Identification

Name
Risedronate
Accession Number
DB00884  (APRD00410, DB02782)
Type
Small Molecule
Groups
Approved, Investigational
Description

Risedronate is a bisphosphonate used to strengthen bone, treat or prevent osteoporosis, and treat Paget's disease of bone.

Structure
Thumb
Synonyms
  • Acide risédroniqe
  • Acido risedronico
  • Acidum risedronicum
  • Ridron
  • Risedronate
  • Risedronic acid
  • Risedronsäure
External IDs
M05BA07 / NE-58095
Product Ingredients
IngredientUNIICASInChI Key
Risedronate sodiumOFG5EXG60L115436-72-1DRFDPXKCEWYIAW-UHFFFAOYSA-M
Risedronate sodium hemi-pentahydrateHU2YAQ274O329003-65-8HYFDYHPNTXOPPO-UHFFFAOYSA-L
Risedronate sodium monohydrateF67L43UT5C353228-19-0KLQNARDFMJRXSF-UHFFFAOYSA-M
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ActonelTablet, film coated150 mg/1OralPhysicians Total Care, Inc.2009-10-05Not applicableUs
ActonelTablet35 mgOralAllergan Pharma Co.2002-12-10Not applicableCanada
ActonelTablet, film coated5 mg/1OralWarner Chilcott2000-04-14Not applicableUs
ActonelTablet, film coated75 mg/1OralWarner Chilcott2007-04-162010-03-31Us
ActonelTablet, film coated35 mg/1OralPhysicians Total Care, Inc.2002-09-16Not applicableUs
ActonelTablet5 mgOralAllergan Pharma Co.2000-07-25Not applicableCanada
ActonelTablet75 mgOralWarner Chilcott2007-08-132016-08-05Canada
ActonelTablet, film coated30 mg/1OralWarner Chilcott1998-03-27Not applicableUs
ActonelTablet, film coated150 mg/1OralWarner Chilcott2008-04-22Not applicableUs
ActonelTablet, film coated5 mg/1OralPhysicians Total Care, Inc.2002-03-15Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-risedronateTablet150 mgOralApotex Corporation2012-05-17Not applicableCanada
Apo-risedronateTablet35 mgOralApotex Corporation2010-11-10Not applicableCanada
Auro-risedronateTablet5 mgOralAuro Pharma IncNot applicableNot applicableCanada
Auro-risedronateTablet150 mgOralAuro Pharma Inc2016-04-13Not applicableCanada
Auro-risedronateTablet30 mgOralAuro Pharma IncNot applicableNot applicableCanada
Auro-risedronateTablet35 mgOralAuro Pharma Inc2013-07-08Not applicableCanada
Dom-risedronateTablet35 mgOralDominion Pharmacal2011-04-19Not applicableCanada
Jamp-risedronateTablet35 mgOralJamp Pharma Corporation2011-10-04Not applicableCanada
Mylan-risedronateTablet35 mgOralMylan Pharmaceuticals2011-06-16Not applicableCanada
Mylan-risedronateTablet150 mgOralMylan Pharmaceuticals2013-09-30Not applicableCanada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
ActonelRisedronate sodium hemi-pentahydrate (30.1 mg/1) + Risedronate sodium monohydrate (4.9 mg/1)Tablet, film coatedOralAllergan2002-05-17Not applicableUs00430 0472 03 nlmimage10 08400400
ActonelRisedronate sodium hemi-pentahydrate (25.8 mg/1) + Risedronate sodium monohydrate (4.2 mg/1)Tablet, film coatedOralAllergan1998-03-27Not applicableUs
ActonelRisedronate sodium hemi-pentahydrate (4.3 mg/1) + Risedronate sodium monohydrate (0.7 mg/1)Tablet, film coatedOralAllergan2000-04-14Not applicableUs
ActonelRisedronate sodium hemi-pentahydrate (64.5 mg/1) + Risedronate sodium monohydrate (10.5 mg/1)Tablet, film coatedOralAllergan2007-04-162010-03-31Us
ActonelRisedronate sodium hemi-pentahydrate (30.1 mg/1) + Risedronate sodium monohydrate (4.9 mg/1)Tablet, film coatedOralAllergan2002-05-17Not applicableUs00430 0472 03 nlmimage10 08400400
ActonelRisedronate sodium hemi-pentahydrate (129 mg/1) + Risedronate sodium monohydrate (21 mg/1)Tablet, film coatedOralAllergan2008-04-22Not applicableUs
ActonelRisedronate sodium hemi-pentahydrate (64.5 mg/1) + Risedronate sodium monohydrate (10.5 mg/1)Tablet, film coatedOralAllergan2007-04-162010-03-31Us
ActonelRisedronate sodium hemi-pentahydrate (25.8 mg/1) + Risedronate sodium monohydrate (4.2 mg/1)Tablet, film coatedOralAllergan1998-03-27Not applicableUs
ActonelRisedronate sodium hemi-pentahydrate (4.3 mg/1) + Risedronate sodium monohydrate (0.7 mg/1)Tablet, film coatedOralAllergan2000-04-14Not applicableUs
ActonelRisedronate sodium hemi-pentahydrate (129 mg/1) + Risedronate sodium monohydrate (21 mg/1)Tablet, film coatedOralAllergan2008-04-22Not applicableUs
International/Other Brands
Benet (Takeda )
Categories
UNII
KM2Z91756Z
CAS number
105462-24-6
Weight
Average: 283.1123
Monoisotopic: 283.001074735
Chemical Formula
C7H11NO7P2
InChI Key
IIDJRNMFWXDHID-UHFFFAOYSA-N
InChI
InChI=1S/C7H11NO7P2/c9-7(16(10,11)12,17(13,14)15)4-6-2-1-3-8-5-6/h1-3,5,9H,4H2,(H2,10,11,12)(H2,13,14,15)
IUPAC Name
[1-hydroxy-1-phosphono-2-(pyridin-3-yl)ethyl]phosphonic acid
SMILES
OC(CC1=CN=CC=C1)(P(O)(O)=O)P(O)(O)=O

Pharmacology

Indication

For the treatment of Paget's disease of the bone (osteitis deformans), postmenopausal and glucocorticoid-induced osteoporosis

Associated Conditions
Pharmacodynamics

Risedronate is a pyridinyl bisphosphonate that inhibits osteoclast-mediated bone resorption and modulates bone metabolism and is indicated for the treatment and prevention of osteoporosis in postmenopausal women.

Mechanism of action

The action of risedronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Risedronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates (such as pamidronate, alendronate, risedronate, ibandronate and zoledronate) appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass.

TargetActionsOrganism
AFarnesyl pyrophosphate synthase
inhibitor
Human
AHydroxylapatite
antagonist
Human
Absorption

Rapid absorption (~1 hr) after an oral dose, occurs throughout the upper gastrointestinal tract

Volume of distribution
  • 13.8 L/kg
Protein binding

~24%

Metabolism

No evidence found for metabolization of risedronate in humans or mammals

Route of elimination

Risedronate is excreted unchanged primarily via the kidney. Insignificant amounts (<0.1% of intravenous dose) of drug are excreted in the bile in rats.

Half life

1.5 hours

Clearance
  • 122 mL/min
  • 73 mL/min [osteopenic postmenopausal women]
Toxicity

Side effects include abdominal pain, anxiety, back pain, belching, bladder irritation, bone disorders and pain, bronchitis, bursitis, cataracts, chest pain, colitis, constipation, depression, diarrhea, difficulty breathing, dizziness, dry eyes, eye infection, flu-like symptoms, gas, headache, high blood pressure, infection, insomnia, itching, joint disorders and pain, leg cramps, muscle pain, muscle weakness, nausea, neck pain, nerve pain, pain, pneumonia, rash, ringing in ears, sinus problems, sore throat, stomach bleeding, stuffy or runny nose, swelling, tendon problems, tumor, ulcers, urinary tract infection, vertigo, vision problems, and weakness.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Risedronate Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
AceclofenacThe risk or severity of gastrointestinal bleeding can be increased when Aceclofenac is combined with Risedronate.
AcemetacinThe risk or severity of gastrointestinal bleeding can be increased when Acemetacin is combined with Risedronate.
Acetylsalicylic acidThe risk or severity of gastrointestinal bleeding can be increased when Acetylsalicylic acid is combined with Risedronate.
AcipimoxThe risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Risedronate is combined with Acipimox.
AcyclovirThe risk or severity of nephrotoxicity and hypocalcemia can be increased when Acyclovir is combined with Risedronate.
AdefovirThe risk or severity of nephrotoxicity and hypocalcemia can be increased when Adefovir is combined with Risedronate.
Adefovir DipivoxilThe risk or severity of nephrotoxicity and hypocalcemia can be increased when Adefovir Dipivoxil is combined with Risedronate.
AlclofenacThe risk or severity of gastrointestinal bleeding can be increased when Alclofenac is combined with Risedronate.
Alendronic acidThe risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Alendronic acid is combined with Risedronate.
AlmasilateThe serum concentration of Risedronate can be decreased when it is combined with Almasilate.
Food Interactions
Not Available

References

Synthesis Reference

Srinivasa Rao V.N Divvela, Lenin Racha, Sivakumaran Meenakshisunderam, Ramesh Dandala, "Process for the preparation of risedronate sodium hemi-pentahydrate." U.S. Patent US20070173484, issued July 26, 2007.

US20070173484
General References
Not Available
External Links
Human Metabolome Database
HMDB0015022
KEGG Compound
C08233
PubChem Compound
5245
PubChem Substance
46507526
ChemSpider
5055
BindingDB
12576
ChEBI
8869
ChEMBL
CHEMBL923
Therapeutic Targets Database
DAP000658
PharmGKB
PA451255
HET
RIS
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Risedronate
ATC Codes
M05BB02 — Risedronic acid and calcium, sequentialM05BA07 — Risedronic acidM05BB04 — Risedronic acid, calcium and colecalciferol, sequentialM05BB07 — Risedronic acid and colecalciferol
AHFS Codes
  • 92:24.00 — Bone Resorption Inhibitors
PDB Entries
1rqj / 1yhl / 1yq7 / 1yv5 / 2o1o / 2qis / 4kpd / 4kqs / 4n9u / 4ng6
show 6 more
FDA label
Download (1.52 MB)
MSDS
Download (57 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableBioavailability1
1CompletedNot AvailableNon-lactating / One to five years postmenopausal / Surgically Sterile1
1CompletedNot AvailableOsteopenia / Osteoporosis1
1CompletedNot AvailableOsteoporosis1
1, 2CompletedOtherCognitive Changes / Memory Losses / Postmenopausal Syndrome1
2CompletedBasic ScienceOsteogenesis Imperfecta1
2CompletedTreatmentPostmenopausal Osteoporosis (PMO)2
2CompletedTreatmentPostmenopausal Women1
2CompletedTreatmentOne to five years postmenopausal1
2, 3Active Not RecruitingTreatmentInvolutional Osteoporosis1
2, 3CompletedTreatmentAnorexia Nervosa (AN)1
2, 3CompletedTreatmentInvolutional Osteoporosis1
2, 3Unknown StatusTreatmentFibrous Dysplasia of Bone1
3Active Not RecruitingTreatmentOsteopenia1
3CompletedDiagnosticCancer, Breast / Osteoporosis1
3CompletedPreventionOsteopenia1
3CompletedPreventionPostmenopausal Osteoporosis (PMO)1
3CompletedPreventionProstate Cancer1
3CompletedPreventionSpinal Cord Injury, Acute1
3CompletedSupportive CareCancer, Breast / Osteoporosis1
3CompletedSupportive CareOsteoporosis / Prostate Cancer1
3CompletedTreatmentBack Pain / Postmenopausal Osteoporosis (PMO) / Vertebral Fractures1
3CompletedTreatmentCancer, Breast / Menopause / Osteopenia1
3CompletedTreatmentGlucocorticoid-induced Ostepor / Steroid-induced Osteopor / Steroid-induced Osteopor, Glucocorticoid-induced Ostepor / Steroid-induced Osteopor., Glucocorticoid-induced Ostepor1
3CompletedTreatmentLeukemias / Malignant Lymphomas1
3CompletedTreatmentOsteogenesis Imperfecta1
3CompletedTreatmentOsteoporosis7
3CompletedTreatmentOther Osteoporosis1
3CompletedTreatmentPaget's Disease of Bone2
3CompletedTreatmentPostmenopausal Osteoporosis (PMO)5
3CompletedTreatmentPostmenopausal Women Osteoporosis1
3CompletedTreatmentPostmenopausal Women With Osteoporosis1
3TerminatedPreventionMetastatic Hormone Refractory Prostate Cancer1
3TerminatedTreatmentProsthesis Loosening1
3WithdrawnSupportive CareCancer, Breast / Osteoporosis1
4CompletedNot AvailableCrohn's Disease (CD) / Low Bone Mineral Density1
4CompletedNot AvailableOsteoporosis1
4CompletedPreventionBone Loss / Cancer, Breast / Osteoporosis1
4CompletedPreventionBone Loss / Epilepsies / Fracture Bone / Osteoporosis1
4CompletedPreventionCystic Fibrosis (CF) / Muscular Dystrophy / Osteoporosis1
4CompletedPreventionPostmenopausal Osteoporosis (PMO)1
4CompletedTreatmentBone Loss1
4CompletedTreatmentCancer, Breast1
4CompletedTreatmentColles' Fracture1
4CompletedTreatmentOsteoporosis4
4CompletedTreatmentPostmenopausal Osteoporosis (PMO)7
4CompletedTreatmentProstate Cancer1
4RecruitingSupportive CareBariatric Surgery Candidate / Bone Loss / Obese experiencing rapid weight loss1
4RecruitingTreatmentFracture of Neck of Femur / Osteoporotic Fractures1
4TerminatedPreventionPostmenopausal Osteoporosis (PMO)1
4TerminatedTreatmentOsteoporosis2
4Unknown StatusPreventionPeriodontal Diseases1
4Unknown StatusTreatmentOsteoporosis1
Not AvailableActive Not RecruitingTreatmentAnorexia Nervosa (AN) / Osteopenia / Osteoporosis1
Not AvailableCompletedNot AvailableAdenocarcinomas / Esophageal Cancers / Squamous Cell Carcinoma (SCC)1
Not AvailableCompletedNot AvailableOsseous Paget's Disease1
Not AvailableCompletedNot AvailableOsteoporosis2
Not AvailableCompletedPreventionHip Fractures1
Not AvailableCompletedPreventionOsteoporosis1
Not AvailableEnrolling by InvitationNot AvailableAtypical Femoral Fractures / Bisphosphonate Therapy / Osteoporosis1
Not AvailableTerminatedTreatmentOsteopenia1

Pharmacoeconomics

Manufacturers
  • Warner chilcott co llc
  • Teva pharmaceuticals usa
  • Procter & Gamble
Packagers
  • Diversified Healthcare Services Inc.
  • Lake Erie Medical and Surgical Supply
  • Murfreesboro Pharmaceutical Nursing Supply
  • Norwich Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Procter & Gamble
  • Resource Optimization and Innovation LLC
  • Stat Rx Usa
  • Warner Chilcott Co. Inc.
  • WC Pharmaceuticals
Dosage forms
FormRouteStrength
TabletOral75 mg
Tablet, film coatedOral150 mg/1
Tablet, film coatedOral30 mg/1
Tablet, film coatedOral35 mg/1
Tablet, film coatedOral5 mg/1
Tablet, film coatedOral75 mg/1
Tablet, delayed releaseOral35 mg
Granule, effervescent; kit; tabletOral
Kit
TabletOral150 mg
TabletOral
Tablet, delayed releaseOral
Tablet, delayed releaseOral35 mg/1
Tablet, film coatedOral
TabletOral30 mg
TabletOral35 mg
TabletOral5 mg
Kit; tabletOral
Prices
Unit descriptionCostUnit
Actonel 150 mg tablet125.1USD tablet
Actonel 4 35 mg tablet Disp Pack119.43USD disp
Actonel 75 mg tablet54.83USD tablet
Actonel 30 mg tablet29.32USD tablet
Actonel 35 mg tablet28.75USD tablet
Actonel 5 mg tablet4.13USD tablet
Actonel with calcium tablet3.92USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6096342No2000-08-012011-11-22Us
CA2294595No2001-08-212018-07-17Canada
CA2399976No2007-03-272021-02-01Canada
US7192938Yes2007-03-202023-11-06Us
US7718634Yes2010-05-182023-11-06Us
US6165513Yes2000-12-262018-12-10Us
US5994329Yes1999-11-302019-01-17Us
US6015801Yes2000-01-182019-01-17Us
US6432932Yes2002-08-132019-01-17Us
US6465443Yes2002-10-152019-02-14Us
US7645459No2010-01-122028-01-09Us
US7645460No2010-01-122028-01-09Us
US8246989No2012-08-212026-01-16Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP-3.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility10.4 mg/mLALOGPS
logP-0.75ALOGPS
logP-3.3ChemAxon
logS-1.4ALOGPS
pKa (Strongest Acidic)0.68ChemAxon
pKa (Strongest Basic)4.91ChemAxon
Physiological Charge-2ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count5ChemAxon
Polar Surface Area148.18 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity57.12 m3·mol-1ChemAxon
Polarizability21.91 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.9357
Blood Brain Barrier+0.9172
Caco-2 permeable-0.6795
P-glycoprotein substrateNon-substrate0.6846
P-glycoprotein inhibitor INon-inhibitor0.9582
P-glycoprotein inhibitor IINon-inhibitor1.0
Renal organic cation transporterNon-inhibitor0.9542
CYP450 2C9 substrateNon-substrate0.8452
CYP450 2D6 substrateNon-substrate0.8162
CYP450 3A4 substrateNon-substrate0.7208
CYP450 1A2 substrateNon-inhibitor0.8778
CYP450 2C9 inhibitorNon-inhibitor0.8792
CYP450 2D6 inhibitorNon-inhibitor0.9062
CYP450 2C19 inhibitorNon-inhibitor0.8777
CYP450 3A4 inhibitorNon-inhibitor0.9068
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.989
Ames testNon AMES toxic0.7663
CarcinogenicityNon-carcinogens0.8386
BiodegradationNot ready biodegradable0.5058
Rat acute toxicity2.1053 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9095
hERG inhibition (predictor II)Non-inhibitor0.9303
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as bisphosphonates. These are organic compounds containing two phosphonate groups linked together through a carbon atoms.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Organic phosphonic acids and derivatives
Sub Class
Bisphosphonates
Direct Parent
Bisphosphonates
Alternative Parents
Pyridines and derivatives / Organic phosphonic acids / Heteroaromatic compounds / Azacyclic compounds / Organopnictogen compounds / Organophosphorus compounds / Organooxygen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives
Substituents
Bisphosphonate / Pyridine / Heteroaromatic compound / Organophosphonic acid / Azacycle / Organoheterocyclic compound / Organic nitrogen compound / Organic oxygen compound / Organopnictogen compound / Organic oxide
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
pyridines (CHEBI:8869)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Poly(a) rna binding
Specific Function
Key enzyme in isoprenoid biosynthesis which catalyzes the formation of farnesyl diphosphate (FPP), a precursor for several classes of essential metabolites including sterols, dolichols, carotenoids...
Gene Name
FDPS
Uniprot ID
P14324
Uniprot Name
Farnesyl pyrophosphate synthase
Molecular Weight
48275.03 Da
References
  1. Bergstrom JD, Bostedor RG, Masarachia PJ, Reszka AA, Rodan G: Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000 Jan 1;373(1):231-41. [PubMed:10620343]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  3. Coxon FP, Ebetino FH, Mules EH, Seabra MC, McKenna CE, Rogers MJ: Phosphonocarboxylate inhibitors of Rab geranylgeranyl transferase disrupt the prenylation and membrane localization of Rab proteins in osteoclasts in vitro and in vivo. Bone. 2005 Sep;37(3):349-58. [PubMed:16006204]
  4. Dunford JE, Thompson K, Coxon FP, Luckman SP, Hahn FM, Poulter CD, Ebetino FH, Rogers MJ: Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates. J Pharmacol Exp Ther. 2001 Feb;296(2):235-42. [PubMed:11160603]
  5. Ortiz-Gomez A, Jimenez C, Estevez AM, Carrero-Lerida J, Ruiz-Perez LM, Gonzalez-Pacanowska D: Farnesyl diphosphate synthase is a cytosolic enzyme in Leishmania major promastigotes and its overexpression confers resistance to risedronate. Eukaryot Cell. 2006 Jul;5(7):1057-64. [PubMed:16835450]
  6. Russell RG, Xia Z, Dunford JE, Oppermann U, Kwaasi A, Hulley PA, Kavanagh KL, Triffitt JT, Lundy MW, Phipps RJ, Barnett BL, Coxon FP, Rogers MJ, Watts NB, Ebetino FH: Bisphosphonates: an update on mechanisms of action and how these relate to clinical efficacy. Ann N Y Acad Sci. 2007 Nov;1117:209-57. [PubMed:18056045]
Kind
Small molecule
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
References
  1. Jahnke W, Henry C: An in vitro assay to measure targeted drug delivery to bone mineral. ChemMedChem. 2010 May 3;5(5):770-6. doi: 10.1002/cmdc.201000016. [PubMed:20209564]
  2. Nancollas GH, Tang R, Phipps RJ, Henneman Z, Gulde S, Wu W, Mangood A, Russell RG, Ebetino FH: Novel insights into actions of bisphosphonates on bone: differences in interactions with hydroxyapatite. Bone. 2006 May;38(5):617-27. Epub 2005 Jul 20. [PubMed:16046206]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inducer
General Function
Prostaglandin-endoperoxide synthase activity
Specific Function
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and...
Gene Name
PTGS2
Uniprot ID
P35354
Uniprot Name
Prostaglandin G/H synthase 2
Molecular Weight
68995.625 Da
References
  1. Valenti MT, Giannini S, Donatelli L, Zanatta M, Bertoldo F, Sella S, Vilei MT, Ossi E, Realdi G, Lo Cascio V, Dalle Carbonare L: The effect of risedronate on osteogenic lineage is mediated by cyclooxygenase-2 gene upregulation. Arthritis Res Ther. 2010;12(4):R163. doi: 10.1186/ar3122. Epub 2010 Aug 25. [PubMed:20738860]

Drug created on June 13, 2005 07:24 / Updated on November 17, 2018 07:27