Identification
- Summary
Pamidronic acid is a bisphosphonate used to treat Paget's disease, to treat hypercalcemia of malignancy, and to treat osteolytic bone lesions.
- Brand Names
- Pamisol
- Generic Name
- Pamidronic acid
- DrugBank Accession Number
- DB00282
- Background
Pamidronic acid is a second generation, nitrogen containing bisphosphonate similar to neridronic acid and alendronic acid.2 Pamidronic acid was first described in the literature in 1977.9 The second generation bisphosphonates are less common as third generation bisphosphonates, such as ibandronic acid, zoledronic acid, minodronic acid, and risedronic acid are becoming more popular.2
Pamidronic acid was granted FDA approval on 31 October 1991.10
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Pamidronic acid (DB00282)
- Weight
- Average: 235.0695
Monoisotopic: 235.001074735 - Chemical Formula
- C3H11NO7P2
- Synonyms
- Acide pamidronique
- Acido pamidronico
- Acidum pamidronicum
- Pamidronate
- Pamidronic acid
Pharmacology
- Indication
Pamidronate is indicated to treat moderate to severe hypercalcemia of malignancy, moderate to severe Paget's disease of bone, osteolytic bone metastases of breast cancer, and osteolytic lesions of multiple myeloma.11
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Hypercalcemia of malignancy •••••••••••• ••••••••• Treatment of Osteolytic lesion •••••••••••• ••••••••• Treatment of Paget's disease •••••••••••• ••••••••• Treatment of Osteolytic bone metastases •••••••••••• ••••••••• - Contraindications & Blackbox Warnings
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Pamidronic acid is a second generation, nitrogen containing bisphosphonate that inhibits osteoclast mediated bone loss2,3,11 It has a wide therapeutic index and a long duration of action as it can be given every 3-4 weeks for certain indications.11 Patients should be counselled regarding the risk of elevated blood urea nitrogen, renal tubular necrosis, and nephrotoxicity.11
- 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.3 Endocytic vesicles become acidified, releasing bisphosphonates into the cytosol of osteoclasts where they act.3
Osteoclasts mediate resorption of bone.4 When osteoclasts bind to bone they form podosomes, ring structures of F-actin.4 Disruption of the podosomes causes osteoclasts to detach from bones, preventing bone resorption.4
Nitrogen containing bisphosphonates such as pamidronate 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.5,6,2 These components are essential for post-translational prenylation of GTP-binding proteins like Rap1.5,6 The lack of prenylation of these proteins interferes with their function, and in the case of Rap1, leads to apoptosis.5,6 pamidronate also activated caspases 3 and 9 which further contribute to apoptosis.5,6,7
Target Actions Organism AFarnesyl pyrophosphate synthase inhibitorHumans AHydroxylapatite antagonistHumans UGeranylgeranyl pyrophosphate synthase inhibitorHumans UCaspase-3 activatorHumans UCaspase-9 activatorHumans - Absorption
In patients with a creatinine clearance >90mL/min, a 90mg intravenous dose reached a Cmax of 1.92±1.08µg/mL, with a Tmax of 4h, and an AUC of 10.2±6.95µg*h/mL.8
In patients with a creatinine clearance 61-90mL/min, a 90mg intravenous dose reached a Cmax of 1.86±0.50µg/mL, with a Tmax of 4h, and an AUC of 10.7—3.91µg*h/mL.[A203264
In patients with a creatinine clearance 30-60mL/min, a 90mg intravenous dose reached a Cmax of 1.84±0.58µg/mL, with a Tmax of 4h, and an AUC of 10.1±3.38µg*h/mL.8
In patients with a creatinine clearance <30mL/min, a 90mg intravenous dose reached a Cmax of 1.93±0.53µg/mL, with a Tmax of 4h, and an AUC of 34.0±8.37µg*h/mL.8
- Volume of distribution
Not Available
- Protein binding
Pamidronate is approximately 54% protein bound in serum.12
- Metabolism
Pamidronate is not metabolized in vivo.11
- Route of elimination
Pamidronate is exclusively eliminated in the urine.11 By 120 hours after administration, 46±16% of the dose has been eliminated in the urine.11
- Half-life
The mean elimination half life of pamidronate is 28±7 hours.11
- Clearance
The mean total clearance of pamidronate is 107±50mL/min and the mean renal clearance is 49±28mL/min.11
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Patients experiencing and overdose may present with hypocalcemia, fever, hypotension, and taste perversion.11 Overdose can be managed by symptomatic and supportive treatment which may include the administration of steroids and intravenous calcium.11
- Pathways
Pathway Category Pamidronate 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 softwareAbacavir Pamidronic acid may decrease the excretion rate of Abacavir which could result in a higher serum level. Aceclofenac The risk or severity of gastrointestinal bleeding can be increased when Aceclofenac is combined with Pamidronic acid. Acemetacin The risk or severity of gastrointestinal bleeding can be increased when Acemetacin is combined with Pamidronic acid. Acetaminophen Pamidronic acid may decrease the excretion rate of Acetaminophen which could result in a higher serum level. Acetylsalicylic acid The risk or severity of gastrointestinal bleeding can be increased when Acetylsalicylic acid is combined with Pamidronic acid. - Food Interactions
- No interactions found.
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 Pamidronate Disodium C7S8VWP5DH 109552-15-0 CEYUIFJWVHOCPP-UHFFFAOYSA-L - International/Other Brands
- Aminomux / Pamimed / Ribodroat
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Aredia Powder, for solution 60 mg / vial Intravenous Novartis 1994-12-31 2001-07-30 Canada 
Aredia Injection, powder, lyophilized, for solution 90 mg/10mL Intravenous Novartis 1991-10-03 2011-09-30 US 
Aredia Injection, powder, lyophilized, for solution 30 mg/10mL Intravenous Novartis 1991-10-31 2012-02-29 US Aredia 30mg Powder, for solution 30 mg / vial Intravenous Novartis 1994-12-31 2016-02-23 Canada Aredia 90mg Powder, for solution 90 mg / vial Intravenous Novartis 1994-12-31 2016-02-23 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Pamidronate Disodium Injection, solution 9 mg/1mL Intravenous AMERICAN REGENT, INC. 2010-08-09 2012-11-01 US Pamidronate Disodium Injection 3 mg/1mL Intravenous Mylan Institutional 2011-05-10 2018-11-30 US Pamidronate Disodium Injection, solution 3 mg/1mL Intravenous Fresenius Kabi USA, LLC 2002-05-19 2015-08-27 US Pamidronate Disodium Injection, solution 3 mg/1mL Intravenous Pfizer Laboratories Div Pfizer Inc. 2011-05-10 2017-12-31 US Pamidronate Disodium Injection, powder, lyophilized, for solution 3 mg/1mL Intravenous Areva Pharmaceuticals Inc. 2013-08-06 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image AREDIA 90 MG/10 ML FLAKON, 1 ADET Pamidronic acid (90 mg/10ml) Solution Intravenous NOVARTİS ÜRÜNLERİ 2018-02-20 2022-04-11 Turkey 
PAMIDRIA 90 MG/10 ML IV INFUZYON ICIN KONSANTRE COZELTI ICEREN FLAKON, 1 ADET Pamidronic acid (90 mg/10ml) Injection, solution, concentrate Intravenous PHARMADA İLAÇ SAN. VE TİC. A.Ş. 2018-02-20 2024-01-23 Turkey PAMIDRONAT DISODYUM DBL 90 MG/10 ML FLAKON, 1 ADET Pamidronate Disodium (90 mg/10ml) Solution Intravenous ORNA İLAÇ TEKSTİL KİMYEVİ MAD. SAN. VE DIŞ TİC. LTD. ŞTİ. 2019-04-30 Not applicable Turkey
Categories
- ATC Codes
- M05BA03 — Pamidronic acid
- 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 / Organopnictogen compounds / Organophosphorus compounds / Organooxygen compounds / Organic oxides / Monoalkylamines / 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
- OYY3447OMC
- CAS number
- 40391-99-9
- InChI Key
- WRUUGTRCQOWXEG-UHFFFAOYSA-N
- InChI
- InChI=1S/C3H11NO7P2/c4-2-1-3(5,12(6,7)8)13(9,10)11/h5H,1-2,4H2,(H2,6,7,8)(H2,9,10,11)
- IUPAC Name
- (3-amino-1-hydroxy-1-phosphonopropyl)phosphonic acid
- SMILES
- NCCC(O)(P(O)(O)=O)P(O)(O)=O
References
- Synthesis Reference
Edward C. Shinal, "Method for preparation of disodium pamidronate." U.S. Patent US6268524, issued February, 1988.
US6268524- General References
- Zarychanski R, Elphee E, Walton P, Johnston J: Osteonecrosis of the jaw associated with pamidronate therapy. Am J Hematol. 2006 Jan;81(1):73-5. [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]
- 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]
- Ullen A, Schwarz S, Lennartsson L, Kalkner KM, Sandstrom P, Costa F, Lennernas B, Linder S, Nilsson S: Zoledronic acid induces caspase-dependent apoptosis in renal cancer cell lines. Scand J Urol Nephrol. 2009;43(2):98-103. doi: 10.1080/00365590802475904. [Article]
- Wada A, Fukui K, Sawai Y, Imanaka K, Kiso S, Tamura S, Shimomura I, Hayashi N: Pamidronate induced anti-proliferative, apoptotic, and anti-migratory effects in hepatocellular carcinoma. J Hepatol. 2006 Jan;44(1):142-50. doi: 10.1016/j.jhep.2005.09.022. Epub 2005 Nov 9. [Article]
- Berenson JR, Rosen L, Vescio R, Lau HS, Woo M, Sioufi A, Kowalski MO, Knight RD, Seaman JJ: Pharmacokinetics of pamidronate disodium in patients with cancer with normal or impaired renal function. J Clin Pharmacol. 1997 Apr;37(4):285-90. doi: 10.1002/j.1552-4604.1997.tb04304.x. [Article]
- Bijvoet OL, Reitsma PH, Frijlink WB: Bisphosphonates and Paget's disease. Lancet. 1980 Jun 28;1(8183):1416-7. doi: 10.1016/s0140-6736(80)92679-3. [Article]
- FDA Approved Drug Products: Aredia Pamidronate Intravenous Injection (Discontinued) [Link]
- FDA Approved Drug Products: Aredia Pamidronate Intravenous Injection [Link]
- Pfizer Canada: Pamidronate Disodium Injection [Link]
- External Links
- Human Metabolome Database
- HMDB0014427
- KEGG Drug
- D07281
- KEGG Compound
- C07395
- PubChem Compound
- 4674
- PubChem Substance
- 46504823
- ChemSpider
- 4512
- BindingDB
- 12581
- 11473
- ChEBI
- 7903
- ChEMBL
- CHEMBL834
- ZINC
- ZINC000003812862
- Therapeutic Targets Database
- DAP001416
- PharmGKB
- PA450767
- PDBe Ligand
- 210
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Pamidronic_acid
- PDB Entries
- 2f89 / 3sdr / 4kpj / 4nkf / 4ogu / 5erm / 5ero / 7kj8 / 8su1
- FDA label
- Download (59.5 KB)
- MSDS
- Download (49.3 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 Completed Other Breast Cancer / Metastatic Cancer 1 4 Completed Treatment Bone Loss 1 4 Completed Treatment Breast Cancer 1 4 Completed Treatment Breast Cancer / Metastatic Cancer / Prostate Cancer 1 4 Completed Treatment Complications of Heart-lung Transplant / Osteopenia (Disorder) / Other Complications of Lung Transplant 1
Pharmacoeconomics
- Manufacturers
- Novartis pharmaceuticals corp
- Aesgen inc
- Akorn strides llc
- App pharmaceuticals llc
- Bedford laboratories div ben venue laboratories inc
- Cipla ltd
- Generamedix inc
- Hospira inc
- Mn pharmaceuticals
- Pharmaforce inc
- Pliva lachema as
- Sun pharma global inc
- Teva parenteral medicines inc
- Packagers
- Akorn Inc.
- American Regent
- APP Pharmaceuticals
- Barr Pharmaceuticals
- Bedford Labs
- Ben Venue Laboratories Inc.
- Hospira Inc.
- Novartis AG
- Otn Generics Inc.
- Pharmaforce Inc.
- Pliva Inc.
- Sagent Pharmaceuticals
- Sandoz
- Strides Arcolab Limited
- Teva Pharmaceutical Industries Ltd.
- Dosage Forms
Form Route Strength Injection, powder, lyophilized, for solution Intravenous 30 mg/10mL Injection, powder, lyophilized, for solution Intravenous 90 mg/10mL Powder, for solution Intravenous Powder, for solution Intravenous 60 mg / vial Powder, for solution Intravenous 30 mg / vial Solution Intravenous 90 mg/10ml Powder, for solution Intravenous 90 mg / vial Liquid Intravenous 3 mg / mL Injection, powder, lyophilized, for solution Intravenous 15 mg Injection, powder, lyophilized, for solution Intravenous 30 mg Injection, powder, lyophilized, for solution Intravenous 60 mg Injection, powder, for solution Intravenous 90 mg Injection, powder, lyophilized, for solution Intravenous 90 mg Injection, solution, concentrate Intravenous 90 mg/10ml Injection, solution, concentrate Intravenous 3 mg/ml Injection, solution, concentrate Intravenous 6 mg/ml Injection, solution, concentrate Intravenous 9 mg/ml Injection Intravenous 3 mg/1mL Injection Intravenous 9 mg/1mL Injection, powder, lyophilized, for solution Intravenous 3 mg/1mL Injection, powder, lyophilized, for solution Intravenous 6 mg/1mL Injection, powder, lyophilized, for solution Intravenous 9 mg/1mL Injection, solution Intravenous 3 mg/1mL Injection, solution Intravenous 6 mg/1mL Injection, solution Intravenous 9 mg/1mL Solution Intravenous 3 mg/1mL Solution Intravenous 6 mg/1mL Solution Intravenous 9 mg/1mL Solution, concentrate Intravenous 3 mg/1mL Solution, concentrate Intravenous 9 mg/1mL Solution Intravenous 3 mg / mL Solution Intravenous 6 mg / mL Solution Intravenous 3.0 mg / mL Solution Intravenous 6.0 mg / mL Solution Intravenous 9.0 mg / mL Powder Parenteral 15 MG/5ML Powder Parenteral 30 MG/10ML Powder Parenteral 60 MG/10ML Powder Parenteral 90 MG/10ML Injection Intravenous 3 mg/ml Injection Intravenous 9 mg/ml Injection Intravenous 90 MG/10ML Injection, solution, concentrate Intravenous Powder, for solution Intravenous 15 mg / vial Injection, solution Parenteral 15 MG/5ML Injection, solution Parenteral 30 MG/10ML Injection, solution Parenteral 60 MG/10ML Injection, solution Parenteral 90 MG/10ML Solution Intravenous 9 mg / mL Injection, solution, concentrate Intravenous 15 mg/5ml - Prices
Unit description Cost Unit Aredia 90 mg vial 839.59USD each Pamidronate disod 90 mg vial 755.64USD each Aredia 90 mg/vial 548.05USD vial Aredia 30 mg vial 279.86USD each Pamidronate Disodium 90 mg/vial 258.28USD vial Pamidronate Disodium Omega 90 mg/vial 258.28USD vial Pms-Pamidronate 90 mg/vial 258.28USD vial Aredia 30 mg/vial 182.69USD vial Pamidronate Disodium 60 mg/vial 129.14USD vial Pamidronate disod 30 mg vial 111.94USD each Pamidronate Disodium 30 mg/vial 86.09USD vial Pamidronate Disodium Omega 30 mg/vial 86.09USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 254-262 ChemSpider - Predicted Properties
Property Value Source Water Solubility 15.8 mg/mL ALOGPS logP -1.4 ALOGPS logP -4.5 Chemaxon logS -1.2 ALOGPS pKa (Strongest Acidic) 0.67 Chemaxon pKa (Strongest Basic) 9.86 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 4 Chemaxon Refractivity 42.62 m3·mol-1 Chemaxon Polarizability 17.34 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 - 0.9635 Blood Brain Barrier + 0.6175 Caco-2 permeable - 0.6924 P-glycoprotein substrate Non-substrate 0.6937 P-glycoprotein inhibitor I Non-inhibitor 0.937 P-glycoprotein inhibitor II Non-inhibitor 0.9868 Renal organic cation transporter Non-inhibitor 0.9254 CYP450 2C9 substrate Non-substrate 0.8427 CYP450 2D6 substrate Non-substrate 0.7949 CYP450 3A4 substrate Non-substrate 0.6827 CYP450 1A2 substrate Non-inhibitor 0.7892 CYP450 2C9 inhibitor Non-inhibitor 0.9049 CYP450 2D6 inhibitor Non-inhibitor 0.9336 CYP450 2C19 inhibitor Non-inhibitor 0.9049 CYP450 3A4 inhibitor Non-inhibitor 0.8539 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9924 Ames test Non AMES toxic 0.6692 Carcinogenicity Non-carcinogens 0.7877 Biodegradation Ready biodegradable 0.6385 Rat acute toxicity 1.7722 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8231 hERG inhibition (predictor II) Non-inhibitor 0.8926
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-001i-9010000000-c609aeb84dc854acef5e Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-001i-9040000000-f4c409a9c97500f29937 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-001i-0090000000-aee21797c786ae2e7407 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-000i-0970000000-90566973ba94566c8de8 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-03e9-9000000000-57db758a0656fb4481a5 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-9000000000-5a63a0e8491ead7d58a8 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0080-9500000000-4d73f3515952cbd8bf9a 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]- 144.852441 predictedDarkChem Lite v0.1.0 [M-H]- 144.257341 predictedDarkChem Lite v0.1.0 [M-H]- 130.70215 predictedDeepCCS 1.0 (2019) [M+H]+ 144.361941 predictedDarkChem Lite v0.1.0 [M+H]+ 145.001941 predictedDarkChem Lite v0.1.0 [M+H]+ 134.53038 predictedDeepCCS 1.0 (2019) [M+Na]+ 144.131741 predictedDarkChem Lite v0.1.0 [M+Na]+ 144.235841 predictedDarkChem Lite v0.1.0 [M+Na]+ 143.32399 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
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- 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]
- 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]
- Notarnicola M, Messa C, Cavallini A, Bifulco M, Tecce MF, Eletto D, Di Leo A, Montemurro S, Laezza C, Caruso MG: Higher farnesyl diphosphate synthase activity in human colorectal cancer inhibition of cellular apoptosis. Oncology. 2004;67(5-6):351-8. [Article]
- Riebeling C, Forsea AM, Raisova M, Orfanos CE, Geilen CC: The bisphosphonate pamidronate induces apoptosis in human melanoma cells in vitro. Br J Cancer. 2002 Jul 29;87(3):366-71. [Article]
- Zhang PL, Lun M, Siegelmann-Danieli N, Blasick TM, Brown RE: Pamidronate resistance and associated low ras levels in breast cancer cells: a role for combinatorial therapy. Ann Clin Lab Sci. 2004 Summer;34(3):263-70. [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]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Metal ion binding
- Specific 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.
- Gene Name
- GGPS1
- Uniprot ID
- O95749
- Uniprot Name
- Geranylgeranyl pyrophosphate synthase
- Molecular Weight
- 34870.625 Da
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]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Activator
- General Function
- Phospholipase a2 activator activity
- Specific Function
- Involved in the activation cascade of caspases responsible for apoptosis execution. At the onset of apoptosis it proteolytically cleaves poly(ADP-ribose) polymerase (PARP) at a '216-Asp-|-Gly-217' ...
- Gene Name
- CASP3
- Uniprot ID
- P42574
- Uniprot Name
- Caspase-3
- Molecular Weight
- 31607.58 Da
References
- Wada A, Fukui K, Sawai Y, Imanaka K, Kiso S, Tamura S, Shimomura I, Hayashi N: Pamidronate induced anti-proliferative, apoptotic, and anti-migratory effects in hepatocellular carcinoma. J Hepatol. 2006 Jan;44(1):142-50. doi: 10.1016/j.jhep.2005.09.022. Epub 2005 Nov 9. [Article]
- Riebeling C, Forsea AM, Raisova M, Orfanos CE, Geilen CC: The bisphosphonate pamidronate induces apoptosis in human melanoma cells in vitro. Br J Cancer. 2002 Jul 29;87(3):366-71. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Activator
- General Function
- Involved in the activation cascade of caspases responsible for apoptosis execution. Binding of caspase-9 to Apaf-1 leads to activation of the protease which then cleaves and activates caspase-3. Promotes DNA damage-induced apoptosis in a ABL1/c-Abl-dependent manner. Proteolytically cleaves poly(ADP-ribose) polymerase (PARP).
- Specific Function
- Cysteine-type endopeptidase activity
- Gene Name
- CASP9
- Uniprot ID
- P55211
- Uniprot Name
- Caspase-9
- Molecular Weight
- 46280.325 Da
References
- Wada A, Fukui K, Sawai Y, Imanaka K, Kiso S, Tamura S, Shimomura I, Hayashi N: Pamidronate induced anti-proliferative, apoptotic, and anti-migratory effects in hepatocellular carcinoma. J Hepatol. 2006 Jan;44(1):142-50. doi: 10.1016/j.jhep.2005.09.022. Epub 2005 Nov 9. [Article]
- Riebeling C, Forsea AM, Raisova M, Orfanos CE, Geilen CC: The bisphosphonate pamidronate induces apoptosis in human melanoma cells in vitro. Br J Cancer. 2002 Jul 29;87(3):366-71. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55