loading...| 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 |
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| Accepted_Therapeutic_Use_For |
metastatic non-small cell lung cancer (NSCLC) whose tumors have non-resistant epidermal growth factor receptor (EGFR) mutations |
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| CAS_Registry |
850140-73-7 |
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| code |
C97273 |
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| 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 |
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| Has_Free_Acid_Or_Base_Form | ||
| Has_Target | ||
| 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 |
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| Is_Value_For_GDC_Property | ||
| 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 |
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| prefixIRI |
NCIT:C97273 |
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| prefLabel |
Afatinib Dimaleate |
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| Semantic_Type |
Pharmacologic Substance |
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| UMLS_CUI |
C1879772 |
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| subClassOf |