Drug Information

Drug (ID: DG02147) and It's Reported Resistant Information

• Name: DB2Py
• Synonyms: DB2Py
• Indication:
  In total 1 Indication(s)
  . .; .; [1]

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

Unspecified malignant neoplasms of unspecified sites [ICD-11: 2D4Z]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Key Molecule: P-glycoprotein (ABCB1) [1]

• Sensitive Disease: cancer [ICD-11: 2D4Z]
• Molecule Alteration: Expression; Up-regulation
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HBL-100/DOX cells; epithelial cell; Homo sapiens (Human); N.A.
• Experiment for Drug Resistance: Microculture tetrazolium assay
• Mechanism Description: The investigated bis-benzimidazole-pyrroles did not belong to the P-gp substrates. The HBL-100/DOX resistance to DB2Py(4) was 9-fold higher if compared to that to HBL-100, whereas the resistance of P-gpoverexpressing cells to such classical P-gp substrates as doxorubicin and paclitaxel increased 50-100 times and more. In this respect, a conclusion can be drawn that DB2Py(4) is a weak P-gp substrate; i.e., only the monomeric MB2Py and MB2Py(Ac) are able to completely overcome the MDR associated with P-gp overexpression.

References

• Ref 1: Dimeric Bis-Benzimidazole-Pyrroles DB2Py(n) - AT-Site-Specific Ligands: Synthesis, Physicochemical Analysis, and Biological Activity. Acta Naturae. 2024 Jan-Mar;16(1):86-100.