| Attributes | Values |
|---|
| rdf:type
| |
| http://linked.open...gbank/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. (en)
|
| http://linked.open...y/drugbank/dosage
| |
| http://linked.open...generalReferences
| |
| http://linked.open...gy/drugbank/group
| |
| http://linked.open...drugbank/halfLife
| - Cancer patients, repeat dosing = 37 hours (en)
|
| http://linked.open...ugbank/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. (en)
|
| sameAs
| |
| Title
| |
| adms:identifier
| |
| http://linked.open...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. (en)
|
| http://linked.open...outeOfElimination
| - 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. (en)
|
| http://linked.open.../drugbank/synonym
| - Afatinibum (en)
- BIBW 2992 (en)
|
| http://linked.open...drugbank/toxicity
| - Most common adverse reactions (≥20%) are diarrhea, rash/dermatitis, acneiform, stomatitis, paronychia, dry skin, decreased appetite, pruritus. (en)
|
| http://linked.open.../drug/hasAHFSCode
| |
| http://linked.open...k/foodInteraction
| - When given with a high-fat meal, Cmax decreases by 50% and AUC by 39% relative to the fasted state. (en)
|
| http://linked.open...nk/proteinBinding
| - 95% bound to human plasma protein. (en)
|
| http://linked.open...ogy/drugbank/salt
| |
| foaf:page
| |
| http://linked.open...ugbank/IUPAC-Name
| |
| http://linked.open...gy/drugbank/InChI
| |
| http://linked.open...Molecular-Formula
| |
| http://linked.open.../Molecular-Weight
| |
| http://linked.open...noisotopic-Weight
| |
| http://linked.open...y/drugbank/SMILES
| |
| http://linked.open.../Water-Solubility
| |
| http://linked.open...ogy/drugbank/logP
| |
| http://linked.open...ogy/drugbank/logS
| |
| http://linked.open...l/drug/hasATCCode
| |
| http://linked.open...nd-Acceptor-Count
| |
| http://linked.open...-Bond-Donor-Count
| |
| http://linked.open...drugbank/InChIKey
| |
| http://linked.open...urface-Area--PSA-
| |
| http://linked.open...nk/Polarizability
| |
| http://linked.open...bank/Refractivity
| |
| http://linked.open...atable-Bond-Count
| |
| http://linked.open...ugbank/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. (en)
|
| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
|
| http://linked.open...casRegistryNumber
| |
| http://linked.open...k/Bioavailability
| |
| http://linked.open...bank/Ghose-Filter
| |
| http://linked.open...nk/MDDR-Like-Rule
| |
| http://linked.open...k/Number-of-Rings
| |
| http://linked.open...siological-Charge
| |
| http://linked.open...bank/Rule-of-Five
| |
| http://linked.open...tional-IUPAC-Name
| |
| http://linked.open...strongest-acidic-
| |
| http://linked.open...-strongest-basic-
| |
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