12 (70.59)24.3611
2020's1 (5.88)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 92.44

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index92.44 (24.57)
Research Supply Index2.89 (2.92)
Research Growth Index5.21 (4.65)
Search Engine Demand Index157.98 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (92.44)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (5.88%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (94.12%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (7)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Pilot Study of Technetium [99Tc] Methylene Diphosphonate in the Treatment of Psoriatic Arthritis [NCT05000086]Phase 420 participants (Actual)Interventional2019-06-01Completed
A Double-masked, Methylprednisolone-control, Efficacy and Safety Study of 99Tc-MDP for Thyroid Associated Ophthalmopathy. [NCT03948191]Phase 450 participants (Actual)Interventional2017-10-16Completed
Combined 18F-NaF/18F-FDG PET/MRI for Detection of Skeletal Metastases [NCT00375830]Phase 2114 participants (Actual)Interventional2006-01-31Completed
F-18 NaF PET for Detection of Bone Metastases in Men With Prostate Cancer: Exploratory Study [NCT00956163]Early Phase 150 participants (Actual)Interventional2010-03-31Completed
Efficacy of Ra-223 in PSMA PET Optimally Selected Patients [NCT05924672]Phase 254 participants (Anticipated)Interventional2023-12-18Not yet recruiting
A Randomized, Open-Label, Crossover, Controlled, Multi-center Clinical Study to Assess the Diagnostic Performance and Safety of 18F-NaF-PET/CT in Bone Metastases of Malignant Tumors Compared With 99mTc⁃MDP-BS±SPECT [NCT05614518]Phase 3280 participants (Actual)Interventional2021-03-29Completed
Prospective Trial of 99Tc-MDP and Fosamax in Postmenopausal Women With Differentiated Thyroid Cancer and Osteoporosis Treated With Supraphysiological Doses of Thyroid Hormone [NCT02304757]142 participants (Actual)Interventional2015-01-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00375830 (9) [back to overview]Cohort 3 - Skeletal Lesions Identified by 99mTc MDP WBBS vs 18F-NaF / 18F-FDG PET/MRI
NCT00375830 (9) [back to overview]Cohort 3 - Total Skeletal Lesions Identified, Tc-99m MDP WBBS vs 18F-NaF / 18F-FDG PET/MRI
NCT00375830 (9) [back to overview]Cohort 1 - 18F-NaF PET/CT vs 18F-FDG PET/CT
NCT00375830 (9) [back to overview]Cohort 1 - NaF PET/CT vs 99mTc-MDP Bone Scintigraphy
NCT00375830 (9) [back to overview]Cohort 2 - 18F-NaF/18F-FDG PET/CT vs Whole-body MRI for Detection of Extraskeletal Lesions
NCT00375830 (9) [back to overview]Cohort 2 - 18F-NaF/18F-FDG vs 99mTc-MDP Bone Scintigraphy for Detection of Skeletal Lesions
NCT00375830 (9) [back to overview]Cohort 2 - 18F-NaF/18F-FDG vs Whole-body MRI for Detection of Skeletal Lesions
NCT00375830 (9) [back to overview]Cohort 2 - Overall Sensitivity and Accuracy for 18F-NaF/18F-FDG vs Whole-body MRI
NCT00375830 (9) [back to overview]Cohort 2 - Overall Sensitivity and Accuracy for 18F-NaF/18F-FDG vs Whole-body MRI/99mTc-MDP Bone Scintigraphy
NCT02304757 (4) [back to overview]Bone Turnover Markers
NCT02304757 (4) [back to overview]Health Related Quality of Life by 36-item Short Form Health Status Survey Questionnaire (0-100)
NCT02304757 (4) [back to overview]Percent Change of Bone Mineral Density in Lumbar and Hip
NCT02304757 (4) [back to overview]Side Effects

Cohort 3 - Skeletal Lesions Identified by 99mTc MDP WBBS vs 18F-NaF / 18F-FDG PET/MRI

Participants in Cohort 3 received 99mTc-methylene diphosphonate (MDP) whole-body bone scintigraphy (WBBS) and 18F-sodium fluoride (NaF) / 18F-fluorodeoxyglucose (FDG) positron emission tomography / magnetic imaging resonance (PET/MRI) scans. On the basis of the scans, participants with skeletal lesions were identified. The outcome is reported as the number of Cohort 3 participants for whom skeletal lesions were identified by each scan methodology, a number without dispersion. (NCT00375830)
Timeframe: 30 days

InterventionParticipants (Count of Participants)
Cohort 3 - 99mTc-methyl Diphosphonate (MDP) Bone Scan37
Cohort 3 - 18F-NaF / 18F-FDG PET/MRI45

[back to top]

Cohort 3 - Total Skeletal Lesions Identified, Tc-99m MDP WBBS vs 18F-NaF / 18F-FDG PET/MRI

Participants in Cohort 3 received 99mTc-methylene diphosphonate (MDP) whole-body bone scintigraphy (WBBS) and 18F-sodium fluoride (NaF) / 18F-fluorodeoxyglucose (FDG) positron emission tomography / magnetic imaging resonance (PET/MRI) scans. On the basis of the scans, the total number skeletal lesions identified in the participants was determined. The outcome is reported as the total number skeletal lesions identified by each scan methodology, a number without dispersion. (NCT00375830)
Timeframe: 30 days

Interventionlesions (Number)
Cohort 3 - 99mTc-methyl Diphosphonate (MDP) Bone Scan81
Cohort 3 - 18F-NaF / 18F-FDG PET/MRI140

[back to top]

Cohort 1 - 18F-NaF PET/CT vs 18F-FDG PET/CT

The medical value of 18F-sodium fluoride (NaF) positron emission tomography / computed tomography (PET/CT) vs 18F-fluorodeoxyglucose (FDG) positron emission tomography / computed tomography (PET/CT) was assessed on the basis of the radiation oncologist's medical assessment of image quality and detected extent of disease, for each participant diagnosed with osseous (skeletal) metastases. Per protocol, the data were collected and the outcome is reported for Cohort 1 only. The outcome is reported as the number of participants for whom the medical value of the image was superior for 18-NaF PET/CT compared to 18F-FDG PET/CT, the same between both scans, or inferior for 18-NaF PET/CT compared to 18F-FDG PET/CT. The outcome result is represented as a number without dispersion. (NCT00375830)
Timeframe: 30 days

InterventionParticipants (Count of Participants)
18F-NaF > 18F-FDG18F-NaF = 18F-FDG18F-NaF < 18F-FDG
Cohort 1 Pilot-WB-MRI & Combined 18F-NaF-CT/18F-FDG-PET Scans300

[back to top]

Cohort 1 - NaF PET/CT vs 99mTc-MDP Bone Scintigraphy

"The medical value of 18F-sodium fluoride (NaF) positron emission tomography / computed tomography (PET/CT) vs 99mTc-methylene diphosphonate (MDP) bone scintigraphy was assessed on the basis of the radiation oncologist's medical assessment of image quality and detected extent of disease, for each participant. Per protocol, the data were collected and the outcome is reported for Cohort 1 only. The outcome is reported as the number of participants for whom the medical value of the image was superior for 18F-NaF vs 99mTc-MDP bone scintigraphy (18F-NaF > 99mTc-MDP), the same between both scans (18F-NaF = 99mTc-MDP), or inferior for 18F-NaF vs 99mTc-MDP bone scintigraphy (18F-NaF < 99mTc-MDP)." (NCT00375830)
Timeframe: 30 days

InterventionParticipants (Count of Participants)
18F-NaF > 99mTc-MDP18F-NaF = 99mTc-MDP18F-NaF < 99mTc-MDP
Cohort 1 Pilot-WB-MRI & Combined 18F-NaF-CT/18F-FDG-PET Scans1000

[back to top]

Cohort 2 - 18F-NaF/18F-FDG PET/CT vs Whole-body MRI for Detection of Extraskeletal Lesions

"Sensitivity; positive predictive value (PPV); and accuracy for the detection of extraskeletal lesions was assessed for 18F-sodium fluoride (NaF) / 18F-fluorodeoxyglucose (FDG) positron emission tomography / computed tomography (PET/CT) and for whole body magnetic imaging resonance (WB-MRI).~Sensitivity is a percentage that defines the proportion of true positive participants with the disease in a total group of participants.~PPV is the probability that participants with a positive screening test truly have the disease.~Accuracy is the proportion of true results (both true positives and true negatives) among the total number of cases examined.~Per protocol, the data were collected and the outcome is reported for Cohort 2 only. Sensitivity, PPV, and accuracy are reported as a percentage, a number without dispersion. Higher numbers represent better detection." (NCT00375830)
Timeframe: 30 days

,
Interventionpercentage of particpants (Number)
SensitivityPositive predictive valueAccuracy
Cohort 2 - Combined 18F-NaF-CT/18F-FDG-PET Scan92.981.376.5
Cohort 2 - Whole Body-MRI Scan92.986.782.4

[back to top]

Cohort 2 - 18F-NaF/18F-FDG vs 99mTc-MDP Bone Scintigraphy for Detection of Skeletal Lesions

Sensitivity and accuracy for the detection of skeletal lesions was assessed for 18F-sodium fluoride (NaF) / 18F-fluorodeoxyglucose (FDG) positron emission tomography / computed tomography (PET/CT) and for 99mTc-methylene diphosphonate (MDP) bone scintigraphy. Per protocol, the data were collected and the outcome is reported for Cohort 2 only. Sensitivity and accuracy are reported as a percentage, a number without dispersion. Higher numbers represent better detection. (NCT00375830)
Timeframe: 30 days

,
Interventionpercentage of participants (Number)
SensitivityAccuracy
Cohort 2 - 99mTc-MDP Bone Scintigraphy Scan64.665.9
Cohort 2 Combined 18F-NaF-CT/18F-FDG-PET Scan96.289.8

[back to top]

Cohort 2 - 18F-NaF/18F-FDG vs Whole-body MRI for Detection of Skeletal Lesions

Sensitivity and accuracy for the detection of skeletal lesions was assessed for 18F-sodium fluoride (NaF) / 18F-fluorodeoxyglucose (FDG) positron emission tomography / computed tomography (PET/CT) and for whole body magnetic imaging resonance (WB-MRI). Per protocol, the data were collected and the outcome is reported for Cohort 2 only. Sensitivity and accuracy are reported as a percentage, a number without dispersion. Higher numbers represent better detection. (NCT00375830)
Timeframe: 30 days

,
Interventionpercentage of particpants (Number)
SensitivityAccuracy
Cohort 2 - Combined 18F-NaF-CT/18F-FDG-PET Scan96.289.8
Cohort 2 - WB-MRI Scan81.474.7

[back to top]

Cohort 2 - Overall Sensitivity and Accuracy for 18F-NaF/18F-FDG vs Whole-body MRI

Overall sensitivity and accuracy for the detection of tumor lesions was assessed for 18F-sodium fluoride (NaF) / 18F-fluorodeoxyglucose (FDG) positron emission tomography / computed tomography (PET/CT) and for whole body magnetic imaging resonance (WB-MRI). Per protocol, the data were collected and the outcome is reported for Cohort 2 only. Sensitivity and accuracy are reported as a percentage, a number without dispersion. Higher numbers represent better detection. (NCT00375830)
Timeframe: 30 days

,
Interventionpercentage of participants (Number)
SensitivityAccuracy
Cohort 2 - Combined 18F-NaF-CT/18F-FDG-PET Scan95.787.6
Cohort 2 - Whole Body Magnetic Resonance Imaging (WB-MRI) Scan83.376.0

[back to top]

Cohort 2 - Overall Sensitivity and Accuracy for 18F-NaF/18F-FDG vs Whole-body MRI/99mTc-MDP Bone Scintigraphy

Overall sensitivity and accuracy for the detection of tumor lesions was assessed for 18F-sodium fluoride (NaF) / 18F-fluorodeoxyglucose (FDG) positron emission tomography / computed tomography (PET/CT) and for 99mTc-methylene diphosphonate (MDP) bone scintigraphy. Per protocol, the data were collected and the outcome is reported for Cohort 2 only. Sensitivity and accuracy are reported as a percentage, a number without dispersion. Higher numbers represent better detection. (NCT00375830)
Timeframe: 30 days

,
Interventionpercentage of participants (Number)
SensitivityAccuracy
Cohort 2 Combined 18F-NaF-CT/18F-FDG-PET Scan95.787.6
Cohort 2 WB-MRI & 99mTc-MDP Bone Scintigraphy91.683.0

[back to top]

Bone Turnover Markers

bone turnover markers including C-telopeptides of type I collagen (CTX), Type I N-procollagen terminal propeptide(PINP) (NCT02304757)
Timeframe: baseline and 12 months

,
Interventionng/ml (Mean)
PINP before treatmentPINP at 12monthsCTX before treatmentCTX at 12months
99Tc-MDP43.772552.64220.46570.3707
Fosamax29.25520.561230.15260.1771

[back to top] [back to top]

Percent Change of Bone Mineral Density in Lumbar and Hip

Percent change of bone mineral density in lumbar and hip by dual energy x-ray absorptiometry (NCT02304757)
Timeframe: baseline, 6 months, and 12 months

,
Interventionpercentage change (Mean)
Percentage change of lumbar spine at month 6Percentage change of lumbar spine month 12Percentage change of total hip at month 6Percentage change of total hip at month 12
99Tc-MDP3.03.80.95.1
Fosamax3.25.14.94.6

[back to top]

Side Effects

A transient rash and phlebitis, gastrointestinal reaction. (NCT02304757)
Timeframe: 6 months, and 12 months

,
Interventionside effects (Number)
abdominal paindyspepsia
99Tc-MDP00
Fosamax24

[back to top]