First-Ever Presentation of Various Next-Generation Anticancer Agents
Including Targeted, Immuno-Oncology, and Synthetic Lethality Therapies
Daewoong Pharmaceutical has unveiled three next-generation anticancer drug pipelines.
Daewoong Pharmaceutical announced on the 28th that it will introduce three anticancer drug pipelines?'DWP216', 'DWP217', and 'DWP223'?at the American Association for Cancer Research (AACR 2025), held in Chicago, USA, from the 25th to the 30th of next month, presenting preclinical results of the candidate substances in a total of four posters.
The anticancer drug candidates being announced this time are the targeted anticancer drug 'DWP216', the immuno-oncology drug 'DWP217', and the synthetic lethality anticancer drug 'DWP223'. All three are being unveiled for the first time on the global stage and aim to become First-in-Class.
'Targeted Anticancer Drug DWP216' Precisely Targeting Mutant Cancer Cells
DWP216 is a targeted anticancer drug that precisely targets only the TEAD1 protein to treat NF2 mutant cancers. When mutations occur in the tumor suppressor gene NF2, the activity of TEAD, which induces the expression of cancer-related genes, increases. DWP216 selectively inhibits this activity, thereby demonstrating therapeutic effects. In a situation where there are no targeted therapies specialized for NF2 mutant cancers, it is gaining attention as a new treatment option. Unlike existing inhibitors that suppress all types of TEAD (1 to 4), DWP216 selectively inhibits only TEAD1, minimizing the risk of kidney damage while showing strong anticancer effects. It was selected last year as a national new drug development project.
The upcoming presentation will reveal selectivity verification results and data on substances with excellent tumor growth inhibition effects. Notably, the selected candidate substances can cross the Blood-Brain Barrier (BBB), enabling treatment of brain cancers and brain metastases. In animal models, they demonstrated superior tumor suppression effects compared to existing TEAD1-selective inhibitors and pan-TEAD inhibitors.
Additionally, when combined with existing anticancer drugs in non-small cell lung cancer and pancreatic cancer caused by EGFR and KRAS mutations, DWP216 reduced cancer cell resistance and enhanced the efficacy of existing anticancer drugs. The excellent drug-likeness and efficacy, along with minimal adverse reactions, highlight the safety and promise of Daewoong Pharmaceutical’s research results.
'Immuno-Oncology Drug DWP217' Helping Immune Cells Attack Cancer Cells
DWP217 is an immuno-oncology drug that improves the immunosuppressive environment by inhibiting arginase, an enzyme that suppresses immunity. Currently, widely used PD-1 targeted immuno-oncology drugs induce immune cells to recognize and attack cancer rather than directly attacking cancer cells. However, the complex biological environment around cancer cells, called the tumor microenvironment (TME), often interferes with this immune action, resulting in less than expected efficacy.
DWP217 blocks the action of arginase, which reduces immune cell activity, thereby helping immune cells attack cancer cells more strongly. In animal experiments, it showed stronger effects than existing arginase inhibitors and improved the immunosuppressive environment within tumors, enabling immune cells to attack cancer more actively. This research suggests that DWP217 can improve the therapeutic response of immuno-oncology drugs and indicates the potential for development as a combination therapy with PD-1 targeted immuno-oncology drugs in the future.
'Synthetic Lethality Anticancer Drug DWP223' Blocking Cancer Cell Survival Pathways
DWP223 is an anticancer drug with a synthetic lethality mechanism that selectively kills cancer cells by blocking the DNA repair pathway that serves as a survival means in BRCA mutant cancers. It is a new class of precision targeted therapy developed to address cases where existing anticancer drugs (PARP inhibitors) applied to cancers with BRCA1/2 mutations, such as breast and ovarian cancers, show poor response or develop resistance.
Some cancer cells survive through an alternative pathway involving the protein Polθ (Pol Theta) due to insufficient normal repair function after DNA damage. DWP223 inhibits Polθ, cutting off the last survival route of cancer cells and selectively eliminating cancer cells while having minimal effects on normal cells.
In animal experiments, DWP223 showed strong anticancer effects even at low doses, and when combined with existing anticancer drugs (PARP inhibitors), it demonstrated more than 50% tumor reduction. No weight loss or hematologic toxicity was observed, showing significant advantages in terms of safety. DWP223 is currently in preclinical development, with plans to apply for clinical trials (IND) in 2025.
Park Sung-soo, CEO of Daewoong Pharmaceutical, stated, "This AACR presentation is a meaningful achievement demonstrating the possibility of developing First-in-Class anticancer drugs based on Daewoong’s new drug development experience and research capabilities." He added, "Following the fields of autoimmune diseases and fibrosis, we will accelerate the development of global innovative new drugs in the oncology field as well."
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