Therapex CEO Koo Lee PhD (left) presenting the follow-up results of the preclinical study of the non-small cell lung cancer targeted 

anti-cancer drug "TRX-221" during the poster session of the European Society for Medical Oncology in Madrid, Spain, on October 23rd.

Therapex, a subsidiary of Gradient, announced on October 24th that it presented the follow-up results of the preclinical study of the non-small cell lung cancer targeted anti-cancer drug "TRX-221" during the poster session of the European Society for Medical Oncology.

At this conference, Therapex presented the pharmacokinetics/pharmacodynamics (PK/PD) modeling of TRX-221, along with the results of multiple experiments, including in vivo selectivity and blood-brain barrier (BBB) permeability, in wild-type mouse models of tumor transplantation.

According to Therapex, the EGFR wild-type tumor transplant mouse model, unlike the EGFR mutation tumor transplant mouse model, exhibits greater selectivity towards tumor mutations, with a decrease in tumor growth inhibition efficacy compared to EGFR normal cells.

The results of the study with a high dose of TRX-221 in mouse models of wild-type EGFR lung cancer showed significantly lower tumor growth inhibition efficacy compared to Gefitinib (first-generation inhibitor) and Osimertinib (third-generation inhibitor).

In previous studies, researchers found that TRX-221 exhibited a higher rate of tumor growth inhibition in the EGFR-mutant tumor transplant model compared to Gefitinib and Osimertinib. This demonstrated that TRX-221 has a high selectivity for EGFR mutations.

In addition, TRX-221 was repeatedly administered to Osimertinib-resistant tumor cells in an intracranial tumor transplantation mouse model to measure the drug levels in the brain and blood. As a result, the level of drug exposure above the appropriate threshold was observed, confirming the brain permeability of TRX-221.

CEO Koo Lee PhD stated, “We will strive to conduct the first patient administration as soon as possible for TRX-221, which has entered the clinical pipeline,” and added, “We aim to become a company that achieves continuous growth by further strengthening our research and development capabilities.”

Source: Korea Economic Magazine, Reporter Park In Hyuck (https://www.hankyung.com/article/202310242100i)