LIXTE Biotechnology Announces Preclinical Results of its Collaboration With the Netherlands Cancer Institute, Revealing Striking Anti-Cancer Activity

LIXTE Biotechnology Holdings, Inc. recently announced Professor René Bernards, Netherlands Cancer Institute (NKI), Amsterdam, presented new data from promising drug combinations of LIXTE’s lead clinical cancer compound, LB-100, at the Annual Meeting of American Association for Cancer Research (AACR) in New Orleans, LA, on Monday, April 11, 2022.

In brief, LIXTE’s first-in-class lead clinical compound and protein phosphatase 2A (PP2A) inhibitor, LB-100, induces further activation of oncogenic signaling in a number of KRAS-mutant cancers, rendering them particularly vulnerable to anti-cancer therapy. Professor Bernards’ presentation, titled Unconventional Approaches to the Treatment of Cancer, was delivered as part of the events celebrating Professor Bernards’ selection as the awardee of the 2022 AACR Princess Takamatsu Memorial Lectureship. The AACR has stated that this award “recognizes an individual scientist whose novel and significant work has had or may have a far-reaching impact on the detection, diagnosis, treatment, or prevention of cancer, and who embodies the dedication of [Princess Takamatsu] to multinational collaborations.” AACR is the largest cancer research organization in the world, with more than 50,000 members residing in 129 countries and territories.

Professor Bernards discussed his paradoxical approach to developing more effective cancer therapies. The initial studies, done in collaboration with LIXTE, reveal that the vigorous activation of several oncogenic-signaling pathways by LB-100 is associated with marked increases in DNA damage and mitotic stress. CRISPR-based genetic screening and screening of selected investigational compounds both showed that LB-100 is synthetically lethal in combination with inhibitors of the mitotic entry kinase WEE1. Results were confirmed in a group of colorectal cancer cell lines bearing diverse mutations. The mechanisms responsible for these unexpected activities of LB-100 combined with WEE1 kinase inhibitors, were presented.

John S. Kovach MD, Founder and CEO of LIXTE Biotechnology Holdings, Inc., said “we are delighted to be working with Professor Bernards and his team. Professor Bernards’ insights and contributions enable us to take full advantage of the unique anti-cancer properties of LB-100. His creativity in developing new anti-cancer drug combinations has already had a significant impact on cancer care. His current observations of unexpected synergy of LB-100 with a variety of standard agents and with investigational compounds with only modest activity on their own are promising leads to a new approach to cancer chemotherapy.”

LIXTE Biotechnology Holdings, Inc. is a clinical-stage pharmaceutical company focused on new targets for cancer drug development and developing and commercializing cancer therapies. Major drivers of cancer are defects in the switches that turn the biochemical pathways in cells on or off. Most cancer research over the past 30 years has focused on the “on” switches because the “off” switches, especially the master “off” switch protein phosphatase (PP2A), were believed to cause intolerable toxicity in patients. LIXTE has achieved a breakthrough with its novel, first-in-class lead clinical compound and PP2A inhibitor, LB-100, demonstrating that LB-100 is readily tolerated in cancer patients at doses associated with anti-cancer activity. Based on extensive published preclinical data (see www.lixte.com), LB–100 has the potential to significantly improve outcomes for patients undergoing various chemotherapies or immunotherapies. LIXTE’s new approach has no known competitors and is covered by a comprehensive patent portfolio. Initial proof-of-concept clinical trials are in progress.