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Identification
NameRisedronate
Accession NumberDB00884  (APRD00410, DB02782)
TypeSmall Molecule
GroupsApproved, Investigational
Description

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

Structure
Thumb
Synonyms
SynonymLanguageCode
Acide risédroniqeFrenchOS: DCF
Acido risedronicoSpanishNot Available
Acidum risedronicumLatinNot Available
RidronNot AvailableNot Available
RisedronateNot AvailableNot Available
Risedronic acidNot AvailableOS: BAN
RisedronsäureGermanNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Actoneltablet, film coated30 mgoralWarner Chilcott Pharmaceuticals Inc.1998-03-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Actoneltablet, film coated5 mgoralWarner Chilcott Pharmaceuticals Inc.2000-04-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Actoneltablet, film coated35 mgoralWarner Chilcott Pharmaceuticals Inc.2002-05-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Actoneltablet, film coated150 mgoralWarner Chilcott Pharmaceuticals Inc.2008-04-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Actoneltablet, film coated25.8; 4.2 mg/1; mgoralWarner Chilcott (US), LLC1998-03-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Actoneltablet, film coated4.3; .7 mg/1; mgoralWarner Chilcott (US), LLC2000-04-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Actoneltablet, film coated30.1; 4.9 mg/1; mgoralWarner Chilcott (US), LLC2002-05-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Actoneltablet, film coated129; 21 mg/1; mgoralWarner Chilcott (US), LLC2008-04-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Atelviatablet, delayed release30.1; 4.9 mg/1; mgoralWarner Chilcott (US), LLC2010-12-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Risedronate Sodiumtablet, film coated129; 21 mg/1; mgoralActavis Pharma, Inc.2014-06-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Risedronate Sodiumtablet, film coated64.5; 10.5 mg/1; mgoralActavis Pharma, Inc.2014-06-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Risedronate Sodiumtablet, film coated30.1; 4.9 mg/1; mgoralActavis Pharma, Inc.2014-06-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Risedronate Sodiumtablet, film coated4.3; .7 mg/1; mgoralActavis Pharma, Inc.2014-06-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Risedronate Sodiumtablet, film coated25.8; 4.2 mg/1; mgoralActavis Pharma, Inc.2014-06-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Actoneltablet, film coated5 mgoralPhysicians Total Care, Inc.2002-03-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Actoneltablet, film coated35 mgoralPhysicians Total Care, Inc.2002-09-16Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Actoneltablet, film coated150 mgoralPhysicians Total Care, Inc.2009-10-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Actoneltablet30 mgoralWarner Chilcott Canada CoNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Actoneltablet5 mgoralWarner Chilcott Canada CoNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Actoneltablet35 mgoralWarner Chilcott Canada CoNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Actoneltablet75 mgoralWarner Chilcott Canada CoNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Actoneltablet150 mgoralWarner Chilcott Canada CoNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Risedronate Sodiumtablet, film coated150 mgoralMylan Pharmaceuticals Inc.2014-06-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Risedronate Sodiumtablet, film coated75 mgoralMylan Pharmaceuticals Inc.2014-06-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Risedronate Sodiumtablet, film coated75 mgoralSun Pharma Global FZE2014-06-11Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Risedronate Sodiumtablet, film coated150 mgoralSun Pharma Global FZE2014-06-11Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Risedronate Sodiumtablet, film coated75 mgoralApotex Corp.2014-06-11Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Risedronate Sodiumtablet, film coated150 mgoralApotex Corp.2014-06-11Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Risedronatetablet35 mgoralPro Doc LimiteeNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Risedronatetablet35 mgoralSivem Pharmaceuticals UlcNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Risedronatetablet35 mgoralSanis Health IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Over the Counter ProductsNot Available
International Brands
NameCompany
BenetTakeda
Brand mixtures
Brand NameIngredients
Actonal Plus Calcium (Warner Chilcott)risedronate sodium hemi-pentahydrate + calcium carbonate
Actonel with Calcium (Procter & Gamble)risedronate sodium + calcium carbonate
Salts
Name/CASStructureProperties
Risedronate sodium
Thumb
  • InChI Key: DRFDPXKCEWYIAW-UHFFFAOYNA-M
  • Monoisotopic Mass: 304.983019378
  • Average Mass: 305.0941
DBSALT000494
Categories
CAS number105462-24-6
WeightAverage: 283.1123
Monoisotopic: 283.001074735
Chemical FormulaC7H11NO7P2
InChI KeyIIDJRNMFWXDHID-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
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassOrganophosphorus compounds
ClassOrganic phosphonic acids and derivatives
Sub ClassBisphosphonates
Direct ParentBisphosphonates
Alternative Parents
Substituents
  • Bisphosphonate
  • Pyridine
  • Heteroaromatic compound
  • Organophosphonic acid
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of Paget's disease of the bone (osteitis deformans), postmenopausal and glucocorticoid-induced osteoporosis
PharmacodynamicsRisedronate 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 actionThe 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.
AbsorptionRapid 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 eliminationRisedronate is excreted unchanged primarily via the kidney. Insignificant amounts (<0.1% of intravenous dose) of drug are excreted in the bile in rats.
Half life1.5 hours
Clearance
  • 122 mL/min
  • 73 mL/min [osteopenic postmenopausal women]
ToxicitySide 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 substrateNon-inhibitor0.8792
CYP450 2D6 substrateNon-inhibitor0.9062
CYP450 2C19 substrateNon-inhibitor0.8777
CYP450 3A4 substrateNon-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
Pharmacoeconomics
Manufacturers
  • Warner chilcott co llc
  • Teva pharmaceuticals usa
  • Procter & Gamble
Packagers
Dosage forms
FormRouteStrength
Tabletoral150 mg
Tabletoral30 mg
Tabletoral35 mg
Tabletoral5 mg
Tabletoral75 mg
Tablet, delayed releaseoral30.1; 4.9 mg/1; mg
Tablet, film coatedoral129; 21 mg/1; mg
Tablet, film coatedoral150 mg
Tablet, film coatedoral25.8; 4.2 mg/1; mg
Tablet, film coatedoral30 mg
Tablet, film coatedoral30.1; 4.9 mg/1; mg
Tablet, film coatedoral35 mg
Tablet, film coatedoral4.3; .7 mg/1; mg
Tablet, film coatedoral5 mg
Tablet, film coatedoral64.5; 10.5 mg/1; mg
Tablet, film coatedoral75 mg
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
CountryPatent NumberApprovedExpires (estimated)
Canada22945952001-08-212018-07-17
Canada23999762007-03-272021-02-01
United States60963421994-11-222011-11-22
United States71929382003-11-062023-11-06
Properties
StateSolid
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 FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot 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 ReferenceNot Available
External Links
ATC CodesM05BA07
AHFS Codes
  • 92:00.00
PDB Entries
FDA labelDownload (1.52 MB)
MSDSDownload (57 KB)
Interactions
Drug Interactions
Drug
Aluminum hydroxideMay decrease the serum concentration of Bisphosphonate Derivatives.
AmikacinMay enhance the hypocalcemic effect of Bisphosphonate Derivatives.
AmobarbitalBarbiturates may increase the metabolism of Calcium Channel Blockers.
ArbekacinMay enhance the hypocalcemic effect of Bisphosphonate Derivatives.
AtracuriumMay enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).
ButabarbitalBarbiturates may increase the metabolism of Calcium Channel Blockers.
ButalbitalBarbiturates may increase the metabolism of Calcium Channel Blockers.
Calcium AcetateCalcium Salts may diminish the therapeutic effect of Calcium Channel Blockers.
Calcium carbonateMay decrease the serum concentration of Bisphosphonate Derivatives.
Calcium ChlorideCalcium Salts may diminish the therapeutic effect of Calcium Channel Blockers.
CimetidineCimetidine may increase the serum concentration of Calcium Channel Blockers.
Cisatracurium BesylateMay enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).
ClarithromycinMacrolide Antibiotics may decrease the metabolism of Calcium Channel Blockers.
ClopidogrelMay diminish the therapeutic effect of Clopidogrel. Exceptions: Clevidipine.
DeferasiroxBisphosphonate Derivatives may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased.
DoxazosinAlpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers.
EsomeprazoleProton Pump Inhibitors may diminish the therapeutic effect of Risedronate. Proton Pump Inhibitors may increase the serum concentration of Risedronate. This applies specifically to use of delayed-release risedronate.
FamotidineH2-Antagonists may increase the serum concentration of Risedronate. This applies specifically to delayed-release risedronate.
FluconazoleFluconazole may increase the serum concentration of Calcium Channel Blockers. Exceptions: Clevidipine.
FosphenytoinMay increase the serum concentration of Fosphenytoin.
FramycetinMay enhance the hypocalcemic effect of Bisphosphonate Derivatives.
GentamicinMay enhance the hypocalcemic effect of Bisphosphonate Derivatives.
ItraconazoleAntifungal Agents (Azole Derivatives, Systemic) may enhance the adverse/toxic effect of Calcium Channel Blockers. Specifically, itraconazole may enhance the negative inotropic effects of verapamil or diltiazem. Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Calcium Channel Blockers. Fluconazole and isavuconazonium likely exert weaker effects than other azoles and are addressed in separate monographs.
KanamycinMay enhance the hypocalcemic effect of Bisphosphonate Derivatives.
LansoprazoleProton Pump Inhibitors may diminish the therapeutic effect of Risedronate. Proton Pump Inhibitors may increase the serum concentration of Risedronate. This applies specifically to use of delayed-release risedronate.
Magnesium oxideMay decrease the serum concentration of Bisphosphonate Derivatives.
Magnesium salicylateMay enhance the adverse/toxic effect of Magnesium Salts. Magnesium Salts may enhance the hypotensive effect of Calcium Channel Blockers.
MethohexitalBarbiturates may increase the metabolism of Calcium Channel Blockers.
NafcillinNafcillin may increase the metabolism of Calcium Channel Blockers. Exceptions: Clevidipine.
NeomycinMay enhance the hypocalcemic effect of Bisphosphonate Derivatives.
NetilmicinMay enhance the hypocalcemic effect of Bisphosphonate Derivatives.
NitroprussideMay enhance the hypotensive effect of Nitroprusside.
NizatidineH2-Antagonists may increase the serum concentration of Risedronate. This applies specifically to delayed-release risedronate.
OmeprazoleProton Pump Inhibitors may diminish the therapeutic effect of Risedronate. Proton Pump Inhibitors may increase the serum concentration of Risedronate. This applies specifically to use of delayed-release risedronate.
PancuroniumMay enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).
PantoprazoleProton Pump Inhibitors may diminish the therapeutic effect of Risedronate. Proton Pump Inhibitors may increase the serum concentration of Risedronate. This applies specifically to use of delayed-release risedronate.
PentobarbitalBarbiturates may increase the metabolism of Calcium Channel Blockers.
PhenobarbitalBarbiturates may increase the metabolism of Calcium Channel Blockers.
PhenoxybenzamineAlpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers.
PhentolamineAlpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers.
PhenytoinMay increase the serum concentration of Phenytoin.
PosaconazoleAntifungal Agents (Azole Derivatives, Systemic) may enhance the adverse/toxic effect of Calcium Channel Blockers. Specifically, itraconazole may enhance the negative inotropic effects of verapamil or diltiazem. Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Calcium Channel Blockers. Fluconazole and isavuconazonium likely exert weaker effects than other azoles and are addressed in separate monographs.
PrazosinAlpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers.
RabeprazoleProton Pump Inhibitors may diminish the therapeutic effect of Risedronate. Proton Pump Inhibitors may increase the serum concentration of Risedronate. This applies specifically to use of delayed-release risedronate.
RanitidineH2-Antagonists may increase the serum concentration of Risedronate. This applies specifically to delayed-release risedronate.
RibostamycinMay enhance the hypocalcemic effect of Bisphosphonate Derivatives.
RifampicinRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
RifapentineRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
RocuroniumMay enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).
SecobarbitalBarbiturates may increase the metabolism of Calcium Channel Blockers.
SilodosinAlpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers.
SpectinomycinMay enhance the hypocalcemic effect of Bisphosphonate Derivatives.
StreptomycinMay enhance the hypocalcemic effect of Bisphosphonate Derivatives.
SulfisoxazoleMacrolide Antibiotics may decrease the metabolism of Calcium Channel Blockers.
TamsulosinAlpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers.
TelithromycinMacrolide Antibiotics may decrease the metabolism of Calcium Channel Blockers.
TerazosinAlpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers.
TobramycinMay enhance the hypocalcemic effect of Bisphosphonate Derivatives.
VecuroniumMay enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).
VoriconazoleAntifungal Agents (Azole Derivatives, Systemic) may enhance the adverse/toxic effect of Calcium Channel Blockers. Specifically, itraconazole may enhance the negative inotropic effects of verapamil or diltiazem. Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Calcium Channel Blockers. Fluconazole and isavuconazonium likely exert weaker effects than other azoles and are addressed in separate monographs.
Food InteractionsNot Available

Targets

1. Farnesyl pyrophosphate synthase

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Farnesyl pyrophosphate synthase P14324 Details

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
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  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
  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
  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
  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

2. Hydroxylapatite

Kind: small molecule

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details

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. Pubmed
  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

Enzymes

1. Prostaglandin G/H synthase 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Prostaglandin G/H synthase 2 P35354 Details

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. Epub 2010 Aug 25. Pubmed

Comments
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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:12