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Association details:
Biomarker:KEAP1 expression
Cancer:Chronic Lymphocytic Leukemia
Drug:brusatol (NRF2 inhibitor)
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: D – Preclinical
Source:
Title:

NRF2 INHIBITION IN COMBINATION WITH IBRUTINIB IN THE TREATMENT OF CHRONIC LYMPHOCYTIC LEUKEMIA– AN IN VITRO STUDY

Published date:
05/11/2023
Excerpt:
The aim of this work was to evaluate the therapeutic potential of an NRF2 inhibitor, Brusatol (BRU), in monotherapy and in association with the BTK inhibitor Ibrutinib (IBR), in an in vitro CLL model, the HG-3 cell line….The results showed that HG-3 cells express NFE2L2 and KEAP-1 genes....BRU in monotherapy and in association with IBR induce a cytostatic and cytotoxic effect, mediated by cell cycle arrest in phase G0/G1 and apoptosis, respectively....Our results suggest that BRU could be a potential pharmacological agent for the therapeutic approach of CLL, in monotherapy and as an adjuvant to treatment with IBR.