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Namespace Prefixes

PrefixIRI
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n13http://linked.opendata.cz/resource/atc/
n12http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB08889
rdf:type
n3:Drug
n3:description
Carfilzomib is an injectable antineoplastic agent (IV only). Chemically, it is a modified tetrapeptidyl epoxide and an analog of epoxomicin. It is also a selective proteasome inhibitor. FDA approved on July 20, 2012.
n3:dosage
n5:271B5ADD-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Kortuem KM, Stewart AK: Carfilzomib. Blood. 2013 Feb 7;121(6):893-7. doi: 10.1182/blood-2012-10-459883. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23393020 # Kuhn DJ, Chen Q, Voorhees PM, Strader JS, Shenk KD, Sun CM, Demo SD, Bennett MK, van Leeuwen FW, Chanan-Khan AA, Orlowski RZ: Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma. Blood. 2007 Nov 1;110(9):3281-90. Epub 2007 Jun 25. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17591945
n3:group
approved
n3:halfLife
Following intravenous administration of doses ≥ 15 mg/m^2, carfilzomib was rapidly cleared from the systemic circulation with a half-life of ≤ 1 hour on Day 1 of Cycle 1.
n3:indication
Carfilzomib is indicated for the treatment of patients with multiple myeloma who have received at least two prior therapies including bortezomib and an immunomodulatory agent and have demonstrated disease progression on or within 60 days of completion of the last therapy. Approval is based on response rate.
owl:sameAs
n8:DB08889
dcterms:title
Carfilzomib
adms:identifier
n10:DB08889 n11:D08880 n14:65347 n15:76075-101-01 n16:Carfilzomib
n3:mechanismOfAction
Carfilzomib is made up of four modified peptides and acts as a proteasome inhibitor. Carfilzomib irreversibly and selectively binds to N-terminal threonine-containing active sites of the 20S proteasome, the proteolytic core particle within the 26S proteasome. This 20S core has 3 catalytic active sites: the chymotrypsin, trypsin, and caspase-like sites. Inhibition of the chymotrypsin-like site by carfilzomib (β5 and β5i subunits) is the most effective target in decreasing cellular proliferation, ultimately resulting in cell cycle arrest and apoptosis of cancerous cells. At higher doses, carfilzomib will inhibit the trypsin-and capase-like sites.
n3:patent
n6:7417042 n6:7491704 n6:8129346 n6:8207125 n6:8207126 n6:8207127 n6:8207297 n6:7737112 n6:7232818
n3:synonym
Kyprolis PR-171
n3:toxicity
Most commonly reported adverse reactions (incidence ≥ 30%) are fatigue, anemia, nausea, thrombocytopenia, dyspnea, diarrhea, and pyrexia. The two dose limiting toxicities are thrombocytopenia and febrile neutropenia. Maximum tolerate dose = 15 mg/m^2
n3:volumeOfDistribution
Vd, steady state, 20 mg/m^2 = 28 L
n12:hasAHFSCode
n17:10-00%20
n3:proteinBinding
Over the concentration range of 0.4 - 4 micromolar, carfilzomib was 97% protein bound.
foaf:page
n19:kyprolis-drug.htm n21:kyprolis.html
n3:IUPAC-Name
n4:271B5AE2-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B5AE8-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B5AE7-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B5AE4-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B5AE5-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B5AE6-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B5AE0-363D-11E5-9242-09173F13E4C5 n4:271B5AF8-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B5AE1-363D-11E5-9242-09173F13E4C5 n4:271B5ADE-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B5ADF-363D-11E5-9242-09173F13E4C5
n3:pKa
n4:271B5AF9-363D-11E5-9242-09173F13E4C5
n12:hasATCCode
n13:L01XX45
n3:H-Bond-Acceptor-Count
n4:271B5AEE-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B5AEF-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B5AE9-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B5AEA-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B5AEC-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B5AEB-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B5AED-363D-11E5-9242-09173F13E4C5
n3:absorption
Cmax, single IV dose of 27 mg/m^2 = 4232 ng/mL; AUC, single IV dose of 27 mg/m^2 = 379 ng•hr/mL; Carfilzomib does not accumulation in the systemic. At doses between 20 and 36 mg/m2, there was a dose-dependent increase in exposure.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
868540-17-4
n3:category
n3:clearance
Systemic clearance = 151 - 263 L/hour. As this value exceeds hepatic blood flow, it suggests that carfilozmib is cleared extrahepatically.
n3:Bioavailability
n4:271B5AF4-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B5AF6-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B5AF7-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B5AF3-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B5AF2-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B5AF5-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B5AE3-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B5AF0-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B5AF1-363D-11E5-9242-09173F13E4C5