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Namespace Prefixes

PrefixIRI
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n6http://bio2rdf.org/drugbank:
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owlhttp://www.w3.org/2002/07/owl#
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n10http://linked.opendata.cz/resource/atc/
n8http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB08916
rdf:type
n3:Drug
n3:description
Afatinib is a tyrosine kinase inhibitor which is a 4-anilinoquinazoline. It is prepared has the dimaleate salt. FDA approved on July 12, 2013.
n3:dosage
n7:271B5D01-363D-11E5-9242-09173F13E4C5 n7:271B5D02-363D-11E5-9242-09173F13E4C5 n7:271B5D03-363D-11E5-9242-09173F13E4C5 n7:271B5D04-363D-11E5-9242-09173F13E4C5 n7:271B5D05-363D-11E5-9242-09173F13E4C5 n7:271B5D06-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# FDA label
n3:group
approved
n3:halfLife
Cancer patients, repeat dosing = 37 hours
n3:indication
Afatinib is a kinase inhibitor indicated for the first-line treatment of patient with metastatic non-small cell lung cancer (NSCLC) whose tumours have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test.
owl:sameAs
n6:DB08916
dcterms:title
Afatinib
adms:identifier
n12:0597-0138-30 n13:Afatinib n15:DB08916 n16:D09724
n3:mechanismOfAction
Afatinib is an irreversible kinase inhibitor and binds to the kinase domains of EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) to inhibit tyrosine kinase autophosphorylation. This results in a downregulation of ErbB signalling and subsequent inhibition of proliferation of cell lines expressing wild-type EGFR, selected EGFR exon 19 deletion mutations, or exon 21 L858R mutations. It also inhibited in vitro proliferation of cell lines overexpressing HER2. Overall, tumour growth was inhibited.
n3:routeOfElimination
Excretion of afatinib is primarily via the feces (85%), with 4% recovered in the urine following a single oral dose of afatinib solution. The parent compound accounted for 88% of the recovered dose.
n3:synonym
BIBW 2992 Afatinibum
n3:toxicity
Most common adverse reactions (≥20%) are diarrhea, rash/dermatitis, acneiform, stomatitis, paronychia, dry skin, decreased appetite, pruritus.
n8:hasAHFSCode
n9:10-00%20
n3:foodInteraction
When given with a high-fat meal, Cmax decreases by 50% and AUC by 39% relative to the fasted state.
n3:proteinBinding
95% bound to human plasma protein.
n3:salt
foaf:page
n18:gilotrif.html
n3:IUPAC-Name
n4:271B5D0B-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B5D11-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B5D10-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B5D0D-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B5D0E-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B5D0F-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B5D09-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B5D07-363D-11E5-9242-09173F13E4C5 n4:271B5D0A-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B5D08-363D-11E5-9242-09173F13E4C5
n8:hasATCCode
n10:L01XE13
n3:H-Bond-Acceptor-Count
n4:271B5D17-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B5D18-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B5D12-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B5D13-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B5D15-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B5D14-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B5D16-363D-11E5-9242-09173F13E4C5
n3:absorption
Following oral administration, time to peak plasma concentration (Tmax) is 2 to 5 hours. The geometric mean relative bioavailability of 20 mg tablets was 92% as compared to an oral solution. Food decreases Cmax and AUC relative to the fasted state.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
850140-72-6
n3:Bioavailability
n4:271B5D1D-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B5D1F-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B5D20-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B5D1C-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B5D1B-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B5D1E-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B5D0C-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B5D19-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B5D1A-363D-11E5-9242-09173F13E4C5