Accelerating the Development of New Drugs Targeting KRAS-Mutant Solid Tumors
SK Biopharmaceuticals announced that it presented the latest research results on its KRAS G12D inhibitor in a poster session at the American Association for Cancer Research (AACR) 2025 Annual Meeting, held in Chicago, USA, from April 25 to April 30.
KRAS mutations are representative genetic alterations that drive the growth and proliferation of cancer cells. They are commonly found in various solid tumors, including pancreatic cancer, colorectal cancer, and lung cancer. Among these, the KRAS G12D mutation is one of the most frequently observed KRAS mutations and is closely associated with cancer cell proliferation. In particular, it has been reported to occur at a frequency approximately 2.5 times higher than the KRAS G12C mutation, for which existing treatments have been developed. However, there are currently no therapies targeting the KRAS G12D mutation.
At this year's AACR, SK Biopharmaceuticals presented research results on the efficacy and pharmacological properties, such as plasma exposure levels, of its orally administered KRAS G12D inhibitor developed based on a novel compound structure, using preclinical models. According to the research, oral administration of the inhibitor in KRAS G12D-mutant pancreatic ductal adenocarcinoma (PDAC) animal models demonstrated a strong antitumor effect. No significant adverse effects, such as weight loss, were observed.
According to the study, this inhibitor showed high selectivity and strong binding affinity for KRAS G12D, and powerfully suppressed the proliferation of cancer cell lines harboring this mutation. In contrast, it exhibited 50 to 1000 times lower inhibitory effects on the proliferation of other KRAS mutations, and its impact on normal cell growth was found to be minimal. Notably, it demonstrated superior plasma exposure levels compared to previously reported KRAS G12D inhibitor candidates. The inhibitor also showed excellent performance in terms of oral bioavailability and effectively inhibited pERK (phosphorylated ERK) within tumor tissues at low concentrations.
SK Biopharmaceuticals considers the demonstration of this inhibitor's efficacy against pancreatic cancer to be a significant advancement. The company is currently conducting lead optimization with the goal of securing a 'best-in-class' new drug candidate that precisely targets KRAS G12D within the first half of the year.
Lee Donghoon, CEO of SK Biopharmaceuticals, stated, "KRAS G12D represents an area with a significant treatment gap, so we are continuously strengthening our global research capabilities to provide innovative therapeutic options," adding, "We will continue to focus on developing next-generation anticancer drugs to address unmet medical needs."
© The Asia Business Daily(www.asiae.co.kr). All rights reserved.
