Inhibitor overcomes drug resistance in HER2-positive breast cancer

Medical professional examining mammogram

Korean scientists have found that HVH-2930, an innovative HSP90 inhibitor, demonstrates promising efficacy in inducing cancer cell apoptosis and overcoming treatment resistance in HER2-positive breast cancer.

Unlike previous HSP90 inhibitors, the compound circumvents limitations by bypassing heat shock response (HSR) induction.

Professor Jae Hong Seo, Korea University, who led the research, said: “We have highlighted the pivotal role of HSP90, an oncogenic protein, in fuelling tumour growth by activating key receptor tyrosine kinases, including HER2. While previous N-terminal HSP90 inhibitors faced challenges like inducing the HSR and toxicity, HVH-2930, a C-terminal HSP90 inhibitor, shows promise.”

The study utilised both in vivo and in vitro methods to investigate HER2-positive breast cancer and potential treatments.

The findings revealed that HVH-2930 effectively induced apoptosis in breast cancer cells without triggering the HSR. By selectively targeting HSP90, HVH-2930 downregulated HER2 signalling, crucial in breast cancer progression.

In xenograft mouse models, HVH-2930 inhibited tumour growth, angiogenesis, and cancer stem cell-like properties without causing toxicity.

Moreover, when combined with paclitaxel, HVH-2930 exhibited a synergistic antitumour effect, suggesting its potential as a promising therapeutic strategy for HER2-positive breast cancer.

Professor Seo added: “HVH-2930 stands as a groundbreaking advancement in meeting the critical needs of HER2-positive breast cancer patients, notably those resistant to trastuzumab. With its potential application in other HER2-overexpressing cancers like gastric and esophageal cancers, it holds promise for treating a wider range of patients.

“Moreover, its anticipated affordability compared to current therapies could significantly enhance accessibility, particularly in resource-limited settings such as underdeveloped countries.”

Diana Spencer, Senior Digital Content Editor, DDW

Related Articles

Join FREE today and become a member
of Drug Discovery World

Membership includes:

  • Full access to the website including free and gated premium content in news, articles, business, regulatory, cancer research, intelligence and more.
  • Unlimited App access: current and archived digital issues of DDW magazine with search functionality, special in App only content and links to the latest industry news and information.
  • Weekly e-newsletter, a round-up of the most interesting and pertinent industry news and developments.
  • Whitepapers, eBooks and information from trusted third parties.
Join For Free