This HTML5 document contains 85 embedded RDF statements represented using HTML+Microdata notation.

The embedded RDF content will be recognized by any processor of HTML5 Microdata.

Namespace Prefixes

PrefixIRI
n2http://linked.opendata.cz/resource/drugbank/drug/
dctermshttp://purl.org/dc/terms/
n17http://linked.opendata.cz/resource/AHFS/
n19http://linked.opendata.cz/resource/drugbank/company/
n21http://linked.opendata.cz/resource/drugbank/drug/DB00399/identifier/wikipedia/
foafhttp://xmlns.com/foaf/0.1/
n10http://linked.opendata.cz/resource/mesh/concept/
n30http://linked.opendata.cz/resource/drugbank/drug/DB00399/identifier/pharmgkb/
n13http://linked.opendata.cz/resource/drugbank/dosage/
n25http://linked.opendata.cz/resource/drugbank/drug/DB00399/identifier/pdb/
n23http://linked.opendata.cz/resource/drugbank/drug/DB00399/identifier/bindingdb/
n7http://linked.opendata.cz/resource/drugbank/drug/DB00399/identifier/pubchem-compound/
n18http://bio2rdf.org/drugbank:
n27http://linked.opendata.cz/resource/drugbank/drug/DB00399/identifier/pubchem-substance/
admshttp://www.w3.org/ns/adms#
n26http://linked.opendata.cz/resource/drugbank/drug/DB00399/identifier/kegg-drug/
n29http://www.rxlist.com/cgi/generic/
n22http://linked.opendata.cz/resource/drugbank/drug/DB00399/identifier/drugbank/
n4http://linked.opendata.cz/resource/drugbank/patent/
n15http://wifo5-03.informatik.uni-mannheim.de/drugbank/resource/drugs/
rdfhttp://www.w3.org/1999/02/22-rdf-syntax-ns#
n24http://linked.opendata.cz/resource/drugbank/drug/DB00399/identifier/national-drug-code-directory/
n16http://linked.opendata.cz/resource/drugbank/medicinal-product/
n9http://linked.opendata.cz/ontology/mesh/
owlhttp://www.w3.org/2002/07/owl#
n3http://linked.opendata.cz/ontology/drugbank/
n8http://linked.opendata.cz/resource/drugbank/property/
xsdhhttp://www.w3.org/2001/XMLSchema#
n20http://linked.opendata.cz/resource/drugbank/drug/DB00399/identifier/chemspider/
n12http://linked.opendata.cz/resource/atc/
n11http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB00399
rdf:type
n3:Drug
n3:description
Zoledronate (zoledronic acid, marketed by Novartis under the trade names Zometa and Reclast) is a bisphosphonate. Zometa is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. An annual dose of Zoledronate may also prevent recurring fractures in patients with a previous hip fracture. Zoledronate is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the FDA also approved Reclast for the treatment of postmenopausal osteoporosis.
n3:dosage
n13:271B4391-363D-11E5-9242-09173F13E4C5 n13:271B4392-363D-11E5-9242-09173F13E4C5 n13:271B4393-363D-11E5-9242-09173F13E4C5 n13:271B4394-363D-11E5-9242-09173F13E4C5 n13:271B438C-363D-11E5-9242-09173F13E4C5 n13:271B438D-363D-11E5-9242-09173F13E4C5 n13:271B438F-363D-11E5-9242-09173F13E4C5 n13:271B4390-363D-11E5-9242-09173F13E4C5 n13:271B4395-363D-11E5-9242-09173F13E4C5 n13:271B4396-363D-11E5-9242-09173F13E4C5 n13:271B438E-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Lyles KW, Colon-Emeric CS, Magaziner JS, Adachi JD, Pieper CF, Mautalen C, Hyldstrup L, Recknor C, Nordsletten L, Moore KA, Lavecchia C, Zhang J, Mesenbrink P, Hodgson PK, Abrams K, Orloff JJ, Horowitz Z, Eriksen EF, Boonen S: Zoledronic Acid and Clinical Fractures and Mortality after Hip Fracture. N Engl J Med. 2007 Sep 26;. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17878149 # Reid IR, Brown JP, Burckhardt P, Horowitz Z, Richardson P, Trechsel U, Widmer A, Devogelaer JP, Kaufman JM, Jaeger P, Body JJ, Brandi ML, Broell J, Di Micco R, Genazzani AR, Felsenberg D, Happ J, Hooper MJ, Ittner J, Leb G, Mallmin H, Murray T, Ortolani S, Rubinacci A, Saaf M, Samsioe G, Verbruggen L, Meunier PJ: Intravenous zoledronic acid in postmenopausal women with low bone mineral density. N Engl J Med. 2002 Feb 28;346(9):653-61. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11870242 # Durie BG, Katz M, Crowley J: Osteonecrosis of the jaw and bisphosphonates. N Engl J Med. 2005 Jul 7;353(1):99-102; discussion 99-102. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16000365
n3:group
approved
n3:halfLife
146 hours
n3:indication
For the treatment of hypercalcemia of malignancy. Also for the treatment of patients with multiple myeloma and patients with documented bone metastases from solid tumors, in conjunction with standard antineoplastic therapy. In May of 2007, the drug was approved for treatment of Paget’s Disease.
n3:manufacturer
n19:271B4388-363D-11E5-9242-09173F13E4C5
owl:sameAs
n15:DB00399 n18:DB00399
dcterms:title
Zoledronate
adms:identifier
n7:68740 n20:61986 n21:Zoledronate n22:DB00399 n23:12578 n24:0078-0387-25 n25:ZOL n26:D01968 n27:46507310 n30:PA10235
n3:mechanismOfAction
The action of zoledronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Zoledronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates such as zoledronate appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass.
n3:packager
n19:271B4387-363D-11E5-9242-09173F13E4C5
n3:patent
n4:1338895 n4:1338937 n4:4939130
n3:routeOfElimination
In 64 patients with cancer and bone metastases, on average (± s.d.) 39 ± 16% of the administered zoledronic acid dose was recovered in the urine within 24 hours, with only trace amounts of drug found in urine post-Day 2.
n3:synonym
ZOL (1-Hydroxy-2-(1H-imidazol-1-yl)ethylidene)bisphosphonic acid Reclast (1-Hydroxy-2-imidazol-1-ylethylidene)diphosphonic acid Zoledronic acid
n3:toxicity
There is no experience of acute overdose. Two patients received zoledronate (32 mg) over 5 minutes in clinical trials. Neither patient experienced any clinical or laboratory toxicity. Overdosage may cause clinically significant hypocalcemia, hypophosphatemia, and hypomagnesemia.
n11:hasAHFSCode
n17:92-00-00
n3:proteinBinding
Approximately 22% bound in human plasma, independent of the concentration. However, Canadian product information states binding to human plasma protein is approximately 56%.
n3:synthesisReference
Judith Aronhime, Revital Lifshitz-Liron, "Zoledronic acid crystal forms, zoledronate sodium salt crystal forms, amorphous zoledronate sodium salt, and processes for their preparation." U.S. Patent US20050054616, issued March 10, 2005.
n9:hasConcept
n10:M0234599
foaf:page
n29:zometa.htm
n3:IUPAC-Name
n8:271B439B-363D-11E5-9242-09173F13E4C5
n3:InChI
n8:271B43A1-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n8:271B43A0-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n8:271B439D-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n8:271B439E-363D-11E5-9242-09173F13E4C5
n3:SMILES
n8:271B439F-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n8:271B43B1-363D-11E5-9242-09173F13E4C5 n8:271B4399-363D-11E5-9242-09173F13E4C5
n3:logP
n8:271B4397-363D-11E5-9242-09173F13E4C5 n8:271B439A-363D-11E5-9242-09173F13E4C5 n8:271B43B2-363D-11E5-9242-09173F13E4C5
n3:logS
n8:271B4398-363D-11E5-9242-09173F13E4C5
n11:hasATCCode
n12:M05BA08
n3:H-Bond-Acceptor-Count
n8:271B43A7-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n8:271B43A8-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n8:271B43A2-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n8:271B43A3-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n8:271B43A5-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n8:271B43A4-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n8:271B43A6-363D-11E5-9242-09173F13E4C5
n3:absorption
Poorly absorbed (oral absorption is about 1% of what intravenous absorption is).
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
118072-93-8
n3:category
n3:clearance
* Renal cl=3.7 +/- 2.0 L/h
n3:containedIn
n16:271B438B-363D-11E5-9242-09173F13E4C5 n16:271B4389-363D-11E5-9242-09173F13E4C5 n16:271B438A-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n8:271B43AD-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n8:271B43AF-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n8:271B43B0-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n8:271B43AC-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n8:271B43AB-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n8:271B43AE-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n8:271B439C-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n8:271B43A9-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n8:271B43AA-363D-11E5-9242-09173F13E4C5