loading...| Preferred Name |
Afatinib Dimaleate |
|
| Synonyms |
BIBW 2992MA2 Afatinib Dimaleate BIBW2992 MA2 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) (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) AFATINIB DIMALEATE Gilotrif |
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| 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://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C97273 |
|
| 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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| Concept_In_Subset |
http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C176424 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157711 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157712 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116978 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116977 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C128784 |
|
| Contributing_Source |
CTRP FDA GDC |
|
| 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 |
|
| FULL_SYN |
BIBW 2992MA2 Afatinib Dimaleate BIBW2992 MA2 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) (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) AFATINIB DIMALEATE Gilotrif |
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| Has_Free_Acid_Or_Base_Form | ||
| Has_Target | ||
| 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 |
|
| prefixIRI |
Thesaurus:C97273 |
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| Semantic_Type |
Pharmacologic Substance |
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| UMLS_CUI |
C1879772 |
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| subClassOf |