China Approves Innovent's Dupert for Lung Cancer

China’s National Medical Products Administration (NMPA) has granted approval for Innovent Biologics’ KRAS G12C inhibitor, Dupert (fulzerasib), for the treatment of advanced non-small cell lung cancer (NSCLC) in adults. This approval is specific to adults with the KRAS G12C mutation who have undergone at least one form of systemic therapy.

Dupert is an oral medication that targets the guanosine triphosphate/guanosine diphosphate exchange by covalently and irreversibly modifying the cysteine residue of the KRAS G12C protein. Preclinical research has demonstrated that fulzerasib is highly selective for the G12C mutation, effectively inhibiting downstream signaling pathways. This inhibition leads to programmed cell death (apoptosis) and arrest of the cell cycle in tumor cells.

The approval of Dupert is based on the outcomes of a Phase II clinical study that evaluated the efficacy and safety of fulzerasib as a monotherapy in Chinese patients with advanced NSCLC and the KRAS G12C mutation. As of December 13, 2023, the study had enrolled 116 evaluable participants. The results showed that fulzerasib was generally well-tolerated and displayed promising antitumor activity.

The Independent Radiology Review Committee (IRRC) confirmed an objective response rate (ORR) of 49.1% and a disease control rate of 90.5%. The median duration of response and overall survival have not yet been reached, but the median progression-free survival was recorded at 9.7 months.

In September 2021, Innovent Biologics entered into an exclusive licensing agreement with GenFleet Therapeutics for the development and commercialization of fulzerasib in China, including mainland China, Hong Kong, Macau, and Taiwan. The therapy has been granted breakthrough therapy designation (BTD) by the Center for Drug Evaluation (CDE) of China’s NMPA on two occasions: first in January 2023 for advanced NSCLC and then in May 2023 for advanced colorectal cancer with the KRAS G12C mutation.

Innovent's senior vice-president, Dr. Hui Zhou, expressed optimism about the approval, stating, “Patients with advanced NSCLC harboring KRAS G12C mutations have limited treatment options, with traditional chemotherapy offering minimal benefits. We are excited that Dupert has become the first KRAS G12C inhibitor approved in China, marking the beginning of a new era in targeted therapy for KRAS mutations. As Innovent’s eleventh drug, Dupert further strengthens our robust oncology portfolio.”