Preferred Name

Afatinib Dimaleate

Synonyms
Definitions

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.

ID

http://purl.obolibrary.org/obo/NCIT_C97273

Accepted_Therapeutic_Use_For

metastatic non-small cell lung cancer (NSCLC) whose tumors have non-resistant epidermal growth factor receptor (EGFR) mutations

CAS_Registry

850140-73-7

code

C97273

Contributing_Source

CTRP

FDA

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.

Display_Name

Afatinib Dimaleate

FDA_UNII_Code

V1T5K7RZ0B

Has_Free_Acid_Or_Base_Form

http://purl.obolibrary.org/obo/NCIT_C66940

Has_Target

http://purl.obolibrary.org/obo/NCIT_C17068

http://purl.obolibrary.org/obo/NCIT_C17319

in_subset

http://purl.obolibrary.org/obo/NCIT_C63923

http://purl.obolibrary.org/obo/NCIT_C177537

http://purl.obolibrary.org/obo/NCIT_C176424

http://purl.obolibrary.org/obo/NCIT_C116977

http://purl.obolibrary.org/obo/NCIT_C116978

http://purl.obolibrary.org/obo/NCIT_C128784

http://purl.obolibrary.org/obo/NCIT_C157711

http://purl.obolibrary.org/obo/NCIT_C157712

Is_Value_For_GDC_Property

http://purl.obolibrary.org/obo/NCIT_C1909

label

Afatinib Dimaleate

Maps_To

Afatinib Dimaleate

NCI_Drug_Dictionary_ID

537572

PDQ_Closed_Trial_Search_ID

537572

PDQ_Open_Trial_Search_ID

537572

Preferred_Name

Afatinib Dimaleate

prefixIRI

NCIT:C97273

prefLabel

Afatinib Dimaleate

Semantic_Type

Pharmacologic Substance

UMLS_CUI

C1879772

subClassOf

http://purl.obolibrary.org/obo/NCIT_C2167

http://purl.obolibrary.org/obo/NCIT_C129825

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