Identification
- Summary
Alendronic acid is a bisphosphonate drug that prevents osteoclastic bone resorption which is used for the prevention and treatment of osteoporosis.
- Brand Names
- Adrovance, Binosto, Fosamax, Fosamax Plus D, Fosavance
- Generic Name
- Alendronic acid
- DrugBank Accession Number
- DB00630
- Background
Alendronic acid is a second generation bisphosphonate that is used for the treatment of some forms of osteoperosis and Paget's diseaseLabel1,5. It functions by preventing resorption of boneLabel1.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Alendronic acid (DB00630)
- Weight
- Average: 249.096
Monoisotopic: 249.016724799 - Chemical Formula
- C4H13NO7P2
- Synonyms
- (4-amino-1-hydroxybutane-1,1-diyl)bis(phosphonic acid)
- (4-amino-1-hydroxybutylidene)bisphosphonic acid
- 4-amino-1-hydroxybutane-1,1-diphosphonic acid
- ABDP
- Acide Alendronique
- Acido Alendronico
- Acidum Alendronicum
- Alendronate
- Alendronic acid
- External IDs
- G 704650
- GTH 4
- L 670
- L 670452
- MK 217
Pharmacology
- Indication
Alendronic acid is indicated for the treatment and prevention of osteoporosis in men and postmenopausal women, treatment of glucocorticoid-induced osteoporosis, and Paget's disease of boneLabel1,2. However, alendronic acid is not indicated for use in pediatric populations or patients with a creatinine clearance <35mL/minLabel.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Osteogenesis imperfecta ••• ••••• Used in combination to treat Osteoporosis Combination Product in combination with: Calcitriol (DB00136) •••••••••••• ••••••• ••••••• ••••••• Prevention of Osteoporosis •••••••••••• ••••••••••••••• Treatment of Osteoporosis •••••••••••• ••••••••••••••• Used in combination to manage Osteoporosis Combination Product in combination with: Cholecalciferol (DB00169) •••••••••••• •••••••••••••• - Contraindications & Blackbox Warnings
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Alendronic acid tablets have a very low oral bioavialabilityLabel2. After administration it distributes into soft tissue and bone or is excreted in the urineLabel. Alendronic acid does not undergo metabolismLabel.
- Mechanism of action
Alendronic acid binds to bone hydroxyapatiteLabel. Bone resorption causes local acidification, releasing alendronic acid which is that taken into osteoclasts by fluid-phase endocytosis1. Endocytic vesicles are acidified, releasing alendronic acid to the cytosol of osteoclasts where they induce apoptosis1. Inhibition of osteoclasts results in decreased bone resorption which is shown through decreased urinary calcium, deoxypyridinoline and cross-linked N-telopeptidases of type I collagenLabel.
Target Actions Organism AFarnesyl pyrophosphate synthase inhibitorHumans AHydroxylapatite antagonistHumans UTyrosine-protein phosphatase non-receptor type 4 inhibitorHumans UReceptor-type tyrosine-protein phosphatase S inhibitorHumans UReceptor-type tyrosine-protein phosphatase epsilon inhibitorHumans UV-type proton ATPase catalytic subunit A inhibitorHumans - Absorption
Mean oral bioavailability of alendronic acid in women is 0.64% and in men is 0.59%Label2. Bioavailability of alendronic acid decreases by up to 40% if it is taken within an hour of a mealLabel.
- Volume of distribution
28LLabel.
- Protein binding
78%Label. Studies in rats show that plasma protein binding increases with decreasing alendronic acid plasma concentration3 and increasing pH4.
- Metabolism
Urinary excretion is the sole method of elimination of alendronic acid and no metabolites are detected upon urine collection2.
- Route of elimination
Administration of radiolabeled alendronic acid results in 50% recovery in urine within 72 hoursLabel4. No alendronic acid is recovered in the fecesLabel2,3. Men excrete less alendronic acid than women, though race and advanced age do not affect eliminationLabel.
- Half-life
Due to alendronic acid being incorporated into the skeleton, the terminal half life is estimated to be over 10 yearsLabel.
- Clearance
71mL/minLabel.
- Adverse Effects
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In clinical studies, ≥3% of patients experience abdominal pain, acid regurgitation, constipation, diarrhea, dyspepsia, musculoskeletal pain, and nauseaLabel.
No information for treatment of overdose is available, however patients should be given milk or antacids to bind alendronic acid and vomiting should not be inducedLabel. Patients may experience hypocalcemia, hypophosphatemia, and upper gastrointestinal events.Label.
There are currently no studies for safety and efficacy in pregnancy, though studies in pregnant rats show fetal and maternal complications at 4 times the clinical dose and pregnant rabbits do not show complications at as high as 10 times the clincal doseLabel.
Excretion in breast milk, and therefore safety in lactation, is unknownLabel.
Alendronic acid has been studied for use in pediatric patientsLabel. The oral bioavailability is similar to that in adult patients, but an increase in the portion of patients experiencing vomitingLabel.
There is no significant difference in efficacy or safety of alendronic acid in geriatric populations, though there is potential for even greater sensitivity in patients at a further advanced age than those in the studyLabel.
Alendronic acid is not recommended for patients with creatinine clearance <35mL/min, but no dosage adjustment is necessary in hepatic impairmentLabel.
- Pathways
Pathway Category Alendronate Action Pathway Drug action - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAceclofenac The risk or severity of adverse effects can be increased when Aceclofenac is combined with Alendronic acid. Acemetacin The risk or severity of adverse effects can be increased when Acemetacin is combined with Alendronic acid. Acetylsalicylic acid The risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Alendronic acid. Acipimox The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Alendronic acid is combined with Acipimox. Acyclovir The risk or severity of nephrotoxicity and hypocalcemia can be increased when Acyclovir is combined with Alendronic acid. - Food Interactions
- Administer vitamin supplements. Patients may require supplemental vitamin D.
- Avoid multivalent ions. Calcium, antacids, and divalent ions may interfere with the absorption of this medication.
- Take before a meal. Take 30-60 minutes before breakfast.
- Take with a full glass of water.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Alendronate calcium 3JTA994BVH 137504-90-6 VFAZUESUCBECNE-UHFFFAOYSA-L Alendronate disodium I2U0WCC042 134606-40-9 LMWOPQOPFYJQLI-UHFFFAOYSA-L Alendronate sodium 2UY4M2U3RA 121268-17-5 DCSBSVSZJRSITC-UHFFFAOYSA-M Alendronate sodium anhydrous 4988K7X26P 129318-43-0 CAKRAHQRJGUPIG-UHFFFAOYSA-M - Product Images
- International/Other Brands
- Alenotop (Pliva) / Alned (Laboratorios Belmac) / Arendal (Ivax) / Beenos (Gedeon Richter) / Berlex (Duncan) / Denfos (Biofarma) / Densidron (Mepha) / Dronat (Farmavita) / Durost (Perumed) / Fixopan (Grupo Farma) / Forosa (Kemofarmacija) / Fosagen (Aspen Pharmacare) / Fosalen (Teriak) / Fosmin (Hospimedikka) / Fostolin (Actavis) / Fosval (Saval) / Huesobone (Farmaceutica Latina) / Lendrate (Actavis) / Oseolen (Intipharma) / Ostemax (Polpharma)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Act Alendronate Tablet 70 mg Oral Actavis Pharma Company 2005-06-14 2018-06-12 Canada 
Act Alendronate Tablet 40 mg Oral Actavis Pharma Company 2005-06-14 2019-07-08 Canada Alendronate Tablet 10 mg Oral Sanis Health Inc Not applicable Not applicable Canada Alendronate Tablet 70 mg Oral Cobalt Laboratories Not applicable Not applicable Canada Alendronate Tablet 70 mg Oral Sorres Pharma Inc 2009-02-26 2014-06-20 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Accel-alendronate Tablet 5 mg Oral Accel Pharma Inc Not applicable Not applicable Canada Accel-alendronate Tablet 70 mg Oral Accel Pharma Inc 2015-03-26 2017-09-13 Canada Accel-alendronate Tablet 10 mg Oral Accel Pharma Inc 2015-03-26 2017-09-13 Canada Ach-alendronate Tablet 10 mg Oral Accord Healthcare Inc 2012-03-20 Not applicable Canada Ach-alendronate Tablet 70 mg Oral Accord Healthcare Inc 2012-03-20 Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image ACIDO ALENDRONICO E COLECALCIFEROLO AUROBINDO Alendronic acid (70 MG) + Cholecalciferol (5600 IU) Tablet Oral Aurobindo Pharma (Italia) S.R.L. 2018-03-01 Not applicable Italy 
ACIDO ALENDRONICO E COLECALCIFEROLO AUROBINDO Alendronic acid (70 MG) + Cholecalciferol (2800 IU) Tablet Oral Aurobindo Pharma (Italia) S.R.L. 2018-03-01 Not applicable Italy ACIDO ALENDRONICO E COLECALCIFEROLO EG Alendronic acid (70 MG) + Cholecalciferol (5600 IU) Tablet Oral Eg S.P.A. 2018-03-15 Not applicable Italy ACIDO ALENDRONICO E COLECALCIFEROLO EG Alendronic acid (70 MG) + Cholecalciferol (2800 IU) Tablet Oral Eg S.P.A. 2018-03-15 Not applicable Italy ACIDO ALENDRONICO E COLECALCIFEROLO EG Alendronic acid (70 MG) + Cholecalciferol (2800 IU) Tablet Oral Eg S.P.A. 2018-03-15 Not applicable Italy
Categories
- ATC Codes
- M05BB03 — Alendronic acid and colecalciferol
- M05BB — Bisphosphonates, combinations
- M05B — DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION
- M05 — DRUGS FOR TREATMENT OF BONE DISEASES
- M — MUSCULO-SKELETAL SYSTEM
- M05BA — Bisphosphonates
- M05B — DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION
- M05 — DRUGS FOR TREATMENT OF BONE DISEASES
- M — MUSCULO-SKELETAL SYSTEM
- M05BB — Bisphosphonates, combinations
- M05B — DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION
- M05 — DRUGS FOR TREATMENT OF BONE DISEASES
- M — MUSCULO-SKELETAL SYSTEM
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- 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
- Organic phosphonic acids / Organopnictogen compounds / Organophosphorus compounds / Organooxygen compounds / Organic oxides / Monoalkylamines / Hydrocarbon derivatives
- Substituents
- Aliphatic acyclic compound / Amine / Bisphosphonate / Hydrocarbon derivative / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organonitrogen compound / Organooxygen compound / Organophosphonic acid
- Molecular Framework
- Aliphatic acyclic compounds
- External Descriptors
- primary amino compound, 1,1-bis(phosphonic acid) (CHEBI:2567)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- X1J18R4W8P
- CAS number
- 66376-36-1
- InChI Key
- OGSPWJRAVKPPFI-UHFFFAOYSA-N
- InChI
- InChI=1S/C4H13NO7P2/c5-3-1-2-4(6,13(7,8)9)14(10,11)12/h6H,1-3,5H2,(H2,7,8,9)(H2,10,11,12)
- IUPAC Name
- (4-amino-1-hydroxy-1-phosphonobutyl)phosphonic acid
- SMILES
- NCCCC(O)(P(O)(O)=O)P(O)(O)=O
References
- Synthesis Reference
Masahiko Dohi, Yuji Makino, Takao Hujii, "Sodium alendronate preparation for local administration." U.S. Patent US5958908, issued September, 1997.
US5958908- General References
- Russell RG, Watts NB, Ebetino FH, Rogers MJ: Mechanisms of action of bisphosphonates: similarities and differences and their potential influence on clinical efficacy. Osteoporos Int. 2008 Jun;19(6):733-59. doi: 10.1007/s00198-007-0540-8. [Article]
- Porras AG, Holland SD, Gertz BJ: Pharmacokinetics of alendronate. Clin Pharmacokinet. 1999 May;36(5):315-28. doi: 10.2165/00003088-199936050-00002. [Article]
- Lin JH, Chen IW, Deluna FA, Hichens M: Renal handling of alendronate in rats. An uncharacterized renal transport system. Drug Metab Dispos. 1992 Jul-Aug;20(4):608-13. [Article]
- Lin JH, Chen IW, deLuna FA, Hichens M: Role of calcium in plasma protein binding and renal handling of alendronate in hypo- and hypercalcemic rats. J Pharmacol Exp Ther. 1993 Nov;267(2):670-5. [Article]
- Cremers S, Drake MT, Ebetino FH, Bilezikian JP, Russell RGG: Pharmacology of bisphosphonates. Br J Clin Pharmacol. 2019 Jun;85(6):1052-1062. doi: 10.1111/bcp.13867. Epub 2019 Feb 28. [Article]
- FDA Approved Drugs: Alendronate [Link]
- External Links
- Human Metabolome Database
- HMDB0001915
- KEGG Compound
- C07752
- PubChem Compound
- 2088
- PubChem Substance
- 46507199
- ChemSpider
- 2004
- BindingDB
- 25313
- 236083
- ChEBI
- 2567
- ChEMBL
- CHEMBL870
- ZINC
- ZINC000003801919
- Therapeutic Targets Database
- DAP000182
- PharmGKB
- PA448082
- PDBe Ligand
- 212
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Alendronic_acid
- PDB Entries
- 5dz2 / 8b4m
- FDA label
- Download (383 KB)
- MSDS
- Download (24.7 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Osteoporosis / Postmenopausal Osteoporosis 1 4 Completed Prevention Arteriosclerosis / Calcifications, Vascular 1 4 Completed Prevention Cystic Fibrosis (CF) / Duchenne Muscular Dystrophy (DMD) / Osteoporosis 1 4 Completed Prevention Osteopenia (Disorder) / Osteoporosis 1 4 Completed Treatment Cardiorenal Syndrome (CRS) / Chronic Allograft Nephropathy (CAN) 1
Pharmacoeconomics
- Manufacturers
- Merck and co inc
- Apotex inc
- Aurobindo pharma ltd
- Austarpharma llc
- Barr laboratories inc
- Cadista pharmaceuticals inc
- Dr reddys laboratories ltd
- Genpharm ulc
- Mylan pharmaceuticals inc
- Sandoz inc
- Sun pharma global inc
- Teva pharmaceuticals usa
- Watson laboratories
- Watson laboratories inc
- Packagers
- Amerisource Health Services Corp.
- Apotex Inc.
- Arrow Pharm Malta Ltd.
- A-S Medication Solutions LLC
- Aurobindo Pharma Ltd.
- Barr Pharmaceuticals
- Cipla Ltd.
- Cobalt Pharmaceuticals Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Doctor Reddys Laboratories Ltd.
- Lake Erie Medical and Surgical Supply
- Merck & Co.
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Northstar Rx LLC
- Nucare Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Rebel Distributors Corp.
- Southwood Pharmaceuticals
- Sun Pharmaceutical Industries Ltd.
- Teva Pharmaceutical Industries Ltd.
- UDL Laboratories
- Watson Pharmaceuticals
- Dosage Forms
Form Route Strength Tablet Oral 35 mg Tablet, effervescent Oral Tablet Oral 70 mg Tablet, film coated Oral Solution Oral 70 MG Tablet, film coated Oral 70 mg Tablet Oral 10 mg/1 Tablet Oral 40 mg/1 Tablet Oral 70 mg/1 Tablet Oral 91.35 mg Tablet, film coated Oral Tablet Oral 70 MG/2800IE Tablet Oral 70 MG/5600IE Tablet Oral 5 MG Tablet Oral Tablet, effervescent Oral 70 mg/1 Tablet, effervescent Oral 91.37 mg/1 Tablet, effervescent Oral 70 MG Solution Oral Tablet, effervescent Oral Tablet, effervescent Oral 70.00 mg Tablet Oral 10.000 mg Solution Oral 70 mg/75mL Solution Oral 70 mg / 75 mL Tablet Oral 35 mg/1 Tablet Oral 40 mg Tablet Oral 5 mg/1 Tablet, coated Oral 10 mg/1 Tablet Oral Tablet Oral 70 mg Capsule, liquid filled Oral 70 mg Tablet Oral 10.0 mg Tablet Oral 5.0 mg Tablet Oral 70.0 mg Tablet, film coated Oral 7000000 mg Capsule Oral 10 mg Solution Intravenous 5.000 mg Tablet Oral 70.000 mg Tablet Oral 10 mg Tablet Tablet, effervescent Oral 91.37 mg Tablet, delayed release Oral - Prices
Unit description Cost Unit Fosamax Plus D 4 70-2800 mg-Unit tablet Disp Pack 107.66USD disp Fosamax Plus D 4 70-5600 mg-Unit tablet Disp Pack 107.66USD disp Fosamax 1 Package = 4 tablet (70 mg) Package 101.96USD package Fosamax 1 Package = 4 tablet (35 mg) Package 97.2USD package Alendronate Sodium 4 35 mg tablet Package 85.23USD package Alendronate Sodium 4 70 mg tablet Package 85.23USD package Fosamax 70 mg/75ml Solution 75ml Bottle 34.75USD bottle Fosamax plus d 70 mg-5600 iu 25.88USD each Fosamax 70 mg tablet 24.51USD tablet Fosamax 35 mg tablet 23.36USD tablet Fosamax plus d 70 mg-2800 iu 21.85USD each Alendronate sodium 35 mg tablet 20.49USD tablet Alendronate sodium 70 mg tablet 20.49USD tablet Fosamax 40 mg tablet 7.52USD tablet Alendronate sodium 40 mg tablet 6.73USD tablet Fosamax 5 mg tablet 3.4USD tablet Fosamax 10 mg tablet 3.4USD tablet Alendronate sodium 10 mg tablet 2.99USD tablet Alendronate sodium 5 mg tablet 2.99USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5358941 No 1994-10-25 2012-12-02 US 
CA2190148 No 2006-02-14 2015-05-12 Canada CA2294595 No 2001-08-21 2018-07-17 Canada US5994329 Yes 1999-11-30 2019-01-17 US US6015801 Yes 2000-01-18 2019-01-17 US US6225294 Yes 2001-05-01 2019-01-17 US US7964212 No 2011-06-21 2023-03-06 US US7488496 No 2009-02-10 2023-08-11 US US9592195 No 2017-03-14 2031-12-05 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 235 https://www.tcichemicals.com/eshop/en/us/commodity/A2120/ pKa 2.72 (at 25 °C) MERCK INDEX (1996) - Predicted Properties
Property Value Source Water Solubility 16.9 mg/mL ALOGPS logP -1.3 ALOGPS logP -4.2 Chemaxon logS -1.2 ALOGPS pKa (Strongest Acidic) 0.69 Chemaxon pKa (Strongest Basic) 9.91 Chemaxon Physiological Charge -2 Chemaxon Hydrogen Acceptor Count 8 Chemaxon Hydrogen Donor Count 6 Chemaxon Polar Surface Area 161.31 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 47.37 m3·mol-1 Chemaxon Polarizability 19.4 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.9554 Blood Brain Barrier + 0.7065 Caco-2 permeable - 0.7079 P-glycoprotein substrate Non-substrate 0.6606 P-glycoprotein inhibitor I Non-inhibitor 0.947 P-glycoprotein inhibitor II Non-inhibitor 0.9894 Renal organic cation transporter Non-inhibitor 0.9205 CYP450 2C9 substrate Non-substrate 0.8536 CYP450 2D6 substrate Non-substrate 0.7997 CYP450 3A4 substrate Non-substrate 0.6792 CYP450 1A2 substrate Non-inhibitor 0.7567 CYP450 2C9 inhibitor Non-inhibitor 0.9089 CYP450 2D6 inhibitor Non-inhibitor 0.9344 CYP450 2C19 inhibitor Non-inhibitor 0.9091 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9914 Ames test Non AMES toxic 0.7079 Carcinogenicity Non-carcinogens 0.7783 Biodegradation Ready biodegradable 0.6547 Rat acute toxicity 1.6956 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8571 hERG inhibition (predictor II) Non-inhibitor 0.8929
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 153.41846 predictedDarkChem Lite v0.1.0 [M-H]- 153.45226 predictedDarkChem Lite v0.1.0 [M-H]- 135.94868 predictedDeepCCS 1.0 (2019) [M+H]+ 153.55836 predictedDarkChem Lite v0.1.0 [M+H]+ 153.35606 predictedDarkChem Lite v0.1.0 [M+H]+ 139.53654 predictedDeepCCS 1.0 (2019) [M+Na]+ 153.51436 predictedDarkChem Lite v0.1.0 [M+Na]+ 153.31266 predictedDarkChem Lite v0.1.0 [M+Na]+ 148.16539 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- 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. [Article]
- Guo RT, Cao R, Liang PH, Ko TP, Chang TH, Hudock MP, Jeng WY, Chen CK, Zhang Y, Song Y, Kuo CJ, Yin F, Oldfield E, Wang AH: Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases. Proc Natl Acad Sci U S A. 2007 Jun 12;104(24):10022-7. Epub 2007 May 29. [Article]
Yes
Antagonist
References
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Non-membrane spanning protein tyrosine phosphatase activity
- Specific Function
- May act at junctions between the membrane and the cytoskeleton.
- Gene Name
- PTPN4
- Uniprot ID
- P29074
- Uniprot Name
- Tyrosine-protein phosphatase non-receptor type 4
- Molecular Weight
- 105910.315 Da
References
- Opas EE, Rutledge SJ, Golub E, Stern A, Zimolo Z, Rodan GA, Schmidt A: Alendronate inhibition of protein-tyrosine-phosphatase-meg1. Biochem Pharmacol. 1997 Sep 15;54(6):721-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Transmembrane receptor protein tyrosine phosphatase activity
- Specific Function
- Interacts with LAR-interacting protein LIP.1.
- Gene Name
- PTPRS
- Uniprot ID
- Q13332
- Uniprot Name
- Receptor-type tyrosine-protein phosphatase S
- Molecular Weight
- 217039.825 Da
References
- Opas EE, Rutledge SJ, Golub E, Stern A, Zimolo Z, Rodan GA, Schmidt A: Alendronate inhibition of protein-tyrosine-phosphatase-meg1. Biochem Pharmacol. 1997 Sep 15;54(6):721-7. [Article]
- Schmidt A, Rutledge SJ, Endo N, Opas EE, Tanaka H, Wesolowski G, Leu CT, Huang Z, Ramachandaran C, Rodan SB, Rodan GA: Protein-tyrosine phosphatase activity regulates osteoclast formation and function: inhibition by alendronate. Proc Natl Acad Sci U S A. 1996 Apr 2;93(7):3068-73. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Transmembrane receptor protein tyrosine phosphatase activity
- Specific Function
- Isoform 1 plays a critical role in signaling transduction pathways and phosphoprotein network topology in red blood cells. May play a role in osteoclast formation and function (By similarity).Isofo...
- Gene Name
- PTPRE
- Uniprot ID
- P23469
- Uniprot Name
- Receptor-type tyrosine-protein phosphatase epsilon
- Molecular Weight
- 80641.165 Da
References
- Schmidt A, Rutledge SJ, Endo N, Opas EE, Tanaka H, Wesolowski G, Leu CT, Huang Z, Ramachandaran C, Rodan SB, Rodan GA: Protein-tyrosine phosphatase activity regulates osteoclast formation and function: inhibition by alendronate. Proc Natl Acad Sci U S A. 1996 Apr 2;93(7):3068-73. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Proton-transporting atpase activity, rotational mechanism
- Specific Function
- Catalytic subunit of the peripheral V1 complex of vacuolar ATPase. V-ATPase vacuolar ATPase is responsible for acidifying a variety of intracellular compartments in eukaryotic cells.
- Gene Name
- ATP6V1A
- Uniprot ID
- P38606
- Uniprot Name
- V-type proton ATPase catalytic subunit A
- Molecular Weight
- 68303.5 Da
References
- David P, Nguyen H, Barbier A, Baron R: The bisphosphonate tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. J Bone Miner Res. 1996 Oct;11(10):1498-507. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55