AI Article Synopsis
- Gefitinib is a drug used to treat non-small cell lung cancer (NSCLC) in patients with certain EGFR mutations, but most patients eventually develop resistance to the treatment.
- A new compound called NBDHEX, which inhibits the enzyme GSTPi, has shown promise by promoting cell death in gefitinib-resistant NSCLC cells and reducing tumor growth in mice.
- These results suggest that NBDHEX could be a potential new treatment option for NSCLC patients who are resistant to conventional therapies.
Article Abstract
Gefitinib, a first-generation EGFR tyrosine kinase inhibitor (EGFR-TKI), is recommended for treatment of non-small cell lung cancer (NSCLC) patients who harbor activating EGFR mutations. However, the tumors of most patients initially sensitive to gefitinib will develop resistance within several months of therapy. Drug resistance is a major obstacle to NSCLC treatment. The novel glutathione transferase P1 (GSTPi) inhibitor 6-(7-nitro-2, 1, 3-benzoxadiazol-4-ylthio) hexanol (NBDHEX) has recently been shown to be active against tumors. In this study, we investigated the and efficacy of NBDHEX against NSCLC. Treatment with NBDHEX inhibited GSTpi enzymatic activity and promoted apoptosis of gefinitb-resistant NSCLC cells. Moreover, NBDHEX reduced tumor growth in mice. These findings indicated that NBDHEX is a good candidate for treatment of NSCLC patients, and that NBDHEX offers a new approach to cancer therapy.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7646187 | PMC |
| http://dx.doi.org/10.7150/jca.46461 | DOI Listing |
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