Afatinib Dimaleate

Preferred Label : Afatinib Dimaleate;

NCIt synonyms : (2E)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(((3S)-tetrahydrofuran-3-yl)oxy)quinazolin- 6-yl)-4-(dimethylamino)but-2-enamide bis(hydrogen (2Z)-but-2-enedioate); 2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-,(2E)-, (2Z)-2-Butenedioate (1:2);

NCIt definition : The dimaleate salt form of afatinib, an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity. Upon administration, afatinib selectively and irreversibly binds to and inhibits the epidermal growth factor receptors 1 (ErbB1; EGFR), 2 (ErbB2; HER2), and 4 (ErbB4; HER4), and certain EGFR mutants, including those caused by EGFR exon 19 deletion mutations or exon 21 (L858R) mutations. This may result in the inhibition of tumor growth and angiogenesis in tumor cells overexpressing these RTKs. Additionally, afatinib inhibits the EGFR T790M gatekeeper mutation which is resistant to treatment with first-generation EGFR inhibitors. EGFR, HER2 and HER4 are RTKs that belong to the EGFR superfamily; they play major roles in both tumor cell proliferation and tumor vascularization and are overexpressed in many cancer cell types.;

UNII : V1T5K7RZ0B;

InChIKey : USNRYVNRPYXCSP-JUGPPOIOSA-N;

CAS number : 850140-73-7; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 850140-73-7 alt lien vers site G-SRS target _blank img src /img/logos/logo_g-srs.png alt Logo G-SRS /a ;

Drug name : Gilotrif;

Molecule name : BIBW2992 MA2; BIBW 2992MA2;

Details

Origin ID

C97273;

UMLS CUI

C3273321;

Semantic type(s)
- Organic Chemical [UMLS semantic type]
- Pharmacologic Substance [UMLS semantic type]
UMLS correspondences (same concept)
- Afatinib dimaleate (substance) [SNOMED CT concept]
chemical_or_drug_affects_gene_product
- Epidermal Growth Factor Receptor [NCIt concept]
- Receptor Tyrosine-Protein Kinase erbB-2 [NCIt concept]
chemical_or_drug_has_physiologic_effect
- Inhibition of Cell Proliferation [NCIt concept]
- Positive Regulation of Apoptosis [NCIt concept]
- Signal Transduction Inhibition [NCIt concept]
concept_is_in_subset
- CTRP Agent Terminology [NCIt concept]
- CTRP Terminology [NCIt concept]
- FDA Established Names and Unique Ingredient Identifier Codes Terminology [NCIt concept]
- GDC Terminology [NCIt concept]
- GDC Therapeutic Agent Terminology [NCIt concept]
- GDC Value Terminology [NCIt concept]
- NCI Drug Dictionary Terminology [NCIt concept]
- NCIt Antineoplastic Agent Terminology [NCIt concept]
has_free_acid_or_base_form
- Afatinib [NCIt concept]
has_target
- Epidermal Growth Factor Receptor [NCIt concept]
- Receptor Tyrosine-Protein Kinase erbB-2 [NCIt concept]
is_component_of_chemotherapy_regimen
- Afatinib/Cetuximab Regimen [NCIt concept]
is_salt_form_of
- Afatinib [NCIt concept]

Keyword's position in hierarchy(ies) :

Main resources

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