Drug Information

Drug (ID: DG01663) and It's Reported Resistant Information

• Name: Necitumumab
• Synonyms: SCHEMBL20425500
• Indication:
  In total 1 Indication(s)
  Colorectal cancer [ICD-11: 2B91]; Phase 2; [1]
• Target: Epidermal growth factor receptor (EGFR); EGFR_HUMAN; [1]
• Formula: 8
• IsoSMILES: CC(=O)OCN1C=C(C2=CC(=NC=C21)C3=CC(=CC(=C3)OC)NC(=O)C=C)C4=CC(=NC=C4)C#N
• InChI: InChI=1S/C26H21N5O4/c1-4-26(33)30-19-8-18(9-21(10-19)34-3)24-11-22-23(17-5-6-28-20(7-17)12-27)14-31(15-35-16(2)32)25(22)13-29-24/h4-11,13-14H,1,15H2,2-3H3,(H,30,33)
• InChIKey: HGDHLYSCURABOE-UHFFFAOYSA-N
• PubChem CID: 135263756
• DrugBank ID: DB09559

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

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.S492R (c.1476C>G)
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Hela cells; Cervix uteri; Homo sapiens (Human); CVCL_0030
• In Vitro Model: LK2 cells; Ascites; Homo sapiens (Human); CVCL_W132
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: FACS assay

References

• Ref 1: Molecular Basis for Necitumumab Inhibition of EGFR Variants Associated with Acquired Cetuximab ResistanceMol Cancer Ther. 2018 Feb;17(2):521-531. doi: 10.1158/1535-7163.MCT-17-0575. Epub 2017 Nov 20.