Drug Information

Drug (ID: DG00541) and It's Reported Resistant Information

• Name: Brentuximab vedotin
• Synonyms: Brentuximab; Brentuximab vedotin; Brentuximab vedotin brentuximab; Brentuximab vedotina; cAC10-vcMMAE; Moab, chimeric, SGN-30, to CD30 antigen; Monoclonal antibody SGN-30
• Indication:
  In total 1 Indication(s)
  Hodgkin lymphoma [ICD-11: 2B30]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
  Hodgkin lymphoma [ICD-11: 2B30]; [1]
• Target: Brentuximab vedotin; TNR8_HUMAN; [1]
• Formula: C6476H9930N1690O2030S40
• DrugBank ID: DB08870

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

Hodgkin lymphoma [ICD-11: 2B30]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Key Molecule: Pleiotropic ABC efflux transporter of multiple drugs CDR /Multidrug resistance protein 1 (CDR1/ABCB1) [1]

• Molecule Alteration: Expression; Up-regulation
• Resistant Disease: Hodgkin lymphoma [ICD-11: 2B30.0]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Cell apoptosis; Inhibition; hsa04210
• Cell Pathway Regulation: Cell proliferation; Activation; hsa05200
• In Vitro Model: L428 cells; Lymph; Homo sapiens (Human); CVCL_1361
• In Vitro Model: KM-H2 cells; Lymph; Homo sapiens (Human); CVCL_1330
• In Vivo Model: Female NSG mouse model; Mus musculus
• Experiment for Molecule Alteration: Flow cytometry
• Experiment for Drug Resistance: MTS assay
• Mechanism Description: Competitive inhibition of MDR1 restored sensitivity to BV in our BV-resistant cell lines by increasing intracellular MMAE levels, and potentiated BV activity in BV-resistant HL tumors in a human xenograft mouse model.

References

• Ref 1: Inhibition of MDR1 Overcomes Resistance to Brentuximab Vedotin in Hodgkin LymphomaClin Cancer Res. 2020 Mar 1;26(5):1034-1044. doi: 10.1158/1078-0432.CCR-19-1768. Epub 2019 Dec 6.