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Identification
- Summary
Ibandronate is a bisphosphonate used to treat osteoporosis in postmenopausal women.
- Brand Names
- Bondronat, Boniva, Bonviva, Iasibon
- Generic Name
- Ibandronate
- DrugBank Accession Number
- DB00710
- Background
Ibandronate, or BM 21.0955, is a third generation, nitrogen containing bisphosphonate similar to zoledronic acid, minodronic acid, and risedronic acid.1,2 It is used to prevent and treat postmenopausal osteoporosis.11,12 Ibandronate was first described in the literature in 1993 as a treatment for bone loss in dogs.2
Ibandronate was granted FDA approval on 16 May 2003.11
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Ibandronate (DB00710)
- Weight
- Average: 319.2289
Monoisotopic: 319.094975119 - Chemical Formula
- C9H23NO7P2
- Synonyms
- ácido ibandrónico
- Ibandronic acid
- External IDs
- R484
Pharmacology
- Indication
For the treatment and prevention of osteoporosis in postmenopausal women.11,12
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Bone metastases ••• ••••• Treatment of Hypercalcemia of malignancy ••• ••••• Management of Osteoporosis •••••••••••• •••••••••••••• •••••••••• •••••• Prevention of Osteoporosis •••••••••••• •••••••••••••• •••••• - Contraindications & Blackbox Warnings
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Ibandronate is a nitrogen containing bisphosphonate used to treat and prevent osteoporosis in postmenopausal women.11,12 The therapeutic index is wide as overdoses are not especially toxic, and the duration of action is long as the half life can be up to 157 hours.11,12 Patients should be counselled regarding the risk of upper GI adverse reactions, hypocalcemia, musculoskeletal pain, osteonecrosis of the jaw, atypical fractures of the femur, and severe renal impairment.11,12
- Mechanism of action
Bisphosphonates are taken into the bone where they bind to hydroxyapatite. Bone resorption by osteoclasts causes local acidification, releasing the bisphosphonate, which is taken into the osteoclast by fluid-phase endocytosis.5 Endocytic vesicles become acidified, releasing bisphosphonates into the cytosol of osteoclasts where they act.5
Osteoclasts mediate resorption of bone.6 When osteoclasts bind to bone they form podosomes, ring structures of F-actin.6 Disruption of the podosomes causes osteoclasts to detach from bones, preventing bone resorption.6
Nitrogen containing bisphosphonates such as ibandronate are known to induce apoptosis of hematopoietic tumor cells by inhibiting the components of the mevalonate pathway farnesyl diphosphate synthase, farnesyl diphosphate, and geranylgeranyl diphosphate.7,3 These components are essential for post-translational prenylation of GTP-binding proteins like Rap1.7 The lack of prenylation of these proteins interferes with their function, and in the case of Rap1, leads to apoptosis.7 ibandronate also activated caspase-3 which contribute to apoptosis.4
Target Actions Organism AHydroxylapatite antagonistHumans AGeranylgeranyl pyrophosphate synthase inhibitorHumans AFarnesyl pyrophosphate synthase inhibitorHumans - Absorption
Oral ibandronate is 0.63% bioavailable.8 In a study of healthy males, a 10mg oral dose had a Tmax of 1.1±0.6h and a Cmax of 4.1±2.6ng/mL.10 The Tmax is approximately 1 hour, while Cmax varies depending on dose.10
A 2mg intravenous dose of ibandronate has an AUC of 316ng*h/mL, a 4mg intravenous dose of ibandronate has an AUC of 581ng*h/mL, and a 6mg intravenous dose of ibandronate has an AUC of 908ng*h/mL.9
- Volume of distribution
The apparent terminal volume of distribution of ibandronate is 90-368L in headlthy subjects and 103L in postmenopausal women with osteopenia.8,11,12
- Protein binding
Ibandronate's protein binding in serum varies from 85.7-99.5% over a concentration of 0.5-10ng/mL,11 but is generally 86% across a concentration range of 20-2000ng/mL.12
- Metabolism
- Route of elimination
Ibandronate is predominantly eliminated in the urine and the unabsorbed drug is eliminated unchanged in the feces.8,11,12
- Half-life
The half life of ibandronate in postmenopausal women ranges from 37-157 hours.11,12
- Clearance
- Adverse Effects
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Patients experiencing an overdose may present with hypocalcemia, hypophosphatemia, upset stomach, dyspepsia, esophagitis, and uclers.11,12 Oral overdose can be managed by giving patients milk or antacids to bind excess unabsorbed ibandronate.11 Overdoses can be managed by providing intravenous electrolytes and dialysis is not expected to remove excess drug from serum.11,12
- Pathways
Pathway Category Ibandronate Action Pathway Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- 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 gastrointestinal bleeding can be increased when Aceclofenac is combined with Ibandronate. Acemetacin The risk or severity of gastrointestinal bleeding can be increased when Acemetacin is combined with Ibandronate. Acetylsalicylic acid The risk or severity of gastrointestinal bleeding can be increased when Acetylsalicylic acid is combined with Ibandronate. Acipimox The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ibandronate is combined with Acipimox. Acrivastine The risk or severity of QTc prolongation can be increased when Ibandronate is combined with Acrivastine. - Food Interactions
- Take on an empty stomach.
- Take with a full glass of water. Do not take this medication with other liquids.
Products
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Ingredient UNII CAS InChI Key Ibandronate sodium J12U072QL0 138926-19-9 VBDRTGFACFYFCT-UHFFFAOYSA-M - Product Images
- International/Other Brands
- ADRONiL
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Bondenza Injection, solution 3 mg Intravenous Roche Registration Limited 2016-09-07 2013-03-27 EU 
Bondenza Tablet, film coated 150 mg Oral Roche Registration Limited 2016-09-07 2013-03-27 EU Bondenza Tablet, film coated 150 mg Oral Roche Registration Limited 2016-09-07 2013-03-27 EU Bondenza Injection, solution 3 mg Intravenous Roche Registration Limited 2016-09-07 2013-03-27 EU Bondronat Injection, solution, concentrate 6 mg Intravenous Atnahs Pharma Netherlands B.V. 2021-02-11 Not applicable EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ibandronate Sodium Tablet 150 mg/1 Oral Bionpharma Inc. 2023-05-26 Not applicable US 
Ibandronate Sodium Tablet 150 mg/1 Oral Actavis Pharma, Inc. 2012-03-20 2018-06-30 US 
Ibandronate Sodium Injection 3 mg/3mL Intravenous Apotex Corp. 2016-01-13 Not applicable US Ibandronate sodium Tablet 150 mg/1 Oral Dr. Reddy's Laboratories Limited 2012-06-21 Not applicable US Ibandronate Sodium Injection, solution 3 mg/3mL Intravenous Accord Healthcare Inc. 2024-01-01 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image ASCENDRA TRIO 500CA+1000D3 Ibandronate (1 mg/mL) + Calcium carbonate (500 mg) + Cholecalciferol (1000 IU) Injection, solution Parenteral 2019-04-01 Not applicable Germany 
IBAMIN D3 150 MG/2800 IU FİLM KAPLI TABLET, 3 ADET Ibandronate sodium (168.78 mg) + Cholecalciferol (2800 IU) Tablet, coated Oral CELTİS İLAÇ SAN. VE TİC. A.Ş. 2014-01-28 Not applicable Turkey 
IBAMIN D3 150 MG/2800 IU SAŞE ,3 SAŞE Ibandronate sodium (168.78 mg) + Cholecalciferol (2800 IU) Powder Oral CELTİS İLAÇ SAN. VE TİC. A.Ş. 2013-03-07 Not applicable Turkey IBONE D 30000 Ibandronate (150 mg) + Cholecalciferol (30000 IU) Tablet, coated Oral 2018-01-29 Not applicable Colombia 
IBONE D® Ibandronate sodium (150 mg) + Cholecalciferol (12000 IU) Tablet, coated Oral LABORATORIOS SYNTHESIS S.A.S. 2013-04-18 2024-01-30 Colombia
Categories
- ATC Codes
- M05BA06 — Ibandronic acid
- M05BA — Bisphosphonates
- 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 / 1,3-aminoalcohols / Trialkylamines / Organopnictogen compounds / Organophosphorus compounds / Organooxygen compounds / Organic oxides / Hydrocarbon derivatives
- Substituents
- 1,3-aminoalcohol / Aliphatic acyclic compound / Amine / Bisphosphonate / Hydrocarbon derivative / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organonitrogen compound / Organooxygen compound
- Molecular Framework
- Aliphatic acyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- UMD7G2653W
- CAS number
- 114084-78-5
- InChI Key
- MPBVHIBUJCELCL-UHFFFAOYSA-N
- InChI
- InChI=1S/C9H23NO7P2/c1-3-4-5-7-10(2)8-6-9(11,18(12,13)14)19(15,16)17/h11H,3-8H2,1-2H3,(H2,12,13,14)(H2,15,16,17)
- IUPAC Name
- {1-hydroxy-3-[methyl(pentyl)amino]-1-phosphonopropyl}phosphonic acid
- SMILES
- CCCCCN(C)CCC(O)(P(O)(O)=O)P(O)(O)=O
References
- Synthesis Reference
Revital Lifshitz-Liron, Thomas Bayer, Judith Aronhime, Michael Pinchasov, "Solid and crystalline ibandronate sodium and processes for preparation thereof." U.S. Patent US20070179119, issued August 02, 2007.
US20070179119- General References
- 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]
- Monier-Faugere MC, Friedler RM, Bauss F, Malluche HH: A new bisphosphonate, BM 21.0955, prevents bone loss associated with cessation of ovarian function in experimental dogs. J Bone Miner Res. 1993 Nov;8(11):1345-55. doi: 10.1002/jbmr.5650081109. [Article]
- Cao R, Chen CK, Guo RT, Wang AH, Oldfield E: Structures of a potent phenylalkyl bisphosphonate inhibitor bound to farnesyl and geranylgeranyl diphosphate synthases. Proteins. 2008 Nov 1;73(2):431-9. doi: 10.1002/prot.22066. [Article]
- Hiraga T, Williams PJ, Mundy GR, Yoneda T: The bisphosphonate ibandronate promotes apoptosis in MDA-MB-231 human breast cancer cells in bone metastases. Cancer Res. 2001 Jun 1;61(11):4418-24. [Article]
- 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]
- Murakami H, Takahashi N, Tanaka S, Nakamura I, Udagawa N, Nakajo S, Nakaya K, Abe M, Yuda Y, Konno F, Barbier A, Suda T: Tiludronate inhibits protein tyrosine phosphatase activity in osteoclasts. Bone. 1997 May;20(5):399-404. [Article]
- Miwa A, Takezako N, Hayakawa H, Hayakawa M, Tominaga S, Yanagisawa K: YM-175 induces apoptosis of human native monocyte-lineage cells via inhibition of prenylation. Am J Hematol. 2012 Dec;87(12):1084-8. doi: 10.1002/ajh.23328. Epub 2012 Oct 9. [Article]
- Reginster JY, Neuprez A, Bruyere O: Ibandronate in profile: drug characteristics and clinical efficacy. Expert Opin Drug Metab Toxicol. 2008 Jul;4(7):941-51. doi: 10.1517/17425255.4.7.941. [Article]
- Croom KF, Scott LJ: Intravenous ibandronate: in the treatment of osteoporosis. Drugs. 2006;66(12):1593-601; discussion 1602-3. doi: 10.2165/00003495-200666120-00005. [Article]
- Barrett J, Worth E, Bauss F, Epstein S: Ibandronate: a clinical pharmacological and pharmacokinetic update. J Clin Pharmacol. 2004 Sep;44(9):951-65. doi: 10.1177/0091270004267594. [Article]
- FDA Approved Drug Products: Boniva Ibandronate Oral Tablets [Link]
- FDA Approved Drug Products: Boniva Ibandronate Intravenous Injection [Link]
- External Links
- Human Metabolome Database
- HMDB0014848
- PubChem Compound
- 60852
- PubChem Substance
- 46508134
- ChemSpider
- 54839
- BindingDB
- 12577
- 115264
- ChEMBL
- CHEMBL997
- ZINC
- ZINC000001533877
- Therapeutic Targets Database
- DAP001022
- PharmGKB
- PA10270
- PDBe Ligand
- BFQ
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Ibandronic_acid
- PDB Entries
- 2f94 / 4umj / 6o9p / 6r4v
- FDA label
- Download (296 KB)
- MSDS
- Download (16 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample data4 Completed Prevention Osteopenia (Disorder) / Osteoporosis / Rheumatoid Arthritis 1 somestatus stop reason just information to hide 4 Completed Treatment Cirrhosis of the Liver 1 somestatus stop reason just information to hide 4 Completed Treatment Osteoporosis 3 somestatus stop reason just information to hide 4 Completed Treatment Pain; Bone Neoplasms; Neoplasm Metastasis 2 somestatus stop reason just information to hide 4 Completed Treatment Postmenopausal Osteopenia 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Hoffmann la roche inc
- Packagers
- Diversified Healthcare Services Inc.
- F Hoffmann La Roche Ltd.
- F Hoffmann-La Roche Ltd.
- Physicians Total Care Inc.
- Vetter Pharma Fertigung GmbH and Co. KG
- Dosage Forms
Form Route Strength Tablet, coated Oral 168.8 mg Tablet, coated Oral 16880000 mg Injection, solution Intravenous; Parenteral 3 MG Injection, solution, concentrate Intravenous 3 MG Injection, solution, concentrate Intravenous 6 MG Solution, concentrate Intravenous 2 MG Injection, solution 3 MG Injection, solution, concentrate Intravenous; Parenteral 2 MG Injection, solution, concentrate Intravenous; Parenteral 6 MG Tablet, coated Oral 168.795 mg Injection, solution Parenteral 3 MG Injection, solution Parenteral Injection, solution, concentrate Intravenous 3 mg/3ml Injection, solution Intravenous Injection, solution Intravenous 3 mg Tablet Oral Injection Intravenous 6 mg/6ml Injection, solution, concentrate Intravenous 2 mg Injection, solution, concentrate Intravenous 2 mg/2ml Liquid Intravenous 1 mg / mL Solution Intravenous Solution Parenteral 2 MG Injection, solution, concentrate Intravenous 6 mg/6ml Solution Parenteral 6 MG Solution Parenteral 6 MG/6ML Solution Intravenous 6 mg Capsule, liquid filled Oral 150 mg Injection Intravenous 1 MG/ML Injection, solution Intravenous 3 mg/3mL Tablet, film coated Oral 150 mg/1 Tablet, film coated Oral 2.5 mg/1 Injection, solution Intravenous; Parenteral 3 MG/3ML Tablet Oral 150 MG Injection, solution Parenteral 3 MG/3ML Injection, solution Parenteral 3 MG/ML Tablet, film coated Oral 168.75 mg Solution Intravenous 600000 mg Solution Intravenous 3.207 mg Powder Oral Injection Intravenous 1.125 mg/3ml Tablet Oral 150.000 mg Injection, solution, concentrate Intravenous 1 mg Powder Oral 56.27 mg Powder Oral Solution, concentrate Intravenous 6 mg Injection Intravenous 3 mg/3mL Tablet Oral 150 mg/1 Solution Parenteral 2 MG/2ML Solution Parenteral 4 MG Injection, solution, concentrate Intravenous Tablet, coated Oral Tablet, film coated Oral 50 MG Solution Intravenous 3.000 mg Injection, solution Tablet, film coated Oral Solution Intravenous 3 mg Solution Intravenous 6 mg/6ml Solution Intravenous 3 mg/3ml Tablet Oral Tablet, film coated Oral 150 mg Solution 1 ml/1ml Tablet, coated Oral 150 mg - Prices
Unit description Cost Unit Boniva 3 mg/3ml Kit Box 524.22USD box Boniva 3 mg/3 ml syringe 504.06USD syringe Boniva 3 150 mg tablet Disp Pack 388.93USD disp Boniva 150 mg tablet 124.66USD tablet Boniva 2.5 mg tablet 4.16USD 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 US4927814 No 1990-05-22 2012-03-17 US CA2346662 No 2006-05-09 2019-10-01 Canada 
US7192938 Yes 2007-03-20 2023-11-06 US US7718634 Yes 2010-05-18 2023-11-06 US US7410957 No 2008-08-12 2023-05-06 US US6294196 No 2001-09-25 2019-10-07 US US6143326 No 2000-11-07 2017-04-21 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 113-115 ChemSpider water solubility Freely soluble FDA Label - Predicted Properties
Property Value Source Water Solubility 13.4 mg/mL ALOGPS logP 0.26 ALOGPS logP -2.5 Chemaxon logS -1.4 ALOGPS pKa (Strongest Acidic) 0.66 Chemaxon pKa (Strongest Basic) 9.93 Chemaxon Physiological Charge -2 Chemaxon Hydrogen Acceptor Count 8 Chemaxon Hydrogen Donor Count 5 Chemaxon Polar Surface Area 138.53 Å2 Chemaxon Rotatable Bond Count 9 Chemaxon Refractivity 71.16 m3·mol-1 Chemaxon Polarizability 29.06 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.9664 Blood Brain Barrier - 0.5229 Caco-2 permeable - 0.6012 P-glycoprotein substrate Substrate 0.6888 P-glycoprotein inhibitor I Non-inhibitor 0.8195 P-glycoprotein inhibitor II Non-inhibitor 0.9838 Renal organic cation transporter Non-inhibitor 0.9092 CYP450 2C9 substrate Non-substrate 0.8376 CYP450 2D6 substrate Non-substrate 0.7863 CYP450 3A4 substrate Non-substrate 0.5504 CYP450 1A2 substrate Non-inhibitor 0.832 CYP450 2C9 inhibitor Non-inhibitor 0.8159 CYP450 2D6 inhibitor Non-inhibitor 0.8987 CYP450 2C19 inhibitor Non-inhibitor 0.8045 CYP450 3A4 inhibitor Non-inhibitor 0.8901 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9945 Ames test Non AMES toxic 0.6527 Carcinogenicity Non-carcinogens 0.683 Biodegradation Not ready biodegradable 0.8346 Rat acute toxicity 2.4278 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.6061 hERG inhibition (predictor II) Non-inhibitor 0.6622
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-08gl-9130000000-f1a145132fe5a1d4852e Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-00di-1009000000-b91babff237e94d7337b Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-014i-0009000000-d9cc0555c13a02809e68 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-00di-0039000000-603f288312f291170d98 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-014i-5009000000-62c5339f86fe4740b707 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0fai-9020000000-094fe73207638a11acb0 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0abc-9000000000-2129b5ed133d437d0bf7 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 175.7775975 predictedDarkChem Lite v0.1.0 [M-H]- 176.8889975 predictedDarkChem Lite v0.1.0 [M-H]- 158.6963 predictedDeepCCS 1.0 (2019) [M+H]+ 173.7716975 predictedDarkChem Lite v0.1.0 [M+H]+ 175.1557975 predictedDarkChem Lite v0.1.0 [M+H]+ 161.05434 predictedDeepCCS 1.0 (2019) [M+Na]+ 174.3732975 predictedDarkChem Lite v0.1.0 [M+Na]+ 175.7929975 predictedDarkChem Lite v0.1.0 [M+Na]+ 167.24304 predictedDeepCCS 1.0 (2019)
Targets
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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
- Yes
- Actions
- Inhibitor
- General Function
- Catalyzes the trans-addition of the three molecules of IPP onto DMAPP to form geranylgeranyl pyrophosphate, an important precursor of carotenoids and geranylated proteins
- Specific Function
- Dimethylallyltranstransferase activity
- Gene Name
- GGPS1
- Uniprot ID
- O95749
- Uniprot Name
- Geranylgeranyl pyrophosphate synthase
- Molecular Weight
- 34870.625 Da
References
- 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]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General 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, and ubiquinones. FPP also serves as substrate for protein farnesylation and geranylgeranylation. Catalyzes the sequential condensation of isopentenyl pyrophosphate with the allylic pyrophosphates, dimethylallyl pyrophosphate, and then with the resultant geranylpyrophosphate to the ultimate product farnesyl pyrophosphate
- Specific Function
- Dimethylallyltranstransferase activity
- Gene Name
- FDPS
- Uniprot ID
- P14324
- Uniprot Name
- Farnesyl pyrophosphate synthase
- Molecular Weight
- 48275.03 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Chapurlat RD, Delmas PD: Drug insight: Bisphosphonates for postmenopausal osteoporosis. Nat Clin Pract Endocrinol Metab. 2006 Apr;2(4):211-9; quiz following 238. [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]
- Rondeau JM, Bitsch F, Bourgier E, Geiser M, Hemmig R, Kroemer M, Lehmann S, Ramage P, Rieffel S, Strauss A, Green JR, Jahnke W: Structural basis for the exceptional in vivo efficacy of bisphosphonate drugs. ChemMedChem. 2006 Feb;1(2):267-73. [Article]
Drug created at June 13, 2005 13:24 / Updated at August 02, 2024 07:33