LG Chem is taking on the challenge of developing treatments in uncharted oncology areas where there are no approved therapies and where treatment and survival time extension remain limited.

LG Chem announced on the 30th that it has received clearance from the U.S. Food and Drug Administration (FDA) for an Investigational New Drug (IND) application to conduct a phase 1/2 clinical trial of its anticancer drug candidate “LG00313112.”

LG00313112 is a new drug substance that LG Chem in-licensed from U.S.-based Frontier Medicines in April. At that time, the company signed an agreement for exclusive global rights (excluding Greater China, including China and Taiwan) for development and commercialization.

This drug candidate targets the “TP53 Y220C” mutation, which is found in 1–3% of all cancer patients. TP53 Y220C is a missense mutation occurring in the tumor suppressor gene TP53. Normal p53 protein plays the role of a “guardian of the genome” by detecting DNA damage in cells and inducing apoptosis; when this protein is mutated, it can trigger cancer.

Structurally, the 220th amino acid of the p53 protein, tyrosine (Y), is replaced by cysteine (C). Targeted therapy for the TP53 Y220C mutation has recently drawn considerable attention in new drug development and precision medicine. A missense mutation is a genetic mutation in which a different amino acid is incorporated into the protein, changing the composition of the protein and altering the function or role of the final synthesized protein. Proteins beneficial to the body can thereby be transformed into tumor-promoting proteins.

LG Chem explained that LG00313112 works by stabilizing the structurally destabilized p53 protein caused by the mutation, thereby restoring its original tumor-suppressive function. The company particularly emphasized that, as the first covalent-based drug design in its class, the candidate is expected to exhibit stable binding affinity to the target and sustained pharmacological activity.

In preclinical studies, superior anticancer efficacy and durability of response were observed even at low doses. LG Chem added that anticancer activity was maintained in tumor models harboring co-occurring KRAS mutations—representative oncogenic driver mutations in solid tumors—that are expressed in various tumors.

According to data from The Cancer Genome Atlas (TCGA) compiled by the U.S. National Cancer Institute (NCI), the average post-treatment survival time for cancer patients with TP53 gene mutations is 29 months. This is more than 50% shorter than the 63 months observed in patients without the mutation. To date, there are no commercialized drugs specifically targeting this mutation.

LG Chem stated that to accelerate development, it has designed a clinical trial that integrates phase 1 and phase 2 into a single protocol. Through this, the company aims to secure dosage and efficacy data early in the initial clinical phase and shorten the overall development timeline. Specifically, in phase 1, the trial will evaluate safety, tolerability, recommended phase 2 dose, and preliminary efficacy in patients with advanced solid tumors such as ovarian, lung, and breast cancers that harbor the TP53 Y220C mutation. Based on the phase 1 results, phase 2 will further refine and intensify the evaluation of efficacy.

Kim Hye-jin, Head of Clinical Development Group at LG Chem, said, “By leveraging a precision medicine approach grounded in clear biomarkers, we will efficiently identify patients in whom a treatment response can be expected, thereby increasing the likelihood of success in new drug development,” adding, “We will accelerate new drug development so that cancer patients with limited treatment options can maintain healthier lives for a longer period.”

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