Pamidronic acid

Identification

Name
Pamidronic acid
Accession Number
DB00282
Description

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
Thumb
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

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

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

TargetActionsOrganism
AFarnesyl pyrophosphate synthase
inhibitor
Humans
AHydroxylapatite
antagonist
Humans
UGeranylgeranyl pyrophosphate synthase
inhibitor
Humans
UCaspase-3
cleavage
Humans
UCaspase-9
cleavage
Humans
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
Learn about our commercial Adverse Effects data.
Learn More
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

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Pamidronate Action PathwayDrug 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.
DrugInteraction
AbacavirPamidronic acid may decrease the excretion rate of Abacavir which could result in a higher serum level.
AcarbosePamidronic acid may decrease the excretion rate of Acarbose which could result in a higher serum level.
AceclofenacThe risk or severity of gastrointestinal bleeding can be increased when Aceclofenac is combined with Pamidronic acid.
AcemetacinThe risk or severity of gastrointestinal bleeding can be increased when Acemetacin is combined with Pamidronic acid.
AcetaminophenPamidronic acid may decrease the excretion rate of Acetaminophen which could result in a higher serum level.
Acetylsalicylic acidThe risk or severity of gastrointestinal bleeding can be increased when Acetylsalicylic acid is combined with Pamidronic acid.
AcipimoxThe risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Pamidronic acid is combined with Acipimox.
AclidiniumPamidronic acid may decrease the excretion rate of Aclidinium which could result in a higher serum level.
AcrivastinePamidronic acid may decrease the excretion rate of Acrivastine which could result in a higher serum level.
AcyclovirThe risk or severity of nephrotoxicity and hypocalcemia can be increased when Acyclovir is combined with Pamidronic acid.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
No interactions found.

Products

Product Ingredients
IngredientUNIICASInChI Key
Pamidronate DisodiumC7S8VWP5DH109552-15-0CEYUIFJWVHOCPP-UHFFFAOYSA-L
International/Other Brands
Aminomux / Pamimed / Ribodroat
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ArediaInjection, powder, lyophilized, for solution90 mg/10mLIntravenousNovartis1991-10-032011-09-30Us
ArediaPowder, for solution60 mgIntravenousNovartis1994-12-312001-07-30Canada
ArediaInjection, powder, lyophilized, for solution30 mg/10mLIntravenousNovartis1991-10-312012-02-29Us
Aredia 30mgPowder, for solutionIntravenousNovartis1994-12-312016-02-23Canada
Aredia 90mgPowder, for solutionIntravenousNovartis1994-12-312016-02-23Canada
Aredia Liq Inj 3mg/mlLiquidIntravenousGeigy Pharmaceuticals, Ciba Geigy Canada Ltd.1992-12-311996-09-09Canada
Pamidronate DisodiumInjection, solution3 mg/1mLIntravenousBedford Pharmaceuticals2002-03-282010-09-30Us
Pamidronate DisodiumInjection9 mg/1mLIntravenousAkorn-Strides, LLC2008-11-14Not applicableUs
Pamidronate DisodiumInjection, solution9 mg/1mLIntravenousGeneraMedix, Inc.2009-02-04Not applicableUs
Pamidronate DisodiumInjection3 mg/1mLIntravenousAkorn-Strides, LLC2008-11-14Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Pamidronate DisodiumInjection, solution9 mg/1mLIntravenousHospira Worldwide, Inc.2011-06-232011-06-23Us
Pamidronate DisodiumInjection, powder, lyophilized, for solution3 mg/1mLIntravenousAreva Pharmaceuticals Inc.2013-08-06Not applicableUs
Pamidronate DisodiumInjection, solution9 mg/1mLIntravenousAMERICAN REGENT, INC.2010-08-092012-11-01Us
Pamidronate DisodiumInjection, solution3 mg/1mLIntravenousFresenius Kabi USA, LLC2002-05-192015-08-27Us
Pamidronate DisodiumInjection, solution6 mg/1mLIntravenousHospira, Inc.2003-07-28Not applicableUs
Pamidronate DisodiumInjection, powder, lyophilized, for solution90 mg/10mLIntravenousBedford Pharmaceuticals2001-12-032012-12-31Us
Pamidronate DisodiumInjection, solution3 mg/1mLIntravenousPfizer Laboratories Div Pfizer Inc.2011-05-102017-12-31Us
Pamidronate DisodiumSolution6 mg/1mLIntravenousBarr Laboratories2008-09-112012-05-22Us
Pamidronate DisodiumInjection9 mg/1mLIntravenousMylan Institutional2015-08-182018-06-30Us
Pamidronate DisodiumInjection, powder, lyophilized, for solution9 mg/1mLIntravenousAreva Pharmaceuticals Inc.2013-08-06Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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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

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
  1. 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. [PubMed:16369966]
  2. 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. [PubMed:30650219]
  3. 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. [PubMed:18214569]
  4. 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. [PubMed:9145236]
  5. 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. [PubMed:23044853]
  6. 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. [PubMed:19101859]
  7. 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. [PubMed:16298452]
  8. 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. [PubMed:9115053]
  9. 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. [PubMed:6104199]
  10. FDA Approved Drug Products: Aredia Pamidronate Intravenous Injection (Discontinued) [Link]
  11. FDA Approved Drug Products: Aredia Pamidronate Intravenous Injection [Link]
  12. Pfizer Canada: Pamidronate Disodium Injection [Link]
Human Metabolome Database
HMDB0014427
KEGG Drug
D07281
KEGG Compound
C07395
PubChem Compound
4674
PubChem Substance
46504823
ChemSpider
4512
BindingDB
12581
RxNav
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
Pamidronate
AHFS Codes
  • 92:24.00 — Bone Resorption Inhibitors
PDB Entries
2f89 / 3sdr / 4kpj / 4nkf / 4ogu / 5erm / 5ero
FDA label
Download (59.5 KB)
MSDS
Download (49.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentBreast Cancer / Metastasis / Prostate Cancer1
4CompletedOtherBreast Cancer / Neoplasms Metastasis1
4CompletedTreatmentBone Diseases, Metabolic1
4CompletedTreatmentBone Loss1
4CompletedTreatmentBreast Cancer1
4CompletedTreatmentComplications of Heart-lung Transplant / Osteopenia / Other Complications of Lung Transplant1
4CompletedTreatmentOsteogenesis Imperfecta (OI) / Osteoporosis / Paget's Disease of Bone1
4CompletedTreatmentOsteopenia / Renal Osteodystrophy1
4CompletedTreatmentSpondyloarthropathies1
4Not Yet RecruitingPreventionAnkylosing Spondylitis (AS)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
FormRouteStrength
Injection, powder, lyophilized, for solutionIntravenous30 mg/10mL
Injection, powder, lyophilized, for solutionIntravenous90 mg/10mL
Powder, for solutionIntravenous60 mg
LiquidIntravenous
InjectionIntravenous3 mg/1mL
InjectionIntravenous9 mg/1mL
Injection, powder, lyophilized, for solutionIntravenous3 mg/1mL
Injection, powder, lyophilized, for solutionIntravenous6 mg/1mL
Injection, powder, lyophilized, for solutionIntravenous9 mg/1mL
Injection, solutionIntravenous3 mg/1mL
Injection, solutionIntravenous6 mg/1mL
Injection, solutionIntravenous9 mg/1mL
SolutionIntravenous3 mg/1mL
SolutionIntravenous6 mg/1mL
SolutionIntravenous9 mg/1mL
Solution, concentrateIntravenous3 mg/1mL
Solution, concentrateIntravenous9 mg/1mL
SolutionIntravenous
Powder, for solutionIntravenous
Prices
Unit descriptionCostUnit
Aredia 90 mg vial839.59USD each
Pamidronate disod 90 mg vial755.64USD each
Aredia 90 mg/vial548.05USD vial
Aredia 30 mg vial279.86USD each
Pamidronate Disodium 90 mg/vial258.28USD vial
Pamidronate Disodium Omega 90 mg/vial258.28USD vial
Pms-Pamidronate 90 mg/vial258.28USD vial
Aredia 30 mg/vial182.69USD vial
Pamidronate Disodium 60 mg/vial129.14USD vial
Pamidronate disod 30 mg vial111.94USD each
Pamidronate Disodium 30 mg/vial86.09USD vial
Pamidronate Disodium Omega 30 mg/vial86.09USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)254-262ChemSpider
Predicted Properties
PropertyValueSource
Water Solubility15.8 mg/mLALOGPS
logP-1.4ALOGPS
logP-4.5ChemAxon
logS-1.2ALOGPS
pKa (Strongest Acidic)0.67ChemAxon
pKa (Strongest Basic)9.86ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count6ChemAxon
Polar Surface Area161.31 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity42.62 m3·mol-1ChemAxon
Polarizability17.34 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption-0.9635
Blood Brain Barrier+0.6175
Caco-2 permeable-0.6924
P-glycoprotein substrateNon-substrate0.6937
P-glycoprotein inhibitor INon-inhibitor0.937
P-glycoprotein inhibitor IINon-inhibitor0.9868
Renal organic cation transporterNon-inhibitor0.9254
CYP450 2C9 substrateNon-substrate0.8427
CYP450 2D6 substrateNon-substrate0.7949
CYP450 3A4 substrateNon-substrate0.6827
CYP450 1A2 substrateNon-inhibitor0.7892
CYP450 2C9 inhibitorNon-inhibitor0.9049
CYP450 2D6 inhibitorNon-inhibitor0.9336
CYP450 2C19 inhibitorNon-inhibitor0.9049
CYP450 3A4 inhibitorNon-inhibitor0.8539
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9924
Ames testNon AMES toxic0.6692
CarcinogenicityNon-carcinogens0.7877
BiodegradationReady biodegradable0.6385
Rat acute toxicity1.7722 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8231
hERG inhibition (predictor II)Non-inhibitor0.8926
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

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

Targets

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
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Bergstrom JD, Bostedor RG, Masarachia PJ, Reszka AA, Rodan G: Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000 Jan 1;373(1):231-41. [PubMed:10620343]
  3. Dunford JE, Thompson K, Coxon FP, Luckman SP, Hahn FM, Poulter CD, Ebetino FH, Rogers MJ: Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates. J Pharmacol Exp Ther. 2001 Feb;296(2):235-42. [PubMed:11160603]
  4. 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. [PubMed:15713990]
  5. 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. [PubMed:12177810]
  6. 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. [PubMed:15487700]
Kind
Small molecule
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
References
  1. Jahnke W, Henry C: An in vitro assay to measure targeted drug delivery to bone mineral. ChemMedChem. 2010 May 3;5(5):770-6. doi: 10.1002/cmdc.201000016. [PubMed:20209564]
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
  1. 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. [PubMed:30650219]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Cleavage
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
  1. 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. [PubMed:16298452]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Cleavage
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
  1. 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. [PubMed:16298452]

Drug created on June 13, 2005 07:24 / Updated on August 14, 2020 04:25

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