Drug Information

Drug (ID: DG00332) and It's Reported Resistant Information

• Name: Pazopanib HCl
• Synonyms: Votrient (TN)
• Indication:
  In total 1 Indication(s)
  Renal cell carcinoma [ICD-11: 2C90]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
  Synovial sarcoma [ICD-11: 2B5A]; [1]
• Target: Platelet-derived growth factor receptor (PDGFR); NOUNIPROTAC; [1]
• Target: Tyrosine-protein kinase Kit (KIT); KIT_HUMAN; [1]
• Target: Vascular endothelial growth factor receptor 2 (KDR); VGFR2_HUMAN; [1]
• Formula: C21H24ClN7O2S
• IsoSMILES: CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N.Cl
• InChI: 1S/C21H23N7O2S.ClH/c1-13-5-6-15(11-19(13)31(22,29)30)24-21-23-10-9-20(25-21)27(3)16-7-8-17-14(2)28(4)26-18(17)12-16;/h5-12H,1-4H3,(H2,22,29,30)(H,23,24,25);1H
• InChIKey: MQHIQUBXFFAOMK-UHFFFAOYSA-N
• PubChem CID: 11525740
• ChEBI ID: CHEBI:71217
• TTD Drug ID: D0F0ZY
• VARIDT ID: DR00185
• DrugBank ID: DB06589

Type(s) of Resistant Mechanism of This Drug

  EADR: Epigenetic Alteration of DNA, RNA or Protein

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Synovial sarcoma [ICD-11: 2B5A]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: Prelamin-A/C (LMNA) [1]

• Molecule Alteration: Expression; Down-regulation
• Resistant Disease: Synovial sarcoma [ICD-11: 2B5A.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: 1273/99 cells; Sarcoma; Homo sapiens (Human); CVCL_N588
• In Vitro Model: HS-SYII cells; Sarcoma; Homo sapiens (Human); CVCL_8719
• In Vitro Model: SYO-1 cells; Sarcoma; Homo sapiens (Human); CVCL_7146
• In Vitro Model: YaFuSS cells; Sarcoma; Homo sapiens (Human); CVCL_L809
• Experiment for Molecule Alteration: qRT-PCR
• Experiment for Drug Resistance: EV isolation, immunoblotting, and nanoparticle tracking analysis
• Mechanism Description: Extracellular vesicle-encapsulated microRNA-761 enhances pazopanib resistance in synovial sarcoma by down-regulating TRIP6, LMNA, and SIRT3 expression.

Key Molecule: hsa-miR-761 [1]

• Molecule Alteration: Expression; Up-regulation
• Resistant Disease: Synovial sarcoma [ICD-11: 2B5A.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: 1273/99 cells; Sarcoma; Homo sapiens (Human); CVCL_N588
• In Vitro Model: HS-SYII cells; Sarcoma; Homo sapiens (Human); CVCL_8719
• In Vitro Model: SYO-1 cells; Sarcoma; Homo sapiens (Human); CVCL_7146
• In Vitro Model: YaFuSS cells; Sarcoma; Homo sapiens (Human); CVCL_L809
• Experiment for Molecule Alteration: RT-PCR
• Experiment for Drug Resistance: EV isolation, immunoblotting, and nanoparticle tracking analysis
• Mechanism Description: Extracellular vesicle-encapsulated microRNA-761 enhances pazopanib resistance in synovial sarcoma by down-regulating TRIP6, LMNA, and SIRT3 expression.

Key Molecule: NAD-dependent protein deacetylase sirtuin-3 (SIRT3) [1]

• Molecule Alteration: Expression; Down-regulation
• Resistant Disease: Synovial sarcoma [ICD-11: 2B5A.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: 1273/99 cells; Sarcoma; Homo sapiens (Human); CVCL_N588
• In Vitro Model: HS-SYII cells; Sarcoma; Homo sapiens (Human); CVCL_8719
• In Vitro Model: SYO-1 cells; Sarcoma; Homo sapiens (Human); CVCL_7146
• In Vitro Model: YaFuSS cells; Sarcoma; Homo sapiens (Human); CVCL_L809
• Experiment for Molecule Alteration: qRT-PCR
• Experiment for Drug Resistance: EV isolation, immunoblotting, and nanoparticle tracking analysis
• Mechanism Description: Extracellular vesicle-encapsulated microRNA-761 enhances pazopanib resistance in synovial sarcoma by down-regulating TRIP6, LMNA, and SIRT3 expression.

Key Molecule: Thyroid receptor-interacting protein 6 (TRIP6) [1]

• Molecule Alteration: Expression; Down-regulation
• Resistant Disease: Synovial sarcoma [ICD-11: 2B5A.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: 1273/99 cells; Sarcoma; Homo sapiens (Human); CVCL_N588
• In Vitro Model: HS-SYII cells; Sarcoma; Homo sapiens (Human); CVCL_8719
• In Vitro Model: SYO-1 cells; Sarcoma; Homo sapiens (Human); CVCL_7146
• In Vitro Model: YaFuSS cells; Sarcoma; Homo sapiens (Human); CVCL_L809
• Experiment for Molecule Alteration: qRT-PCR
• Experiment for Drug Resistance: EV isolation, immunoblotting, and nanoparticle tracking analysis
• Mechanism Description: Extracellular vesicle-encapsulated microRNA-761 enhances pazopanib resistance in synovial sarcoma by down-regulating TRIP6, LMNA, and SIRT3 expression.

References

• Ref 1: Extracellular vesicle-encapsulated microRNA-761 enhances pazopanib resistance in synovial sarcoma. Biochem Biophys Res Commun. 2018 Jan 1;495(1):1322-1327. doi: 10.1016/j.bbrc.2017.11.164. Epub 2017 Nov 27.