Drug Information

Drug (ID: DG00168) and It's Reported Resistant Information

• Name: Fentanyl
• Synonyms: Fentanyl; Fentanil; Phentanyl; Fentora; Sublimaze; Fentanila; Fentanest; Duragesic; Fentanylum; Durogesic; Sentonil; 437-38-7; Duragesic-100; IONSYS; Duragesic-25; Duragesic-75; Duragesic-50; Duragesic-12; Fentanyl-25; Fentanyl-75; Fentanyl-12; Fentanyl-50; Fentanylum [INN-Latin]; Fentanila [INN-Spanish]; Fentanyl-100; 1-Phenethyl-4-N-propionylanilinopiperidine; Matrifen; Sublimase; N-(1-Phenethylpiperidin-4-yl)-N-phenylpropionamide; N-(1-Phenethyl-4-piperidyl)propionanilide; N-Phenethyl-4-(N-propionylanilino)piperidine; Fentanil [DCIT]; Subsys; Fentanyl-37; Fentanyl-62; Fentanyl-87; Abstral; Actiq; Lazanda; Onsolis; Fentanyl Citrate; Fentanyl Citrate Preservative Free; Sublimaze Preservative Free; fentanyl (transmucosal film, pain), Auxilium Pharmaceuticals
• Indication:
  In total 3 Indication(s)
  Sensation disturbance [ICD-11: MB40]; Approved; [1]
  Chronic pain [ICD-11: MG30]; Phase 3; [1]
  Pain [ICD-11: MG30]; Phase 3; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
  Colorectal cancer [ICD-11: 2B91]; [1]
• Target: Opioid receptor mu (MOP); OPRM_HUMAN; [1]
• Formula: C22H28N2O
• IsoSMILES: CCC(=O)N(C1CCN(CC1)CCC2=CC=CC=C2)C3=CC=CC=C3
• InChI: 1S/C22H28N2O/c1-2-22(25)24(20-11-7-4-8-12-20)21-14-17-23(18-15-21)16-13-19-9-5-3-6-10-19/h3-12,21H,2,13-18H2,1H3
• InChIKey: PJMPHNIQZUBGLI-UHFFFAOYSA-N
• PubChem CID: 3345
• ChEBI ID: CHEBI:119915
• TTD Drug ID: D0E1WI
• VARIDT ID: DR00430
• DrugBank ID: DB00813

Type(s) of Resistant Mechanism of This Drug

  EADR: Epigenetic Alteration of DNA, RNA or Protein

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Colorectal cancer [ICD-11: 2B91]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: BRAF-activated non-protein coding RNA (BANCR) [1]

• Molecule Alteration: Expression; Up-regulation
• Resistant Disease: Colorectal cancer [ICD-11: 2B91.1]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Cell apoptosis; Inhibition; hsa04210
• Cell Pathway Regulation: Cell invasion; Activation; hsa05200
• Cell Pathway Regulation: Cell migration; Activation; hsa04670
• Cell Pathway Regulation: Cell proliferation; Activation; hsa05200
• In Vitro Model: SW480 cells; Colon; Homo sapiens (Human); CVCL_0546
• In Vitro Model: LOVO cells; Colon; Homo sapiens (Human); CVCL_0399
• In Vivo Model: Nude mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blot analysis
• Experiment for Drug Resistance: Transwell assay
• Mechanism Description: Fentanyl inhibits the invasion and migration of colorectal cancer cells via inhibiting the negative regulation of Ets-1 on BANCR.

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Protein C-ets-1 (ETS1) [1]

• Molecule Alteration: Expression; Down-regulation
• Resistant Disease: Colorectal cancer [ICD-11: 2B91.1]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Cell apoptosis; Inhibition; hsa04210
• Cell Pathway Regulation: Cell invasion; Activation; hsa05200
• Cell Pathway Regulation: Cell migration; Activation; hsa04670
• Cell Pathway Regulation: Cell proliferation; Activation; hsa05200
• In Vitro Model: SW480 cells; Colon; Homo sapiens (Human); CVCL_0546
• In Vitro Model: LOVO cells; Colon; Homo sapiens (Human); CVCL_0399
• Experiment for Molecule Alteration: qPCR
• Experiment for Drug Resistance: Transwell assay
• Mechanism Description: Fentanyl inhibits the invasion and migration of colorectal cancer cells via inhibiting the negative regulation of Ets-1 on BANCR.

References

• Ref 1: Fentanyl inhibits the invasion and migration of colorectal cancer cells via inhibiting the negative regulation of Ets-1 on BANCR. Biochem Biophys Res Commun. 2015 Sep 25;465(3):594-600. doi: 10.1016/j.bbrc.2015.08.068. Epub 2015 Aug 18.