Drug Information

Drug (ID: DG01753) and It's Reported Resistant Information

• Name: Everolimus/PLX4720
• Synonyms: Everolimus/PLX4720
• 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

Brain cancer [ICD-11: 2A00]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) [1]

• Molecule Alteration: Missense mutation; p.V600E (c.1799T>A)
• Sensitive Disease: Brain glioma [ICD-11: 2A00.0]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: BRAF/MEK/MAPK signaling pathway; Inhibition; hsa04010
• In Vitro Model: DBTRG cells; Brain; Homo sapiens (Human); CVCL_1169
• In Vitro Model: SF9427 cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: SF8628 cells; Brain; Homo sapiens (Human); CVCL_IT46
• In Vitro Model: SF188 cells; Brain; Homo sapiens (Human); CVCL_6948
• In Vitro Model: BT40 cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: AM-38 cells; Brain; Homo sapiens (Human); CVCL_1070
• In Vivo Model: NSG mouse PDX model; Mus musculus
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: Promega assay
• Mechanism Description: Combination therapy in BRAFV600E-mutant human glioma cells enhances cell cycle arrest and apoptosis and reduces proliferation compared to monotherapy.

References

• Ref 1: BRAF Status in Personalizing Treatment Approaches for Pediatric GliomasClin Cancer Res. 2016 Nov 1;22(21):5312-5321. doi: 10.1158/1078-0432.CCR-15-1101. Epub 2016 May 23.