Drug Information

Drug (ID: DG01679) and It's Reported Resistant Information

• Name: Ibrutinib/Ruxolitinib
• Synonyms: Ibrutinib/Ruxolitinib
• Target: .; NOUNIPROTAC; [1]

Type(s) of Resistant Mechanism of This Drug

  UAPP: Unusual Activation of Pro-survival Pathway

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

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Granulocyte colony-stimulating factor receptor (CSF3R) [1]

• Molecule Alteration: Nonsense; p.Q741* (c.2221C>T)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: BTK signaling pathway; Inhibition; hsa04662
• Experiment for Drug Resistance: Trypan blue staining assay
• Mechanism Description: G-CSFR mutants showed abnormal kinetics of canonical STAT3, STAT5 and MAPK phosphorylation, and aberrant activation of Bruton's Tyrosine Kinase (Btk).

Key Molecule: Granulocyte colony-stimulating factor receptor (CSF3R) [1]

• Molecule Alteration: Missense mutation; p.T618I (c.1853C>T)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: BTK signaling pathway; Inhibition; hsa04662
• Experiment for Drug Resistance: Trypan blue staining assay
• Mechanism Description: G-CSFR mutants showed abnormal kinetics of canonical STAT3, STAT5 and MAPK phosphorylation, and aberrant activation of Bruton's Tyrosine Kinase (Btk).

References

• Ref 1: Time resolved quantitative phospho-tyrosine analysis reveals Bruton's Tyrosine kinase mediated signaling downstream of the mutated granulocyte-colony stimulating factor receptorsLeukemia. 2019 Jan;33(1):75-87. doi: 10.1038/s41375-018-0188-8. Epub 2018 Jul 5.