Medicilon congratulates Genfleet Therapeutics on the approval and launch of their KRAS G12C inhibitor, Fuzerelisib.

Recently, Genfleet Therapeutics launched its KRAS G12C inhibitor, Dabote® (Fuzerelisib Tablets, GFH925/IBI351).  This product, as a monotherapy, is indicated for adult patients with KRAS G12C-mutant advanced non-small cell lung cancer (NSCLC) who have received at least one prior systemic therapy. It is the first KRAS G12C inhibitor approved in China and the third KRAS G12C inhibitor to be launched globally.

Shanghai Medicilon Inc. (Medicilon) leveraged its well-established pharmacokinetics research platform to provide early-stage animal pharmacokinetic services for Fuzerelisib. By ensuring efficiency and precision in the research process, Medicilon contributed to the early development of Fuzerelisib.

China's First KRAS G12C Inhibitor, Fuzerelisib
Breaking Through the Treatment Challenges of KRAS G12C-Mutant NSCLC

Fuzerelisib, as a highly effective oral small-molecule KRAS G12C inhibitor, works by covalently and irreversibly modifying the cysteine residue of the KRAS G12C protein mutant. This inhibits the GTP/GDP exchange mediated by the protein, thereby reducing the activation level of the KRAS protein.

In a monotherapy registrational study targeting KRAS G12C-mutant advanced NSCLC patients who had failed or were intolerant to standard treatments, Fuzerelisib demonstrated outstanding clinical efficacy.  The study results showed that Fuzerelisib had a generally good tolerance profile. As of December 13, 2023, a total of 116 NSCLC subjects were included in the analysis.  The confirmed objective response rate (cORR) assessed by the Independent Radiology Review Committee (IRRC) reached 49.1% (95% CI: 39.7-58.6), while the disease control rate (DCR) was 90.5% (95% CI: 83.7-95.2). The median duration of response (DoR) was not yet reached. The median progression-free survival (PFS) was 9.7 months (95% CI: 5.6-11.0), and the median overall survival (OS) had not yet been reached.

The successful launch of Fuzerelisib reflects Genfleet Therapeutics' strong expertise and innovative spirit in the field of oncology drug development. It effectively addresses the unmet clinical needs for the treatment of KRAS G12C-mutant NSCLC in China, marking a significant step forward in the country's biopharmaceutical industry's journey toward precision medicine.

Medicilon’s KRAS New Drug Development Service Platform
Supporting One-Stop Preclinical Development for KRAS New Drugs

Daring to venture into the unknown and courageously climbing the peaks of scientific research truly reflects Genfleet Therapeutics' spirit, and it vividly illustrates Medicilon’s unwavering pursuit in the field of biopharmaceutical preclinical development over the past 20 years.  In recent years, the development of targeted anti-cancer drugs has flourished and grown significantly each year. The field of anti-cancer drug development has entered an era of precision-targeted therapy. With the progress of various new targeted drug service projects in recent years, Medicilon has consistently been at the forefront of international innovation and has gradually developed a research and development service platform targeting KRAS.  Currently, in the field of KRAS-targeted drug development, Medicilon offers a one-stop professional service that covers all aspects, from drug discovery to CMC research (API and formulation), pharmacodynamic assessment, pharmacokinetic (PK) studies, and safety evaluation. In the formulation of KRAS research project plans, Medicilon engages in in-depth communication with clients. The research team, leveraging their extensive practical experience and technical expertise, provides high-quality experimental plans and data results tailored to the specific characteristics of each case.

Medicilon congratulates Genfleet Therapeutics on the approval and launch of their KRAS inhibitor, Fuzerelisib. We look forward to this groundbreaking drug quickly benefiting a wide range of patients, offering them longer survival and a higher quality of life. In the future, Medicilon will continue to explore and innovate in the field of drug development targeting key molecules like KRAS. We are committed to providing comprehensive, professional, and efficient biopharmaceutical R&D services, helping more new drugs transition from the laboratory to clinical trials and into the market.

About Genfleet Therapeutics

Genfleet Therapeutics is a global clinical-stage innovative drug development company. The company focuses on highly unmet clinical needs in oncology and immunological diseases, with a core emphasis on disease biology mechanisms and clinical translational medicine. It utilizes a self-reliant, integrated R&D system to target innovative, clinically unverified targets and indications and holds global independent intellectual property.  Since its establishment in 2017, Genfleet Therapeutics has developed over ten self-initiated "global new" large and small molecule projects. Several products have entered global multi-center clinical trials in China (including Taiwan), Europe, the United States, and Australia, including multiple late-stage or pivotal clinical studies. Dabote® (Fuzerelisib) is the first domestically approved product in Genfleet Therapeutics' pipeline and the first KRAS G12C inhibitor approved in China and the third globally. It has received priority review and two breakthrough therapy designations from the National Medical Products Administration. Fuzerelisib, in combination with cetuximab, is also undergoing Phase II studies in Europe, representing the first KRAS and EGFR inhibitor combination therapy for first-line non-small cell lung cancer.  Currently, the company has established an integrated and in-depth matrix for RAS-targeted therapies and is actively expanding its pipeline to include other "global new" targeted drugs and new types of therapies. Additionally, the company has been deepening its commercial collaboration network in recent years, having entered into strategic licensing agreements with multiple domestic and international listed companies and engaged in "global new" clinical collaborations with positive progress. Over the next three to five years, as more in-house and collaborative development projects advance to late-stage clinical research, the company is also expected to enter the industrialization and commercialization phases.