│Shows improved selectivity and blood-brain barrier permeability compared to pre-existing competitors

Kwangwoo Chun, PhD, Managing Director of Drug Discovery of Therapex (center), presented the preclinical results of the EGFR exon 20 insertion-mutant lung cancer therapy 'TRX-211-399' at the American Association for Cancer Research (AACR) Annual Meeting 2024 held in San Diego, USA, on the 8^th of April (local time).

A subsidiary of Gradient, Therapex (CEO Koo Lee, PhD) announced on the 12^th that it presented the preclinical trial results of TRX-211-399, a new drug candidate for EGFR exon 20 insertion-mutant non-small cell lung cancer targeted anticancer agent, at the AACR Annual Meeting 2024 held in San Diego, USA from the 5^th to the 10^th of April.

TRX-211-399 is a small molecule compound discovered by Therapex following its flagship pipeline TRX-221. It targets EGFR exon 20 insertion mutations within the non-small cell lung cancer domain. Therapex suggested the possibility that TRX-211-399, with its improved efficacy and selectivity, could become the best-in-class drug within its category.

At the AACR Annual Meeting, Therapex demonstrated the improved selectivity and blood-brain barrier permeability of TRX-211-399, compared to pre-existing competitors, through poster presentations. According to Therapex, TRX-211-399 not only inhibited EGFR exon 20 insertion mutations, but also strongly inhibited rare EGFR mutations while having reduced inhibition of the growth of wild-type EGFR expressing skin cancer cell line (A431) in Ba/F3 cell growth inhibition experiments, demonstrating selective inhibition of mutant cells. Furthermore, it proved dose-dependent anti-tumor effects in mouse tumor cell xenograft models compared to competitors. Even at the maximum dose, there was no significant weight loss in mouse subjects, indirectly indicating the safety of TRX-211-399.

The company explained that domestic and international experts who attended the conference focused on the brain permeability and intracranial anti-cancer efficacy of TRX-211-399. Furthermore, TRX-211-399 exhibited superior intracranial anti-cancer efficacy compared to Tagrisso (Osimertinib) in mouse intracranial brain tumor cell xenograft models. They revealed that at the end of the experiment they observed some individuals with little to no tumor left to be quantified.

CEO Koo Lee, PhD, of Therapex said, "Participating in this AACR Annual Meeting was a great opportunity to showcase the potential of Therapex's in-house development pipeline, TRX-211-399." He added, "As our clinical pipeline TRX-221 is about to begin first patient dosing, we will continue to strive for further business development, and follow-up project development, to ensure the continuity of our research."

Source: Yakup Newspaper, Reporter Hyuk-jin Kwon hjkwon@yakup.com (https://www.yakup.com/news/index.html?mode=view&cat=12&nid=292977)