Drug Information

Drug (ID: DG00659) and It's Reported Resistant Information

• Name: Vardenafil
• Synonyms: Vardenafil; 224785-90-4; Levitra; Vivanza; UNII-UCE6F4125H; Levitra (TN); 2-{2-ETHOXY-5-[(4-ETHYLPIPERAZIN-1-YL)SULFONYL]PHENYL}-5-METHYL-7-PROPYLIMIDAZO[5,1-F][1,2,4]TRIAZIN-4(1H)-ONE; CHEMBL1520; UCE6F4125H; VDN; CHEBI:46295; BAY38-9456; BAY 38-9456; Vardenafil-d5; 224789-15-5; 2-(2-ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one; 2-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one; Vardenafil ODT; 2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one; 2-{2-ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl}-5-methyl-7-propyl-1H,4H-imidazo[4,3-f][1,2,4]triazin-4-one; HSDB 7304; SR-05000001442; NCGC00167533-01; Vardenafil [USAN:INN:BAN]; Vardenafil (Vivanza); 1189685-70-8; 2-(2-Ethoxy-5-(4-ethylpiperazin-1-yl-1-sulfonyl)phenyl)-5-methyl-7-propyl-3H-imidazo(5,1-f)(1,2,4)triazin-4-one; Vardenafil (USAN/INN); EC 607-088-5; SCHEMBL5772; BSPBio_002392; 1-((3-(3,4-Dihydro-5-methyl-4-oxo-7-propylimidazo(5,1-f)-as-triazin-2-yl)-4-ethoxyphenyl)sulfonyl)-4-ethylpiperazine; GTPL7320; DTXSID3048318; BDBM14776; HMS2089K04; HMS3715F19; BCP02961; EX-A2806; HY-B0442; STK642629; ZINC18324776; AKOS005574038; AKOS015994765; AKOS022186043; BAY-389456; CCG-221149; DB00862; GS-6519; KS-5073; MCULE-5211071344; SB17349; NCGC00167533-03; 2-{2-ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl}-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4-ol; Piperazine, 1-((3-(1,4-dihydro-5-methyl-4-oxo-7-propylimidazo(5,1-f)(1,2,4)triazin-2-yl)-4-ethoxyphenyl)sulfonyl)-4-ethyl-; BCP0726000254; SBI-0206836.P001; FT-0631204; FT-0675783; 85V904; D08668; AB00698215-08; AB01274740-01; AB01274740_02; AB01274740_03; AB01275440-01; Q424161; J-014730; SR-05000001442-1; SR-05000001442-2; BRD-K13926615-003-01-7; BRD-K13926615-003-02-5; Z2790753946; 2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo(5,1-f)triazin-4(3H)-one; 2-(2-ethoxy-5-(4-ethylpiperazin-1-ylsulfonyl)phenyl)-5-methyl-7-propylimidazo[1,5-f][1,2,4]triazin-4(1H)-one; 2-[2-ethoxy-5-(4-ethyl-piperazine-1-sulphonyl)-phenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one; 2-[2-ethoxy-5-(4-ethyl-piperazine-1-sulphonyl)-phenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazine-4-one; 2-[2-ethoxy-5-(4-ethylpiperazine-1-sulfonyl)phenyl]-5-methyl-7-propyl-1H,4H-imidazo[4,3-f][1,2,4]triazin-4-one; 2-[2-ethoxy-5-[(4-ethyl-1-piperazinyl)sulfonyl]phenyl]-5-methyl-7-propyl-imidazo[5,1-f][1,2,4]triazin-4-one; 2-{2-ethoxy-5-[(4-ethylpiperazine-1-)sulfonyl]phenyl}-5-methyl-7-propyl-3H,4H-imidazo[1,5-a][1,2,4]triazin-4-one; citric acid;2-[2-ethoxy-5-(4-ethylpiperazino)sulfonyl-phenyl]-5-methyl-7-propyl-1H-imidazo[5,1-f][1,2,4]triazin-4-one
• Indication:
  In total 1 Indication(s)
  Erectile dysfunction [ICD-11: HA00-HA01]; Approved; [1]
• Target: Phosphodiesterase 5A (PDE5A); PDE5A_HUMAN; [1]
• Formula: C23H32N6O4S
• IsoSMILES: CCCC1=NC(=C2N1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)CC)OCC)C
• InChI: 1S/C23H32N6O4S/c1-5-8-20-24-16(4)21-23(30)25-22(26-29(20)21)18-15-17(9-10-19(18)33-7-3)34(31,32)28-13-11-27(6-2)12-14-28/h9-10,15H,5-8,11-14H2,1-4H3,(H,25,26,30)
• InChIKey: SECKRCOLJRRGGV-UHFFFAOYSA-N
• PubChem CID: 135400189
• ChEBI ID: CHEBI:46295
• TTD Drug ID: D0C9SY
• VARIDT ID: DR00169
• DrugBank ID: DB00862

Type(s) of Resistant Mechanism of This Drug

  IDUE: Irregularity in Drug Uptake and Drug Efflux

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

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Key Molecule: Multidrug resistance protein 1 (ABCB1) [1]

• Molecule Alteration: Expression; Down-regulation
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: MCF-7 cells; Breast; Homo sapiens (Human); CVCL_0031
• In Vitro Model: SJG 2 cells; Ora cavity; Homo sapiens (Human); CVCL_WV26
• In Vitro Model: ATCC 293T cells; Fetal kidney; Homo sapiens (Human); CVCL_0063
• Experiment for Molecule Alteration: Western blotting analysis; Immunofluorescence analysis
• Experiment for Drug Resistance: MTT assay
• Mechanism Description: Vardenafil reverses ABCB1-mediated MDR by directly blocking the drug efflux function of ABCB1.

References

• Ref 1: The phosphodiesterase-5 inhibitor vardenafil is a potent inhibitor of ABCB1/P-glycoprotein transporter .PLoS One. 2011 Apr 28;6(4):e19329. doi: 10.1371/journal.pone.0019329. 10.1371/journal.pone.0019329