Drug Information

Drug (ID: DG01007) and It's Reported Resistant Information

• Name: Conivaptan
• Synonyms: Conivaptan; 210101-16-9; YM087; YM-087; Conivaptan (INN); Conivaptan [INN]; UNII-0NJ98Y462X; N-[4-(2-methyl-4,5-dihydro-3H-imidazo[4,5-d][1]benzazepine-6-carbonyl)phenyl]-2-phenylbenzamide; CHEBI:681850; 0NJ98Y462X; Conivaptan-d4; 4'-((4,5-dihydro-2-methylimidazo(4,5-d)(1)benzazepin-6(1H)-yl)carbonyl)-2-biphenylcarboxanilide; CHEMBL1755; SCHEMBL49815; GTPL2203; BDBM85095; DTXSID80175220; HMS3745C21; BCP07817; PDSP1_001735; PDSP2_001718; ZINC12503187; AKOS015917893; CAS_151171; DB00872; NSC_151171; NCGC00345881-02; NCGC00345881-03; NCGC00345881-04; NCGC00345881-05; AC-30626; N-{4-[(2-methyl-4,5-dihydroimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl}biphenyl-2-carboxamide; DB-066404; AM20090722; FT-0724257; D07748; AB01565868_02; L001073; L001531; Q5161126; (1,1'-Biphenyl)-2-carboxamide, N-(4-(4,5-dihydro-2-methylimidazo(4,5-d)(1)benzazepin-6(1H)-yl)carbonyl)phenyl)-; [1,1'-Biphenyl]-2-carboxamide, N-[4-[(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl]-; 4'-[(2-Methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepin-6-yl)carbonyl]-2-phenylbenzanilide; N-[4-({4-methyl-3,5,9-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),2(6),3,11,13-pentaen-9-yl}carbonyl)phenyl]-2-phenylbenzamide; N-[4-(2-methyl4,5-dihydro-3H-imidazo[5,4-d][1]benzazepine-6-carbonyl)phenyl]-2-phenylbenzamide; N-[4-[(4,5-Dihydro-2-methylimidazo[4,5-d][benzazepin-6(1H)-yl)carbonyl]phenyl-[1,1'-biphenyl]-2-carboxamide hydrochloride
• Indication:
  In total 1 Indication(s)
  Euvolemic hyponatremia [ICD-11: 5C72]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]; [1]
• Target: Vasopressin V1a receptor (V1AR); V1AR_HUMAN; [1]
• Target: Vasopressin V2 receptor (V2R); V2R_HUMAN; [1]
• Formula: C32H26N4O2
• IsoSMILES: CC1=NC2=C(N1)CCN(C3=CC=CC=C32)C(=O)C4=CC=C(C=C4)NC(=O)C5=CC=CC=C5C6=CC=CC=C6
• InChI: 1S/C32H26N4O2/c1-21-33-28-19-20-36(29-14-8-7-13-27(29)30(28)34-21)32(38)23-15-17-24(18-16-23)35-31(37)26-12-6-5-11-25(26)22-9-3-2-4-10-22/h2-18H,19-20H2,1H3,(H,33,34)(H,35,37)
• InChIKey: IKENVDNFQMCRTR-UHFFFAOYSA-N
• PubChem CID: 151171
• ChEBI ID: CHEBI:681850
• TTD Drug ID: D0VU2X
• DrugBank ID: DB00872

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 Resistance Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Heme oxygenase 1 (HMOX1) [1]

• Molecule Alteration: Function; Inhibition
• Resistant Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: ATCC 293T cells; Fetal kidney; Homo sapiens (Human); CVCL_0063
• Experiment for Molecule Alteration: Resazurin assay
• Mechanism Description: HMOX1, PRKCA, and NEIL2 contribute to anthracycline resistance within the more complex MDR phenotype, while P-glycoprotein/ABCB1 overexpression causes not only anthracycline resistance but also resistance to other anticancer drug classes. Conivaptan has the potential to be used as the dual inhibitor of HMOX1 and PRKCA, whereas bexarotene has the potential as an HMOX1 inhibitor and desloratadine as a PRKCA inhibitor.

Key Molecule: Protein kinase C alpha (PRKCA) [1]

• Molecule Alteration: Function; Inhibition
• Resistant Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: ATCC 293T cells; Fetal kidney; Homo sapiens (Human); CVCL_0063
• Experiment for Molecule Alteration: Resazurin assay
• Mechanism Description: HMOX1, PRKCA, and NEIL2 contribute to anthracycline resistance within the more complex MDR phenotype, while P-glycoprotein/ABCB1 overexpression causes not only anthracycline resistance but also resistance to other anticancer drug classes. Conivaptan has the potential to be used as the dual inhibitor of HMOX1 and PRKCA, whereas bexarotene has the potential as an HMOX1 inhibitor and desloratadine as a PRKCA inhibitor.

References

• Ref 1: Identification of Novel Anthracycline Resistance Genes and Their Inhibitors .Pharmaceuticals (Basel). 2021 Oct 16;14(10):1051. doi: 10.3390/ph14101051. 10.3390/ph14101051