Drug Information

Drug (ID: DG01630) and It's Reported Resistant Information

• Name: Nazartinib
• Synonyms: Nazartinib; EGF816; 1508250-71-2; EGF-816; UNII-KE7K32EME8; EGF 816; NVP-EGF816-NX; KE7K32EME8; CHEMBL3787344; NVS-816; N-[7-chloro-1-[(3R)-1-[(E)-4-(dimethylamino)but-2-enoyl]azepan-3-yl]benzimidazol-2-yl]-2-methylpyridine-4-carboxamide; N-{7-chloro-1-[(3R)-1-[(2E)-4-(dimethylamino)but-2-enoyl]azepan-3-yl]-1H-1,3-benzodiazol-2-yl}-2-methylpyridine-4-carboxamide; Nazartinib [USAN]; Nazartinib(EGF816); Nazartinib (USAN/INN); GTPL9204; SCHEMBL16767232; SCHEMBL16767240; EX-A1640; BDBM50160870; NSC787027; s7824; Nazartinib (EGF816, NVS-816); ZINC210610738; CCG-269658; NSC-787027; compound 47 [PMID: 27433829]; (R,E)-N-(7-chloro-1-(1-(4-(dimethylamino)but-2-enoyl)azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide; AC-29881; AS-75243; HY-12872; B5889; J3.535.960E; A14416; C72867; D11430; A884136; Q27087855; 4-Pyridinecarboxamide, N-[7-chloro-1-[(3R)-1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]hexahydro-1H-azepin-3-yl]-1H-benzimidazol-2-yl]-2-methyl-; N-[7-chloro-1-[(3r)-1-[(2e)-4-(dimethylamino)-1-oxo-2-buten-1-yl]hexahydro-1h-azepin-3-yl]-1h-benzimidazol-2-yl]-2-methyl-4-pyridinecarboxamide
• Target: .; NOUNIPROTAC; [1]
• Formula: 6
• IsoSMILES: CC1=NC=CC(=C1)C(=O)NC2=NC3=C(N2[C@@H]4CCCCN(C4)C(=O)/C=C/CN(C)C)C(=CC=C3)Cl
• InChI: InChI=1S/C26H31ClN6O2/c1-18-16-19(12-13-28-18)25(35)30-26-29-22-10-6-9-21(27)24(22)33(26)20-8-4-5-15-32(17-20)23(34)11-7-14-31(2)3/h6-7,9-13,16,20H,4-5,8,14-15,17H2,1-3H3,(H,29,30,35)/b11-7+/t20-/m1/s1
• InChIKey: IOMMMLWIABWRKL-WUTDNEBXSA-N
• PubChem CID: 72703790
• DrugBank ID: DB16250

Type(s) of Resistant Mechanism of This Drug

  EADR: Epigenetic Alteration of DNA, RNA or Protein

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Solid tumour/cancer [ICD-11: 2A00-2F9Z]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: Epidermal growth factor receptor (EGFR) [1]

• Molecule Alteration: Duplication; p.S768_D770 (c.2302_2310)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vitro Model: HCC827 cells; Lung; Homo sapiens (Human); CVCL_2063
• In Vitro Model: HaCaT cells; Tongue; Homo sapiens (Human); CVCL_0038
• In Vitro Model: A431 cells; Skin; Homo sapiens (Human); CVCL_0037
• In Vitro Model: H3255 cells; Lung; Homo sapiens (Human); CVCL_6831
• In Vivo Model: NSG mouse PDX model; Mus musculus
• Experiment for Drug Resistance: Promega assay
• Mechanism Description: EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor

Key Molecule: Epidermal growth factor receptor (EGFR) [1]

• Molecule Alteration: Duplication; p.N771_H773 (c.2311_2319)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vitro Model: HCC827 cells; Lung; Homo sapiens (Human); CVCL_2063
• In Vitro Model: HaCaT cells; Tongue; Homo sapiens (Human); CVCL_0038
• In Vitro Model: A431 cells; Skin; Homo sapiens (Human); CVCL_0037
• In Vitro Model: H3255 cells; Lung; Homo sapiens (Human); CVCL_6831
• In Vivo Model: NSG mouse PDX model; Mus musculus
• Experiment for Drug Resistance: Promega assay
• Mechanism Description: EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor

Lung cancer [ICD-11: 2C25]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: Epidermal growth factor receptor (EGFR) [1]

• Molecule Alteration: Duplication; p.N771_H773 (c.2311_2319)
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vitro Model: HCC827 cells; Lung; Homo sapiens (Human); CVCL_2063
• In Vitro Model: HaCaT cells; Tongue; Homo sapiens (Human); CVCL_0038
• In Vitro Model: A431 cells; Skin; Homo sapiens (Human); CVCL_0037
• In Vitro Model: H3255 cells; Lung; Homo sapiens (Human); CVCL_6831
• In Vivo Model: NSG mouse PDX model; Mus musculus
• Experiment for Drug Resistance: Promega assay
• Mechanism Description: EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor

References

• Ref 1: EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF ReceptorCancer Res. 2016 Mar 15;76(6):1591-602. doi: 10.1158/0008-5472.CAN-15-2581. Epub 2016 Jan 29.