Dupert® Becomes First China-Originated KRAS G12C Inhibitor Approved in Macau for Advanced NSCLC

Recently, China's first domestically developed KRAS G12C inhibitor, Dupert® (Fulzerasib Tablets), has been officially approved for marketing by the Pharmaceutical Administration Bureau (ISAF) of the Macau Special Administrative Region of China. Dupert® is approved for treating patients with advanced non-small cell lung cancer (NSCLC) carrying the KRAS G12C mutation who have received at least one systemic treatment. Dupert® has become the first China-developed KRAS G12C inhibitor approved by Macau, bringing a new precision targeted therapy option for patients with KRAS G12C-mutated advanced NSCLC. As an innovative drug from Innovent Biologics, Dupert® specifically inhibits the oncogenic KRAS G12C protein in patients with KRAS G12C mutation, blocking tumor cell proliferation signals and filling an unmet clinical need. In a Phase II clinical trial among Chinese patients with KRAS G12C mutated NSCLC, Fulzerasib monotherapy achieved an ORR of 49.1%, median PFS of 9.7 months, 12-month OS rate of 54.4%, and a 12-month DoR rate of 53.7%. Most common treatment-related adverse events were grade 1-2, such as anemia and lab abnormalities, which could be managed with dose modification and supportive care, with no unexpected severe toxicities observed. Fulzerasib has earned Class 1 recommendation in treatment for KRAS G12C-mutated NSCLC in the 2025 CSCO guidelines, offering patients a new option of precison targeted therapy, with durable efficacy and good tolerability. Dupert®’s approval in Macau marks another milestone for Innovent Biologics in the Greater China region. Other innovative products from Innovent, such as Tyvyt®, BYVASDA®, Sintbilo®, and Pemazyre® have been approved in Indonesia, Hong Kong, Macau, and Taiwan, with more products planned for registration in Brazil, Mexico, Colombia, India, and other countries, aiming to bring innovative therapies to more patients in Latin America and Southeast Asia. About Dupert® (Fulzerasib, KRAS G12C Inhibitor) Fulzerasib is a novel, orally active, potent KRAS G12C inhibitor designed to effectively target the GTP/GDP exchange, an essential step in pathway activation, by modifying the cysteine residue of KRAS G12C protein covalently and irreversibly. Preclinical cysteine selectivity studies demonstrated high selectivity of fulzerasib towards G12C. Subsequently, fulzerasib effectively inhibits the downstream signaling pathway to induce tumor cell apoptosis and cell cycle arrest. In September 2021, Innovent and GenFleet Therapeutics entered into an exclusive license agreement for the development and commercialization of fulzerasib (Innovent R&D code: IBI351, GenFleet R&D code: GFH925) in China (including mainland China, Hong Kong, Macau and Taiwan). In January 2023, the Center for Drug Evaluation (CDE) of China’s National Medical Products Administration (NMPA) has granted Breakthrough Therapy Designation (BTD) for fulzerasib for the treatment of patients with advanced NSCLC harboring KRAS G12C mutation who have received at least one systemic therapy. In May 2023, the CDE of China’s NMPA granted another BTD for fulzerasib for the treatment of advanced CRC patients with KRAS G12C mutation who have received at least two systemic therapies. In August 2024, the CDE of NMPA has approved fulzerasib for the treatment of advanced NSCLC adult patients harboring KRAS G12C mutation who have received at least one systemic therapy. About Innovent Biologics Innovent is a leading biopharmaceutical company founded in 2011 with the mission to empower patients worldwide with affordable, high-quality biopharmaceuticals. The company discovers, develops, manufactures and commercializes innovative medicines that target some of the most intractable diseases. Its pioneering therapies treat cancer, cardiovascular and metabolic, autoimmune and eye diseases. Innovent has launched 16 products in the market. It has 2 new drug applications under regulatory review, 4 assets in Phase 3 or pivotal clinical trials and 15 more molecules in early clinical stage. Innovent partners with over 30 global healthcare companies, including Eli Lilly, Sanofi, Incyte, LG Chem and MD Anderson Cancer Center. Guided by the motto, “Start with Integrity, Succeed through Action” Innovent maintains the highest standard of industry practices and works collaboratively to advance the biopharmaceutical industry so that first-rate pharmaceutical drugs can become widely accessible. For more information, visit www.innoventbio.com, or follow Innovent on Facebook and LinkedIn. Statement: Innovent does not recommend the use of any unapproved drug (s)/indication (s).

The release as fetched from its publisher. innoventbio.com ↗