Drug Information

Drug (ID: DG01631) and It's Reported Resistant Information

• Name: Abivertinib
• Synonyms: Avitinib; Abivertinib; 1557267-42-1; AC0010; N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide; UNII-CER0OPG92L; CER0OPG92L; AC0010MA; EX-ACEA0010; ACEA100610; Abivertinib (USAN); Abivertinib [USAN]; 1557267-42-1 (free base); AC-0010; A610; N-[3-[[2-[3-fluoro-4-(4-methylpiperazin-1-yl)anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenyl]prop-2-enamide; 2-Propenamide, N-[3-[[2-[[3-fluoro-4-(4-methyl-1-piperazinyl)phenyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenyl]-; N-(3-{2-[3-Fluoro-4-(4-methyl-piperazin-1-yl)-phenylamino]-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy-phenyl)-acrylamide; Avitinib free base; 2-Propenamide, N-(3-((2-((3-fluoro-4-(4-methyl-1-piperazinyl)phenyl)amino)-7H-pyrrolo(2,3-d)pyrimidin-4-yl)oxy)phenyl)-; FUJOVEE; Avitinib (AC0010); avitinib (superceded INN); CHEMBL4297865; SCHEMBL15453394; GTPL10044; EX-A783; BDBM294480; Avitinib(AC0010/AC0010MA); BCP16381; US9586965, Cpd 3; MFCD29089376; s8741; ZINC142081723; AC 0010; CS-W008904; DB15327; DS-19269; HY-19816; N-(3-{2-[3-Fluoro-4-(4-methyl-piperazin-1-yl)-phenylamino]-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy}-phenyl)-acrylamide; CS-0016789; A16826; D11308; F17427; A927386; N-(3-((2-((3-fluoro-4-(4-methylpiperazin-1- yl)phenyl)amino)-7H-pyrrolo[2,3-d]- pyrimidin-4-yl)oxy)phenyl)acrylamide; N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo(2,3-d)pyrimidin-4-yl)oxy)phenyl)prop-2-enamide; N-(3-(2-(3-Fluoro-4-(4-methylpiperazin-1-yl)phenylamino)-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy)phenyl)acrylamide; N-[3-[[2-[[3-fluoro-4-(4-methyl-1-piperazinyl)phenyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenyl]-2-propenamide
• Indication:
  In total 2 Indication(s)
  Non-small-cell lung cancer [ICD-11: 2C25]; Patented; [1]
  Non-small-cell lung cancer [ICD-11: 2C25]; Patented; [1]
• Target: Epidermal growth factor receptor (EGFR); EGFR_HUMAN; [1]
• Formula: 7
• IsoSMILES: CN1CCN(CC1)C2=C(C=C(C=C2)NC3=NC4=C(C=CN4)C(=N3)OC5=CC=CC(=C5)NC(=O)C=C)F
• InChI: InChI=1S/C26H26FN7O2/c1-3-23(35)29-17-5-4-6-19(15-17)36-25-20-9-10-28-24(20)31-26(32-25)30-18-7-8-22(21(27)16-18)34-13-11-33(2)12-14-34/h3-10,15-16H,1,11-14H2,2H3,(H,29,35)(H2,28,30,31,32)
• InChIKey: UOFYSRZSLXWIQB-UHFFFAOYSA-N
• PubChem CID: 72734520
• TTD Drug ID: D0K7FY
• DrugBank ID: DB15327

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Lung cancer [ICD-11: 2C25]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

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

• Molecule Alteration: Missense mutation; p.T790M (c.2369C>T)
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: A549 cells; Lung; Homo sapiens (Human); CVCL_0023
• In Vitro Model: Hela cells; Cervix uteri; Homo sapiens (Human); CVCL_0030
• In Vitro Model: HCC827 cells; Lung; Homo sapiens (Human); CVCL_2063
• In Vitro Model: NCI-H460 cells; Lung; Homo sapiens (Human); CVCL_0459
• In Vitro Model: BEAS-2B cells; Bronchus; Homo sapiens (Human); CVCL_0168
• In Vitro Model: A431 cells; Skin; Homo sapiens (Human); CVCL_0037
• In Vitro Model: NCI-H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vitro Model: NIH 3T3 cells; Colon; Homo sapiens (Human); CVCL_0594
• In Vitro Model: HT1080 cells; Acetabulum; Homo sapiens (Human); CVCL_0317
• In Vivo Model: Nu/Nu nude mouse xenograft model; Mus musculus
• Experiment for Drug Resistance: WST-1 assay

Unusual Activation of Pro-survival Pathway (UAPP)

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

• Molecule Alteration: IF-deletion; p.E746_A750delELREA (c.2236_2250del15)
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Experimental Note: Identified from the Human Clinical Data
• Cell Pathway Regulation: EGFR signaling pathway; Inhibition; hsa01521
• In Vitro Model: A549 cells; Lung; Homo sapiens (Human); CVCL_0023
• In Vitro Model: Hela cells; Cervix uteri; Homo sapiens (Human); CVCL_0030
• In Vitro Model: HCC827 cells; Lung; Homo sapiens (Human); CVCL_2063
• In Vitro Model: NCI-H460 cells; Lung; Homo sapiens (Human); CVCL_0459
• In Vitro Model: BEAS-2B cells; Bronchus; Homo sapiens (Human); CVCL_0168
• In Vitro Model: A431 cells; Skin; Homo sapiens (Human); CVCL_0037
• In Vitro Model: NCI-H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vitro Model: NIH 3T3 cells; Colon; Homo sapiens (Human); CVCL_0594
• In Vitro Model: HT1080 cells; Acetabulum; Homo sapiens (Human); CVCL_0317
• In Vivo Model: Nude mouse PDX model; Mus musculus
• Experiment for Molecule Alteration: Immunoblotting analysis; ELISA assay
• Experiment for Drug Resistance: WST-1 assay

References

• Ref 1: AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer PatientsMol Cancer Ther. 2016 Nov;15(11):2586-2597. doi: 10.1158/1535-7163.MCT-16-0281. Epub 2016 Aug 29.