"IND application
for Phase 1 study in Korea and the U.S. in the first half of this year... initiate
clinical trials in the second half"
The
American Association for Cancer Research (AACR) Annual Meeting
is one of the largest international oncology meetings held annually, and is set
to be held this year from April 14th onwards.
Therapex announced on February 10th its plans to
attend the AACR 2023 and present the preclinical results of “TRX-221.” TRX-221,
developed in collaboration with Yonsei University's Industry-Academia
Cooperation Division, is a fourth-generation EGFR tyrosine kinase inhibitor
(EGFR TKI) capable of inhibiting C797S mutations. These mutations typically
arise from the use of third-generation EGFR inhibitors such as Tagrisso
(Osimertinib), a standard treatment for EGFR mutant non-small cell lung cancer.
Besides C797S, TRX-221 can target EGFR mutations like Del19, L858R, and T790M.
So far, there is no targeted therapy for the C797S EGFR
mutation, and Therapex explained that their currently ongoing clinical trials for
the “first-in-class” fourth-generation EGFR TKI drug are known to have relatively
insufficient efficacy against C797S double mutations compared to TRX-221.
In cell line-based in vitro experiments, TRX-221
demonstrated inhibitory efficacy against double mutations (Del19/C797S,
L858R/C797S) and triple mutations (Del19/T790M/C797S, L858R/T790M/C797S). These
results were also reproduced in in vivo tumor models.
Therapex confirmed the dose-dependent tumor growth inhibition
efficacy of TRX-221 in various EGFR-mutant tumor models, including those with
the C797S mutation, through once-daily oral administration. Its safety has been
confirmed as no evidence of weight loss was observed.
TRX-221 also proved effective in inhibiting tumor growth in
Patient-Derived Organoid Xenograft (PDOX) mouse models, which were transplanted
with tumors from Tagrisso-resistant patients, showing efficacy even in brain
tumor models due to its blood-brain barrier (BBB) permeability.
CEO Koo Lee Ph.D. stated, "To address unmet needs, we plan
to submit the Investigational New Drug (IND) application for the Phase 1 study
of TRX-221 to the Ministry of Food and Drug Safety of the Republic of Korea
(MFDS) and the U.S. Food and Drug Administration (FDA) in the first half of
this year and initiate clinical trials in the second half." He further
added, "Given the differentiated efficacy profile of TRX-221, we will
still strive to provide effective treatment options to non-small cell lung
cancer patients."
Therapex was established in 2020 by Gradient (formerly
Interpark), having rebranded from “Interpark Bioconvergence.” It specializes in
researching and developing anticancer drugs, with a focus on immunotherapeutic
agents, targeted anticancer agents, and proteolysis-targeting chimeras (TPD).
Source: Reporter Kim Sungmin (http://www.biospectator.com/view/news_view.php?varAtcId=18250)