Targeting L858R Mutation in Non-Small Cell Lung Cancer

HK Innoen announced on the 21st that its research on candidate targeted anticancer drugs targeting gene mutations in non-small cell lung cancer has been selected for the support project of the "New Drug Research and Development (R&D) Ecosystem Establishment Research" led by the Korea Drug Development Fund (KDDF).


HK Inno.N BI. [Image provided by HK Inno.N]

HK Inno.N BI. [Image provided by HK Inno.N]

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HK Innoen plans to derive a next-generation epidermal growth factor receptor (EGFR) inhibitor candidate substance that produces synergistic effects when combined with standard treatments through a mechanism of action differentiated from existing inhibitors.


The "allosteric EGFR inhibitor" being developed by HK Innoen is a fourth-generation targeted anticancer drug targeting the non-small cell lung cancer L858R mutation. This treatment works by binding to the allosteric site (one of the protein sites) in the EGFR protein structure to inhibit EGFR. HK Innoen explained that this substance is expected to produce synergistic effects when combined with the standard treatment for patients with the L858R mutation in non-small cell lung cancer due to its mechanism differentiated from existing inhibitors.


According to cell-based drug efficacy evaluation results, this substance showed excellent efficacy against major drug-resistant EGFR resistance mutations, including the L858R mutation (double or triple mutations of T790M and C797S). Additionally, it is characterized by having almost no inhibitory effect on normal EGFR, which can minimize side effects such as skin rash caused by existing EGFR tyrosine kinase inhibitors (TKIs).


According to global market forecasts, as of last year, the market size for non-small cell lung cancer treatments reached approximately 30 trillion KRW. Among this, the market size for non-small cell lung cancer EGFR mutation treatments is about 5 trillion KRW, with more than half of this market occupied by the third-generation EGFR TKI drug Osimertinib.


Osimertinib has attracted industry attention as it is known to significantly extend progression-free survival in non-small cell lung cancer patients compared to existing drugs. HK Innoen explained that the allosteric EGFR inhibitor under development is expected to have high market potential in the future due to overcoming resistance to third-generation EGFR TKIs and synergistic effects when combined with these products.


Kim Bong-tae, Director (Executive Director) of HK Innoen’s New Drug Research Institute, said, "Although various treatments are currently being developed to overcome resistance to existing therapies, there is no allosteric EGFR inhibitor in the clinical development stage yet. We will focus on developing next-generation treatments that not only overcome resistance mutations but also demonstrate excellent efficacy in brain metastasis models and produce synergistic effects when combined with existing inhibitors."


The National New Drug Development Project is a government-led, cross-ministerial R&D initiative that supports the entire cycle of new drug development to enhance the global competitiveness of the domestic pharmaceutical and bio industries and improve public health. With the selection for this National New Drug Development Project support task, HK Innoen will receive government funding for research and development to derive next-generation EGFR inhibitor candidate substances.



Meanwhile, the L858R mutation accounts for about 40% of the non-small cell lung cancer EGFR mutation treatment market. However, existing treatments have limitations in efficacy for patients with the L858R mutation, and there are no treatment options for drug-resistant EGFR mutations that arise after drug administration, highlighting the need for drug development to improve this situation.


This content was produced with the assistance of AI translation services.

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